Journal articles: 'Anti-HIV treatment'

1

Hirschel, Bernard. "Planned interruptions of anti-HIV treatment." Lancet Infectious Diseases 1, no. 1 (August 2001): 53–59. http://dx.doi.org/10.1016/s1473-3099(01)00022-6.

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Eron, Joseph J., and Pietro Vernazza. "Alternative strategies for anti-HIV treatment." AIDS 15 (2001): S161—S169. http://dx.doi.org/10.1097/00002030-200100005-00020.

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Hill, Andrew M. "CD4 RISES DURING ANTI-HIV TREATMENT." AIDS 8, Supplement 4 (November 1994): S3. http://dx.doi.org/10.1097/00002030-199411004-00011.

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4

Karpas, Abraham, Stephen Ash, and Douglas Bainbridge. "Are anti-HIV drugs an effective treatment?" Nature Medicine 3, no. 10 (October 1997): 1052. http://dx.doi.org/10.1038/nm1097-1052a.

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Wurtman, Richard J. "Are anti-HIV drugs an effective treatment?" Nature Medicine 3, no. 10 (October 1997): 1052. http://dx.doi.org/10.1038/nm1097-1052b.

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LIM, SENG G., CHRISTINE A. LEE, and PETER B. A. KERNOFF. "Zidovudine treatment for anti-HIV positive haemophiliacs." Clinical & Laboratory Haematology 12, no. 4 (June 28, 2008): 367–78. http://dx.doi.org/10.1111/j.1365-2257.1990.tb00348.x.

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7

Piliero, Peter J. "Early Factors in Successful Anti-HIV Treatment." Journal of the International Association of Physicians in AIDS Care 2, no. 1 (January 2003): 10–20. http://dx.doi.org/10.1177/154510970300200102.

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8

Kang, Dongwei, Jinxuan Yang, Lingjin Kong, Ronghua Luo, Xusheng Huang, Tao Zhang, Mengdi Ma, et al. "Structure-Based Discovery and Characterization of a Preclinical Drug Candidate for the Treatment of HIV-1 Infection." Viruses 14, no. 11 (October 28, 2022): 2390. http://dx.doi.org/10.3390/v14112390.

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HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) area key component of the current HIV-1 combination drug regimens. Although they exhibit potent anti-HIV-1 activity and modest toxicity, the emergence of mutant strains limits their application in clinical. Our previous research efforts contributed to the identification of compound K-5a2, which exhibits nanomolar activity in HIV-1-infected MT-4 cells. In this study, K-5a2 was shown to have a high level of anti-HIV-1 activity against various lab-adapted strains and clinical isolate strains, being comparable to ETR. Moreover, we showed the feasibility of K-5a2 as a preclinical anti-HIV-1 candidate by establishing its synergistic or additive anti-HIV-1 activity in combination with other representative anti-HIV-1 drugs and candidates. In addition, K-5a2 exhibited no inhibitory activity to the primary CYP isoforms and favorable pharmacokinetics. Taken together, its robust anti-HIV-1 potency, synergistic or additive effects with other anti-HIV drugs, and favorable pharmacokinetic and safety profiles make K-5a2 a potent alternative drug for HIV/AIDS treatment.

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Scaradavou, Andromachi, Bonnie Woo, B. M. R. Woloski, Susanna Cunningham-Rundles, Lawrence J. Ettinger, Louis M. Aledort, and James B. Bussel. "Intravenous Anti-D Treatment of Immune Thrombocytopenic Purpura: Experience in 272 Patients." Blood 89, no. 8 (April 15, 1997): 2689–700. http://dx.doi.org/10.1182/blood.v89.8.2689.

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Abstract We report the results of intravenous anti-D (WinRho, WinRho SD) therapy in 261 non-splenectomized patients treated at the New York Hospital-Cornell Medical Center over the period from 1987 to 1994. Children (n = 124) and adult patients (n = 137) with classic immune thrombocytopenic purpura (ITP; n = 156) or human immunodeficiency virus (HIV) related thrombocytopenia (n = 105) and acute (n = 75) or chronic (n = 186) disease at the time of the initial anti-D treatment were studied. In addition, 11 previously splenectomized patients were treated as a separate group. Our objectives were to evaluate the following. (1) Efficacy of anti-D: The response after the initial infusion was analyzed according to clinical parameters, such as patient's age, HIV status, gender, disease duration, pretreatment platelet count, and hemoglobin value, as well as treatment-related factors, including the dose of anti-D, the solvent detergent treatment of the preparation, and the type of administration. (2) Use of anti-D as maintenance therapy: The duration of response after the initial infusion and the results of subsequent treatments were evaluated. (3) Safety/toxicity of anti-D: Postinfusion reactions and hemoglobin decrease after treatment were studied. Anti-D is a safe treatment providing a hemostatic platelet increase in greater than 70% of the Rh+ non-splenectomized patients. The group with the best results is HIV− children, but all patient groups respond and the effect lasts more than 21 days in 50% of the responders. Duration of response is not influenced by HIV status; furthermore, HIV+ patients show no adverse effects on hemoglobin decrease or HIV disease progression. Patients with chronic ITP after splenectomy have minimal or no response to intravenous anti-D.

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Huerta-Reyes, Maira, Luis O. Sánchez-Vargas, Getsemaní S. Villanueva-Amador, and Luis A. Gaitán-Cepeda. "Anti-HIV and Anti-Candidal Effects of Methanolic Extract from Heteropterys brachiata." International Journal of Environmental Research and Public Health 18, no. 14 (July 7, 2021): 7270. http://dx.doi.org/10.3390/ijerph18147270.

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Nowadays, the HIV pandemic is far from controlled. HIV+/AIDS patients show a serious risk of developing resistance to HIV antiretroviral drugs and to be orally colonized by albicans and non-albicans Candida strains resistant to antifungals. As a consequence, new drugs that possess anti-candidal and anti-HIV effects would represent an alternative in the comprehensive treatment of HIV+/AIDS patients. The present study evaluates the possible anti-HIV and anti-Candida effects of a methanolic extract from Heteropterys brachiata (Hb MeOH), an American tropical plant. The anti-HIV effect of Hb MeOH was tested using a non-radioactive colorimetric method (Lenti RT® Activity Assay; Cavidi Tech) that uses reverse transcriptase of HIV-1 enzyme as enzymatic target. The anti-candidal effect of HbMeOH extract was evaluated by following a standardized test protocol of microdilution for yeast using the Candida albicans strain ATCC® 90028. The Hb MeOH at 1 mg/mL concentration shows 38.5% RT-HIV inhibition, while Hb MeOH at 10 mg/mL concentration produced 98% C. albicans growth inhibition. Our findings show that the Hb MeOH possesses a strong anti-candidal activity and moderate anti-HIV effect and suggests that the plant extract could be considered as a potential candidate for HIV/AIDS treatment.

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11

Gjerset, GF, MJ Clements, RB Counts, AS Halvorsen, and AR Thompson. "Treatment type and amount influenced human immunodeficiency virus seroprevalence of patients with congenital bleeding disorders." Blood 78, no. 6 (September 15, 1991): 1623–27. http://dx.doi.org/10.1182/blood.v78.6.1623.bloodjournal7861623.

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Two hundred and eighty-two patients with congenital bleeding disorders received blood component replacement therapy between January 1979 and April 1985, were followed-up by the Puget Sound Blood Center's Hemophilia Care Program, and were tested for antibody to human immunodeficiency virus (HIV). Serologic results were obtained at least 1 year after the last exposure to volunteer donor products that were prepared before donor HIV screening or after the last exposure to concentrates produced before the manufacturer's use of treatment methods for inactivation of HIV. In all, 106 patients were anti-HIV positive. The risk of HIV infection was greater in patients with more severe bleeding tendencies, greater exposure to components, and exposure to lyophilized concentrates from large pools of donors. Of 100 patients with hemophilia A who only received cryoprecipitate from volunteer donors from Washington State (during the 6.3-year period), 14% had become anti-HIV positive. Of 27 patients receiving mostly cryoprecipitate but also being exposed to a single lot of concentrate during the same period, 13 (48%) were positive. Of 49 patients treated predominantly or solely with factor VIII concentrates during this period, 43 (88%) were anti-HIV positive. Of 29 patients with von Willebrand disease, four were anti-HIV positive, including 2 of 26 receiving only cryoprecipitate and two of three who had received a single dose of factor VIII concentrate. Of 19 patients who were treated solely with volunteer donor plasma, all remained anti-HIV negative. Of 47 patients exposed to factor IX concentrate, 28 (60%) were positive. Data relevant to the risk of HIV transmission subsequent to screening of the volunteer donor population were also obtained. Treatment records of 55 hemophilia A patients who have remained anti-HIV negative through at least June 1990 showed exposure to 71,173 screened donors from May 1985 through December 1989, and all 55 patients have remained anti-HIV negative.

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Gjerset, GF, MJ Clements, RB Counts, AS Halvorsen, and AR Thompson. "Treatment type and amount influenced human immunodeficiency virus seroprevalence of patients with congenital bleeding disorders." Blood 78, no. 6 (September 15, 1991): 1623–27. http://dx.doi.org/10.1182/blood.v78.6.1623.1623.

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Abstract Two hundred and eighty-two patients with congenital bleeding disorders received blood component replacement therapy between January 1979 and April 1985, were followed-up by the Puget Sound Blood Center's Hemophilia Care Program, and were tested for antibody to human immunodeficiency virus (HIV). Serologic results were obtained at least 1 year after the last exposure to volunteer donor products that were prepared before donor HIV screening or after the last exposure to concentrates produced before the manufacturer's use of treatment methods for inactivation of HIV. In all, 106 patients were anti-HIV positive. The risk of HIV infection was greater in patients with more severe bleeding tendencies, greater exposure to components, and exposure to lyophilized concentrates from large pools of donors. Of 100 patients with hemophilia A who only received cryoprecipitate from volunteer donors from Washington State (during the 6.3-year period), 14% had become anti-HIV positive. Of 27 patients receiving mostly cryoprecipitate but also being exposed to a single lot of concentrate during the same period, 13 (48%) were positive. Of 49 patients treated predominantly or solely with factor VIII concentrates during this period, 43 (88%) were anti-HIV positive. Of 29 patients with von Willebrand disease, four were anti-HIV positive, including 2 of 26 receiving only cryoprecipitate and two of three who had received a single dose of factor VIII concentrate. Of 19 patients who were treated solely with volunteer donor plasma, all remained anti-HIV negative. Of 47 patients exposed to factor IX concentrate, 28 (60%) were positive. Data relevant to the risk of HIV transmission subsequent to screening of the volunteer donor population were also obtained. Treatment records of 55 hemophilia A patients who have remained anti-HIV negative through at least June 1990 showed exposure to 71,173 screened donors from May 1985 through December 1989, and all 55 patients have remained anti-HIV negative.

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13

Sacchi, Viola. "Maraviroc (Celsentri) in HIV treatment." Farmeconomia. Health economics and therapeutic pathways 9, no. 4 (January 15, 2008): 219–22. http://dx.doi.org/10.7175/fe.v9i4.239.

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Since 1996, the prognosis of people living with immunodeficiency virus (HIV) and acquired immunodeficiency syndrome (AIDS) has improved significantly, due to highly active antiretroviral therapies (HAART) based on a combination of 3-4 anti-HIV drugs; the use ofthese drugs can achieve a durable suppression of HIV viraemia, turning HIV infection into a chronic illness. The three first licensed classes of antiretroviral agents are nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs) and protease inhibitors (PIs). Until recently, treatment options for individuals developing resistanceto these drugs have been limited, but new drugs in existing classes (second generation NNRTIs and novel PIs) and novel classes of drugs (integrase inhibitors, CCR5 antagonists and fusion inhibitors) have become clinically available.

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14

Huerta, Leonor. "Editorial: Anti-infective 2020: HIV—From pathogenesis to treatment." Current Opinion in Pharmacology 54 (October 2020): x—xii. http://dx.doi.org/10.1016/j.coph.2020.12.001.

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15

Ribeiro, Ruy M. "Quantifying the activity of anti-HIV treatment in silico." Nature Medicine 18, no. 3 (March 2012): 355–56. http://dx.doi.org/10.1038/nm.2698.

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Weinberger, Ariel D., Alan S. Perelson, Ruy M. Ribeiro, and Leor S. Weinberger. "Accelerated Immunodeficiency by Anti-CCR5 Treatment in HIV Infection." PLoS Computational Biology 5, no. 8 (August 14, 2009): e1000467. http://dx.doi.org/10.1371/journal.pcbi.1000467.

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17

Cohen, J. "AIDS TREATMENT: A Step Toward Cheaper Anti-HIV Therapy." Science 307, no. 5710 (February 4, 2005): 653b. http://dx.doi.org/10.1126/science.307.5710.653b.

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18

Filippini, P., N. Coppola, C. Scolastico, G. Liorre, R. Nocera, E. Sagnelli, and F. Piccinino. "Can HCV affect the efficacy of anti-HIV treatment?" Archives of Virology 145, no. 5 (May 2000): 937–44. http://dx.doi.org/10.1007/s007050050685.

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19

Reekie, Joanne, Amanda Mocroft, James Neaton, and Jens D. Lundgren. "Clinical outcomes in clinical trials of anti-HIV treatment." Future HIV Therapy 1, no. 3 (September 2007): 251–58. http://dx.doi.org/10.2217/17469600.1.3.251.

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20

Nadler, Jeffrey. "New Anti-HIV Protease Inhibitors Provide More Treatment Options." AIDS Patient Care and STDs 17, no. 11 (November 2003): 551–64. http://dx.doi.org/10.1089/108729103322555944.

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21

Kumar, Davinder, Virender Kumar, Rakesh Marwaha, and Gajendra Singh. "Oxadiazole-An Important Bioactive Scaffold for Drug Discovery and Development Process Against HIV and Cancer- A Review." Current Bioactive Compounds 15, no. 3 (May 7, 2019): 271–79. http://dx.doi.org/10.2174/1573407213666171017160359.

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Background: Acquired immunodeficiency syndrome (AIDS) and cancer treatment have been a major task for research scientists and pharmaceutical industry for the last many years. Seeking to the development, many promising chemical entities especially five-membered heterocyclic rings like oxadiazole have revealed good anticancer and anti HIV activities. The current review enlists some recently developed anti-HIV and anti-cancer oxadiazole moieties. Methods: on the basis of structural modification for the syntheses of new oxadiazole analogs, the new anti-HIV and anti-cancer agents have been summarized, which can improve treatment of AIDs and cancer. Results: The oxadiazole ring is more potent in comparison to some other heterocyclic rings (five and six membered) towards anti-HIV and anti-cancer activities. The important mechanisms involved for anti HIV and anticancer activity are mainly inhibition of enzymes like protease, HIV-integrase, telomerase, histone deacetylase, methionine amino peptidase, thymidylate synthase and focal adhesion kinase and inhibition of some growth factors. Conclusion: By reviving the past literature about 50 most potent oxadiazole derivatives, depending upon activity and structural modifications, have been selected as potent anti-HIV, and anti-cancer agents. Thus, oxadiazole seems to be a ‘privileged structure’ for further screening and syntheses of the new drug analogs against life threatening HIV and cancer like diseases.

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Toro-Zapata, Hernán, Angélica Caicedo-Casso, and Sunmi Lee. "The Role of Immune Response in Optimal HIV Treatment Interventions." Processes 6, no. 8 (July 26, 2018): 102. http://dx.doi.org/10.3390/pr6080102.

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A mathematical model for the transmission dynamics of human immunodeficiency virus (HIV) within a host is developed. Our model focuses on the roles of immune response cells or cytotoxic lymphocytes (CTLs). The model includes active and inactive cytotoxic immune cells. The basic reproduction number and the global stability of the virus free equilibrium is carried out. The model is modified to include anti-retroviral treatment interventions and the controlled reproduction number is explored. Their effects on the HIV infection dynamics are investigated. Two different disease stage scenarios are assessed: early-stage and advanced-stage of the disease. Furthermore, optimal control theory is employed to enhance healthy CD4+ T cells, active cytotoxic immune cells and minimize the total cost of anti-retroviral treatment interventions. Two different anti-retroviral treatment interventions (RTI and PI) are incorporated. The results highlight the key roles of cytotoxic immune response in the HIV infection dynamics and corresponding optimal treatment strategies. It turns out that the combined control (both RTI and PI) and stronger immune response is the best intervention to maximize healthy CD4+ T cells at a minimal cost of treatments.

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Chu, Y., and H. Liu. "Advances of Research on Anti-HIV Agents from Traditional Chinese Herbs." Advances in Dental Research 23, no. 1 (March 25, 2011): 67–75. http://dx.doi.org/10.1177/0022034511399912.

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The current approach for dealing with the global pandemic of AIDS focuses on pharmaceuticals. The classic treatment of AIDS is highly active antiretroviral therapy, but most people living with HIV/AIDS—especially those in developing countries—have little or no access to the treatment because of the high cost of the therapy. Such treatment is associated with toxic side effects and drug resistance. As such, the search for better anti-HIV agents continues, with much attention focused on natural sources—particularly, plant species. Thousands of herbs have been screened for anti-HIV activity, and new compounds have been discovered from the extracts, many of which demonstrate inhibitory activity against HIV. Their mechanisms of action include inhibiting the activities of reverse transcriptase, protease, and integrase; weakening infection at the level of viral entry; and downregulating related gene expression. This provides researchers with new clues to synthesize drugs for the anti-HIV battle. Some synthetic derivatives of the anti-HIV natural products have stronger inhibitory effects in vitro than do their natural counterparts. Various mixed preparations of these anti-HIV herbs are in clinical trials or are applied in the treatment of people living with HIV/AIDS—some of which yield lower plasma viral load, enhance immune function, relieve related symptoms and signs, improve the quality of life, or, in combination with highly active antiretroviral therapy, alleviate the side effects of biomedical drugs. This article reviews current laboratory findings and clinical trials of anti-HIV agents from traditional herbs—particularly, herbs in traditional Chinese medicine. Drug interactions with highly active antiretroviral therapy and criteria for clinical evaluation of traditional Chinese medicine treatment are also discussed.

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Kostova, I., S. Raleva, P. Genova, and R. Argirova. "Structure-Activity Relationships of Synthetic Coumarins as HIV-1 Inhibitors." Bioinorganic Chemistry and Applications 2006 (2006): 1–9. http://dx.doi.org/10.1155/bca/2006/68274.

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HIV/AIDS pandemics is a serious threat to health and development of mankind, and searching for effective anti-HIV agents remains actual. Considerable progress has been made in recent years in the field of drug development against HIV. A lot of structurally different coumarins were found to display potent anti-HIV activity. The current review demonstrates the variety of synthetic coumarins having unique mechanism of action referring to the different stages of HIV replication. Recent studies based on the account of various synthetic coumarins seem to indicate that some of them serve as potent non-nucleoside RT-inhibitors, another as inhibitors of HIV-integrase or HIV-protease. The merits of selecting potential anti-HIV agents to be used in rational combination drugs design and structure-activity relationships are discussed.The scientific community is looking actively for new drugs and combinations for treatment of HIV infection effective for first-line treatment, as well as against resistant mutants. The investigation on chemical anti-HIV agents gives hope and optimism about it. This review article describes recent progress in the discovery, structure modification, and structure-activity relationship studies of potent anti-HIV coumarin derivatives.

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Fatmawati and Hengki Tasman. "An Optimal Treatment Control of TB-HIV Coinfection." International Journal of Mathematics and Mathematical Sciences 2016 (2016): 1–11. http://dx.doi.org/10.1155/2016/8261208.

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An optimal control on the treatment of the transmission of tuberculosis-HIV coinfection model is proposed in this paper. We use two treatments, that is, anti-TB and antiretroviral, to control the spread of TB and HIV infections, respectively. We first present an uncontrolled TB-HIV coinfection model. The model exhibits four equilibria, namely, the disease-free, the HIV-free, the TB-free, and the coinfection equilibria. We further obtain two basic reproduction ratios corresponding to TB and HIV infections. These ratios determine the existence and stability of the equilibria of the model. The optimal control theory is then derived analytically by applying the Pontryagin Maximum Principle. The optimality system is performed numerically to illustrate the effectiveness of the treatments.

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Serumula, William, Geronimo Fernandez, Victor M. Gonzalez, and Raveen Parboosing. "Anti-HIV Aptamers: Challenges and Prospects." Current HIV Research 20, no. 1 (January 2022): 7–19. http://dx.doi.org/10.2174/1570162x19666210908114825.

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: Human Immunodeficiency Virus (HIV) infection continues to be a significant health burden in many countries around the world. Current HIV treatment through a combination of different antiretroviral drugs (cART) effectively suppresses viral replication, but drug resistance and crossresistance are significant challenges. This has prompted the search for novel targets and agents, such as nucleic acid aptamers. Nucleic acid aptamers are oligonucleotides that attach to the target sites with high affinity and specificity. This review provides a target-by-target account of research into anti-HIV aptamers and summarises the challenges and prospects of this therapeutic strategy, specifically in the unique context of HIV infection.

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Sun, Guofang. "Advances in the Treatment of Human Immunodeficiency Virus and Hepatitis B Virus Co-infection." Infection International 5, no. 2 (June 1, 2016): 54–58. http://dx.doi.org/10.1515/ii-2017-0131.

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AbstractHepatitis B virus (HBV) and human immunodeficiency virus (HIV) are transmitted through the same pathways. Therefore, the incidence of HBV in the HIV-infected population is higher than that in the healthy population, and is more obvious in China given the high HBV prevalence in the country. HIV and HBV co-infection can accelerate the disease process of HBV. Moreover, the incidence of cirrhosis and end-stage liver disease is higher in patients co-infected with HIV and HBV than in patients infected HBV alone. When treating patients co-infected with HIV and HBV for HBV infection alone, care should be taken to avoid the induction of HIV resistance. HBV should be considered during drug selection for anti-retroviral treatment. Furthermore, the effective HBV treatment should be retained if anti-retroviral drugs require changing.

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Anthony-Gonda, Kim, Ariola Bardhi, Alex Ray, Nina Flerin, Mengyan Li, Weizao Chen, Christina Ochsenbauer, et al. "Multispecific anti-HIV duoCAR-T cells display broad in vitro antiviral activity and potent in vivo elimination of HIV-infected cells in a humanized mouse model." Science Translational Medicine 11, no. 504 (August 7, 2019): eaav5685. http://dx.doi.org/10.1126/scitranslmed.aav5685.

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Adoptive immunotherapy using chimeric antigen receptor–modified T cells (CAR-T) has made substantial contributions to the treatment of certain B cell malignancies. Such treatment modalities could potentially obviate the need for long-term antiretroviral drug therapy in HIV/AIDS. Here, we report the development of HIV-1–based lentiviral vectors that encode CARs targeting multiple highly conserved sites on the HIV-1 envelope glycoprotein using a two-molecule CAR architecture, termed duoCAR. We show that transduction with lentiviral vectors encoding multispecific anti-HIV duoCARs confer primary T cells with the capacity to potently reduce cellular HIV infection by up to 99% in vitro and >97% in vivo. T cells are the targets of HIV infection, but the transduced T cells are protected from genetically diverse HIV-1 strains. The CAR-T cells also potently eliminated PBMCs infected with broadly neutralizing antibody-resistant HIV strains, including VRC01/3BNC117-resistant HIV-1. Furthermore, multispecific anti-HIV duoCAR-T cells demonstrated long-term control of HIV infection in vivo and prevented the loss of CD4+T cells during HIV infection using a humanized NSG mouse model of intrasplenic HIV infection. These data suggest that multispecific anti-HIV duoCAR-T cells could be an effective approach for the treatment of patients with HIV-1 infection.

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Arshad, P., P. Dineshkumar, K. Naga Jyothi, M. Karthik, and Govindaraj Saravanan. "Dendrimers as a Novel Carrier in Anti-HIV Therapy." Journal of Drug Delivery and Therapeutics 9, no. 5-s (October 22, 2019): 195–200. http://dx.doi.org/10.22270/jddt.v9i5-s.3650.

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The present treatments for HIV transfection include chemical agents and gene therapies. Although many chemical drugs, peptides and genes have been developed for HIV inhibition, a variety of non-ignorable drawbacks limited the efficiency of these materials. Dendrimers has ability to carrier of antiviral drugs due to some properties such as mono-dispersity, defined structure, amenability for functionalization using diverse ligands and its low-nanometer size. In this review, we discuss the application of dendrimers as both therapeutic agents and non-viral vectors of chemical agents and genes for HIV treatment. In one way, dendrimers with functional end groups combine with the gp120 of HIV and CD4 molecule of host cell to suppress the attachment of HIV to the host cell. In another way, dendrimers are also able to transfer chemical drugs and genes into the host cells, which increase the anti-HIV activity of these materials. Dendrimers as therapeutic tools provide a potential treatment for HIV infection. Keywords: Dendrimers, Drug release, Drug targeting, gp120, CD4, Antiviral drug

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Saag, Lauren A., Peter F. Rebeiro, Marcelo Cordeiro-Santos, Afranio Kritski, Bruno B. Andrade, Betina Durovni, Solange Calvacante, et al. "3166 Association between HIV and early weight loss and the impact on subsequent treatment outcomes among patients with tuberculosis." Journal of Clinical and Translational Science 3, s1 (March 2019): 34. http://dx.doi.org/10.1017/cts.2019.82.

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OBJECTIVES/SPECIFIC AIMS: Previous research suggests that weight loss during early TB treatment (first two months of anti-TB therapy) is a predictor of poor tuberculosis (TB) treatment outcomes among HIV-negative populations, but the relationship has not been well studied in the context of HIV. We examined the association between HIV and weight change during the first two months of anti-tuberculosis treatment, and also assessed the effects of HIV and early weight change on tuberculosis (TB) treatment outcomes. METHODS/STUDY POPULATION: Adults with culture-confirmed, drug-susceptible, pulmonary TB, regardless of HIV status, were enrolled into the Regional Prospective Observational Research for Tuberculosis (RePORT)-Brazil cohort and followed on standard anti-TB therapy. For the primary analysis, we compared weight change in persons living with HIV (PLWH) and HIV-negative patients between baseline and two months using multivariable bootstrapped quantile regression and modified Poisson regression. For secondary analysis, we examined the separate effects of HIV and weight change on poor TB treatment outcome (treatment failure, TB recurrence, or death) using Cox proportional hazards regression. RESULTS/ANTICIPATED RESULTS: Among 323 participants, 45 (14%) were HIV-positive. On average, PLWH lost 0.7% (interquartile range (IQR): −5.1%, 4.4%) of their baseline body weight between baseline and two months; those without HIV gained 3.5% (IQR: 0.8%, 6.7%). After adjusting for age, sex, and baseline BMI, PLWH lost 4.1% (95% confidence interval (CI): −6.5%, −1.6%) more weight during the first two months of anti-TB treatment than HIV-negative individuals. HIV infection was associated with weight loss ≥5% (adjusted odds ratio = 9.3; 95% CI: 4.2-20.6). Regarding the secondary analysis, 14 patients had a poor TB treatment outcome: 2 treatment failures, 4 cases of recurrent TB, and 8 deaths. PLWH and patients who lost ≥5% weight had significantly increased risk of poor TB treatment outcome with hazard ratios of 8.77 (95% CI: 2.96-25.94) and 4.09 (95% CI: 1.11-15.14), respectively. DISCUSSION/SIGNIFICANCE OF IMPACT: Our results suggest that HIV is associated with weight loss during early TB treatment, and both HIV and early weight loss were associated with poor treatment outcome. Future research should examine the potential etiologies of these findings and identify the types of interventions that would best promote weight gain during TB treatment, especially among PLWH, in order to prevent poor TB treatment outcomes.

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Frankline, Tireito, Lawi George, and Okaka Colleta. "Mathematical Analysis of HIV/AIDS Anti-Retroviral Treatment Incorporating Adherence." Asian Research Journal of Mathematics 10, no. 2 (August 1, 2018): 1–13. http://dx.doi.org/10.9734/arjom/2018/42830.

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Ma, Xiaowei, Dongliang Wang, Yan Wu, Rodney J. Y. Ho, Lee Jia, Peixuan Guo, Liming Hu, Gengmei Xing, Yi Zeng, and Xing-Jie Liang. "AIDS Treatment with Novel Anti-HIV Compounds Improved by Nanotechnology." AAPS Journal 12, no. 3 (April 6, 2010): 272–78. http://dx.doi.org/10.1208/s12248-010-9187-z.

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Bogorodskaya, E. M. "161 Anti-tuberculosis Treatment for HIV-positive Patients in Moscow." JAIDS Journal of Acquired Immune Deficiency Syndromes 65 (April 2014): 69. http://dx.doi.org/10.1097/01.qai.0000446745.22473.3a.

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Liu, Baochi, Lei Zhang, Ruizhang Guo, Jinsong Su, Lei Li, and Yanhui Si. "Anti-infective treatment in HIV-infected patients during perioperative period." AIDS Research and Therapy 9, no. 1 (2012): 36. http://dx.doi.org/10.1186/1742-6405-9-36.

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35

Stephenson, J. "New anti-HIV drugs and treatment strategies buoy AIDS researchers." JAMA: The Journal of the American Medical Association 275, no. 8 (February 28, 1996): 579–80. http://dx.doi.org/10.1001/jama.275.8.579.

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36

Stephenson, Joan. "New Anti-HIV Drugs and Treatment Strategies Buoy AIDS Researchers." JAMA: The Journal of the American Medical Association 275, no. 8 (February 28, 1996): 579. http://dx.doi.org/10.1001/jama.1996.03530320007003.

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37

Hagberg, Lars, Lars-Magnus Andersson, Sahra Abdulle, and Magnus Gisslén. "Clinical Application of Cerebrospinal Fluid Neopterin Concentrations in HIV Infection." Pteridines 15, no. 3 (August 2004): 102–6. http://dx.doi.org/10.1515/pteridines.2004.15.3.102.

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Abstract HIV-1 infects the central nervous system (CNS) and may cause AIDS dementia complex (ADC) and other neurologic complications. The cerebrospinal fluid (CSF) virus load is usually 0,5 -1 log lower than in blood, but in some patients the CSF quantitative HIV-1 RNA values exceed the paired blood samples. CSF neopterin concentrations are increased in all stages of HIV-1 infection, with the highest concentrations in AIDS patients and patients with CNS opportunistic infections. CD4 cell count and quantitative HIV RNA PCR tests in peripheral blood are used in clinical practice to monitor the HIV-1 infection and the anti-retroviral treatment effect. In most patients the anti-retroviral treatment response is similar in the cerebrospinal fluid (CSF) compare to the peripheral blood and the CSF viral load and neopterin concentrations are markedly reduced following treatment. ADC has become a rare complication. In spite of virological effective treatment many patients have a low grade intrathecal immunoactivation, measured as CSF neopterin concentrations above the 95% confidence interval found in IIIV-1 negative controls, after such a long time as after 2 years of anti-retroviral treatment. The risk of long term intrathecal immunoactivation and which anti-retroviral combination treatment has the best effect on CSF parameters is not known. CSF neopterin concentrations are at present not used in clinical practice but may add valuable information.

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Yu, Zaikuan J., Eric P. Mosher, and Namandjé N. Bumpus. "Pharmacogenomics of Antiretroviral Drug Metabolism and Transport." Annual Review of Pharmacology and Toxicology 61, no. 1 (January 6, 2021): 565–85. http://dx.doi.org/10.1146/annurev-pharmtox-021320-111248.

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Antiretroviral therapy has markedly reduced morbidity and mortality for persons living with human immunodeficiency virus (HIV). Individual tailoring of antiretroviral regimens has the potential to further improve the long-term management of HIV through the mitigation of treatment failure and drug-induced toxicities. While the mechanisms underlying anti-HIV drug adverse outcomes are multifactorial, the application of drug-specific pharmacogenomic knowledge is required in order to move toward the personalization of HIV therapy. Thus, detailed understanding of the metabolism and transport of antiretrovirals and the influence of genetics on these pathways is important. To this end, this review provides an up-to-date overview of the metabolism of anti-HIV therapeutics and the impact of genetic variation in drug metabolism and transport on the treatment of HIV. Future perspectives on and current challenges in pursuing personalized HIV treatment are also discussed.

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Singh, Kamal, Stefan G. Sarafianos, and Anders Sönnerborg. "Long-Acting Anti-HIV Drugs Targeting HIV-1 Reverse Transcriptase and Integrase." Pharmaceuticals 12, no. 2 (April 20, 2019): 62. http://dx.doi.org/10.3390/ph12020062.

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One of the major factors contributing to HIV-1 drug resistance is suboptimal adherence to combination antiretroviral therapy (cART). Currently, recommended cART for HIV-1 treatment is a three-drug combination, whereas the pre-exposure prophylaxis (PrEP) regimens consist of one or two antivirals. Treatment regimens require adherence to a once or twice (in a subset of patients) daily dose. Long-acting formulations such as injections administered monthly could improve adherence and convenience, and thereby have potential to enhance the chances of expected outcomes, although long-lasting drug concentrations can also contribute to clinical issues like adverse events and development of drug resistance. Globally, two long-acting antivirals have been approved, and fifteen are in clinical trials. More than half of investigational long-acting antivirals target HIV-1 reverse transcriptase (HIV-1 RT) and/or integrase (HIV-1 IN). Here, we discuss the status and potential of long-acting inhibitors, including rilpivirine (RPV), dapivirine (DPV), and 4-ethynyl-2-fluoro-2-deoxyadenosine (EFdA; also known as MK-8591), which target RT, and cabotegravir (CAB), which targets IN. The outcomes of various clinical trials appear quite satisfactory, and the future of long-acting HIV-1 regimens appears bright.

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De Clercq, Erik. "New developments in anti-HIV chemotherapy." Pure and Applied Chemistry 73, no. 1 (January 1, 2001): 55–66. http://dx.doi.org/10.1351/pac200173010055.

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Virtually all the compounds that are currently used, or under advanced clinical trial, for the treatment of HIV infections, belong to one of the following classes: (i) nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs): i.e., zidovudine, didanosine, zalcitabine, stavudine, lamivudine, abacavir, emtricitabine, tenofovir (PMPA), and disoproxil fumarate; (ii) non-nucleoside reverse transcriptase inhibitors (NNRTIs): i.e., nevirapine, delavirdine, efavirenz, and emivirine; and (iii) protease inhibitors (PIs): i.e., saquinavir, ritonavir, indinavir, nelfinavir, and amprenavir. In addition, various other events in the HIV replicative cycle are potential targets for chemotherapeutic intervention: (i) viral adsorption, through binding to the viral envelope glycoprotein gp120; (ii) viral entry, through blockade of the viral coreceptors CXCR4 and CCR5; (iii) virus-cell fusion; (iv) viral assembly and disassembly; (v) proviral DNA integration; and (vi) viral mRNA transcription. Also, new NRTIs, NNRTIs, and PIs have been developed that possess respectively improved metabolic characteristics, or increased activity against NNRTI-resistant HIV strains or, as in the case of PIs, a different, nonpeptidic scaffold. Given the multitude of molecular targets with which anti-HIV agents can interact, one should be cautious in extrapolating from cell-free enzymatic assays to the mode of action of these agents in intact cells.

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Greggs, Willie M., Christine L. Clouser, Steven E. Patterson, and Louis M. Mansky. "Discovery of drugs that possess activity against feline leukemia virus." Journal of General Virology 93, no. 4 (April 1, 2012): 900–905. http://dx.doi.org/10.1099/vir.0.039909-0.

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Feline leukemia virus (FeLV) is a gammaretrovirus that is a significant cause of neoplastic-related disorders affecting cats worldwide. Treatment options for FeLV are limited, associated with serious side effects, and can be cost-prohibitive. The development of drugs used to treat a related retrovirus, human immunodeficiency virus type 1 (HIV-1), has been rapid, leading to the approval of five drug classes. Although structural differences affect the susceptibility of gammaretroviruses to anti-HIV drugs, the similarities in mechanism of replication suggest that some anti-HIV-1 drugs may also inhibit FeLV. This study demonstrates the anti-FeLV activity of four drugs approved by the US FDA (Food and Drug Administration) at non-toxic concentrations. Of these, tenofovir and raltegravir are anti-HIV-1 drugs, while decitabine and gemcitabine are approved to treat myelodysplastic syndromes and pancreatic cancer, respectively, but also have anti-HIV-1 activity in cell culture. Our results indicate that these drugs may be useful for FeLV treatment and should be investigated for mechanism of action and suitability for veterinary use.

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Ji, Xiangkai, Jing Li, Prem Prakash Sharma, Xiangyi Jiang, Brijesh Rathi, Zhen Gao, Lide Hu, et al. "Design, Synthesis and Structure—Activity Relationships of Phenylalanine-Containing Peptidomimetics as Novel HIV-1 Capsid Binders Based on Ugi Four-Component Reaction." Molecules 27, no. 18 (September 14, 2022): 5995. http://dx.doi.org/10.3390/molecules27185995.

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As a key structural protein, HIV capsid (CA) protein plays multiple roles in the HIV life cycle, and is considered a promising target for anti-HIV treatment. Based on the structural information of CA modulator PF-74 bound to HIV-1 CA hexamer, 18 novel phenylalanine derivatives were synthesized via the Ugi four-component reaction. In vitro anti-HIV activity assays showed that most compounds exhibited low-micromolar-inhibitory potency against HIV. Among them, compound I-19 exhibited the best anti-HIV-1 activity (EC50 = 2.53 ± 0.84 μM, CC50 = 107.61 ± 27.43 μM). In addition, I-14 displayed excellent HIV-2 inhibitory activity (EC50 = 2.30 ± 0.11 μM, CC50 > 189.32 μM) with relatively low cytotoxicity, being more potent than that of the approved drug nevirapine (EC50 > 15.02 μM, CC50 > 15.2 μM). Additionally, surface plasmon resonance (SPR) binding assays demonstrated direct binding to the HIV CA protein. Moreover, molecular docking and molecular dynamics simulations provided additional information on the binding mode of I-19 to HIV-1 CA. In summary, we further explored the structure–activity relationships (SARs) and selectivity of anti-HIV-1/HIV-2 of PF-74 derivatives, which is conducive to discovering efficient anti-HIV drugs.

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Kulkarni, Rima, Rebecca Hluhanich, Damian M. McColl, Michael D. Miller, and Kirsten L. White. "The Combined Anti-HIV-1 Activities of Emtricitabine and Tenofovir plus the Integrase Inhibitor Elvitegravir or Raltegravir Show High Levels of SynergyIn Vitro." Antimicrobial Agents and Chemotherapy 58, no. 10 (August 4, 2014): 6145–50. http://dx.doi.org/10.1128/aac.03591-14.

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ABSTRACTHighly active antiretroviral therapy (HAART) involves combination treatment with three or more antiretroviral agents. The antiviral effects of combinations of emtricitabine (FTC) plus tenofovir (TFV) plus antiretroviral agents of all the major drug classes were investigated. Combinations of FTC and TFV with a nonnucleoside reverse transcriptase inhibitor (NNRTI) (efavirenz or rilpivirine) or with a protease inhibitor (PI) (atazanavir, lopinavir, or darunavir) showed additive to synergistic anti-HIV-1 activity. FTC-TFV with an HIV-1 integrase strand transfer inhibitor (INSTI) (elvitegravir or raltegravir) showed the strongest synergy. Anti-HIV-1 synergy suggests enhancement of individual anti-HIV-1 activities within cells that may contribute to potent treatment efficacy and open new areas of research into interactions between reverse transcriptase (RT) and integrase inhibitors.

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Donovan, Joseph, Nguyen Hoan Phu, Nguyen Thi Hoang Mai, Le Tien Dung, Darma Imran, Erlina Burhan, Lam Hong Bao Ngoc, et al. "Adjunctive dexamethasone for the treatment of HIV-infected adults with tuberculous meningitis (ACT HIV): Study protocol for a randomised controlled trial." Wellcome Open Research 3 (March 20, 2018): 31. http://dx.doi.org/10.12688/wellcomeopenres.14006.1.

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Background: Tuberculous meningitis (TBM) is the most severe form of tuberculosis. Co-infection with HIV increases the risk of developing TBM, complicates treatment, and substantially worsens outcome. Whether corticosteroids confer a survival benefit in HIV-infected patients with TBM remains uncertain. Hepatitis is the most common drug-induced serious adverse event associated with anti-tuberculosis treatment, occurring in 20% of HIV-infected patients. The suggested concentration thresholds for stopping anti-tuberculosis drugs are not evidence-based. This study aims to determine whether dexamethasone is a safe and effective addition to the first 6-8 weeks of anti-tuberculosis treatment of TBM in patients with HIV, and investigate alternative management strategies in a subset of patients who develop drug induced liver injury (DILI) that will enable the safe continuation of rifampicin and isoniazid therapy. Methods: We will perform a parallel group, randomised (1:1), double blind, placebo-controlled multi-centre Phase III trial, comparing the effect of dexamethasone versus placebo on overall survival in HIV-infected patients with TBM, in addition to standard anti-tuberculosis and antiretroviral treatment. The trial will be set in two hospitals in Ho Chi Minh City, Vietnam, and two hospitals in Jakarta, Indonesia. The trial will enrol 520 HIV-infected adults. An ancillary study will perform a randomised comparison of three DILI management strategies with the aim of demonstrating which strategy results in the least interruption in rifampicin and isoniazid treatment. An identical ancillary study will also be performed in the linked randomised controlled trial of dexamethasone in HIV-uninfected adults with TBM stratified by LTA4H genotype (LAST ACT). Discussion: Whether corticosteroids confer a survival benefit in HIV-infected patients remains uncertain, and the current evidence base for using corticosteroids in this context is limited. Interruptions in anti-tuberculosis chemotherapy is a risk factor for death from TBM. Alternative management strategies in DILI may allow the safe continuation of rifampicin and isoniazid therapy.

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Donovan, Joseph, Nguyen Hoan Phu, Nguyen Thi Hoang Mai, Le Tien Dung, Darma Imran, Erlina Burhan, Lam Hong Bao Ngoc, et al. "Adjunctive dexamethasone for the treatment of HIV-infected adults with tuberculous meningitis (ACT HIV): Study protocol for a randomised controlled trial." Wellcome Open Research 3 (June 20, 2018): 31. http://dx.doi.org/10.12688/wellcomeopenres.14006.2.

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Background: Tuberculous meningitis (TBM) is the most severe form of tuberculosis. Co-infection with HIV increases the risk of developing TBM, complicates treatment, and substantially worsens outcome. Whether corticosteroids confer a survival benefit in HIV-infected patients with TBM remains uncertain. Hepatitis is the most common drug-induced serious adverse event associated with anti-tuberculosis treatment, occurring in 20% of HIV-infected patients. The suggested concentration thresholds for stopping anti-tuberculosis drugs are not evidence-based. This study aims to determine whether dexamethasone is a safe and effective addition to the first 6-8 weeks of anti-tuberculosis treatment of TBM in patients with HIV, and investigate alternative management strategies in a subset of patients who develop drug induced liver injury (DILI) that will enable the safe continuation of rifampicin and isoniazid therapy. Methods: We will perform a parallel group, randomised (1:1), double blind, placebo-controlled multi-centre Phase III trial, comparing the effect of dexamethasone versus placebo on overall survival in HIV-infected patients with TBM, in addition to standard anti-tuberculosis and antiretroviral treatment. The trial will be set in two hospitals in Ho Chi Minh City, Vietnam, and two hospitals in Jakarta, Indonesia. The trial will enrol 520 HIV-infected adults. An ancillary study will perform a randomised comparison of three DILI management strategies with the aim of demonstrating which strategy results in the least interruption in rifampicin and isoniazid treatment. An identical ancillary study will also be performed in the linked randomised controlled trial of dexamethasone in HIV-uninfected adults with TBM stratified by LTA4H genotype (LAST ACT). Discussion: Whether corticosteroids confer a survival benefit in HIV-infected patients remains uncertain, and the current evidence base for using corticosteroids in this context is limited. Interruptions in anti-tuberculosis chemotherapy is a risk factor for death from TBM. Alternative management strategies in DILI may allow the safe continuation of rifampicin and isoniazid therapy.

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Bressler, P., G. Pantaleo, A. Demaria, and A. S. Fauci. "Anti-CD2 receptor antibodies activate the HIV long terminal repeat in T lymphocytes." Journal of Immunology 147, no. 7 (October 1, 1991): 2290–94. http://dx.doi.org/10.4049/jimmunol.147.7.2290.

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Abstract The CD2 T lymphocyte glycoprotein surface molecule mediates both cell to cell adhesion and T cell activation, two processes that are involved in the spread of HIV infection. Treatment of chronically HIV-infected PBMC with anti-CD2 mAb has been shown to induce the expression of infectious virus from these cultures. In this study we investigated the mechanisms whereby anti-CD2 antibodies stimulate viral production. We demonstrate that treatment of transiently transfected T lymphocytes with anti-CD2 antibodies results in activation of the HIV long terminal repeat. Furthermore, CAT assays using mutated HIV long terminal repeat-CAT constructs and gel shift assays demonstrate that this activation is dependent on the NF-kappa B enhancer. These studies suggest that interaction of CD2 with its natural ligand, LFA-3, may play a role in regulation of HIV expression.

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Maskoep, Wiwiek Indriyani, Nasronudin Nasronudin, Siti Khairunisa, and Sri Agus Sudjarwo. "The Influence of Anti-Hiv-1 Specific IgY In Inhibiting HIV-1 Infection in Binding Phase with Syncytium Examination of CD4 Receptor Density Using the Flowcytometry Method." Folia Medica Indonesiana 56, no. 4 (January 14, 2021): 290. http://dx.doi.org/10.20473/fmi.v56i4.24636.

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HIV/ AIDS infections have increased and spread very quickly in the world, including in Indonesia. The absence of an effective vaccine and the fact that antiretroviral drugs can only suppress the progression of infection but cannot eradicate it lead to the efforts to find materials containing immunoglobulins that can replace the immune system which greatly declines in HIV/ AIDS patients. The successful use of specific IgY in other studies opens up opportunities for the use of anti-HIV-1 specific IgY as passive immunotherapy. This type of research is true experimental research design with post-test only control group design. IgY was obtained from Lohmann Laying hens chicken eggs immunized with the inactivated HIV-1 virus. The concentration of IgY was determined using the Bradford method and then the characterization test was continued using the AGPT, ELISA, SDS-PAGE and Western blot tests which showed anti-HIV-1 specific IgY. The results of the test showed specific anti-HIV-1 IgY was effective in inhibiting the formation of syncytium in HIV-1 infection against CD4+ T lymphocytes in the binding phase (entry stage) in the treatment group p-value 0.000 (p <0.05). The results of CD4 receptor density tests using the Flowcytometry method showed that specific anti-HIV-1 IgY was effective in inhibiting HIV-1 infection against CD4+ T lymphocytes in the binding phase (entry stage) in the treatment group p-value 0.047 (p <0.05).HIV/ AIDS infections have increased and spread very quickly in the world, including in Indonesia. The absence of an effective vaccine and the fact that antiretroviral drugs can only suppress the progression of infection but cannot eradicate it lead to the efforts to find materials containing immunoglobulins that can replace the immune system which greatly declines in HIV/ AIDS patients. The successful use of specific IgY in other studies opens up opportunities for the use of anti-HIV-1 specific IgY as passive immunotherapy. This type of research is true experimental research design with post-test only control group design. IgY was obtained from Lohmann Laying hens chicken eggs immunized with the inactivated HIV-1 virus. The concentration of IgY was determined using the Bradford method and then the characterization test was continued using the AGPT, ELISA, SDS-PAGE and Western blot tests which showed anti-HIV-1 specific IgY. The results of the test showed specific anti-HIV-1 IgY was effective in inhibiting the formation of syncytium in HIV-1 infection against CD4+ T lymphocytes in the binding phase (entry stage) in the treatment group p-value 0.000 (p <0.05). The results of CD4 receptor density tests using the Flowcytometry method showed that specific anti-HIV-1 IgY was effective in inhibiting HIV-1 infection against CD4+ T lymphocytes in the binding phase (entry stage) in the treatment group p-value 0.047 (p <0.05).

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Bolhassani, Azam. "Target Molecules and Delivery Vehicles for Anti-HIV Drugs In vitro and In vivo." Current Pharmaceutical Design 24, no. 29 (December 8, 2018): 3393–401. http://dx.doi.org/10.2174/1381612824666180608124549.

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Acquired Immune Deficiency Syndrome (AIDS) is the most serious stage of Human Immunodeficiency Virus (HIV) infection. The combinatorial Anti-Retroviral Therapy (cART) is widely used in suppressing HIV-1 infection and enhancing life span of infected patients to a significant level. However, delivery of therapeutic molecules is still a major challenge in vivo. The studies showed that the anti-HIV drugs delivered via nanocarriers could be selectively accumulated in infected cells accompanied by low side effects. On the other hand, HIV-1 infection kinetics is different in macrophages and T-cells suggesting various effects of antiretroviral drugs against HIV-1 in these target cells. Current anti-HIV therapeutic studies have focused on developing drug delivery systems targeted specifically to HIV-infected host cells. Indeed, the drug targeting can significantly lead to reduce in drug toxicity, drug dose, and increase in treatment efficacy through localizing its pharmacological activity to the site of interest. This review describes development of novel drug targeting systems used in suppressing the transmission and treatment of HIV infections.

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Martinez, Ana, Carmen Gil, Ana Castro, Concepciön Perez, Myriam Witvrouw, Christophe Pannecouque, Jan Balzarini, and Erik De Clercq. "Anti-HIV-1 Activity of Benzothiadiazine Dioxide." Antiviral Chemistry and Chemotherapy 12, no. 6 (December 2001): 347–51. http://dx.doi.org/10.1177/095632020101200604.

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Antiviral assays carried out on the potent benzothiadiazine dioxide (BTD) human cytomegalovirus (HCMV) inhibitors have led us to find marginal but selective anti-HIV-1 activity. Specific pharmacological studies, such as time of addition experiments and assays on specific viral strains with mutations on its reverse transcriptase, have indicated that BTD compounds act as non-nucleoside reverse transcriptase inhibitors. Theoretical calculations showed a butterfly conformation for the active derivatives that are compatible with their mechanism of action. Therefore, BTD derivatives can be considered as potential lead compounds for the treatment of opportunistic HCMV infections in immunocompromised individuals such as AIDS patients.

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Cox, S., A. Vissgården, and B. Wahren. "Effect upon the anti-HIV Activity of 3′-Azido-3′-Deoxythymidine and 3′-Fluoro-3′-Deoxythymidine of Combination with anti-Herpes Nucleoside Analogues." Antiviral Chemistry and Chemotherapy 4, no. 1 (February 1993): 41–47. http://dx.doi.org/10.1177/095632029300400105.

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The treatment of the severe and often life-threatening herpesvirus infections which commonly occur in AIDS patients is complicated by the need to treat simultaneously with drugs directed against the human immunodeficiency virus (HIV). Combining together different drugs in this way can lead to effects upon the activities of the individual drugs, such as synergism or antagonism. The effect upon the anti-HIV activity of 3′-azido-3′-deoxythymidine (AZT) and 3′-fluoro-3′-deoxythymidine (FLT) of combination with the anti-herpesvirus drugs 9-(1,3-dihydroxy-2-propoxymethyl-)guanine (DHPG; ganciclovir) and (-)-9-[4-hydroxy-2-(hydroxymethyl)butyl]guanine ([-]-2HM-HBG) was investigated. Neither DHPG nor (-)-2HM-HBG showed antiviral activity against HIV-1 up to 50 [AM. When combined with AZT or FLT at ratios of antiherpes:anti-HIV drug of 10:1 or greater, both DHPG and (-)-2HM-HBG antagonized the anti-HIV activity of AZT and FLT. When combined at a lower ratio (1:1), there was no effect upon the anti-HIV activity of either AZT or FLT. The phosphorylation of FLT was found to be unchanged in the presence of DHPG or (-)-2HM-HBG, indicating that the mechanism of the antagonism was not owing to an effect of DHPG or (-)-2HM-HBG upon the metabolism of the anti-HIV drugs. The results suggest that combination chemotherapy with the anti-herpes drugs DHPG/(-)-2HM-HBG and AZT/FLT should be used cautiously. The possibility of such antagonistic interactions should be borne in mind when considering the choice of drug and ratio for treatment of herpesvirus infections in AIDS patients on anti-HIV therapy.

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Journal articles on the topic 'Anti-HIV treatment'

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