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A Review on Pharmacokinetics Properties of Antiretroviral Drugs to Treat HIV-1 Infections

Author(s):

Mohd. Aqueel Khan, Krishna Kant Gupta and Sanjeev Kumar Singh*   Pages 1 - 15 ( 15 )

Abstract:


Background: The HIV-1 pandemic is undoubtedly the major public-health crisis of our time. The extensive research on HIV has deepened our understanding of its pathogenesis and transmission dynamics. Some new entity molecules have been approved by the FDA for HIV treatment but till now protective vaccine remains elusive. Scientists are targeting many important proteins of HIV-1; gp41, gp120, CCR5 coreceptor, integrase, reverse transcriptase and protease. Few compounds are used as nucleotide analogues to stop HIV replication. Altogether, these compounds and their derivatives specifically block HIV entry and DNA replication. Using ADMET studies, people are working on these compounds to reduce toxicity and increase potency.

Objective: Our main aim is to discuss the Pharmacokinetics properties of 23 important FDA antiretroviral drugs used for the treatment of HIV-1 infections.

Methods: We have searched literature related to pharmacokinetics properties in PubMed, Google Scholar search engine.

Conclusion: Here, we have reviewed the pharmacokinetic properties such as absorption, bioavailability, distribution, metabolism, and excretion, of important 23 FDA approved drugs. The drugs namely Fuzeon, Selzentry, Complera, Epivir, Retrovir, Emtriva, Ziagen, Edurant, Intelence, Pifeltro, Sustiva, Viramune, Isentress, Genvoya, Tivicay, Reyataz, Prezista, Lexiva, Invirase, Aptivus etc. are classified into five major classes: fusion inhibitors, Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs), Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs), Integrase Strand transfer inhibitors (INSTIs) and Protease inhibitors (PIs). This Review may helpful for the future development of potent antiretroviral drugs with improved pharmacokinetic properties.

Keywords:

HIV, Pharmacokinetics, Antiretroviral drugs, Protease, Integrase, ADMET, Reverse Transcriptase.

Affiliation:

Computer Aided Drug Designing & Molecular Modelling Lab, Department of Bioinformatics, Alagappa University, Karaikudi-630004, Tamil Nadu, Bioinformatics Division, School of Chemical & Biotechnology, SASTRA Deemed University, Tirumalaisamudram, Thanjavur – 613401, Tamil Nadu, Computer Aided Drug Designing & Molecular Modelling Lab, Department of Bioinformatics, Alagappa University, Karaikudi-630004, Tamil Nadu



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