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.
Synthesis, Biological Activity, Pharmacokinetic Properties and Molecular Modelling Studies of Novel 1H,3H-Oxazolo[3,4-a]Benzimidazoles: Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors
