HIV
... • There are currently 7 FDAapproved NRTI’s and one nucleotide analog. • The first anti-HIV drug approved was the NRTI known as AZT or Zidovudine (1987). • AZT was discovered as a treatment of AIDS during a screening process for the identification of effective AIDS treatments. • Antiviral selectivity ...
... • There are currently 7 FDAapproved NRTI’s and one nucleotide analog. • The first anti-HIV drug approved was the NRTI known as AZT or Zidovudine (1987). • AZT was discovered as a treatment of AIDS during a screening process for the identification of effective AIDS treatments. • Antiviral selectivity ...
An Overview of HIV Drugs
... 1st approved drug for the treatment of AIDS Phosphorylated by 3 cellular enzymes to form an active nucleotide triphosphate Analogue of deoxythymidine where the 3’ hydroxyl is replaced by an azide group The triphosphate is attached to the growing DNA chain, but cannot be extended. Side effe ...
... 1st approved drug for the treatment of AIDS Phosphorylated by 3 cellular enzymes to form an active nucleotide triphosphate Analogue of deoxythymidine where the 3’ hydroxyl is replaced by an azide group The triphosphate is attached to the growing DNA chain, but cannot be extended. Side effe ...
FEP-Guidance for Rapid Lead Optimization of Anti-HIV
... FEP-Guidance for Rapid Lead Optimization of Anti-HIV Agents William L. Jorgensen Department of Chemistry, Yale University, New Haven, CT 06520-8107 Drug development is being pursued through computer-aided design, synthesis, and assaying. The design begins with use of the BOMB program, which rapidly ...
... FEP-Guidance for Rapid Lead Optimization of Anti-HIV Agents William L. Jorgensen Department of Chemistry, Yale University, New Haven, CT 06520-8107 Drug development is being pursued through computer-aided design, synthesis, and assaying. The design begins with use of the BOMB program, which rapidly ...
NRTIs NNRTIs PIs Entry Inhibitor Integrase Inhibitors MOA Inhibits
... Entry/Fusion Inhibitors MOA: CCR5 receptor antagonist—prevents CCR5 tropic HIV entry into cells ...
... Entry/Fusion Inhibitors MOA: CCR5 receptor antagonist—prevents CCR5 tropic HIV entry into cells ...
CFAR research in progress talk
... – Effective but have potential disadvantages – May be the preferred regimen in individual patients Acceptable – Less virologic efficacy, lack of efficacy data, or greater toxicities ...
... – Effective but have potential disadvantages – May be the preferred regimen in individual patients Acceptable – Less virologic efficacy, lack of efficacy data, or greater toxicities ...
HIV Infection in Solid Organ Transplant Patients
... Most PIs are potent CYP3A4 inhibitors Ritonavir (most), saquinavir (least) ...
... Most PIs are potent CYP3A4 inhibitors Ritonavir (most), saquinavir (least) ...
antiretroviral_Hamme..
... viral turnover and the inherent error rate of reverse transcriptase. Therefore, mutations at each base position occur daily. The survival of the resulting viral mutants depends on the replication competence of the mutants and the presence of drug or immune selective pressure. B. The implications of ...
... viral turnover and the inherent error rate of reverse transcriptase. Therefore, mutations at each base position occur daily. The survival of the resulting viral mutants depends on the replication competence of the mutants and the presence of drug or immune selective pressure. B. The implications of ...
Next-Generation NNRTIs: Etravirine and Rilpivirine
... In vitro studies of rilpivirine indicate that the drug candidate is active against NNRTI-resistant strains of HIV— including many with double or triple mutations. Like etravirine, rilpivirine appears to have a higher genetic barrier to resistance compared with older NNRTIs. The in vivo anti-HIV acti ...
... In vitro studies of rilpivirine indicate that the drug candidate is active against NNRTI-resistant strains of HIV— including many with double or triple mutations. Like etravirine, rilpivirine appears to have a higher genetic barrier to resistance compared with older NNRTIs. The in vivo anti-HIV acti ...
Discovery and development of non-nucleoside reverse-transcriptase inhibitors
Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are antiretroviral drugs used in the treatment of human immunodeficiency virus (HIV). NNRTIs inhibit reverse transcriptase (RT), an enzyme that controls the replication of the genetic material of HIV. RT is one of the most popular targets in the field of antiretroviral drug development.Discovery and development of NNRTIs began in the late 1980s and in the end of 2009 four NNRTI had been approved by regulatory authorities and several others were undergoing clinical development. Drug resistance develops quickly if NNRTIs are administered as monotherapy and therefore NNRTIs are always given as part of combination therapy, the highly active antiretroviral therapy (HAART).