BIOMAT Database Logo BIOMAT Database Logo

The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic. 2019

Vigneshwaran Namasivayam, and Murugesan Vanangamudi, and Victor G Kramer, and Sonali Kurup, and Peng Zhan, and Xinyong Liu, and Jacob Kongsted, and Siddappa N Byrareddy
Pharmaceutical Institute, Pharmaceutical Chemistry II , University of Bonn , 53121 Bonn , Germany.

Human immunodeficiency virus (HIV) infection is now pandemic. Targeting HIV-1 reverse transcriptase (HIV-1 RT) has been considered as one of the most successful targets for the development of anti-HIV treatment. Among the HIV-1 RT inhibitors, non-nucleoside reverse transcriptase inhibitors (NNRTIs) have gained a definitive place due to their unique antiviral potency, high specificity, and low toxicity in antiretroviral combination therapies used to treat HIV. Until now, >50 structurally diverse classes of compounds have been reported as NNRTIs. Among them, six NNRTIs were approved for HIV-1 treatment, namely, nevirapine (NVP), delavirdine (DLV), efavirenz (EFV), etravirine (ETR), rilpivirine (RPV), and doravirine (DOR). In this perspective, we focus on the six NNRTIs and lessons learned from their journey through development to clinical studies. It demonstrates the obligatory need of understanding the physicochemical and biological principles (lead optimization), resistance mutations, synthesis, and clinical requirements for drugs.

UI MeSH Term Description Entries
D002986 Clinical Trials as Topic Works about pre-planned studies of the safety, efficacy, or optimum dosage schedule (if appropriate) of one or more diagnostic, therapeutic, or prophylactic drugs, devices, or techniques selected according to predetermined criteria of eligibility and observed for predefined evidence of favorable and unfavorable effects. This concept includes clinical trials conducted both in the U.S. and in other countries. Clinical Trial as Topic
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D015497 HIV-1 The type species of LENTIVIRUS and the etiologic agent of AIDS. It is characterized by its cytopathic effect and affinity for the T4-lymphocyte. Human immunodeficiency virus 1,HIV-I,Human Immunodeficiency Virus Type 1,Immunodeficiency Virus Type 1, Human
D015658 HIV Infections Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS). HTLV-III Infections,HTLV-III-LAV Infections,T-Lymphotropic Virus Type III Infections, Human,HIV Coinfection,Coinfection, HIV,Coinfections, HIV,HIV Coinfections,HIV Infection,HTLV III Infections,HTLV III LAV Infections,HTLV-III Infection,HTLV-III-LAV Infection,Infection, HIV,Infection, HTLV-III,Infection, HTLV-III-LAV,Infections, HIV,Infections, HTLV-III,Infections, HTLV-III-LAV,T Lymphotropic Virus Type III Infections, Human
D055808 Drug Discovery The process of finding chemicals for potential therapeutic use. Drug Prospecting,Discovery, Drug,Prospecting, Drug
D018894 Reverse Transcriptase Inhibitors Inhibitors of reverse transcriptase (RNA-DIRECTED DNA POLYMERASE), an enzyme that synthesizes DNA on an RNA template. Reverse Transcriptase Inhibitor,Inhibitors, Reverse Transcriptase,Inhibitor, Reverse Transcriptase,Transcriptase Inhibitor, Reverse
D019380 Anti-HIV Agents Agents used to treat AIDS and/or stop the spread of the HIV infection. These do not include drugs used to treat symptoms or opportunistic infections associated with AIDS. AIDS Drug,AIDS Drugs,Anti-AIDS Agents,Anti-AIDS Drug,Anti-HIV Agent,Anti-HIV Drug,Anti-AIDS Drugs,Anti-HIV Drugs,Agent, Anti-HIV,Agents, Anti-AIDS,Agents, Anti-HIV,Anti AIDS Agents,Anti AIDS Drug,Anti AIDS Drugs,Anti HIV Agent,Anti HIV Agents,Anti HIV Drug,Anti HIV Drugs,Drug, AIDS,Drug, Anti-AIDS,Drug, Anti-HIV,Drugs, AIDS,Drugs, Anti-AIDS,Drugs, Anti-HIV

Related Publications

Vigneshwaran Namasivayam, and Murugesan Vanangamudi, and Victor G Kramer, and Sonali Kurup, and Peng Zhan, and Xinyong Liu, and Jacob Kongsted, and Siddappa N Byrareddy
[Progress in HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs)].
August 2004, Yao xue xue bao = Acta pharmaceutica Sinica,
Vigneshwaran Namasivayam, and Murugesan Vanangamudi, and Victor G Kramer, and Sonali Kurup, and Peng Zhan, and Xinyong Liu, and Jacob Kongsted, and Siddappa N Byrareddy
Current and emerging non-nucleoside reverse transcriptase inhibitors (NNRTIs) for HIV-1 treatment.
October 2019, Expert opinion on drug metabolism & toxicology,
Vigneshwaran Namasivayam, and Murugesan Vanangamudi, and Victor G Kramer, and Sonali Kurup, and Peng Zhan, and Xinyong Liu, and Jacob Kongsted, and Siddappa N Byrareddy
Perspectives of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection.
January 1999, Farmaco (Societa chimica italiana : 1989),
Vigneshwaran Namasivayam, and Murugesan Vanangamudi, and Victor G Kramer, and Sonali Kurup, and Peng Zhan, and Xinyong Liu, and Jacob Kongsted, and Siddappa N Byrareddy
The role of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection.
June 1998, Antiviral research,
Vigneshwaran Namasivayam, and Murugesan Vanangamudi, and Victor G Kramer, and Sonali Kurup, and Peng Zhan, and Xinyong Liu, and Jacob Kongsted, and Siddappa N Byrareddy
Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs).
January 2008, Bioorganic & medicinal chemistry letters,
Vigneshwaran Namasivayam, and Murugesan Vanangamudi, and Victor G Kramer, and Sonali Kurup, and Peng Zhan, and Xinyong Liu, and Jacob Kongsted, and Siddappa N Byrareddy
Non-nucleoside reverse transcriptase inhibitors (NNRTIs): past, present, and future.
January 2004, Chemistry & biodiversity,
Vigneshwaran Namasivayam, and Murugesan Vanangamudi, and Victor G Kramer, and Sonali Kurup, and Peng Zhan, and Xinyong Liu, and Jacob Kongsted, and Siddappa N Byrareddy
Resistance to non-nucleoside inhibitors of HIV-1 reverse transcriptase.
February 1999, Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy,
Vigneshwaran Namasivayam, and Murugesan Vanangamudi, and Victor G Kramer, and Sonali Kurup, and Peng Zhan, and Xinyong Liu, and Jacob Kongsted, and Siddappa N Byrareddy
Hypersusceptibility to non-nucleoside reverse transcriptase inhibitors in HIV-1.
June 2003, AIDS (London, England),
Vigneshwaran Namasivayam, and Murugesan Vanangamudi, and Victor G Kramer, and Sonali Kurup, and Peng Zhan, and Xinyong Liu, and Jacob Kongsted, and Siddappa N Byrareddy
New non-nucleoside reverse transcriptase inhibitors (NNRTIs) in development for the treatment of HIV infections.
October 2004, Current opinion in pharmacology,
Vigneshwaran Namasivayam, and Murugesan Vanangamudi, and Victor G Kramer, and Sonali Kurup, and Peng Zhan, and Xinyong Liu, and Jacob Kongsted, and Siddappa N Byrareddy
Unbinding Dynamics of Non-Nucleoside Inhibitors from HIV-1 Reverse Transcriptase.
February 2019, The journal of physical chemistry. B,
Copied contents to your clipboard!