Literature DB >> 28507107

In Vitro Cross-Resistance Profiles of Rilpivirine, Dapivirine, and MIV-150, Nonnucleoside Reverse Transcriptase Inhibitor Microbicides in Clinical Development for the Prevention of HIV-1 Infection.

Nicholas S Giacobbi1, Nicolas Sluis-Cremer2.   

Abstract

Rilpivirine (RPV), dapivirine (DPV), and MIV-150 are in development as microbicides. It is not known whether they will block infection of circulating nonnucleoside reverse transcriptase inhibitor (NNRTI)-resistant human immunodeficiency virus type 1 (HIV-1) variants. Here, we demonstrate that the activity of DPV and MIV-150 is compromised by many resistant viruses containing single or double substitutions. High DPV genital tract concentrations from DPV ring use may block replication of resistant viruses. However, MIV-150 genital tract concentrations may be insufficient to inhibit many resistant viruses, including those harboring K103N or Y181C.
Copyright © 2017 American Society for Microbiology.

Entities:  

Keywords:  HIV-1; MIV-150; NNRTI; antiretroviral resistance; dapivirine; prevention

Mesh:

Substances:

Year:  2017        PMID: 28507107      PMCID: PMC5487620          DOI: 10.1128/AAC.00277-17

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN: 0066-4804            Impact factor:   5.191


  23 in total

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3.  Phase 1 Safety, Pharmacokinetics, and Pharmacodynamics of Dapivirine and Maraviroc Vaginal Rings: A Double-Blind Randomized Trial.

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Journal:  J Acquir Immune Defic Syndr       Date:  2015-11-01       Impact factor: 3.731

4.  In vitro resistance profile of the candidate HIV-1 microbicide drug dapivirine.

Authors:  Susan M Schader; Maureen Oliveira; Ruxandra-Ilinca Ibanescu; Daniela Moisi; Susan P Colby-Germinario; Mark A Wainberg
Journal:  Antimicrob Agents Chemother       Date:  2011-11-28       Impact factor: 5.191

5.  Resistance and cross-resistance profile of the diaryltriazine NNRTI and candidate microbicide UAMC01398.

Authors:  Kevin K Ariën; Muthusamy Venkatraj; Johan Michiels; Jurgen Joossens; Katleen Vereecken; Pieter Van der Veken; Jan Heeres; Hans De Winter; Leo Heyndrickx; Koen Augustyns; Guido Vanham
Journal:  J Antimicrob Chemother       Date:  2016-02-04       Impact factor: 5.790

6.  Long-acting rilpivirine as potential pre-exposure prophylaxis for HIV-1 prevention (the MWRI-01 study): an open-label, phase 1, compartmental, pharmacokinetic and pharmacodynamic assessment.

Authors:  Ian McGowan; Charlene S Dezzutti; Aaron Siegel; Jarret Engstrom; Alexiy Nikiforov; Kathryn Duffill; Cory Shetler; Nicola Richardson-Harman; Kaleab Abebe; David Back; Laura Else; Deidre Egan; Saye Khoo; James E Egan; Ronald Stall; Peter E Williams; Khaleel K Rehman; Amy Adler; Rhonda M Brand; Beatrice Chen; Sharon Achilles; Ross D Cranston
Journal:  Lancet HIV       Date:  2016-09-16       Impact factor: 12.767

7.  Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.

Authors:  Gerben van 't Klooster; Eva Hoeben; Herman Borghys; Adriana Looszova; Marie-Paule Bouche; Frans van Velsen; Lieven Baert
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8.  Global trends in antiretroviral resistance in treatment-naive individuals with HIV after rollout of antiretroviral treatment in resource-limited settings: a global collaborative study and meta-regression analysis.

Authors:  Ravindra K Gupta; Michael R Jordan; Binta J Sultan; Andrew Hill; Daniel H J Davis; John Gregson; Anthony W Sawyer; Raph L Hamers; Nicaise Ndembi; Deenan Pillay; Silvia Bertagnolio
Journal:  Lancet       Date:  2012-07-23       Impact factor: 79.321

9.  Geographic and temporal trends in the molecular epidemiology and genetic mechanisms of transmitted HIV-1 drug resistance: an individual-patient- and sequence-level meta-analysis.

Authors:  Soo-Yon Rhee; Jose Luis Blanco; Michael R Jordan; Jonathan Taylor; Philippe Lemey; Vici Varghese; Raph L Hamers; Silvia Bertagnolio; Tobias F Rinke de Wit; Avelin F Aghokeng; Jan Albert; Radko Avi; Santiago Avila-Rios; Pascal O Bessong; James I Brooks; Charles A B Boucher; Zabrina L Brumme; Michael P Busch; Hermann Bussmann; Marie-Laure Chaix; Bum Sik Chin; Toni T D'Aquin; Cillian F De Gascun; Anne Derache; Diane Descamps; Alaka K Deshpande; Cyrille F Djoko; Susan H Eshleman; Herve Fleury; Pierre Frange; Seiichiro Fujisaki; P Richard Harrigan; Junko Hattori; Africa Holguin; Gillian M Hunt; Hiroshi Ichimura; Pontiano Kaleebu; David Katzenstein; Sasisopin Kiertiburanakul; Jerome H Kim; Sung Soon Kim; Yanpeng Li; Irja Lutsar; Lynn Morris; Nicaise Ndembi; Kee Peng Ng; Ramesh S Paranjape; Martine Peeters; Mario Poljak; Matt A Price; Manon L Ragonnet-Cronin; Gustavo Reyes-Terán; Morgane Rolland; Sunee Sirivichayakul; Davey M Smith; Marcelo A Soares; Vincent V Soriano; Deogratius Ssemwanga; Maja Stanojevic; Mariane A Stefani; Wataru Sugiura; Somnuek Sungkanuparph; Amilcar Tanuri; Kok Keng Tee; Hong-Ha M Truong; David A M C van de Vijver; Nicole Vidal; Chunfu Yang; Rongge Yang; Gonzalo Yebra; John P A Ioannidis; Anne-Mieke Vandamme; Robert W Shafer
Journal:  PLoS Med       Date:  2015-04-07       Impact factor: 11.069

10.  Exposure to MIV-150 from a high-dose intravaginal ring results in limited emergence of drug resistance mutations in SHIV-RT infected rhesus macaques.

Authors:  Mayla Hsu; Brandon F Keele; Meropi Aravantinou; Noa Krawczyk; Samantha Seidor; Ciby J Abraham; Shimin Zhang; Aixa Rodriguez; Larisa Kizima; Nina Derby; Ninochka Jean-Pierre; Olga Mizenina; Agegnehu Gettie; Brooke Grasperge; James Blanchard; Michael J Piatak; Jeffrey D Lifson; José A Fernández-Romero; Thomas M Zydowsky; Melissa Robbiani
Journal:  PLoS One       Date:  2014-02-27       Impact factor: 3.240

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  8 in total

1.  Conformational Changes in HIV-1 Reverse Transcriptase that Facilitate Its Maturation.

Authors:  Ryan L Slack; Tatiana V Ilina; Zhaoyong Xi; Nicholas S Giacobbi; Gota Kawai; Michael A Parniak; Stefan G Sarafianos; Nicolas Sluis Cremer; Rieko Ishima
Journal:  Structure       Date:  2019-08-27       Impact factor: 5.006

2.  Nonnucleoside Reverse Transcriptase Inhibitor Hypersusceptibility and Resistance by Mutation of Residue 181 in HIV-1 Reverse Transcriptase.

Authors:  John P Barnard; Kelly D Huber; Nicolas Sluis-Cremer
Journal:  Antimicrob Agents Chemother       Date:  2019-07-25       Impact factor: 5.191

3.  Frequent cross-resistance to rilpivirine among subtype C HIV-1 from first-line antiretroviral therapy failures in South Africa.

Authors:  Kerri J Penrose; Chanson J Brumme; Maritsa Scoulos-Hanson; Kristen Hamanishi; Kelley Gordon; Raquel V Viana; Carole L Wallis; P Richard Harrigan; John W Mellors; Urvi M Parikh
Journal:  Antivir Chem Chemother       Date:  2018 Jan-Dec

4.  Long-Acting Rilpivirine (RPV) Preexposure Prophylaxis Does Not Inhibit Vaginal Transmission of RPV-Resistant HIV-1 or Select for High-Frequency Drug Resistance in Humanized Mice.

Authors:  Kevin Melody; Chandra N Roy; Christopher Kline; Mackenzie L Cottrell; Dwayne Evans; Kathleen Shutt; Pleuni S Pennings; Brandon F Keele; Moses Bility; Angela D M Kashuba; Zandrea Ambrose
Journal:  J Virol       Date:  2020-03-31       Impact factor: 6.549

Review 5.  Approved HIV reverse transcriptase inhibitors in the past decade.

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6.  APOBEC3 selects V179I in HIV-1 reverse transcriptase to provide selective advantage for non-nucleoside reverse transcriptase inhibitor-resistant mutants.

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Review 7.  Indolylarylsulfones, a fascinating story of highly potent human immunodeficiency virus type 1 non-nucleoside reverse transcriptase inhibitors.

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8.  Structural basis for potent and broad inhibition of HIV-1 RT by thiophene[3,2-d]pyrimidine non-nucleoside inhibitors.

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