Literature DB >> 29564777

Bictegravir: First Global Approval.

Anthony Markham1.   

Abstract

Gilead Sciences has developed a single tablet anti-HIV-1 medication (Biktarvy®) combining the novel integrase strand transfer inhibitor (INSTI) bictegravir with the nucleos(t)ide reverse transcriptase inhibitors (NRTIs) emtricitabine and tenofovir alafenamide. This fixed dose combination has demonstrated efficacy as treatment for both anti-retroviral naïve and virologically suppressed HIV-1 infection in patients switching therapy, and was recently approved in the USA. This article summarizes the milestones in the development of bictegravir leading to this first approval of bictegravir/emtricitabine/tenofovir alafenamide as treatment for HIV-1 infection.

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Year:  2018        PMID： 29564777     DOI： 10.1007/s40265-018-0896-4

Source DB:  PubMed          Journal:  Drugs        ISSN： 0012-6667            Impact factor:   11.431


  6 in total

1.  Antiretroviral Drugs for Treatment and Prevention of HIV Infection in Adults: 2016 Recommendations of the International Antiviral Society-USA Panel.

Authors:  Huldrych F Günthard; Michael S Saag; Constance A Benson; Carlos del Rio; Joseph J Eron; Joel E Gallant; Jennifer F Hoy; Michael J Mugavero; Paul E Sax; Melanie A Thompson; Rajesh T Gandhi; Raphael J Landovitz; Davey M Smith; Donna M Jacobsen; Paul A Volberding
Journal:  JAMA       Date:  2016-07-12       Impact factor: 56.272

2.  Antiviral Activity of Bictegravir and Cabotegravir against Integrase Inhibitor-Resistant SIVmac239 and HIV-1.

Authors:  Said A Hassounah; Ahmad Alikhani; Maureen Oliveira; Simrat Bharaj; Ruxandra-Ilinca Ibanescu; Nathan Osman; Hong-Tao Xu; Bluma G Brenner; Thibault Mesplède; Mark A Wainberg
Journal:  Antimicrob Agents Chemother       Date:  2017-11-22       Impact factor: 5.191

3.  Coformulated bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir with emtricitabine and tenofovir alafenamide, for initial treatment of HIV-1 infection (GS-US-380-1490): a randomised, double-blind, multicentre, phase 3, non-inferiority trial.

Authors:  Paul E Sax; Anton Pozniak; M Luisa Montes; Ellen Koenig; Edwin DeJesus; Hans-Jürgen Stellbrink; Andrea Antinori; Kimberly Workowski; Jihad Slim; Jacques Reynes; Will Garner; Joseph Custodio; Kirsten White; Devi SenGupta; Andrew Cheng; Erin Quirk
Journal:  Lancet       Date:  2017-08-31       Impact factor: 79.321

4.  Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile.

Authors:  Manuel Tsiang; Gregg S Jones; Joshua Goldsmith; Andrew Mulato; Derek Hansen; Elaine Kan; Luong Tsai; Rujuta A Bam; George Stepan; Kirsten M Stray; Anita Niedziela-Majka; Stephen R Yant; Helen Yu; George Kukolj; Tomas Cihlar; Scott E Lazerwith; Kirsten L White; Haolun Jin
Journal:  Antimicrob Agents Chemother       Date:  2016-11-21       Impact factor: 5.191

5.  Antiviral Activity, Safety, and Pharmacokinetics of Bictegravir as 10-Day Monotherapy in HIV-1-Infected Adults.

Authors:  Joel E Gallant; Melanie Thompson; Edwin DeJesus; Gene W Voskuhl; Xuelian Wei; Heather Zhang; Kirsten White; Andrew Cheng; Erin Quirk; Hal Martin
Journal:  J Acquir Immune Defic Syndr       Date:  2017-05-01       Impact factor: 3.731

6.  Bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir, abacavir, and lamivudine for initial treatment of HIV-1 infection (GS-US-380-1489): a double-blind, multicentre, phase 3, randomised controlled non-inferiority trial.

Authors:  Joel Gallant; Adriano Lazzarin; Anthony Mills; Chloe Orkin; Daniel Podzamczer; Pablo Tebas; Pierre-Marie Girard; Indira Brar; Eric S Daar; David Wohl; Jürgen Rockstroh; Xuelian Wei; Joseph Custodio; Kirsten White; Hal Martin; Andrew Cheng; Erin Quirk
Journal:  Lancet       Date:  2017-08-31       Impact factor: 79.321
  6 in total
  9 in total

1.  Structural Insights to Human Immunodeficiency Virus (HIV-1) Targets and Their Inhibition.

Authors:  Murugesan Vanangamudi; Pramod C Nair; S E Maida Engels; Senthilkumar Palaniappan; Vigneshwaran Namasivayam
Journal:  Adv Exp Med Biol       Date:  2021       Impact factor: 2.622

Review 2.  Recent advances in the discovery of small-molecule inhibitors of HIV-1 integrase.

Authors:  Eungi Choi; Jayapal Reddy Mallareddy; Dai Lu; Srikanth Kolluru
Journal:  Future Sci OA       Date:  2018-09-06

3.  Treatment modification after starting cART in people living with HIV: retrospective analysis of the German ClinSurv HIV Cohort 2005-2017.

Authors:  Melanie Stecher; Philipp Schommers; Christian Kollan; Matthias Stoll; Frieder Kuhlendahl; Hans-Jürgen Stellbrink; Jan-Christian Wasmuth; Christoph Stephan; Laura Hamacher; Clara Lehmann; Christoph Boesecke; Johannes Bogner; Stefan Esser; Carlos Fritzsche; Annette Haberl; Dirk Schürmann; Olaf Degen; Heinz-August Horst; Christian Hoffmann; Björn Jensen; Carolynne Schwarze-Zander; Martin Platten; Gerd Fätkenheuer; Daniel Schmidt; Barbara Gunsenheimer-Bartmeyer; Jörg Janne Vehreschild
Journal:  Infection       Date:  2020-07-01       Impact factor: 3.553

4.  Physiologically-Based Pharmacokinetic Modeling Combined with Swiss HIV Cohort Study Data Supports No Dose Adjustment of Bictegravir in Elderly Individuals Living With HIV.

Authors:  Felix Stader; Perrine Courlet; Laurent A Decosterd; Manuel Battegay; Catia Marzolini
Journal:  Clin Pharmacol Ther       Date:  2021-02-27       Impact factor: 6.875

Review 5.  Pharmacokinetic drug interactions of integrase strand transfer inhibitors.

Authors:  Chi-Hua Lu; Edward M Bednarczyk; Linda M Catanzaro; Alyssa Shon; Jia-Chen Xu; Qing Ma
Journal:  Curr Res Pharmacol Drug Discov       Date:  2021-08-08

6.  7-Step Flow Synthesis of the HIV Integrase Inhibitor Dolutegravir.

Authors:  Robert E Ziegler; Bimbisar K Desai; Jo-Ann Jee; B Frank Gupton; Thomas D Roper; Timothy F Jamison
Journal:  Angew Chem Int Ed Engl       Date:  2018-05-14       Impact factor: 15.336

7.  Epidemiology and Molecular Transmission Characteristics of HIV in the Capital City of Anhui Province in China.

Authors:  Shan Zheng; Jianjun Wu; Zhongwang Hu; Mengze Gan; Lei Liu; Chang Song; Yanhua Lei; Hai Wang; Lingjie Liao; Yi Feng; Yiming Shao; Yuhua Ruan; Hui Xing
Journal:  Pathogens       Date:  2021-11-29

8.  Switching to a Bictegravir Single Tablet Regimen in Elderly People Living with HIV-1: Data Analysis from the BICTEL Cohort.

Authors:  Alessandro Lazzaro; Elio Gentilini Cacciola; Cristian Borrazzo; Giuseppe Pietro Innocenti; Eugenio Nelson Cavallari; Ivano Mezzaroma; Mario Falciano; Caterina Fimiani; Claudio Maria Mastroianni; Giancarlo Ceccarelli; Gabriella d'Ettorre
Journal:  Diagnostics (Basel)       Date:  2021-12-29

Review 9.  Identification of Potential Drug Targets of Broad-Spectrum Inhibitors with a Michael Acceptor Moiety Using Shotgun Proteomics.

Authors:  Hao-Wei Chu; Bidyadhar Sethy; Pei-Wen Hsieh; Jim-Tong Horng
Journal:  Viruses       Date:  2021-09-02       Impact factor: 5.048
  9 in total

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