Literature DB >> 24052331

Dolutegravir: first global approval.

Anita D Ballantyne1, Caroline M Perry.   

Abstract

Dolutegravir, an orally administered HIV-1 integrase strand transfer inhibitor (INSTI), is under development by ViiV Healthcare. Like other drugs belonging in the INSTI class of antiretroviral agents, dolutegravir binds to the integrase site of HIV-1 and blocks the strand transfer integration step, thereby preventing the replication of HIV-1. Dolutegravir is being developed as an unboosted once-daily therapy for use in combination with other antiretroviral agents for the treatment of both treatment-naïve and treatment-experienced patients with HIV-1 infection. Dolutegravir has been approved in the USA for the treatment of HIV-1 infection in combination with other antiretroviral agents and has been filed for approval in the EU and Canada. Phase III development is underway in North America, Europe, South Africa, South America, Australia and Taiwan. This article summarizes the milestones in the development of dolutegravir leading to this first approval for the treatment of HIV-1 infection in both therapy-naïve and -experienced patients.

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Year:  2013        PMID： 24052331     DOI： 10.1007/s40265-013-0121-4

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


  29 in total

1.  Effect of atazanavir and atazanavir/ritonavir on the pharmacokinetics of the next-generation HIV integrase inhibitor, S/GSK1349572.

Authors:  Ivy Song; Julie Borland; Shuguang Chen; Yu Lou; Amanda Peppercorn; Toshihiro Wajima; Sherene Min; Stephen C Piscitelli
Journal:  Br J Clin Pharmacol       Date:  2011-07       Impact factor: 4.335

2.  Dolutegravir versus raltegravir in antiretroviral-experienced, integrase-inhibitor-naive adults with HIV: week 48 results from the randomised, double-blind, non-inferiority SAILING study.

Authors:  Pedro Cahn; Anton L Pozniak; Horacio Mingrone; Andrey Shuldyakov; Carlos Brites; Jaime F Andrade-Villanueva; Gary Richmond; Carlos Beltran Buendia; Jan Fourie; Moti Ramgopal; Debbie Hagins; Franco Felizarta; Jose Madruga; Tania Reuter; Tamara Newman; Catherine B Small; John Lombaard; Beatriz Grinsztejn; David Dorey; Mark Underwood; Sandy Griffith; Sherene Min
Journal:  Lancet       Date:  2013-07-03       Impact factor: 79.321

3.  Prevalent polymorphisms in wild-type HIV-1 integrase are unlikely to engender drug resistance to dolutegravir (S/GSK1349572).

Authors:  Cindy Vavro; Samiul Hasan; Heather Madsen; Joseph Horton; Felix DeAnda; Louise Martin-Carpenter; Akihiko Sato; Robert Cuffe; Shuguang Chen; Mark Underwood; Garrett Nichols
Journal:  Antimicrob Agents Chemother       Date:  2013-01-07       Impact factor: 5.191

4.  Lack of interaction between the HIV integrase inhibitor S/GSK1349572 and tenofovir in healthy subjects.

Authors:  Ivy Song; Sherene S Min; Julie Borland; Yu Lou; Shuguang Chen; Toru Ishibashi; Toshihiro Wajima; Stephen C Piscitelli
Journal:  J Acquir Immune Defic Syndr       Date:  2010-11       Impact factor: 3.731

5.  Effects of etravirine alone and with ritonavir-boosted protease inhibitors on the pharmacokinetics of dolutegravir.

Authors:  Ivy Song; Julie Borland; Sherene Min; Yu Lou; Shuguang Chen; Parul Patel; Toshihiro Wajima; Stephen C Piscitelli
Journal:  Antimicrob Agents Chemother       Date:  2011-05-09       Impact factor: 5.191

6.  Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers.

Authors:  Sherene Min; Ivy Song; Julie Borland; Shuguang Chen; Yu Lou; Tamio Fujiwara; Stephen C Piscitelli
Journal:  Antimicrob Agents Chemother       Date:  2009-11-02       Impact factor: 5.191

7.  Safety, tolerability, and pharmacokinetics of the HIV integrase inhibitor dolutegravir given twice daily with rifampin or once daily with rifabutin: results of a phase 1 study among healthy subjects.

Authors:  Kelly E Dooley; Patrick Sayre; Julie Borland; Elizabeth Purdy; Shuguang Chen; Ivy Song; Amanda Peppercorn; Stephanie Everts; Stephen Piscitelli; Charles Flexner
Journal:  J Acquir Immune Defic Syndr       Date:  2013-01-01       Impact factor: 3.731

8.  Once-daily dolutegravir versus raltegravir in antiretroviral-naive adults with HIV-1 infection: 48 week results from the randomised, double-blind, non-inferiority SPRING-2 study.

Authors:  Francois Raffi; Anita Rachlis; Hans-Jürgen Stellbrink; W David Hardy; Carlo Torti; Chloe Orkin; Mark Bloch; Daniel Podzamczer; Vadim Pokrovsky; Federico Pulido; Steve Almond; David Margolis; Clare Brennan; Sherene Min
Journal:  Lancet       Date:  2013-01-08       Impact factor: 79.321

Review 9.  HIV-1 antiretroviral resistance: scientific principles and clinical applications.

Authors:  Michele W Tang; Robert W Shafer
Journal:  Drugs       Date:  2012-06-18       Impact factor: 9.546

Review 10.  Clinical use of HIV integrase inhibitors: a systematic review and meta-analysis.

Authors:  Peter Messiaen; Annemarie M J Wensing; Axel Fun; Monique Nijhuis; Nele Brusselaers; Linos Vandekerckhove
Journal:  PLoS One       Date:  2013-01-09       Impact factor: 3.240
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  15 in total

1.  Biochemical activity of RAGs is impeded by Dolutegravir, an HIV integrase inhibitor.

Authors:  Namrata M Nilavar; Amita M Paranjape; Sathees C Raghavan
Journal:  Cell Death Discov       Date:  2020-06-12

2.  The R262K substitution combined with H51Y in HIV-1 subtype B integrase confers low-level resistance against dolutegravir.

Authors:  Vincent Cutillas; Thibault Mesplede; Kaitlin Anstett; Said Hassounah; Mark A Wainberg
Journal:  Antimicrob Agents Chemother       Date:  2014-10-27       Impact factor: 5.191

Review 3.  HIV-1 gag: an emerging target for antiretroviral therapy.

Authors:  Philip R Tedbury; Eric O Freed
Journal:  Curr Top Microbiol Immunol       Date:  2015       Impact factor: 4.291

4.  Cellular Immune Response Induced by DNA Immunization of Mice with Drug Resistant Integrases of HIV-1 Clade A Offers Partial Protection against Growth and Metastatic Activity of Integrase-Expressing Adenocarcinoma Cells.

Authors:  Maria Isaguliants; Olga Krotova; Stefan Petkov; Juris Jansons; Ekaterina Bayurova; Dzeina Mezale; Ilze Fridrihsone; Athina Kilpelainen; Philip Podschwadt; Yulia Agapkina; Olga Smirnova; Linda Kostic; Mina Saleem; Oleg Latyshev; Olesja Eliseeva; Anastasia Malkova; Tatiana Gorodnicheva; Britta Wahren; Ilya Gordeychuk; Elizaveta Starodubova; Anastasia Latanova
Journal:  Microorganisms       Date:  2021-06-04

Review 5.  6,7-Dihydroxyisoindolin-1-one and 7,8-Dihydroxy-3,4-Dihydroisoquinolin- 1(2H)-one Based HIV-1 Integrase Inhibitors.

Authors:  Xue Zhi Zhao; Mathieu Metifiot; Steven J Smith; Kasthuraiah Maddali; Christophe Marchand; Stephen H Hughes; Yves Pommier; Terrence R Burke
Journal:  Curr Top Med Chem       Date:  2016       Impact factor: 3.295

Review 6.  Elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate single-tablet regimen (Stribild®): a review of its use in the management of HIV-1 infection in adults.

Authors:  Caroline M Perry
Journal:  Drugs       Date:  2014-01       Impact factor: 11.431

7.  Bicyclic 1-hydroxy-2-oxo-1,2-dihydropyridine-3-carboxamide-containing HIV-1 integrase inhibitors having high antiviral potency against cells harboring raltegravir-resistant integrase mutants.

Authors:  Xue Zhi Zhao; Steven J Smith; Mathieu Métifiot; Barry C Johnson; Christophe Marchand; Yves Pommier; Stephen H Hughes; Terrence R Burke
Journal:  J Med Chem       Date:  2014-02-10       Impact factor: 7.446

8.  4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.

Authors:  Xue Zhi Zhao; Steven J Smith; Mathieu Métifiot; Christophe Marchand; Paul L Boyer; Yves Pommier; Stephen H Hughes; Terrence R Burke
Journal:  J Med Chem       Date:  2014-06-16       Impact factor: 7.446

9.  The M50I polymorphic substitution in association with the R263K mutation in HIV-1 subtype B integrase increases drug resistance but does not restore viral replicative fitness.

Authors:  Melissa Wares; Thibault Mesplède; Peter K Quashie; Nathan Osman; Yingshan Han; Mark A Wainberg
Journal:  Retrovirology       Date:  2014-01-17       Impact factor: 4.602

10.  HIV-1 Integrase Strand Transfer Inhibitors with Reduced Susceptibility to Drug Resistant Mutant Integrases.

Authors:  Xue Zhi Zhao; Steven J Smith; Daniel P Maskell; Mathieu Metifiot; Valerie E Pye; Katherine Fesen; Christophe Marchand; Yves Pommier; Peter Cherepanov; Stephen H Hughes; Terrence R Burke
Journal:  ACS Chem Biol       Date:  2016-02-05       Impact factor: 5.100
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