June 20, 2016
Gilead Presents Preliminary Data on Bictegravir, an Investigational Integrase Strand Transfer Inhibitor for the Treatment of HIV
– Bictegravir Now Being Evaluated in Phase 3 Studies as Part of a Single Tablet HIV Regimen in Combination with Other Antiretroviral Agents –
“We are pleased to share initial results from the bictegravir clinical
program, including data from the first Phase 1 human trial, which
provided proof of concept for further evaluation of bictegravir as part
of a single tablet regimen,” said
Bictegravir (GS-9883) Data at ASM
Poster 413: Bictegravir (GS-9883), a Novel HIV-1 Integrase Strand Transfer Inhibitor (INSTI) with Optimized In Vitro Resistance Profile
- The study examined the in vitro resistance profile of bictegravir compared to currently available INSTIs dolutegravir (DTG), elvitegravir (EVG) and raltegravir (RAL). Bictegravir demonstrated an improved resistance profile compared to DTG and a markedly improved profile compared to EVG and RAL against a panel of HIV integrase mutant viruses. Results also showed an improved resistance profile against all other INSTIs in patient isolates, particularly those with high-level INSTI resistance.
Poster 414: Discovery of GS-9883, an HIV-1 Integrase Strand Transfer Inhibitor (INSTI) with Improved Pharmacokinetics and In Vitro Resistance Profile
- Several INSTI candidates were tested for a range of properties including HIV-1 potency, metabolic stability, cytotoxicity and protein binding. Bictegravir was shown to be a potent INSTI with improved preclinical pharmacokinetics and an enhanced resistance profile compared to all currently available INSTIs—RAL, EVG and DTG. Bictegravir also exhibited a low potential for drug-to-drug interactions.
Poster 415: Novel Integrase Strand Transfer Inhibitor Bictegravir 10 Day Monotherapy in HIV-1 Infected Patients
- Twenty adults (19 male) with chronic HIV infection were treated with bictegravir (5, 25, 50 or 100 mg) or placebo once daily for 10 days to determine changes in HIV-1 RNA levels (viral load). Bictegravir was well tolerated at all dosing levels and provided rapid dose-dependent decreases in viral load that were sustained throughout the treatment period. There were no reports of primary resistance mutations in integrase, no serious adverse events (AEs) and no discontinuations due to AEs.
Poster 416: Antiviral Activity of GS-9883, a Potent Next-Generation HIV-1 Integrase Strand Transfer Inhibitor
- The study analyzed in vitro antiviral activity of bictegravir alone and in combination with TAF, FTC and darunavir (DRV). Bictegravir alone was highly potent against HIV-1 infected target cells and demonstrated no antiviral effect against non-HIV viruses. In combination with TAF, FTC and DRV, bictegravir was highly synergistic against HIV-1. Bictegravir exhibited low cytotoxicity in non-target human cell lines.
Further information about the clinical studies described above can be found at www.clinicaltrials.gov.
Bictegravir, including in combination with TAF and FTC as a single tablet regimen, is an investigational treatment for HIV that has not been determined to be safe or efficacious.
About Gilead Sciences
Gilead Sciences is a biopharmaceutical company that discovers, develops
and commercializes innovative therapeutics in areas of unmet medical
need. The company’s mission is to advance the care of patients suffering
from life-threatening diseases. Gilead has operations in more than 30
countries worldwide, with headquarters in Foster City,
This press release includes forward-looking statements within the
meaning of the Private Securities Litigation Reform Act of 1995 that are
subject to risks, uncertainties and other factors, including the
possibility of unfavorable results from other clinical trials involving
bictegravir. As a result, bictegravir may never be successfully
commercialized. These risks, uncertainties and other factors could cause
actual results to differ materially from those referred to in the
forward-looking statements. The reader is cautioned not to rely on these
forward-looking statements. These and other risks are described in
detail in Gilead’s Quarterly Report on Form 10-Q for the quarter ended
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Gilead Sciences, Inc.
Sung Lee, 650-524-7792
Ryan McKeel, 650-377-3548