Gilead Announces Clinical Data Supporting Development of GS-6207, a Novel Long-Acting HIV-1 Capsid Inhibitor
Mar 12, 2019 09:10
CST Updated
09:10
Gilead Sciences
Antiviral Drug Developer
March 12, 2019/BioonBIOON/--U.S. pharmaceutical giant Gilead Sciences recently announced the results of two clinical studies, which support the further development of GS-6207, a novel, selective, first-in-class HIV-1 capsid inhibitor being developed as part of a long-acting combination therapy for HIV. Interim blinded data from a Phase I clinical study in healthy subjects demonstrated that a single subcutaneous dose of GS-6207 up to 450 mg achieved sustained concentration levels and was well tolerated. Furthermore, in vitro data indicated that GS-6207 exhibits potency at low picomolar levels, including against HIV strains resistant to other classes of antiretroviral (ARV) agents. These data were recently presented at the 2019 Conference on Retroviruses and Opportunistic Infections (CROI) held in Seattle, United States.Meetingpublished above.
John McHutchison, Chief Scientific Officer and Head of Research and Development at Gilead Sciences, stated, “These studies suggest that GS-6207 may represent a novel approach to HIV treatment due to its long-acting properties and potent antiviral activity observed in vitro. The data presented at CROI support advancing GS-6207 to the next phase ofClinical Trials, to further elucidate its potential role as a long-acting agent for individuals living with HIV.”
An ongoing Phase I, randomized, blinded, placebo-controlled study evaluating the safety, tolerability, and pharmacokinetics (PK) of GS-6207 in 40 healthy subjects. Subjects were randomized (4:1) across four staggered single-ascending-dose cohorts to receive either GS-6207 at doses of 30, 100, 300, or 450 mg (n=8 per cohort) or placebo (n=2 per cohort). Over the course of the study, which ranged from 20 weeks for the 30 mg cohort to 4 weeks for the 450 mg cohort, there were no deaths, serious adverse events (AEs), or Grade 3 or 4 AEs. Most adverse events were mild (Grade 1) and resolved. PK parameters have currently been estimated for the 30 mg and 100 mg cohorts; analysis is ongoing for the 300 mg and 450 mg cohorts. The PK profile of subcutaneously administered GS-6207 is consistent with sustained drug exposure, supporting a dosing interval of at least three months for doses greater than 100 mg.
In vitro studies evaluated the pharmacological profile of GS-6207, demonstrating that its potency is more than 100-fold higher than that of certain commonly used antiretroviral agents. Furthermore, GS-6207 exhibits synergistic antiviral activity when used in combination with the antiretroviral drugs tenofovir alafenamide, efavirenz, dolutegravir, or darunavir. In vitro studies also indicate that GS-6207 retains full potency against a broad range of HIV-1 strains resistant to other classes of antiretroviral (ARV) agents.
Gilead has initiated a Phase Ib study of GS-6207 for the treatment of individuals with HIV infection.GS-6207 is an investigational therapy that has not yet been approved by any regulatory agency worldwide; its safety and efficacy have not been established. Currently, there is no cure for HIV or AIDS. (Bioon.com)