Safety, Tolerability, and Pharmacodynamics of GS-4224 in Healthy Participants and Participants With Chronic Hepatitis B - PubMed

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GS-4224, an orally bioavailable PD-L1-binding small molecule, was evaluated in a Phase 1a/b clinical study.
The study involved 60 healthy participants (HPs) and 42 participants with chronic hepatitis B (CHB), assessing single and multiple ascending doses.
GS-4224 was generally safe and well-tolerated, with no Grade ≥3 adverse events (AEs) or serious AEs in HPs.
In CHB participants, no serious AEs or deaths occurred, but two had Grade ≥3 AEs (one unrelated acute hepatitis B exacerbation, one related increased ALT).
PD-L1 receptor occupancy was dose-dependent, peaking at 38% in HPs (1000 mg) and 35% in CHB participants (700 mg).
No changes in hepatitis B surface antigen (HBsAg) levels were observed in CHB participants, indicating no antiviral effect at tested doses.

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