Drug intelligence / Profile preview

APG-1387 + entecavir

Development stage
Unknown
Lead developer
Ascentage Pharma
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**APG-1387 + entecavir** is an investigational combination therapy for chronic hepatitis B (CHB) consisting of APG-1387, a novel small molecule inhibitor of apoptosis proteins (IAP) antagonist, and entecavir, a nucleoside analog reverse transcriptase inhibitor. APG-1387 promotes degradation of IAPs including cIAP1, cIAP2, and XIAP, leading to restoration of caspase activity, induction of apoptosis, and immunomodulation. In preclinical and early clinical studies, APG-1387 demonstrated anti-HBV effects through direct induction of apoptosis in HBV-infected liver cells and enhancement of HBV-specific T cell responses[4][5]. Entecavir suppresses HBV replication by inhibiting the viral DNA polymerase. The combination is being evaluated to determine if APG-1387 can synergize with entecavir for improved functional cure rates for hepatitis B.

02

Targets

XIAP (Baculoviral IAP repeat-containing protein 4)BIRC3 (Baculoviral IAP repeat-containing protein 3)HBV Pol (Hepatitis B virus polymerase)BIRC2 (Cellular inhibitor of apoptosis protein 1)

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