Drug intelligence / Profile preview

simmiparib

Development stage
Phase 2
Lead developer
ACEBRIGHT
Modality
Small Molecules
Administration
Oral
01

Overview

Simmiparib is a highly potent, orally bioavailable small molecule inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and poly(ADP-ribose) polymerase 2 (PARP2), with IC50 values of 1.75 nM and 0.22 nM, respectively[1][3][6]. It demonstrates greater potency than olaparib in preclinical models and exhibits high selectivity for PARP1/2 over other PARP family members[6]. Simmiparib works by binding to PARP enzymes, preventing DNA repair via the base excision repair pathway, leading to accumulation of DNA strand breaks, G2/M cell cycle arrest, genomic instability, and apoptosis—particularly in homologous recombination repair-deficient cancer cells[3][6]. Developed by Shanghai Acebright Pharmaceuticals and the Shanghai Institute of Materia Medica as an antineoplastic agent for solid tumors including breast cancer[4][5], its clinical development was discontinued after Phase I trials in China for solid tumors[4].

Other names
1551355-46-4CHEMBL3907010CHEMBL-3907010CHEMBL 3907010QNQFPYADHVFRKQ-UHFFFAOYSA-N
02

Targets

PARP2 (Poly (adp-ribose) polymerase 2)

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