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ACE-86225106
- Development stage
- Phase 2
- Lead developer
- Acerand Therapeutics
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
ACE-86225106 is a novel, oral, and highly selective small molecule inhibitor of poly (ADP-ribose) polymerase 1 (PARP1), developed by Acerand Therapeutics. It is being investigated as an antineoplastic agent for the treatment of advanced solid tumors, including breast cancer, ovarian cancer, and prostate cancer. The drug acts by inhibiting PARP1, a key enzyme involved in DNA repair pathways; this mechanism can lead to synthetic lethality in tumor cells with defects in homologous recombination repair such as those harboring BRCA mutations. Preclinical studies have shown significant inhibitory effects on PARP1 with potentially reduced hematological toxicity compared to earlier pan-PARP inhibitors. As of April 2024, ACE-86225106 is undergoing Phase I/II clinical trials primarily in China[1][3][6].
- Other names
- Selective PARP1 Inhibitor
02
Targets
PARP1 (Poly (adp-ribose) polymerase 1)
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