Drug intelligence / Profile preview

IDE161

Development stage
Phase 1
Lead developer
IDEAYA Biosciences
Modality
Small Molecules
Administration
Oral
01

Overview

IDE161 is an orally bioavailable, potent, and selective small molecule inhibitor of poly(ADP-ribose) glycohydrolase (PARG), a key enzyme involved in the DNA damage response pathway. By inhibiting PARG, IDE161 disrupts the repair of single-strand DNA breaks via the base excision repair pathway. This mechanism is particularly relevant in tumors with homologous recombination deficiency (HRD), such as those harboring BRCA1/2 mutations or other defects in HR genes. Preclinical studies have shown that IDE161 has antitumor activity even in settings resistant to PARP inhibitors and platinum-based therapies. The drug is being developed as a potential first-in-class therapy for advanced or metastatic solid tumors with HRD alterations[1][3][4][5][6].

02

Targets

PARG (Poly(ADP-ribose) glycohydrolase)

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