Drug intelligence / Profile preview

WXWH0240

Development stage
Phase 1
Lead developer
Cisen Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

WXWH0240 is an orally bioavailable small molecule inhibitor of poly (ADP-ribose) polymerase (PARP), specifically targeting PARP1 and PARP2. Developed by Chenxin Pharmaceutical, it is designed to exploit the concept of synthetic lethality in tumors with homologous recombination repair (HRR) deficiencies, such as those harboring BRCA1 or BRCA2 mutations. By inhibiting PARP enzymes, WXWH0240 prevents the repair of single-strand DNA breaks, which then progress to double-strand breaks that cannot be efficiently repaired in HRR-deficient cancer cells, leading to genomic instability and apoptosis. The drug is currently undergoing clinical evaluation for the treatment of advanced solid tumors, including breast and ovarian cancers.

02

Targets

CDK2 (Cyclin-dependent kinase 2)CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)PARP1 (Poly (adp-ribose) polymerase 1)PARP2 (Poly (adp-ribose) polymerase 2)

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