• Alias: BMN673
    • An orally bioavailable inhibitor of the nuclear enzyme PARP that selectively binds to PARP and prevents PARP-mediated DNA repair of single-strand DNA breaks via the base-excision repair pathway. This enhances the accumulation of DNA-strand breaks, promotes genomic instability, and eventually leads to apoptosis.
    • Phase 2 in BRCA1/2 wild-type, triple-negative, or HER2-negative breast cancer; phase 1/2 study in metastatic solid tumors
    • Recommended phase 2 dose: 1 mg PO daily
    • Half-life: â™50 hours
    • Common side effects: Fatigue, anemia, thrombocytopenia, rash
    (De Bono et al., 2017)
    Other topics in Targeted and Immunotherapy Agents