Olaparib
LYNPARZA
What it isPARP inhibitor exploiting synthetic lethality; BRCA-mutated ovarian, breast, pancreatic and prostate cancer.
Why this oneIt has the broadest tumor-type reach of the PARP inhibitors, including pancreatic and early breast settings.
What limits itMyelosuppression and fatigue. Rare myelodysplasia and pneumonitis; CYP3A4-dependent.
FDA-approved for
- BRCA-mutated ovarian cancer (2014)
- breast, pancreatic and prostate cancer
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| HRR/BRCA-mutated cancers (ovarian, breast, pancreatic, mCRPC) | Adults | 300 mg BID | 300 mg BID | 300 mg BID |
Renal Mild (CLcr 51-80): no change; moderate (CLcr 31-50): 200 mg BID; severe/ESRD (CLcr ≤30): no data
Hepatic Mild-moderate (Child-Pugh A/B): no adjustment; severe (C): no data
Instructions
- Take with or without food
- Swallow tablets whole; do not chew, crush, dissolve, or divide
- For mCRPC, give concurrently with a GnRH analog or after bilateral orchiectomy
- Missed dose: take next normal dose at scheduled time (do not double)
Cautions
- Myelodysplastic syndrome/AML (often fatal); monitor CBC at baseline and monthly
- Pneumonitis (some fatal); interrupt if suspected
- Venous thromboembolism incl. pulmonary embolism (8% in mCRPC)
- Hepatotoxicity/drug-induced liver injury
- Embryo-fetal toxicity
Adverse reactions
- Nausea
- Fatigue/asthenia
- Anemia
- Vomiting
- Diarrhea
- Decreased appetite
- Headache
- Dysgeusia
- Cough
- Neutropenia
- Dyspnea
- Dizziness
- Dyspepsia
Pregnancy Can cause fetal harm (teratogenic/embryo-fetal toxicity in animals); avoid, use effective contraception
Lactation Do not breastfeed during treatment and for 1 month after last dose
NO BOXED WARNINGS
Principal riskMyelosuppression; rare myelodysplasia
Cost, est. cash$5,000–$30,000+/month or cycle
Generic entry2031 est.
Classes and tags
Clinical profile
Legacy pregnancy categoryD
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
Mechanism of action: Olaparib ballicule
