Olaparib

LYNPARZA

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Pronunciation: oe-LAP-a-rib (lin-PAR-za)

Olaparib ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Olaparib ballicule

What it isPARP inhibitor exploiting synthetic lethality; BRCA-mutated ovarian, breast, pancreatic and prostate cancer.

Why this oneHas 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.

Olaparib molecular structure (skeletal formula) — Molecular structure: Olaparib

Olaparib prescription history

Animated chart of estimated U.S. prescriptions per year, Oral anticancer meds (1953–2026). Olaparib enters in 2014 (estimated).

FDA-approved for

BRCA-mutated ovarian cancer (2014)
breast, pancreatic and prostate cancer

Principal riskMyelosuppression; rare myelodysplasia

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryD

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

FDA label

Read the full label on DailyMed ↗

NO BOXED WARNINGS

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)

Available strengths

tab 100, 150 mg

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

Cost

Olaparib (LYNPARZA)

Strength		#/mo	generic $/mo	CostPlus
100 mg	tab	60 BID		not offered
150 mg	tab	60 BID		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Olaparib is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2031 est.

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Self-check

What DNA-repair strategy does olaparib exploit?
Synthetic lethality.
Which CYP pathway governs olaparib interactions?
CYP3A4.