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 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.

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

FDA-approved for

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

FDA label

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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.

NO BOXED WARNINGS

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.

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