Ovarian cancer: First-line maintenance (with BRCA mutation or HRD-positive after platinum response, as monotherapy or with bevacizumab); Maintenance after ≥2 prior platinum-based regimens. Breast cancer: Adjuvant HER2-negative high-risk early breast cancer with germline BRCA mutation after chemo; Germline BRCA-mutated HER2-negative metastatic breast cancer. Pancreatic cancer: First-line maintenance with germline BRCA mutation after platinum response. Prostate cancer: HRR gene-mutated metastatic castration-resistant prostate cancer.
Standard dose: 300 mg (two 150 mg tablets) orally twice daily
Prostate cancer with abiraterone: 300 mg twice daily with abiraterone 1000 mg daily plus prednisone
Dose modifications: Reduce to 250 mg BID, then 200 mg BID for adverse reactions
Renal impairment (CrCl 31-50 mL/min): 200 mg BID
Tablets: 100 mg, 150 mg
Refer to the complete prescribing information for contraindications. Lynparza prescribing should account for patient-specific factors including hypersensitivity to the active ingredient or any excipients.
Nausea (58%), fatigue (55%), anemia (40%), vomiting (32%), diarrhea (21%), decreased appetite (20%), headache (15%), dysgeusia (14%)
Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.
Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.
Consult the full prescribing information for pregnancy-related considerations.
Refer to prescribing information for lactation guidance.
Pediatric safety and efficacy information is detailed in the full label.
Dose modifications for organ impairment are specified in the complete prescribing information.
Olaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP-1, PARP-2, and PARP-3. PARP enzymes are involved in normal cellular functions including DNA repair. Olaparib-induced cytotoxicity involves inhibition of PARP enzymatic activity and trapping of PARP-DNA complexes, resulting in DNA damage, apoptosis, and cell death in cells with deficiencies in homologous recombination repair (HRR), such as those with BRCA1/2 mutations.
Tmax: 1.5 hours. Half-life: 14.9 hours. Protein binding: 82%. Metabolized by CYP3A. Steady-state by Day 3-5. Excreted in urine (44%, 15% unchanged) and feces (42%, 6% unchanged). Dose reduce for CrCl 31-50 mL/min.
Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.
Lynparza has FDA-approved indications across the following cancer types covered on PipelineEvidence: