Your Health, We Care
Another NameOlaparib、奥拉帕尼、Lynparza、Olanib、Olaparix、Lynib
IndicationsBroad-spectrum antitumor agents
Reg No.10 L 1028/23
Inspection NO.
Olaparib is a poly-ADP glycan polymerase (PARP) inhibitor approved by the FDA on December 19, 2014 for advanced ovarian cancer and HER2- metastatic breast cancer harboring BRCA mutations after at least three prior treatments of chemotherapy.
Olaparib has been approved by the United States FDA for the treatment of adult patients with advanced epithelial ovarian, fallopian tube, or primary peritoneal cancer with deleterious or suspected deleterious BRCA gene mutations who have demonstrated a complete or partial response after first-line platinum-based chemotherapy
Olaparib
Adult patients with epithelial ovarian, fallopian tube, or primary peritoneal and prostate cancer
Based on findings in animals and its mechanism of action, Lynparza can cause fetal harm when administered to a pregnant woman. There are no available data on Lynparza use in pregnant women to inform the drug associated risk. In an animal reproduction study, the administration of olaparib to pregnant rats during the period of organogenesis caused teratogenicity and embryo-fetal toxicity at exposures below those in patients receiving the recommended human dose of 300 mg twice daily. Apprise pregnant women of the potential hazard to the fetus and the potential risk for loss of the pregnancy. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown.
No data are available regarding the presence of olaparib in human milk, or on its effects on the breastfed infant or on milk production. Because of the potential for serious adverse reactions in the breastfed infants from Lynparza, advise a lactating woman not to breastfeed during treatment with Lynparza and for one month after receiving the last dose.
Pregnancy testing is recommended for females of reproductive potential prior to initiating treatment with Lynparza. Contraception Females Lynparza can cause fetal harm when administered to a pregnant woman. Advise females of reproductive potential to use effective contraception during treatment with Lynparza and for at least 6 months following the last dose.
The safety and efficacy of Lynparza have not been established in pediatric patients.
In clinical studies of Lynparza enrolling 482 patients with advanced solid tumors who received Lynparza tablets 300 mg twice daily as monotherapy, 135 (28%) patients were aged ≥65 years. There appeared to be no major difference in the safety profile of patients treated with olaparib aged <65 years versus ≥65 years, nor within the age categories of 65 to 74 years, 75 to 84 years. No patients were aged ≥85 years.
No adjustment to the starting dose is required in patients with mild hepatic impairment. A 15% increase in mean exposure (AUC) was observed in patients with mild hepatic impairment (based on Child-Pugh classification A) compared to patients with normal hepatic function. There are no data in patients with moderate or severe hepatic impairment.
No adjustment to the starting dose is required in patients with mild renal impairment, but patients should be monitored closely for toxicity. A 24% increase in mean exposure (AUC) was observed in patients with mild renal impairment (CLcr = 51-80 mL/min) compared to patients with normal renal function (CLcr>80 mL/min). A 44% increase in AUC was observed in patients with moderate renal impairment (CLcr 31-50 mL/min) compared to patients with normal renal function (CLcr >80 mL/min). For patients with moderate renal impairment, reduce the dose of Lynparza to 200 mg twice daily. There are no data in patients with severe renal impairment or end-stage disease (CLcr ≤30 mL/min).
There is no specific treatment in the event of Lynparza overdose, and symptoms of overdose are not established. In the event of an overdose, physicians should follow general supportive measures and should treat the patient symptomatically.
Store at 20ºC to 25ºC (68°F to 77°F), excursions permitted to 15ºC to 30ºC (59ºF to 86ºF). Store in original bottle to protect from moisture.
Following oral administration of olaparib, absorption is rapid with median peak plasma concentrations typically achieved 1.5 hours after dosing. An AUC mean accumulation ratio of 1.8 is observed at steady state following multiple dosing of 300 mg tablets twice daily.
Systemic exposure (single dose AUC) to olaparib increases approximately proportionally with doses over the dose range of 25 mg to 450 mg, Cmax increased slightly less than proportionally for the same dose range.
Co-administration of a high fat meal with olaparib slowed the rate (tmax delayed by 2.5 hours) of absorption, but did not significantly alter the extent of olaparib absorption (mean AUC increased by approximately 8%).
FDA,2021.08
