Breast cancer, Ovarian cancer, Pancreatic cancer, Prostate cancer
藥理
laparib is a potent oral PARP inhibitor which induces synthetic lethality in BRCA1/2 deficient tumor cells through the formation of double-stranded DNA breaks which cannot be accurately repaired, which leads to disruption of cellular homeostasis and cell death.
藥動學
Absorption: Rapid; delayed with a high-fat/high-calorie meal (not significantly).
Protein binding: ~82%.
Metabolism: Primarily hepatic via CYP3A; the majority of metabolism is through oxidation with some metabolites undergoing subsequent glucuronide or sulfate conjugation.
t1/2 elimination, terminal: 14.9 ± 8.2 hours.
Time to peak: 1.5 hours
Excretion: Urine (44%); feces (42%)
Clearance: 7.4 ± 3.9 hours.
禁忌症
Hypersensitivity to olaparib or any component of the formulation.
懷孕分類
In utero exposure to olaparib may cause fetal harm.
哺乳分類
Lactating females should not breastfeed during treatment and for 1 month after the last olaparib dose.