Olaparib

adjuvant or metastatic setting. Patients with hormone receptor (HR)-positive breast cancer should have progressed on or be considered inappropriate for endocrine therapy. Germline BRCA mutation must be confirmed before Olaparib treatment is initiated.

Ovarian Cancer: Olaparib is indicated as monotherapy for the maintenance treatment of adult patients with platinum sensitive relapsed (PSR). High-grade epithelial ovarian, fallopian tube or primary peritoneal cancer who are in response (complete response or partial response) to platinumbased chemotherapy.

Therapeutic Class

Targeted Cancer Therapy

Olaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1, PARP2, and PARP3. PARP enzymes are involved in normal cellular homeostasis, such as DNA transcription, cell cycle regulation, and DNA repair.

Olaparib has been shown to inhibit growth of select tumor cell lines in vitro and decrease tumor growth. in mouse xenograft models of human cancer both as monotherapy or following platinum-based chemotherapy.

Increased cytotoxicity and anti-tumor activity following treatment with olaparib were noted in cell lines and mouse tumor models with deficiencies in BRCA. In vitro studies have shown that olaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity. increased formation of PARP-DNA complex. Resulting in disruption of cellular homeostasis and cell death.