Olaparib (Lynparza)

General information

Class/mechanism: PARP (poly-ADP (adenosine diphosphate)–ribose polymerase) inhibitor. PARP participates in the alternative base-excision repair pathway that helps to repair single-strand DNA breaks. PARP is involved in normal cellular homeostasis processes during DNA transcription and cell cycle regulation. By inhibiting PARP1, PARP2, and PARP3, olaparib leads to the accumulation of single-strand breaks. In patients with a concurrent BRCA1/BRCA2 mutation, in which there are also defects in homologous recombination double strand DNA repair, this inhibition of PARP enzymatic activity and formation of the PARP-DNA complex can lead to irrecoverable DNA damage and cell death.
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the package insert.

Diseases for which it is used

• Breast cancer
• Ovarian cancer
• Pancreatic cancer
• Prostate cancer

Patient drug information

• Olaparib (Lynparza) package insert

History of changes in FDA indication

• 12/19/2014: Initial FDA approval "as monotherapy in patients with deleterious or suspected deleterious germline BRCA mutated (as detected by an FDA-approved test) advanced ovarian cancer who have been treated with three or more prior lines of chemotherapy."

Also known as

AZD2281, AZD-2281, KU-0059436