PARP inhibitors

PARP inhibitors (the acronym PARP stands for: poly-ADP-ribose polymerase) are a currently still small group of drugs that are used for the treatment of various cancers (e.g. ovarian cancer).

Olaparib (^Lynparza®) was the first active ingredient to be approved in 2015. Lynparza can be used as a monotherapy for maintenance treatment in adult patients with platinum-sensitive recurrence of BRCA-mutated high-grade serous epithelial ovarian, fallopian tube or peritoneal cancer. Before starting treatment, a mutation in the BRCA1 or BRCA2 genes must be detected in blood or tumor tissue.

In 2017, the US Food and Drug Administration (FDA) approved another PARP inhibitor, the oral preparation niraparib (^Zejula®), for the treatment of ovarian cancer and related malignancies. Niraparib is used as monotherapy for maintenance treatment in adult patients with recurrence of platinum-sensitive, poorly differentiated serous carcinoma of the ovaries, tubes or with primary peritoneal carcinomatosis who are in remission (complete or partial) after platinum-based chemotherapy.

Another PARP inhibitor is rucaparib (^Rubraca®), which was also approved for the treatment of ovarian cancer in the USA in December 2016. Rucararib is also only used in patients with mutations in BRCA genes.

1. Lord CJ et al (2017) PARP inhibitors: synthetic lethality in the clinic. Science 355:1152-1158.