Olaparib is an inhibitor of poly (ADP-Ribose) polymerase (PARP) Enzymes: A Review Mr. Jain Mayur S.*, Dr. Barhate Shashikant D., Mr. Gayakwad Bhushan P., Mr. Patil Prafull P. Shree. Sureshadada Jain Institutes of Pharmaceutical Education and Research, Jammer, Maharashtra (India) *Corresponding Author E-mail: mayurjain176@gmail.com
Online published on 7 July, 2018. Abstract 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 olaparibinduced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complex, resulting in disruption of cellular homeostasis and cell death(1, 2) Top Keywords Olaparib, Antineoplastic Agents. Top |