Rucaparib治療復發性卵巢癌的檢視

The Role of Rucaparib in the Treatment of Patients with Recurrent Ovarian Cancer

根據最近的研究認為，PARP可用來治療同源重組不足的癌症病患，因PARP可作為鹼基修補酵素，如抑制其作用可使兩股DNA受傷，使得腫瘤細胞死亡。Rucaparib乃一小分子的PARP-1、PARP-2和PARP-3抑制劑，臨床上可抑制卵巢癌或其它實心腫瘤的生長，特別是有BRCA1/2突變和同源重組不足的上皮性卵巢癌，副作用可被接受。美國食品藥物管理局已通過，rucaparib可用在治療BRCA突變或經過兩次化學治療的晚期卵巢癌。

Poly(ADP-ribose) polymerase(PARP) inhibitors have primarily been studied asmonotherapy in cancers with homologous recombination deficiencies based onan early understanding of PARP as a base excision repair enzyme and the ideathat abrogation of two DNA repair pathways damages rapidly dividing cancercells. Rucaparib is a potent small-molecule inhibitor of PARP-1, PARP-2 andPARP-3 that has shown clinical activity in ovarian carcinoma as well as othertypes of solid tumors; it has been extensively investigated in epithelial ovariancancer harboring BRCA1/2 mutations or homologous recombinat deficiencies.Rucaparib has an acceptable toxicity. It has recently received FDA (The Foodand Drug Administration) approval for patients with deleterious BRCA mutation(germline or somatic)-associated advanced ovarian cancer who have beentreated with two or more chemotherapies.