Maiorano Brigida Anna, Maiorano Mauro Francesco Pio, Maiello Evaristo
Oncology Unit, Foundation Casa Sollievo della Sofferenza IRCCS, San Giovanni Rotondo, Italy.
Department of Translational Medicine and Surgery, Catholic University of the Sacred Heart, Rome, Italy.
Front Pharmacol. 2023 Apr 21;14:1162665. doi: 10.3389/fphar.2023.1162665. eCollection 2023.
Ovarian cancer (OC) is women's eighth most common cancer, bearing the highest mortality rates of all female reproductive system malignancies. Poly (ADP-ribose) polymerase inhibitors (PARPis) have reshaped the treatment scenario of metastatic OC as a maintenance post platinum-based chemotherapy. Olaparib is the first PARPi developed for this disease. Results from Study 42, Study 19, SOLO2, OPINION, SOLO1, and PAOLA-1 clinical trials, led to the FDA and EMA approval of olaparib for the maintenance treatment of women with high-grade epithelial ovarian, fallopian tube, or primary peritoneal cancer without platinum progression: in the platinum-sensitive recurrent OC; in the newly diagnosed setting in case Breast Cancer (BRCA) mutations and, in combination with bevacizumab, in case of BRCA mutation or deficiency of homologous recombination genes. In this review, we synthetized olaparib's pharmacokinetic and pharmacodynamic properties and its use in special populations. We summarized the efficacy and safety of the studies leading to the current approvals and discussed the future developments of this agent.
卵巢癌（OC）是女性第八大常见癌症，在所有女性生殖系统恶性肿瘤中死亡率最高。聚（ADP - 核糖）聚合酶抑制剂（PARPis）作为铂类化疗后的维持治疗手段，重塑了转移性OC的治疗格局。奥拉帕利是首个针对该疾病研发的PARPi。42研究、19研究、SOLO2、OPINION、SOLO1和PAOLA - 1临床试验的结果，促使美国食品药品监督管理局（FDA）和欧洲药品管理局（EMA）批准奥拉帕利用于对铂类未进展的高级别上皮性卵巢癌、输卵管癌或原发性腹膜癌女性的维持治疗：在铂敏感复发性OC中；在新诊断的情况下，若存在乳腺癌（BRCA）突变，以及在BRCA突变或同源重组基因缺陷的情况下与贝伐单抗联合使用。在本综述中，我们综合了奥拉帕利的药代动力学和药效学特性及其在特殊人群中的应用。我们总结了促成当前批准的各项研究的疗效和安全性，并讨论了该药物的未来发展。
