[1] Lynparza Becomes Second PARP Inhibitor Approved for Prostate Cancer, Just Days Behind the First [2] 医耘沙龙|PARP抑制剂投资价值深度分析 [3] 首个治疗前列腺癌的PARP抑制剂!美国FDA批准Rubraca,治疗BRCA突变转移去势抵抗前列腺癌(mCRPC) [4] 盘点 ...
精准治疗,检测先行,对于所有mCRPC患者都应进行HRR基因检测以提供临床精准用药指导。目前,他拉唑帕利联合恩扎卢胺已经于2023年6月获得FDA批准用于mCRPC一线治疗,同时也已经提交NMPA审批,期待该治疗方案能尽快在中国获批,为我国mCRPC患者带来可及的用药选择。另外,期待更多生物标志物及新型治疗方案的涌现,拓展精准治疗获益人群...
PARP inhibitorOlaparibCompanion diagnosticsGenetic counselingGenetic testingOvarian cancerBRCA1BRCA2In December 2014, the FDA approved olaparib, a poly(ADP-ribose) polymerase inhibitor (PARPi) for ovarian cancer patients who have failed three or more lines of chemotherapy and have a germline BRCA1/2 ...
[1] Arora S, et al. FDA Approval Summary: Olaparib Monotherapy or in Combination with Bevacizumab for the Maintenance Treatment of Patients with Advanced Ovarian Cancer. Oncologist. 2021 Jan;26(1):e164-e172. [2] Alvarez Secord A, et al. Rationale for combination PARP inhibitor and a...
和几种已经被FDA获批的PARP1 inhibitor(例如Olaparib 和Talazoparib)比起来, nimbolide 展现出了更强的PARP1捕获能力。然而,与传统的PARP抑制剂不同,Nimbolide的处理诱导了PARP1(实际是PARylated-PARP1)和PARylation依赖的DNA损伤修复因子(如XRCC1)的双重捕获,从而...
虽然阻断PARP1酶可能足以阻止HRR缺陷型肿瘤的DNA修复,但美国FDA目前批准的所有PARP抑制剂都会阻断PARP1和PARP2,造成的潜在毒副作用限制了它们的用途。Saruparib是一种PARP1特异性抑制剂,由于saruparib不抑制PARP2的活性,它的毒性比其他PARP抑制剂低,因此可以以更高剂量给药。
PARP抑制剂(PARPi)是FDA批准用于治疗维持期和复发性高级别浆液性卵巢癌(HGSOC)的一类较新的药物。PARPi已显示出对同源重组缺陷(HRD)恶性肿瘤的疗效,但只有大约50%的同源重组缺陷患者对PARP抑制剂治疗有反应。而据研究报道:PARP抑制剂对没有同源重组缺陷的部分患者也有临床益处。因此临床迫切需要开发额外的生物标志物...
objective response and duration of response with the agent compared with chemotherapy. However, SOLO3, an open-label, randomized, controlled study requested by the FDA to further assess olaparib‘s efficacy and safety, found a 33% increased risk for death in those treated with a PARP inhibitor....
PARPis已获得FDA批准用于治疗BRCA1或BRCA2变异(胚系和/或体细胞)的HGSOC患者,这些患者对一线铂类化疗有反应。根据多项研究,约16%-23%的HGSOC样本在诊断时存在BRCA1或BRCA2致病性变异。在遗传性乳腺癌和卵巢癌综合征患者中,大多数这些变异可以在胚系水平上检测到,但这些变异中近30%发生于肿瘤本身,只能在体细胞水...
(HR) repair are hypersensitive to PARP inhibitors39. Since BRCA1 and BRCA2 play indispensable roles in HR repair40, PARP inhibitor treatment specifically kills tumor cells containing mutations inBRCA1andBRCA2genes41,42. Over the past few years, US Food and Drug Administration (FDA) approved ...