One such molecularly targeted therapy is enabled by inhibiting the enzyme poly(ADP-ribose) polymerase (PARP) by small molecule inhibitors in tumors which have a defect in the homologous DNA recombination pathway, most characteristically due to BRCA mutations. Olaparib, a highly potent PARP inhibitor,...
The combination of the PARP inhibitor olaparib and the WEE1 inhibitor AZD1775 as a new therapeutic option for small cell lung cancer. Clin. Cancer Res. 24, 5153–5164 (2018). CAS PubMed Google Scholar Fang, Y. et al. Sequential therapy with PARP and WEE1 inhibitors minimizes toxicity ...
[32]Cho HW, Kim JW, Park JY, et al. 820TiP A randomized phase Ⅱ study of secondary cytoreductive surgery (CRS) in patients with relapsed ovarian cancer who have progressed on PARP inhibitor maintenance (KGOG 3067/SOCCER-P...
Therefore, it is necessary to provide personalized targeted therapy for gene mutations in different sub- groups of patients. PARP inhibitor resistance With the increase in the clinical use of PARP inhibitors, resistance has attracted increasing attention. Through the current study, we have learned ...
loss ofCHEK2confers resistance rather than sensitivity to PARP inhibition through increased expression of BRCA2, a target of CHEK2-TP53-E2F7-mediated transcriptional repression. Combined PARP and ATR inhibition overcomes PARP inhibitor resistance caused byCHEK2loss. Our findings may inform the use of...
(a PARP1 inhibitor) has demonstrated safety and activity in a preliminary analysis of 40 patients, including those with BRCA mutated TNBC, with an ORR of 25% and a disease control rate of 53%. This agent is being investigated for its efficacy either as monotherapy or in combination with ...
HRR缺陷(HRR deficiency, HRD)是决定肿瘤细胞对PARP抑制剂(PARP inhibitor, PARPi) 敏感性的关键因素。利用或促进肿瘤HRD来提高PARPi治疗敏感性已成为提高肿瘤治疗效果的可行方案。胰腺腺癌(Pancreatic adenocarcinoma, PAAD)作为全球最致命的...
In the phase II MEDIOLA, 32 patients with recurrent platinum-sensitive ovarian cancer with germlineBRCAmutations in second-line or later therapy were treated with olaparib (Lynparza) and durvalumab (Imfinzi). Eligible patients had no prior exposure to a PARP inhibitor or immune-oncology agent. ...
There are 9 records for veliparib, and the combination therapy trials are mostly in phase I or II. In addition, rucaparib, talazoparib and niraparib have 4, 3, and 3 records, mostly in phase I or II. Table 1 Clinical trials of PARP inhibitor drugs for pancreatic cancer Full size ...
Targeted therapy for cancer using PARP inhibitors. Poly (ADP-ribose) Polymerase (PARP) has a well-established role in DNA repair processes, and small molecule inhibitors of PARP have been developed as chemo... CJ Lord,A Ashworth - 《Current Opinion in Pharmacology》 被引量: 458发表: 2008年...