在这类测试中,针对神经营养因子受体酪氨酸激酶基因(neurotrophin receptor tyrosine kinase genes)NTRK1,NTRK2或NTRK3进行的临床试验就是个极好的成功实例,证明了通过抑制驱动癌症的激酶活性,就能在不同组织/不同癌症中都达到良好的抑癌效果。近日《Nature Reviews Clinical Oncology》对NTRK融合阳性肿瘤和TRK抑制剂疗法进...
A next-generation TRK kinase inhibitor overcomes acquired resistance to prior TRK kinase inhibition in patients with TRK fusion-positive solid tumors[J].Cancer Discov, 2017,7(9):963—972. DOI: 10.1158/2159—8290.CD—17—0507 . 返回引文位置Google Scholar 百度学术 万方数据 [23] Drilon A ,...
参考文献: [1]Management of Immune-Related Adverse Events in Patients Treated With Immune Checkpoint Inhibitor Therapy:ASCO Guideline Update Bryan J. Schneider, Jarushka Naidoo, Bianca D. Santomasso, Christina Lacchetti, Sh...
107 reported the pan-TRK inhibitor 34 (PF-06273340) through HTS of TRKA/B cells and SAR (IC50 values towards TRKA/B/C were 6, 4, and 3 nmol/L, respectively). A phase I clinical trial was completed for assessment of the analgesic effects of PF-06273340 in healthy volunteers using ...
Cancer therapeutic resistanceTranslational researchTRK fusions are found in a variety of cancer types, lead to oncogenic addiction, and strongly predict tumor-agnostic efficacy of TRK inhibition. With the recent approval of the first selective TRK inhibitor, larotrectinib, for patients with any TRK-...
第15卷 第12 期 2017 年 12 月 临床药物治疗杂志 Clinical Medication Journal Vol.15,No.12 Dec,2017 新药咨讯 国家应急防控药物工程技术研究中心 学术支持 Trk 小分子激酶抑制剂研究进展 2017 年 12 月下旬,拜耳公司和 Loxo Oncology 公司合作开发的口服选 择性原肌球蛋白相关激酶 (Tropomyo- sin-related ...
Additionally, the TRK inhibitor larotrectinib is actually under investigation as single-agent in a phase II NAVIGATE basket trial on NTRK fusion-positive solid cancers, including advanced CCAs (NCT02576431). Moreover, secondary mutations following treatment with TRK inhibitors may cause resistance to...
Zurletrectinib is active against 1st-generation TRK inhibitor resistance mutations in vitro Selitrectinib and repotrectinib are both next-generation TRK inhibitors specifically developed to maintain activity against on-target mutations that are acquired on progression to 1st-generation TRK inhibitors. ...
Selitrectinib (LOXO-195, BAY 2731954) is an orally available, highly potent, and selective TRK kinase inhibitor with low nanomolar inhibitory activity against TRKA G595R, TRKC G623R, and TRKA G667C, IC50s ranging from 2.0 to 9.8 nmol/L. It is more
Roblin et al., “Topical TrkA Kinase Inhibitor CT327 is an Effective, Novel Therapy for the Treatment of Pruritus due to Psoriasis: Results from Experimental Studies, and Efficacy and Safety of CT327 in a Phase 2b Clinical Trial in Patients with Psoriasis,” Acta Derm. Venereal., 2015, 95...