Tyrosine kinase inhibitors (TKIs) represent one of the most advanced class of therapeutics for cancer treatment. Most of them are also cytochrome P450 (CYP) inhibitors and/or substrates thereof. Accordingly, their efficacy and/or toxicity can be affected by CYP-mediated metabolism and by metabolism...
Entrectinib is a multi-kinase inhibitor targeting TRK, ROS1, and ALK. The pooled analysis revealed an ORR of 57.4% in patients with TRK fusion across 10 tumor types [98]. In a recent study, entrectinib produced favorable responses in children and adolescents with refractory CNS and extrac...
TKIs can generally enter the cell and bind to abnormally activated PTKs. However, extensive mutations in some PTKs decrease TKI binding capacity as a direct mechanism of TKI resistance (Table1). On the one hand, intrinsic resistance occurs due to changes in kinase conformation and activity caused...
Entrectinib is a multi-kinase inhibitor targeting TRK, ROS1, and ALK. The pooled analysis revealed an ORR of 57.4% in patients with TRK fusion across 10 tumor types [98]. In a recent study, entrectinib produced favorable responses in children and adolescents with refractory CNS and extrac...
The second promising tyrosine kinase inhibitor against MTC,motesanib diphosphate(AMG-706), is a multikinase inhibitor targeting VEGF, platelet-derived growth factor, and Kit receptors, which lead toantiangiogenicand directantitumor activity. In a phase I trial with AMG-706, one patient with MTC exhi...
discontinuation of multi-kinase inhibitor (MKIs), imatinib therapy due to TKI-associated adverse effects.10Toxicity can be attributed to bothon-targeteffects through excessive inhibition of the intended TK function; and/oroff-targeteffects resulting from the simultaneous inhibition of multiple other ...
EGFR酚基乙氨酸激酶抗化剂(TKI),例如erlotinib和gefitinib,最初被评估了,不用在患者的分子选择有复发的NSCLC的。 翻译结果5复制译文编辑译文朗读译文返回顶部 EGFR tyrosine kinase 抑制剂 (TKI),例如 erlotinib 和 gefitinib,用被重新陷入的 NSCLC 没有在病人中的分子的精选品地最初被评价。 相关内容 amorning dee...
Pyrimidine (imatinib, dasatinib, nilotinib and pazopanib), pyridine (sorafenib) and pyrrole (sunitinib) tyrosine kinase inhibitors (TKIs) are multi-targeted TKIs with high activity towards several families of receptor and non-receptor tyrosine kinases involved in angiogenesis, tumour growth and metastatic...
Medical imagingComputed tomographyBackground: Sunitinib (SU) is a tyrosine kinase inhibitor (TKI) with activity against VEGFR. During VEGFR TKI withdrawal, increased pain at sites of metastasis has been observed, which we hypothesize is due to the proliferative flare. [ 18 F ]‐fluoro‐3′‐...
was positively enriched in shURI cells compared with their control. (Fig.1band Supplementary Fig.1d). These results suggest that URI might play an important role in ferroptosis. Meanwhile, pathways, including EGFR tyrosine kinase inhibitor resistance, regulation of lipolysis, p53 signaling pathway, an...