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Selumetinib is an anticancer drug

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  Selumetinib inhibits a variety of tumors including B-Raf-mutated melanoma and K-Ras mutant non-small cell lung cancer (NSCLC) by regulating key protein kinase MEK levels in the Ras-Raf-MEK-ERK pathway. Growth. Mainly used for the treatment of cholangiocarcinoma, colorectal cancer, NSCLC, etc. Currently, sterminib is in Phase III clinical trials for the treatment of non-small cell lung cancer.

  Selumetinib is the first small molecule MEK inhibitor for clinical trials of thyroid cancer. In a Phase II clinical study of 131 I refractory thyroid papillary carcinoma, 39 patients received oral Selumetinib (100 mg bid) daily for 28 days. The results showed that 21 patients were stable (54%) and 11 patients were worse ( 28%), 49% of patients were stable for 16 weeks, 36% of patients were stable for 24 weeks, and no progression was 32 weeks. The main adverse events were rash (59%), diarrhea (44%), and fatigue (41 %). In the study, Selumetinib was used to treat 20 patients with thyroid cancer for 4 weeks. It was found that Selumetinib can increase the iodine uptake and retention of 131 I refractory thyroid cancer patients.

  Selumetinib is a mitogen extracellular kinase inhibitor that significantly inhibits phosphorylation of ERK1/2 by inhibiting extracellular signal-regulated kinase (ERK/2) and activating the cysteine ​​protease pathway. Selumetinib is mainly used for the treatment of cholangiocarcinoma, colorectal cancer, NSCLC, and the like. A double-blind, randomized study of 87 patients with mutant NSCLC was performed. The total survival time was 9.4 months and 5.2 months, and the PFS was 5.3 months, respectively, in the combination of Selumetinib and Docetaxel (DOC) and the combination of DOC and placebo. In 2.1 months, RR was 37% and 0%, respectively, and the difference was significant. Its main adverse reactions are neutropenia, dermatitis and respiratory failure.