Selumetinib (CAS 606143-52-6) Suppliers and Product Information

Selumetinib is a highly selective MEK1 inhibitor used in the treatment of advanced non-small cell lung cancer (NSCLC) and other cancers. It is currently in stage III clinical trials for NSCLC treatment. The compound acts as a tight-binding, uncompetitive inhibitor of mitogen-activated protein kinase kinases (MEK) 1 and 2.

Frequently Asked Questions about Selumetinib

Q: What is the mechanism of action of Selumetinib?

A: Selumetinib is a MEK1/2 inhibitor that binds to a unique allosteric pocket on the N-terminal domain of MEK1, preventing RAF-induced phosphorylation and locking MEK1/2 into a catalytically inactive state. This blocks the RAS signaling pathway.

Q: What are the main clinical applications of Selumetinib?

A: Selumetinib is primarily used to treat bile duct cancer, colon cancer, and non-small cell lung cancer (NSCLC). It has also shown promise in clinical trials for radioiodine-refractory papillary thyroid carcinoma.

Q: What are the common side effects of Selumetinib?

A: Common side effects include rashes (59%), diarrhea (44%), and weakness (41%). In some studies, neutrophil depletion, dermatitis, and respiratory failure were also reported as main negative reactions.

Q: How is Selumetinib administered?

A: Selumetinib is typically administered orally, with a twice-daily dosing regimen due to its moderate oral bioavailability (62%) and relatively short half-life (6.2 hours).