In this article, we will discuss Selumetinib (Mechanism of Action). So, let’s get started.
Mechanism of Action
Selumetinib is an inhibitor of mitogen-activated protein kinase kinases 1 and 2 (MEK1/2). MEK1/2 proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway. Both MEK and ERK are critical components of the RAS-regulated RAF-MEK-ERK pathway, which is often activated in different types of cancers. In genetically modified mouse models of NF1 that generate neurofibromas that recapitulate the genotype and phenotype of human NF1, oral dosing of selumetinib inhibited ERK phosphorylation, and reduced neurofibroma numbers, volume, and proliferation.
Pharmacodynamics
The exposure-response relationship and time course of pharmacodynamic response for the safety and effectiveness of Selumetinib have not been fully characterized.
Cardiac Electrophysiology
At a dose 1.5 times the maximum recommended dose, Selumetinib does not prolong the QT/QTc interval to any clinically relevant extent.