selumetinib

Selumetinib is an orally administered small molecule that acts as a selective inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1 and MEK2). These enzymes are key components of the RAS-RAF-MEK-ERK signaling pathway, which regulates cell proliferation, differentiation, survival, and angiogenesis. By blocking MEK1/2, selumetinib inhibits downstream signaling, leading to reduced tumor growth. Developed by AstraZeneca, selumetinib is marketed under the brand name Koselugo. It is approved by the FDA for the treatment of pediatric patients aged two years and older with neurofibromatosis type 1 (NF1) who have symptomatic, inoperable plexiform neurofibromas. Selumetinib is also being investigated for other cancer types, including pediatric low-grade glioma, non-small cell lung cancer, and melanoma.

Brand names

Koselugo

Other names

selumetinib