What is the English trade name and full scientific name of selumetinib?

Selumetinib is an oral small molecule inhibitor targeting MEK enzyme. Its scientific name is Selumetinib sulfate, and its full name is selumetinib hydrogen sulfate, which is "selumetinib hydrogen sulfate". It is a selective MEK1/2 (mitogen-activated protein kinase kinase 1 and 2) inhibitor, and its common English name is Selumetinib. It exerts anti-tumor effects by interfering with key signal transduction links in the MAPK/ERK signaling pathway. It is particularly suitable for certain tumor types that are abnormally active due to RAS mutations. In clinical applications, Selumetinib is often used to treat inoperable plexiform neurofibromas (plexiform neurofibromas) related to Neurofibromatosis type 1 (NF1), which has certain breakthrough significance, especially in pediatric patients.

The English trade name of selumetinib is Koselugo, which was jointly developed by AstraZeneca and Merck & Co., Inc. (operating as MSD in the United States and Canada). It was initially approved by the U.S. FDA in 2020 for pediatric patients 2 years old and older with NF1-related plexiform neurofibromas. It is also one of the first drugs approved for this rare disease. The advent of Koselugo is regarded as a progress in the treatment of rare tumors. It not only provides new treatment options, but also opens the door to the use of MEK inhibitors in the treatment of non-malignant tumors.

The pharmacological mechanism of selumetinib is to inhibit the activity of MEK1/2, thereby down-regulating the MAPK/ERK signaling pathway. This pathway is usually overactivated in a variety of tumors, especially tumors carrying RAS mutations, such as neurofibromas and low-grade gliomas. Through this targeted inhibition, selumetinib can inhibit the proliferation of tumor cells, promote their apoptosis, and control their growth in certain benign tumor pathological conditions.

Reference materials:https://www.koselugo.com