drug · small molecule

KOSELUGO

updated 2mo ago

by $AZN ASTRAZENECA PLC🔗 ChEMBL

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Small molecule drug with a maximum clinical stage of Approval (across all indications), with an approval for neurofibromatosis type 1 and neoplasm and 20 investigational indications.

targets

Dual specificity mitogen-activated protein kinase kinase 2Dual specificity mitogen-activated protein kinase kinase; MEK1/2Dual specificity mitogen-activated protein kinase kinase 1

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brand

KOSELUGO

generic

SELUMETINIB

MOA

12.1 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.

indication

1 INDICATIONS AND USAGE KOSELUGO is indicated for the treatment of adult and pediatric patients 1 year of age and older with neurofibromatosis type 1 (NF1) who have symptomatic, inoperable plexiform neurofibromas (PN) [see Dosage and Administration (2) ]. KOSELUGO is a kinase inhibitor indicated for the treatment of adult and pediatric patients 1 year of age and older with neurofibromatosis type 1 (NF1) who have symptomatic, inoperable plexiform neurofibromas (PN). ( 1 )

KOSELUGO

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Trials studying KOSELUGO