Selpercatinib

ATC Code L01EX22

Selpercatinib

Definition

An orally bioavailable selective inhibitor of wild-type, mutant and fusion products involving the proto-oncogene receptor tyrosine kinase rearranged during transfection (RET), with potential antineoplastic activity. Upon oral administration, selpercatinib selectively binds to and targets wild-type RET as well as various RET mutants and RET-containing fusion products. This results in an inhibition of cell growth of tumors cells that exhibit increased RET activity. In addition, selpercatinib targets, binds to and inhibits vascular endothelial growth factor receptor 1 (VEGFR1) and 3 (VEGFR3), and fibroblast growth factor receptor 1 (FGFR1), 2 (FGFR2), and 3 (FGFR3). RET overexpression, activating mutations, and fusions result in the upregulation and/or overactivation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and progression of these cancers.

Also known as 6-(2-Hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo(3.1.1)heptan-3-yl)pyridin-3-yl)pyrazolo(1,5-a)pyridine-3-carbonitrile, LOXO 292, LOXO-292, LOXO292, RET Inhibitor LOXO-292, RET Kinase Inhibitor LOXO-292, Retevmo, Retsevmo, SELPERCATINIB, WHO 10967 — per NCIT

Also identified as

Indications

Disease Relation Source
Non-small cell lung carcinoma may treat MEDRT · Public domain (U.S. Government work)

Organ Effects

Organ Side effect / interaction Source
Lungs may treat a disease of this organ DERIVED · CC BY 4.0

1 entry above is marked DERIVED: Atlas Médico inferred it by combining two sourced claims, and no source asserts this link directly. Treat it as a navigation aid, not as a clinical statement.