Chemical formula: C₂₉H₃₁N₇O₃ Molecular mass: 525.613 g/mol
Selpercatinib is an inhibitor of the rearranged during transfection (RET) receptor tyrosine kinase. Selpercatinib inhibited wild-type RET and multiple mutated RET isoforms as well as VEGFR1 and VEGFR3 with IC50 values ranging from 0.92 nM to 67.8 nM. In in vitro and in vivo tumor models, selpercatinib demonstrated anti-tumor activity in cells harboring constitutive activation of RET protein resulting from gene fusions and mutations, including CCDC6-RET, KIF5B-RET, RET V804M, and RET M918T.
Competent medicine agencies globally have authorized commercialization of this active ingredient according to these medication package inserts (MPIs):
| Title | Information Source | Document Type | |
|---|---|---|---|
| RETSEVMO Hard capsule | European Medicines Agency (EU) | MPI, EU: SmPC | |
| RETEVMO Capsule | FDA, National Drug Code (US) | MPI, US: SPL/PLR |
Selpercatinib is an active ingredient of these brands:
United States (US)Austria (AT)Croatia (HR)Estonia (EE)Finland (FI)France (FR)Ireland (IE)Israel (IL)Italy (IT)Japan (JP)Lithuania (LT)Poland (PL)Romania (RO)Spain (ES)United Kingdom (UK)Note the following: The list of brand names is continuously updated, and thus does not include the total of products circulating worldwide. |
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