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SELPERCATINIB
CAS NO.: 2152628-33-4
Chemical Formula: C29H31N7O3
Molecular Weight: 525.6000
DMF&GMP status: Please contact us for more details.
Description:
Selpercatinib is 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.

Selpercatinib is a kinase inhibitor with enhanced specificity for RET tyrosine kinase receptors (RTKs) over other RTK classes. Enhanced RET (Rearranged during transfection) oncogene expression is a hallmark of many cancers. Although multikinase inhibitors, including [cabozantinib], [ponatinib], [sorafenib], [sunitinib], and [vandetanib], have shown efficacy in RET-driven cancers, their lack of specificity is generally associated with substantial toxicity. Selpercatinib (LOXO-292) and pralsetinib (BLU-667) represent the first generation of specific RET RTK inhibitors for the treatment of RET-driven cancers. Although selpercatinib is currently still under investigation in clinical trial NCT04211337, it was granted accelerated FDA approval on May 8, 2020, for specific RET-driven cancer indications. It is currently marketed under the brand name RETEVMO™ by Loxo Oncology Inc.

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Approvals
Active Ingredient Dosage Form; Route Strength Proprietary Name Applicant
SELPERCATINIBCAPSULE;ORAL40MGRETEVMOLOXO ONCOLOGY INC
SELPERCATINIBCAPSULE;ORAL80MGRETEVMOLOXO ONCOLOGY INC
Patent Data
Patent No. Patent Expiration Drug Substance Claim Drug Product Claim Patent Use Code
1011294210/10/2037DSDP
1013712410/10/2037U-2826 U-2827 U-2828
1017285110/10/2037U-2826 U-2827 U-2828
1058412410/10/2038DSU-2826 U-2827 U-2828
1078648910/10/2038DPU-2971 U-2972 U-2973 U-2974 U-2975 U-2976 U-2977
Exclusive Data
Exclusivity Code Exclusivity Expiration
NCE 05/08/2025
ODE-301 05/08/2027
ODE-302 05/08/2027
ODE-303 05/08/2027