| Drug Name |
Selpercatinib |
| Drug ID |
BADD_D02593 |
| Description |
Selpercatinib is a kinase inhibitor with enhanced specificity for RET tyrosine kinase receptors (RTKs) over other RTK classes.[A202055, A202052, L13604] 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.[A202049, A202055, A202052, L13604]
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.[L13604] |
| Indications and Usage |
Selpercatinib is indicated for the treatment of _RET_ fusion-positive non-small cell lung cancer in adult patients. Selpercatinib is also indicated for the systemic treatment of advanced or metastatic _RET_-mutant medullary thyroid cancer and for the systemic treatment of _RET_ fusion-positive radioactive iodine-refractory thyroid cancer in both adult and pediatric patients aged 12 and over.[L13604]
Selpercatinib is currently approved for these indications under an accelerated approval scheme and continued approval may be contingent on future confirmatory trials.[L13604] |
| Marketing Status |
approved; investigational |
| ATC Code |
L01EX22 |
| DrugBank ID |
DB15685
|
| KEGG ID |
D11713
|
| MeSH ID |
C000656166
|
| PubChem ID |
134436906
|
| TTD Drug ID |
D01KOA
|
| NDC Product Code |
71794-397; 0002-2980; 63419-0597; 71794-298; 0002-3977; 0110-2980; 0110-3977; 63419-0681 |
| UNII |
CEGM9YBNGD
|
| Synonyms |
selpercatinib | serpercatinib | LOXO-292 | 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 |
