| Drug Name |
Pralsetinib |
| Drug ID |
BADD_D02585 |
| Description |
Pralsetinib, similar to the previously approved [selpercatinib], is a kinase inhibitor with enhanced specificity for RET tyrosine kinase receptors (RTKs) over other RTK classes.[A202055, A219751, L15986] Enhanced RET (Rearranged during transfection) oncogene expression is a hallmark of many cancers, including non-small cell lung cancer. 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.[A202055] Pralsetinib (BLU-667) and [selpercatinib] (LOXO-292) represent the first generation of specific RET RTK inhibitors for the treatment of RET-driven cancers.[A202049, A202055, L15986]
Although a phase 1/2 trial of pralsetinib termed ARROW (NCT03037385) is still ongoing, pralsetinib was granted accelerated FDA approval on September 4, 2020, for the treatment of metastatic RET-fusion positive non-small cell lung cancer. It is currently marketed under the brand name GAVRETO™ by Blueprint Medicines.[L15986] |
| Indications and Usage |
Pralsetinib is indicated for the treatment of metastatic non-small cell lung cancer (NSCLC) in adult patients who are confirmed to possess a rearranged during transfection (RET) gene fusion, as determined by an FDA approved test.[L15986] It is also indicated in adult and pediatric patients 12 years of age and older for the treatment of advanced or metastatic _RET_-mutant medullary thyroid cancer, and in this same population for the treatment of advanced or metastatic _RET_ fusion-positive thyroid cancer who require systemic therapy and for whom radioactive iodine is not appropriate.[L15986]
Pralsetinib is currently approved for this indication under an accelerated approval scheme and continued approval may be contingent on future confirmatory trials.[L15986] |
| Marketing Status |
approved; investigational |
| ATC Code |
L01EX23 |
| DrugBank ID |
DB15822
|
| KEGG ID |
D11712
|
| MeSH ID |
C000655704
|
| PubChem ID |
Not Available
|
| TTD Drug ID |
D0OD2I
|
| NDC Product Code |
50242-210; 11014-0438 |
| UNII |
1WPE73O1WV
|
| Synonyms |
pralsetinib | BLU-667 | gavreto | trans-N-((1S)-1-(6-(4-Fluoro-1H-pyrazol-1-yl)-3-pyridinyl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1H-pyrazol-3-yl)amino)-2-pyrimidinyl)cyclohexanecarboxamide | Cyclohexanecarboxamide, N-((1S)-1-(6-(4-fluoro-1H-pyrazol-1-yl)-3-pyridinyl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1H-pyrazol-3-yl)amino)-2-pyrimidinyl)-, trans- |
