2D 3D
	ID	DDInter1504
	Drug Type	small molecule
	Molecular Formula	C27H32FN9O2
	Molecular Weight	533.612
	CAS Number	2097132-94-8
	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]
	ATC Classification	L01EX23
IUPAC Name	(1s,4s)-N-[(1S)-1-[6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethyl]-1-methoxy-4-{4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl}cyclohexane-1-carboxamide
InChI	GBLBJPZSROAGMF-RWYJCYHVSA-N
Canonical SMILES	CO[C@@]1(CC[C@@H](CC1)C1=NC(NC2=NNC(C)=C2)=CC(C)=N1)C(=O)N[C@@H](C)C1=CC=C(N=C1)N1C=C(F)C=N1
Useful Links	DrugBank ChemSpider Wikipedia ChEMBL