Drug Detail

Information about QINLOCK

Generic Name	Ripretinib
IND	DCC-2618
Brand Name (US)	QINLOCK
Manufacturer	Deciphera Pharmaceuticals, LLC
Drug Type	Tyrosine Kinase Inhibitor
Delivery	Oral
Approval Status	Approved for GIST
Indications	4th line GIST
Overall Strategy	KIT Protein Based
Strategy	Block KIT
Drug Category	KIT/PDGFRA inhibitor

On May 15th, 2020, ripretiinib was approved for GIST patients with three or more previous treatments.
DCC-2618 is a new kind of tyrosine kinase inhibitor (TKI). Traditional TKI's work by blocking access of ATP. Deciphera's technology binds to TKI's in a different region of the protein, the "switch pocket". Pre-clinical evidence suggests that these drugs, including DCC-2618, are able to block signaling of a wide range of secondary mutations that cause resistance to Gleevec and other TKI's.
• inhibitor of primary mutant cKIT kinase

• inhibitor of secondary mutations, including exons 14 and 17.

• inhibitor of PDGFR-alpha and KDR kinases

DCC-2618 inhibits the primary mutant form of cKIT kinase ( D JMD-KIT) causative of gastrointestinal stromal tumors (GIST) in 90% of newly diagnosed patients. Importantly, it also inhibits major secondary mutant forms of D JMD-KIT, wherein patients present with additional mutations: V654A, D816V, D816H, or the gatekeeper mutant T670I. Greater than 50% of patients on therapy for GIST develop resistance to currently marketed drugs due to the emergence of these secondary mutations. It was being developed to provide patients with superior coverage of all of the mutant forms of cKIT responsible for both primary and refractory GIST. DCC-2618 has demonstrated potent in vivo inhibition of KIT in animal models.