QINLOCK—MOA
QINLOCK--engineered to block the drivers of resistance in advanced GIST
QINLOCK is the first and only switch-control kinase inhibitor that provided broad-spectrum inhibition of KIT and PDGFRα kinase signaling in vitro through a novel dual mechanism of action
As shown in preclinical studies, QINLOCK binds to both the activation switch and switch pocket of the KIT and PDGFRa kinase and locks the kinase in the inactive ("off") state, inhibiting downstream signaling and cancer cell proliferation.
In preclinical studies, this dual mechanism provided broad spectrum inhibition of KIT and PDGFRα kinase activity, including multiple primary mutations, multiple secondary mutations, and wild type. In vitro studies not designed to assess clinical efficacy.
SELECT SAFETY INFORMATION
There are no contraindications for QINLOCK.
Palmar-plantar erythrodysesthesia syndrome (PPES): In INVICTUS, Grade 1-2 PPES occurred in 21% of the 85 patients who received QINLOCK. PPES led to dose discontinuation in 1.2% of patients, dose interruption in 2.4% of patients, and dose reduction in 1.2% of patients. Based on severity, withhold QINLOCK and then resume at same or reduced dose.
Please see additional safety information and full Prescribing Information above....
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