General Information

Qinlock (ripretinib) is a kinase inhibitor.

Qinlock is specifically indicated for the treatment of adult patients with advanced gastrointestinal stromal tumor (GIST) who have received prior treatment with 3 or more kinase inhibitors, including imatinib.

Qinlock is supplied as a tablet for oral administration. The recommended dosage of Qinlock is 150 mg orally once daily with or without food until disease progression or unacceptable toxicity. Tablets should be swallowed whole. Qinlock should be taken at the same time each day. Advise patients to take a missed dose if less than 8 hours have passed since the missed scheduled dose. Do not take an additional dose if vomiting occurs after taking Qinlock and continue with the next scheduled dose.

Mechanism of Action

Qinlock (ripretinib) is a tyrosine kinase inhibitor that inhibits KIT proto-oncogene receptor tyrosine kinase (KIT) and platelet derived growth factor receptor A (PDGFRA) kinase, including wild type, primary, and secondary mutations. Ripretinib also inhibits other kinases in vitro, such as PDGFRB, TIE2, VEGFR2, and BRAF.

Side Effects

Adverse effects associated with the use of Qinlock may include. but are not limited to, the following:

• alopecia
• fatigue
• nausea
• abdominal pain
• constipation
• myalgia
• diarrhea
• decreased appetite\
• palmarplantar erythrodysesthesia
• vomiting
• laboratory abnormalities (≥4%) were increased lipase and decreased phosphate

Clinical Trial Results

The FDA approval of Qinlock was based on INVICTUS, a Phase 3 randomized, double-blind, placebo-controlled, international, multicenter clinical study evaluating the safety, tolerability, and efficacy of Qinlock compared to placebo in patients with advanced GIST whose previous therapies have included imatinib, sunitinib, and regorafenib. Patients were randomized 2:1 to either 150 mg of Qinlock or placebo once daily. The primary efficacy endpoint was progression-free survival (PFS) as determined by independent radiologic review using modified Response Evaluation Criteria in Solid Tumors (RECIST). The median PFS in the study was 6.3 months compared to 1.0 month in the placebo arm and significantly reduced the risk of disease progression or death by 85%. Secondary endpoints as determined by independent radiologic review using modified RECIST include Objective Response Rate (ORR) and Overall Survival (OS). Qinlock demonstrated an ORR of 9.4% compared with 0% for placebo. Qinlock also demonstrated a median OS of 15.1 months compared to 6.6 months in the placebo arm and reduced the risk of death by 64%.