Ripretinib in GIST:

Metastatic KIT-driven GIST is a disease characterized by many mutations in KIT, with over 90% of individual KIT-driven GIST patients harboring multiple mutations that drive progression of their disease. The complex heterogeneity of KIT mutations within individual tumors and individual patients is a major cause of resistance to existing therapies.

While approved kinase inhibitors control certain initiating and drug resistance-causing mutations in KIT and PDGFRα, the kinases that drive disease progression in most GIST patients, these approved drugs fail to inhibit all known mutations. Ripretinib was specifically designed to improve the treatment of GIST patients by inhibiting the full spectrum of known mutations in KIT and PDGFRα.

Ripretinib is a KIT and PDGFRα inhibitor that blocks initiating KIT mutations in exons 9, 11, 13, 14, 17, and 18, known to be present in GIST patients, and the D816V exon 17 mutation. Ripretinib inhibits PDGFRα mutations in exon 18, including the D842V mutation that drives a subset of GIST.

Currently, ripretinib is approved in the U.S., Canada and Australia – to learn more go to QINLOCK.com. We have an ongoing Phase 3 clinical study, INTRIGUE, in second-line GIST.

Development Status

Tumor TypeStatus
GIST – 4th Line*Approved
GIST – 2nd Line**Phase 3 Pivotal Study – Ongoing
GISTPhase 1 Expansion Study – Ongoing

*Patients who have received 3 or more kinase inhibitors, including imatinib.

**Patients who progressed on or were intolerant to first-line anticancer treatment with imatinib.

Further information related to ripretinib from the 2020 ESMO presentations are available here: 2020 ESMO Phase 3 INVICTUS Presentation

Press Release »   |   Publication – The Lancet »  |   Publication – Journal of Clinical Oncology »

In addition, further information regarding ripretinib and Deciphera’s pipeline is available in the most recent corporate presentation here »

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