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ripretinib (Qinlock)
Indications:
- advanced gastrointestinal stromal tumors (GIST) in patients who have received prior treatment with 3 or more kinase inhibitors, including imatinib.
Contraindications:
- pregnancy, breast feeding
Dosage:
- 150 mg PO QD
Tablets: 50 mg
Pharmacokinetics:
- metabolized by CYP3A
- inhibits CYP2C8
- 1/2 life 15 hours
- no increase in QTc
Adverse effects:
- > 2%
- increase in serum lipase
- hypophosphatemia
- hypertension
- fatigue
- other
- palmar-plantar erythrodysesthesia syndrome
- new primary skin cancers
- left ventricular systolic dysfunction
- impaired woumd healing
- photosensitivity
- embryo-fetal toxicity
- alopecia, myalgia, nausea/vomiting, abdominal pain, constipation, diarrhea
Mechanism of action:
- tyrosine kinase inhibitor
- inhibits KIT, PDGFRA kinase, & other kinases including PDGFRB, TIE2, VEGFR2 & BRAF
General
small inhibitory antineoplastic agent (ib drug)
Database Correlations
PUBCHEM cid=71584930
References
- Aakash B
Deciphera's Cancer Drug Improves PFS in GI Stromal Tumors.
Medscape Aug 13, 2019
https://www.medscape.com/viewarticle/916779
- Dhillon S.
Ripretinib: First Approval.
Drugs. 2020 Jul;80(11):1133-1138.
PMID: 32578014 PMCID: PMC7595980 Free PMC article. Review.
- Fung S, Shirley M.
Ripretinib: A Review in Gastrointestinal Stromal Tumours as Fourth-or Later-Line of Therapy.
Drugs. 2022 Oct;82(15):1541-1548.
PMID: 36282417 Review.
- Blay JY, Serrano C, Heinrich MC et al
Ripretinib in patients with advanced gastrointestinal stromal tumours (INVICTUS):
a double-blind, randomised, placebo-controlled, phase 3 trial.
Lancet Oncol. 2020 Jul;21(7):923-934.
PMID: 32511981 PMCID: PMC8383051 Free PMC article. Clinical Trial.