Klug LR, Khosroyani HM, Kent JD, et al. New treatment strategies for advanced-stage gastrointestinal stromal tumours. Nat Rev Clin Oncol. 2022;19(5):328–41.

Article  Google Scholar 

Patel SR, Reichardt P. An updated review of the treatment landscape for advanced gastrointestinal stromal tumors. Cancer. 2021;127(13):2187–95.

Article  Google Scholar 

Verschoor AJ, Bovee J, Overbeek LIH, et al. The incidence, mutational status, risk classification and referral pattern of gastro-intestinal stromal tumours in the Netherlands: a nationwide pathology registry (PALGA) study. Virchows Arch. 2018;472(2):221–9.

Article  Google Scholar 

Corless CL, Schroeder A, Griffith D, et al. PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib. J Clin Oncol. 2005;23(23):5357–64.

Article  CAS  Google Scholar 

Manley PW, Cowan-Jacob SW, Buchdunger E, et al. Imatinib: a selective tyrosine kinase inhibitor. Eur J Cancer. 2002;38(Suppl 5):S19-27.

Article  Google Scholar 

Heinrich MC, Corless CL, Blanke CD, et al. Molecular correlates of imatinib resistance in gastrointestinal stromal tumors. J Clin Oncol. 2006;24(29):4764–74.

Article  CAS  Google Scholar 

US FDA. Qinlock® (ripretinib) tablets: US prescribing information. 2021. https://www.qinlockhcp.com/. Accessed 28 Sep 2022.

European Medicines Agency. QINLOCK 50 mg tablets: summary of product characteristics. 2021. https://www.ema.europa.eu/. Accessed 28 Sep 2022.

Smith BD, Kaufman MD, Lu WP, et al. Ripretinib (DCC-2618) is a switch control kinase inhibitor of a broad spectrum of oncogenic and drug-resistant KIT and PDGFRA variants. Cancer Cell. 2019;35(5):738-51.e9.

Article  CAS  Google Scholar 

Janku F, Abdul Razak AR, Chi P, et al. Switch control inhibition of KIT and PDGFRA in patients with advanced gastrointestinal stromal tumor: a phase I study of ripretinib. J Clin Oncol. 2020;38(28):3294–303.

Article  CAS  Google Scholar 

Li X, Shelton MJ, Wang J, et al. Effects of CYP3A inhibition, CYP3A induction, and gastric acid reduction on the pharmacokinetics of ripretinib, a switch control KIT tyrosine kinase inhibitor. Clin Pharmacol Drug Dev. 2022. https://doi.org/10.1002/cpdd.1110.

Article  PubMed  PubMed Central  Google Scholar 

Blay J-Y, 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;21(7):923–34.

Article  CAS  Google Scholar 

Bauer S, Heinrich MC, George S, et al. Clinical activity of ripretinib in patients with advanced gastrointestinal stromal tumor harboring heterogeneous KIT/PDGFRA mutations in the phase III INVICTUS study. Clin Cancer Res. 2021;27(23):6333–42.

Article  CAS  Google Scholar 

Eisenhauer EA, Therasse P, Bogaerts J, et al. New response evaluation criteria in solid tumours: revised RECIST guideline (version 1.1). Eur J Cancer. 2009;45(2):228–47.

Article  CAS  Google Scholar 

Demetri GD, Reichardt P, Kang Y-K, et al. Efficacy and safety of regorafenib for advanced gastrointestinal stromal tumours after failure of imatinib and sunitinib (GRID): an international, multicentre, randomised, placebo-controlled, phase 3 trial. Lancet. 2013;381(9863):295–302.

Article  CAS  Google Scholar 

von Mehren M, Heinrich MC, George S, et al. Ripretinib as ≥ 4th-line treatment in patients with advanced gastrointestinal stromal tumor: long-term update from the phase III INVICTUS study [abstract no. 1540P and poster]. Ann Oncol. 2021;32(Suppl 5):S1120–1.

Article  Google Scholar 

Zalcberg JR, Heinrich MC, George S, et al. Clinical benefit of ripretinib dose escalation after disease progression in advanced gastrointestinal stromal tumor: an analysis of the INVICTUS study. Oncologist. 2021;26(11):e2053–60.

Article  CAS  Google Scholar 

Bauer S, Jones RL, Blay JY, et al. Ripretinib versus sunitinib in patients with advanced gastrointestinal stromal tumor after treatment with imatinib (INTRIGUE): a randomized, open-label, phase III trial. J Clin Oncol. 2022;2022:JCO2200294.

Article  Google Scholar 

Robert C, Soria JC, Spatz A, et al. Cutaneous side-effects of kinase inhibitors and blocking antibodies. Lancet Oncol. 2005;6(7):491–500.

Article  CAS  Google Scholar 

Patel A, George S, Janku F, et al. Dermatopathological review of cutaneous squamous cell carcinoma events in patients with gastrointestinal stromal tumors treated with ripretinib [abstract no. P-107 and poster]. Ann Oncol. 2021;32(Suppl 3):S134–5.

Article  Google Scholar 

Chen MH, Kerkela R, Force T. Mechanisms of cardiac dysfunction associated with tyrosine kinase inhibitor cancer therapeutics. Circulation. 2008;118(1):84–95.

Article  Google Scholar 

Li X, Psoinos CM, Shelton MJ, et al. Effect of hepatic impairment on the pharmacokinetics of ripretinib [abstract no. e16031]. J Clin Oncol. 2022;40(16 Suppl):e16031.

Article  Google Scholar 

Casali PG, Blay JY, Abecassis N, et al. Gastrointestinal stromal tumours: ESMO–EURACAN–GENTURIS clinical practice guidelines for diagnosis, treatment and follow-up. Ann Oncol. 2022;33(1):20–33.

Article  CAS  Google Scholar 

National Comprehensive Cancer Network. Gastroinestinal stromal tumors (GISTs): NCCN guidelines version 2.2022. 2022. https://www.nccn.org/. Accessed 28 Sep 2022.

Taiho Pharmaceutical Co. Taiho pharmaceutical obtains approval to manufacture and market HSP90 inhibitor Jeselhy® tablets 40 mg (pimitespib) for gastrointestinal stromal tumor (GIST) [media release]. 20 June 2022. https://www.taiho.co.jp/.