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On May 15, 2020, the FDA approved ripretinib for adult patients with advanced gastrointestinal stromal tumor who have received prior treatment with three or more kinase inhibitors, including imatinib. The approval was based on results from INVICTUS (NCT03353753), an international, multi-center, double-blind, placebo-controlled trial. Patients were randomly allocated (2:1) to receive either ripretinib 150 mg once daily (n = 85) or matching placebo (n = 44). The trial demonstrated a statistically significant improvement in progression-free survival (PFS) as assessed by modified RECIST v1.1 by blinded independent central review for patients randomized to ripretinib, with a median PFS of 6.3 months [95% confidence interval (CI): 4.6-6.9] compared with 1.0 month (95% CI: 0.9-1.7) for placebo [HR: 0.15 (95% CI: 0.09-0.25); P < 0.0001, stratified log-rank test]. There was no statistically significant difference in objective response rate in the ripretinib arm, 9% (95% CI: 4.2-18) compared with placebo 0% [(95% CI: 0-8); P = 0.0504, Fisher exact test]. The median overall survival (OS) in the ripretinib arm was 15.1 months (95% CI: 12.3-15.1) compared with 6.6 months (95% CI: 4.1-11.6) in the placebo arm. A formal statistical comparison of OS was not made due to the prespecified hierarchical analysis plan. The most common (≥20%) adverse events with ripretinib, in order of decreasing frequency, were alopecia, fatigue, nausea, abdominal pain, constipation, myalgia, diarrhea, decreased appetite, palmar-plantar erythrodysesthesia, and vomiting. Other important risks of ripretinib include new primary cutaneous malignancies, hypertension, and cardiac dysfunction.
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http://dx.doi.org/10.1158/1078-0432.CCR-22-2400 | DOI Listing |
Ann Dermatol Venereol
August 2025
Oncodermatology, Oncopole Claudius Regaud, Institut Universitaire du cancer Toulouse Oncopole, France. Electronic address:
Front Oncol
August 2025
Department of Oncology, The First Affiliated Hospital of Nanjing Medical University, Jiangsu, Nanjing, China.
This study reports a 40-year-old male with small intestinal stromal tumor (SIST). After initial surgery and adjuvant imatinib, the tumor recurred. The patient then received multiple rounds of treatment with targeted drugs and surgical interventions.
View Article and Find Full Text PDFBiomed Chromatogr
September 2025
BRIC, UMR1312, Univ. Bordeaux, INSERM, Bordeaux, France.
Therapeutic drug monitoring of protein kinase inhibitors is widely practiced worldwide. Based on the example of ripretinib dosage requested by a clinician, we detailed the process of method development, using a literature-based approach while ensuring the sustainability of the method to be as environmentally friendly as possible. Therefore, a UPLC-MS/MS method for ripretinib and its active metabolite was optimized and validated using the corresponding stable isotopic internal standards in human plasma.
View Article and Find Full Text PDFBackground: Gastrointestinal stromal tumors (GISTs) are rare tumors of the digestive tract that have seen significant advances in diagnosis and treatment in recent years. A key breakthrough was the identification of c-KIT and PDGFRA gene mutations, which enabled the introduction of targeted therapies. The cornerstone of the treatment for localized disease is radical (R0) surgical resection, with adjuvant imatinib recommended for patients at high risk of recurrence.
View Article and Find Full Text PDFEur J Med Chem
November 2025
Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China. Electronic address:
Novel 4-anilinoquinoline and 4-anilinoquinazoline hybrids were designed and synthesized as PDGFR-α inhibitors based on lenvatinib, ripretinib and sorafenib. The target compounds were screened in vitro for their anti-PDGFR-α activity. Most of the compounds had shown promising activity in the PDGFR-α kinase assay.
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