ripretinib

type II tyrosine switch control inhibitor

Also Known As:

1-(4-Bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea; Urea, N-(4-bromo-5-(1-ethyl-1,2-dihydro-7-(methylamino)-2-oxo-1,6-naphthyridin-3-yl)-2-fluorophenyl)-N'-phenyl-

Networked: 56 relevant articles (7 outcomes, 16 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Naphthyridines: 2
      - ripretinib: 56
Organic Chemicals: 133
- Amides: 2428
  - Urea: 15015
    - ripretinib: 56

Experts

1.	Ruiz-Soto, Rodrigo: 8 articles (10/2022 - 01/2019)
2.	George, Suzanne: 7 articles (12/2021 - 01/2020)
3.	Heinrich, Michael C: 7 articles (12/2021 - 01/2019)
4.	Gelderblom, Hans: 6 articles (12/2021 - 01/2020)
5.	Serrano, César: 6 articles (12/2021 - 01/2020)
6.	Meade, Julie: 5 articles (10/2022 - 01/2020)
7.	Blay, Jean-Yves: 5 articles (12/2021 - 01/2020)
8.	Chi, Ping: 5 articles (12/2021 - 01/2020)
9.	Jones, Robin L: 5 articles (12/2021 - 01/2020)
10.	von Mehren, Margaret: 5 articles (12/2021 - 01/2020)

Related Diseases

1.	Gastrointestinal Stromal Tumors (Gastrointestinal Stromal Tumor) 01/01/2023 - "Emerging Data on the Safety and Efficacy of Ripretinib for the Treatment of Gastrointestinal Stromal Tumors." 12/13/2022 - "Patient-reported outcomes in individuals with advanced gastrointestinal stromal tumor treated with ripretinib in the fourth-line setting: analysis from the phase 3 INVICTUS trial." 12/01/2021 - "Clinical Activity of Ripretinib in Patients with Advanced Gastrointestinal Stromal Tumor Harboring Heterogeneous KIT/PDGFRA Mutations in the Phase III INVICTUS Study." 12/01/2021 - "Ripretinib for advanced gastrointestinal stromal tumor: Plain language summary of the INVICTUS study." 01/01/2021 - "The INVICTUS trial assessed the efficacy and safety of ripretinib compared with placebo in the management of advanced gastrointestinal stromal tumors. "
2.	Neoplasms (Cancer) 04/01/2021 - "However, a partial remission (PR) of the tumor was found after 3-courses of ripretinib treatment. " 12/01/2021 - "This study reports the results of an analysis from the phase III INVICTUS study (NCT03353753) characterizing the genomic heterogeneity of tumors from patients with advanced GIST and evaluating ripretinib efficacy across KIT/PDGFRA mutation subgroups. " 12/01/2021 - "The results of the INVICTUS study showed ripretinib increased the length of time participants survived before their cancer got worse. " 12/01/2021 - "Among patients with wild-type KIT/PDGFRA by tumor tissue, PFS ranged from 2 to 23 months for ripretinib versus 0.9 to 10.1 months for placebo. " 11/01/2021 - "Tumor imaging was performed every 28-day cycle for the first four cycles in the ripretinib 150 mg QD period and then every other cycle, including the 150 mg b.i.d. "
3.	Sarcoma (Soft Tissue Sarcoma) 12/01/2021 - "In vitro studies tested the efficacy of MRP-1 inhibitors (nilotinib, ripretinib, selumetinib, and avapritinib) in sarcoma cell lines. "
4.	Disease Progression 01/01/2023 - "In this case report, we show the durable clinical benefit achieved in a patient with GIST by using ripretinib and repeated timely surgical resection of limited disease progression. " 10/01/2022 - "In a pivotal phase III clinical trial in patients with gastrointestinal stromal tumours and who had failure with three or more prior treatments, ripretinib significantly delayed disease progression compared with placebo. " 01/01/2021 - "Patients with advanced GIST who experienced disease progression (PD) at ripretinib 150 mg QD could dose escalate to 150 mg twice daily (BID). " 01/01/2021 - "Ripretinib intrapatient dose escalation after disease progression provides clinically meaningful outcomes in advanced gastrointestinal stromal tumour." 01/01/2020 - "Patients randomly assigned to placebo were permitted to cross over to ripretinib 150 mg at the time of disease progression. "
5.	Diarrhea 01/01/2022 - "Grade III AEs included diarrhea, skin rash, and anemia with one patient (5%) for each AE. Late-line ripretinib use in pretreated Taiwan and Hong Kong patients with advanced GIST showed efficacy consistent with the INVICTUS study. " 01/01/2023 - "Ripretinib is generally well tolerated, with common adverse effects of hair loss, diarrhea, cramps, fatigue and nausea. " 01/01/2021 - "The most common side effects related to ripretinib were hair loss, muscle pain, nausea, fatigue, hand-foot syndrome, and diarrhea, although most events were not very severe. " 10/01/2020 - "The most frequent (> 30%) treatment-emergent adverse events in patients with GIST receiving ripretinib 150 mg once daily (n = 142) were alopecia (n = 88 [62.0%]), fatigue (n = 78 [54.9%]), myalgia (n = 69 [48.6%]), nausea (n = 65 [45.8%]), palmar-plantar erythrodysesthesia (n = 62 [43.7%]), constipation (n = 56 [39.4%]), decreased appetite (n = 48 [33.8%]), and diarrhea (n = 47 [33.1%]). " 01/01/2023 - "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. "

Related Drugs and Biologics

1.	Sunitinib (Sutent)
2.	Imatinib Mesylate (Gleevec)
3.	avapritinib
4.	AZD 6244
5.	nilotinib
6.	multidrug resistance-associated protein 1
7.	Tyrosine Kinase Inhibitors
8.	Platelet-Derived Growth Factor Receptors (Platelet-Derived Growth Factor Receptor)
9.	regorafenib
10.	Phosphotransferases (Kinase)

Related Therapies and Procedures

1.	Therapeutics
2.	Drug Therapy (Chemotherapy)
3.	Bridge Therapy
4.	Aftercare (After-Treatment)
5.	Precision Medicine