avapritinib

targets D816V mutant KIT

Also Known As:

(1S)-1-(4-Fluorophenyl)-1-(2-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrrolo(2,1-f)(1,2,4)triazin-4-yl)-1-piperazinyl)-5-pyrimidinyl)ethanamine; 5-Pyrimidinemethanamine, alpha-(4-fluorophenyl)-alpha-methyl-2-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrrolo(2,1-f)(1,2,4)triazin-4-yl)-1-piperazinyl)-, (alphaS)-; BLU-285; ayvakit

Networked: 68 relevant articles (12 outcomes, 16 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Azoles: 2138
    - Pyrroles: 369
      - avapritinib: 68
    - Pyrazoles: 61
      - avapritinib: 68
  - Triazines: 306
    - avapritinib: 68

Experts

1.	DeAngelo, Daniel J: 5 articles (11/2022 - 11/2017)
2.	Gotlib, Jason: 5 articles (11/2022 - 12/2021)
3.	Reiter, Andreas: 5 articles (11/2022 - 01/2019)
4.	von Mehren, Margaret: 5 articles (01/2022 - 01/2021)
5.	Heinrich, Michael C: 5 articles (10/2021 - 11/2017)
6.	Schöffski, Patrick: 5 articles (10/2021 - 11/2017)
7.	Radia, Deepti H: 4 articles (11/2022 - 12/2021)
8.	Bose, Prithviraj: 4 articles (12/2021 - 01/2019)
9.	Verstovsek, Srdan: 4 articles (12/2021 - 01/2018)
10.	Bauer, Sebastian: 4 articles (10/2021 - 01/2021)

Related Diseases

1.	Systemic Mastocytosis 12/01/2021 - "Safety and efficacy of avapritinib in advanced systemic mastocytosis: the phase 1 EXPLORER trial." 01/01/2023 - "Efficacy of avapritinib in refractory aggressive systemic mastocytosis: a single-patient case." 12/01/2021 - "Efficacy and safety of avapritinib in advanced systemic mastocytosis: interim analysis of the phase 2 PATHFINDER trial." 01/01/2018 - "In a phase I trial of avapritinib (formerly BLU-285), which targets D816V mutant KIT, for the treatment of advanced systemic mastocytosis, patients experienced rapid and durable disease control. " 01/01/2023 - "The clinical experience of compassionate use program for avapritinib: implications for drug positioning in the therapeutic scenario of systemic mastocytosis."
2.	Gastrointestinal Stromal Tumors (Gastrointestinal Stromal Tumor) 11/30/2023 - "Clinical Benefit of Avapritinib in KIT-Mutant Gastrointestinal Stromal Tumors: A Post Hoc Analysis of the Phase I NAVIGATOR and Phase I/II CS3007-001 Studies." 01/01/2023 - "Efficacy and Safety of Avapritinib in Treating Unresectable or Metastatic Gastrointestinal Stromal Tumors: A Phase I/II, Open-Label, Multicenter Study." 10/01/2021 - "Avapritinib in unresectable or metastatic gastrointestinal stromal tumor with PDGFRA exon 18 mutation: safety and efficacy." 01/19/2021 - "Avapritinib in advanced gastrointestinal stromal tumor: case series and review of the literature from a tertiary care center in India." 01/01/2021 - "Identification of Wee1 as a target in combination with avapritinib for gastrointestinal stromal tumor treatment."
3.	Neoplasms (Cancer) 01/01/2017 - "However, phase I trials suggest that the cancer is sensitive to two new agents: BLU-285 and DCC-2618. " 11/16/2023 - "Avapritinib (BLU-285) is a targeted selective inhibitor for mutated KIT and PDGFRA receptors that can be used to treat these tumors. " 01/01/2023 - "Avapritinib was generally well tolerated and showed marked anti-tumor activity in Chinese patients with GIST bearing PDGFRA D842V mutations and notable efficacy as fourth- or later-line monotherapy (ClinicalTrials.gov Identifier: NCT04254939)." 01/01/2022 - "For those with a PDGFRA D842V mutation, avapritinib is the first TKI to lead to tumor response and disease control. " 01/01/2019 - "Moreover, avapritinib restores the chemosensitivity of ABCB1- and ABCG2-overexpressing MDR cancer cells at nontoxic concentrations. "
4.	Sarcoma (Soft Tissue Sarcoma) 10/01/2021 - "Herein, we comprehensively review the available efficacy and safety data on avapritinib, with the final goal of providing practical knowledge to both sarcoma and community-based oncologists for the correct management of this rare GIST subpopulation with this novel therapy. " 01/01/2020 - "The FDA approved avapritinib for the treatment of unresectable or metastatic gastrointestinal stromal tumors with mutations in exon 18 of PDGFRA-genetic alterations that render tumors insensitive to all previously approved therapies for this rare sarcoma of the digestive tract." 12/01/2021 - "In vitro studies tested the efficacy of MRP-1 inhibitors (nilotinib, ripretinib, selumetinib, and avapritinib) in sarcoma cell lines. "
5.	Leukemia 11/14/2023 - "We conducted a preclinical study of avapritinib in a mouse patient-derived xenograft (PDX) model of FIP1L1-PDGFRA and PDGFRA p.D842N leukemia. " 11/14/2023 - "In a T-ALL PDX model, avapritinib treatment led to decreased leukemia burden, significantly prolonged survival, and even cured a subset of mice. "

Related Drugs and Biologics

1.	Tyrosine Kinase Inhibitors
2.	ripretinib
3.	AZD 6244
4.	nilotinib
5.	multidrug resistance-associated protein 1
6.	midostaurin
7.	Dasatinib (BMS 354825)
8.	Antineoplastic Agents (Antineoplastics)
9.	regorafenib
10.	Platelet-Derived Growth Factor Receptors (Platelet-Derived Growth Factor Receptor)

Related Therapies and Procedures

1.	Therapeutics
2.	Immunotherapy
3.	Hematopoietic Stem Cell Transplantation
4.	Drug Therapy (Chemotherapy)
5.	Vitrectomy