Discover Community Create You

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

Avapritinib-based SAR studies unveil a binding pocket in KIT and PDGFRA.

Nature communications - 2 Jan 2024

Teuber A, Schulz T, Fletcher B S, Gontla R, Mühlenberg T, Zischinsky M-L, Niggenaber J, Weisner J, Kleinbölting S B, Lategahn J, Sievers S, Müller M P, Bauer S, Rauh D

Abstract excerpt

Avapritinib is the only potent and selective inhibitor approved for the treatment of D842V-mutant gastrointestinal stromal tumors (GIST), the most common primary mutation of the platelet-derived growth factor receptor α (PDGFRA). The approval was based on the NAVIGATOR trial, which revealed overall response rates of more than 90%. Despite this transformational activity, patients eventually progress, mostly due to...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Antineoplastic Agents
Share to Gastrointestinal Stromal Tumors

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Gastrointestinal Tumor Research and Treatment

Share to Mutation

Share to Proto-Oncogene Proteins c-kit

Share to Pyrazoles

Share to Pyrroles

Share to Receptor, Platelet-Derived Growth Factor alpha

Source

Open in PubMed Open full text

Identifiers

PMID: 38167404
DOI: 10.1038/s41467-023-44376-8
PMCID: PMC10761696

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 4 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Avapritinib-based SAR studies unveil a binding pocket in KIT and PDGFRA.PMID 38167404Read ↗

The EMA assessment of avapritinib in the treatment of gastrointestinal stromal tumours harbouring the PDGFRA D842V mutation.Semantic proximity Read ↗

Avapritinib in unresectable or metastatic gastrointestinal stromal tumor with PDGFRA exon 18 mutation: safety and efficacy.Semantic proximity Read ↗

Efficacy and Safety of Avapritinib in Treating Unresectable or Metastatic Gastrointestinal Stromal Tumors: A Phase I/II, Open-Label, Multicenter Study.Semantic proximity Read ↗

Avapritinib in unresectable or metastatic PDGFRA D842V-mutant gastrointestinal stromal tumours: Long-term efficacy and safety data from the NAVIGATOR phase I trial.Semantic proximity Read ↗

Avapritinib: First Approval.Semantic proximity Read ↗

Structure-based scaffold hopping reveals strategies to overcome oncogenic KIT and PDGFRA mutation-driven drug-resistance in GIST.Semantic proximity Read ↗

Predicting Clinical Sensitivities of PDGFRA Exon 18 Mutations to Imatinib and Avapritinib to Optimize Gastrointestinal Stromal Tumor Treatment.Semantic proximity Read ↗

Structure-based Scaffold Hopping Reveals Strategies to Overcome Oncogenic KIT and PDGFRA Mutation-Driven Drug-Resistance in GISTSemantic proximity Read ↗

Avapritinib for metastatic or unresectable gastrointestinal stromal tumors.Semantic proximity Read ↗

Resistance to Avapritinib in PDGFRA-Driven GIST Is Caused by Secondary Mutations in the PDGFRA Kinase Domain.Semantic proximity Read ↗

Avapritinib in advanced PDGFRA D842V-mutant gastrointestinal stromal tumour (NAVIGATOR): a multicentre, open-label, phase 1 trial.Semantic proximity Read ↗

Clinical efficacy comparison of avapritinib with other tyrosine kinase inhibitors in gastrointestinal stromal tumors with PDGFRA D842V mutation: a retrospective analysis of clinical trial and real-world dataSemantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.