ArticleNature cancer2023
Vepafestinib is a pharmacologically advanced RET-selective inhibitor with high CNS penetration and inhibitory activity against RET solvent front mutations.
Article in Nature cancer, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 20 papers, 1 of them a synthesis that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
20 citing papers in PubMed, 1 synthesis or guideline pooled it, 32 citations in OpenAlex.
- Selpercatinib versus multi-kinase inhibitors for advanced medullary thyroid cancer: A network meta-analysis of RET-targeted therapies.Frontiers in endocrinology · 2026Pooled it
- Combination of Selpercatinib and Trametinib Overcomes Resistance to RET Inhibitors in RET-Mutant Medullary Thyroid Carcinoma.JCO precision oncology · 2026Article
- Dual targeting of RET and SRC synergizes in RET fusion-positive cancer cells.Molecular oncology · 2026Article
- Review
- Targeted therapy in thyroid cancer: molecular alterations and clinical management.Frontiers in endocrinology · 2026Review
- Pralsetinib-Induced Lymphocytic Colitis.ACG case reports journal · 2026Article
- Identification of alkynyl nicotinamide HSN748 as a RET solvent-front mutant inhibitor with intracranial efficacy.RSC medicinal chemistry · 2025Article
- Pan-Cancer Analysis of Oncogenic MET Fusions Reveals Distinct Pathogenomic Subsets with Differential Sensitivity to MET-Targeted Therapy.Cancer discovery · 2025Article
- Oncogenic Fusions in NSCLC: From Mechanisms to Clinical Applications.International journal of molecular sciences · 2025Review
- The Revolution of Targeted Therapies in Thyroid Cancer Treatment: Present and Future Promising Anti-Cancer Drugs.International journal of molecular sciences · 2025Review
- Review
- Mechanisms of resistance to RET-directed therapies.Endocrine-related cancer · 2025Review
- BYS10, a novel selective RET inhibitor, exhibits potent antitumor activity in preclinical models.Frontiers in pharmacology · 2025Article
- Overview of management and therapeutic advances in medullary thyroid cancer.Endocrine oncology (Bristol, England) · 2025Review
- Structure-Based QSAR Modeling of RET Kinase Inhibitors from 49 Different 5,6-Fused Bicyclic Heteroaromatic Cores to Patent-Driven Validation.ACS omega · 2024Article
- Review
- Preclinical evaluation of targeted therapies for central nervous system metastases.Disease models & mechanisms · 2024Review
- Therapeutic advances of targeting receptor tyrosine kinases in cancer.Signal transduction and targeted therapy · 2024Review
- Prediction of protein-ligand binding affinity via deep learning models.Briefings in bioinformatics · 2024Review
- The never-abating excitement for targeted therapies.Nature cancer · 2023Article
Corrections and comments
- Erratum issued
Authors and funding
33 authors at 6 institutions in 4 countries.
Funding
Abstract
RET receptor tyrosine kinase is activated in various cancers (lung, thyroid, colon and pancreatic, among others) through oncogenic fusions or gain-of-function single-nucleotide variants. Small-molecule RET kinase inhibitors became standard-of-care therapy for advanced malignancies driven by RET. The therapeutic benefit of RET inhibitors is limited, however, by acquired mutations in the drug target as well as brain metastasis, presumably due to inadequate brain penetration. Here, we perform preclinical characterization of vepafestinib (TAS0953/HM06), a next-generation RET inhibitor with a unique binding mode. We demonstrate that vepafestinib has best-in-class selectivity against RET, while exerting activity against commonly reported on-target resistance mutations (variants in RET
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.