ReviewExpert opinion on drug discovery2016
The discovery of vemurafenib for the treatment of BRAF-mutated metastatic melanoma.
Review in Expert opinion on drug discovery, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 97 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
97 citing papers in PubMed, 1 synthesis or guideline pooled it.
- New emerging treatment options for metastatic melanoma: a systematic review and meta-analysis of skin cancer therapies.Archives of dermatological research · 2024Pooled it
- Novel Functionalized Pyrrolopyridines to Target Brk.Molecules (Basel, Switzerland) · 2026Article
- Erk inhibitors intercept Erk-mediated negative feedback while imposing cell-cycle arrest and activating p38.iScience · 2026Article
- Article
- New hybrid pyridine-1,2,4-triazole scaffolds: synthesis, in vitro evaluation of anticancer and antimicrobial activity, and in silico insights.Scientific reports · 2026Article
- Heterogeneous, population-level drug-tolerant persisters exhibit ion-channel remodeling and ferroptosis susceptibility.bioRxiv : the preprint server for biology · 2026Article
- Cancer in transition: discovery of tumor-intrinsic transcriptional programs shaping the immune and microenvironmental landscape.Biomarker research · 2026Review
- Melanoma/CSPG4-Enhanced Collagen-Mediated Contact Guidance Requires Mutant Active BRAF and the CSPG4 Core Protein Cytoplasmic Domain.Cellular and molecular bioengineering · 2026Article
- Vemurafenib Induces Apoptosis via JNK Activation and AKT Inhibition in Hepatocellular Carcinoma.Journal of Cancer · 2026Article
- Assessing the accuracy of binding pose prediction for kinase proteins and 7-azaindole inhibitors: a study with AutoDock4, Vina, DOCK 6, and GNINA 1.0.RSC advances · 2025Article
- A novel murine model for sporadic, malignant peripheral nerve sheath tumors, driven by BrafV600E and Pten loss.Disease models & mechanisms · 2025Article
- Targeting Kinase Suppressor of Ras 1 (KSR1) for Cancer Therapy.Pharmaceutics · 2025Review
- Suppression of Sebum Production by Vemurafenib Through Paradoxical ERK Activation Resulted in the Inhibition of the mTOR Pathway in 5α-Dihydrotestosterone-Differentiated Hamster Sebocytes In Vitro.Experimental dermatology · 2025Article
- A highly annotated drug combination resource for catalyzing precision combinatorial therapy.Scientific data · 2025Article
- Anaplastic pleomorphic xanthoastrocytoma with leptomeningeal dissemination presenting with cranial neuropathy in an adult patient: illustrative case.Journal of neurosurgery. Case lessons · 2025Article
- Binding-Site Purification of Actives (B-SPA) Enables Efficient Large-Scale Progression of Fragment Hits by Combining Multi-Step Array Synthesis With HT Crystallography.Angewandte Chemie (International ed. in English) · 2025Article
- Exploring the Genetic Orchestra of Cancer: The Interplay Between Oncogenes and Tumor-Suppressor Genes.Cancers · 2025Review
- Small Molecule B-RAF Inhibitors as Anti-Cancer Therapeutics: Advances in Discovery, Development, and Mechanistic Insights.International journal of molecular sciences · 2025Review
- Clinical implications and molecular mechanism of long noncoding RNA LINC00518 and protein-coding genes in skin cutaneous melanoma by genome‑wide investigation.Archives of dermatological research · 2025Article
- BRAFbioRxiv : the preprint server for biology · 2024Article
37 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors.
Funding
Abstract
introductionIn the era of precision medicine and sophisticated modern genetics, the discovery of the BRAF(V600) inhibitor, vemurafenib, quickly became the model for targeted therapy in melanomas. As early as 2002, the majority of metastatic melanomas were described to harbor the BRAF(V600) mutation, setting the stage for an explosion of interest for targeting this protein as a novel therapeutic strategy. The highly selective BRAF(V600) inhibitor, vemurafenib, was identified initially through a large-scale drug screen. AREAS COVERED: Here we examine vemurafenib's journey from discovery to clinical use in metastatic melanoma. Topics covered include preclinical data, single agent Phase 1,2 and 3 clinical trials, resistance issues and mechanisms, adverse effects including the development of squamous cell cancers, and combination trials. EXPERT OPINION: Due to its tolerance, low toxicity profile, rapid tumor response, and improved outcomes in melanoma patients with BRAF(V600) mutations, vemurafenib was advanced rapidly through clinical trials to receive FDA approval in 2011. While its efficacy is well documented, durability has become an issue for most patients who experience therapeutic resistance in approximately 6-8 months. In addition, a concerning toxicity observed in patients taking the drug include development of localized cutaneous squamous cell carcinomas (SCCs). It is hypothesized that drug resistance and SCC development result from a similar paradoxical activation of protein signaling pathways, specifically MAPK. Identification of these mechanisms has led to additional treatment strategies involving new combination therapies.
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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.