^
Contact us  to learn more about
our Premium Content:  News alerts, weekly reports and conference planners
DRUG:

Tafinlar (dabrafenib)

i
Other names: GSK2118436, GSK436, 2118436, DRB 436, GSK-2118436A, GSK2118436A, GSK-2118436, GSK 2118436, DRB-436, DRB436, GSK 2118436A, GSK-436, GSK 436
Company:
BeOne Medicines, Novartis
Drug class:
BRAF inhibitor
3d
Macrophage-Derived PDGF-BB and GDF-15 Promote Drug Resistance in KRAS-Mutant Colorectal Cancer. (PubMed, bioRxiv)
In contrast, macrophage-conditioned medium had little effect on regorafenib and increased sensitivity to dabrafenib, suggesting that resistance depends on the inhibitory profile of each drug. The multi-kinase inhibitor masitinib-which targets several kinases along this resistance network-strongly restored sensitivity to trametinib and RMC-6236. Together, these data define a macrophage-driven resistance network in KRAS-mutant colorectal cancer organoids and support combined inhibition of RAS-pathway and tyrosine kinase signalling.
Journal
|
KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53) • GDF15 (Growth differentiation factor 15)
|
KRAS mutation
|
Mekinist (trametinib) • Tafinlar (dabrafenib) • Stivarga (regorafenib) • daraxonrasib (RMC-6236) • Kinaction (masitinib)
4d
Durable complete response to pembrolizumab after BRAF/MEK inhibition in recurrent MSI-H/dMMR, BRAF V600E-mutant colon cancer: a case report. (PubMed, Front Oncol)
Given her advanced age and frailty, she was treated with a first-line combination of pembrolizumab, dabrafenib, and trametinib. She achieved a radiographic complete response (CR) and has remained progression-free for over 26 months. This case highlights the potential synergy between MAPK pathway inhibition and immunotherapy, suggesting that even short-course targeted therapy may favorably remodel the tumor microenvironment to enable durable disease control in high-risk MSI-H/BRAF-mutant mCRC.
Journal • MSi-H Biomarker • PD(L)-1 Biomarker • IO biomarker • MSI-H • dMMR
|
BRAF (B-raf proto-oncogene) • MSI (Microsatellite instability)
|
BRAF V600E • MSI-H/dMMR • BRAF V600
|
Keytruda (pembrolizumab) • Mekinist (trametinib) • Tafinlar (dabrafenib)
4d
Pediatric Long-Term Follow-up and Rollover Study (clinicaltrials.gov)
P4, N=165, Recruiting, Novartis Pharmaceuticals | Active, not recruiting --> Recruiting
Enrollment open
|
Mekinist (trametinib) • Tafinlar (dabrafenib)
5d
Synovial Sarcoma With BRAF V600E Mutation: A Case Report and Literature Review. (PubMed, Genes Chromosomes Cancer)
Treatment with combined BRAF and MEK inhibition (dabrafenib and trametinib) resulted in a clinical response. In addition to this index case, a literature review identified multiple additional SS harboring BRAF V600E, supporting its role as a recurrent, potentially targetable alteration in a small subset of SS. These findings highlight the value of comprehensive genomic profiling in SS, particularly in advanced or refractory cases, to identify rare but actionable molecular events that may expand therapeutic options.
Review • Journal
|
BRAF (B-raf proto-oncogene) • SS18 (SS18 Subunit Of BAF Chromatin Remodeling Complex) • SSX1 (SSX Family Member 1)
|
BRAF V600E • BRAF V600
|
Mekinist (trametinib) • Tafinlar (dabrafenib)
6d
Quantitative BRAF p.V600E mutation monitoring in cerebrospinal fluid cell-free DNA reflects therapeutic response to BRAF/MEK inhibitors in papillary craniopharyngioma: a report of two cases. (PubMed, Acta Neuropathol Commun)
Here, we present two patients with BRAF p.V600E-mutant PCP who achieved exceptional tumor volume reductions of 95% and 98% following targeted therapy with dabrafenib and trametinib. Notably, Case 1 maintained the negative mutation status and did not experience recurrence during the 9-month follow-up period. These findings demonstrate that digital polymerase chain reaction-based monitoring of CSF-derived cfDNA is a sensitive and objective tool for assessing molecular response in PCP, reflecting the real-time efficacy of targeted treatment and providing a framework for individualized management and early detection of recurrence in precision neurooncology.
Journal • Tumor mutational burden
|
TMB (Tumor Mutational Burden)
|
BRAF V600E • BRAF V600
|
Mekinist (trametinib) • Tafinlar (dabrafenib)
11d
MULTISARC: Molecular Profiling of Advanced Soft-tissue Sarcomas (clinicaltrials.gov)
P3, N=603, Completed, Institut National de la Santé Et de la Recherche Médicale, France | Active, not recruiting --> Completed
Trial completion • IO biomarker
|
Lynparza (olaparib) • Mekinist (trametinib) • Ibrance (palbociclib) • Tafinlar (dabrafenib) • Imfinzi (durvalumab) • lapatinib • Zykadia (ceritinib) • nilotinib • Lytgobi (futibatinib) • Tabrecta (capmatinib) • Daurismo (glasdegib)
11d
Pathologic and Radiologic Response to Neoadjuvant Therapy in Advanced Differentiated thyroid Cancer. (PubMed, Eur Thyroid J)
Lenvatinib induced vascular remodeling and immune infiltration, in contrast to fibrosis primarily seen with dabrafenib/trametinib. These histologic differences may have implications for future therapeutic decision-making.
Journal
|
BRAF (B-raf proto-oncogene) • CD31 (Platelet and endothelial cell adhesion molecule 1) • PECAM1 (Platelet And Endothelial Cell Adhesion Molecule 1)
|
Mekinist (trametinib) • Tafinlar (dabrafenib) • Lenvima (lenvatinib)
12d
Rapid and profound radiological and plasma ctDNA responses to dabrafenib plus trametinib in BRAF-mutant papillary craniopharyngioma. (PubMed, Neurooncol Adv)
Additional therapeutic trials evaluating upfront BRAF-targeted therapy to minimize local therapies (including surgery and radiation) are needed. Liquid biopsy should be further explored as a non-invasive way of diagnosis and treatment monitoring.
Journal • Circulating tumor DNA
|
BRAF (B-raf proto-oncogene)
|
BRAF V600E • BRAF mutation • BRAF V600
|
Mekinist (trametinib) • Tafinlar (dabrafenib)
13d
In silico evaluation of selected triterpenes as potential inhibitors of BRAF and BRAFV600E kinases for cancer treatment. (PubMed, J Mol Model)
Vemurafenib and dabrafenib are two selective BRAF inhibitors approved by the FDA for clinical use. Molecular dynamics and metadynamics simulations were performed in the Desmond module of the academic version of the Schrödinger-Maestro 2021-4 program, utilizing the OPLS-2005 force field. Finally, all the protein figures presented in this article were made in the PyMOL program and the RMSD graphics were made in the statistical package R and RStudio 2025.05.1.
Journal
|
BRAF (B-raf proto-oncogene)
|
BRAF V600E • BRAF V600 • BRAF wild-type
|
Zelboraf (vemurafenib) • Tafinlar (dabrafenib)
13d
Molecular Mechanisms of Radioiodine Refractoriness in Differentiated Thyroid Cancer: Focus on Sodium/Iodide Symporter Dysregulation. (PubMed, Curr Issues Mol Biol)
Redifferentiation approaches using MAPK pathway inhibitors such as selumetinib and dabrafenib can restore iodine uptake in selected patients, although the overall clinical applicability of these strategies remains under evaluation. A better understanding of these mechanisms may support improved biologic stratification and more selective therapeutic decision-making in radioiodine-refractory DTC.
Review • Journal
|
BRAF (B-raf proto-oncogene) • TERT (Telomerase Reverse Transcriptase) • MIR221 (MicroRNA 221) • MIR146B (MicroRNA 146b) • MIR204 (MicroRNA 204) • MIR222 (MicroRNA 222)
|
BRAF V600E • BRAF V600
|
Tafinlar (dabrafenib) • Koselugo (selumetinib)
14d
CRISPR-Based Gene Dependency Screens Reveal Mechanism of BRAF Inhibitor Resistance in Anaplastic Thyroid Cancer. (PubMed, Mol Carcinog)
TAZ loss represses the UPR, reverses the inhibition of protein synthesis, and triggers increased cell death by ferroptosis in dabrafenib-treated ATC. Collectively, our findings unveil TAZ as a new target to overcome resistance to BRAF inhibitors in undifferentiated thyroid cancer.
Journal
|
WWTR1 (WW Domain Containing Transcription Regulator 1) • TAFAZZIN (Tafazzin)
|
BRAF V600E • BRAF wild-type
|
Tafinlar (dabrafenib)
16d
MegaMOST: A Study Evaluating the Activity of Anti-cancer Treatments Targeting Tumor Molecular Alterations/Characteristics in Advanced / Metastatic Tumors. (clinicaltrials.gov)
P2, N=455, Recruiting, Centre Leon Berard | Trial completion date: Nov 2026 --> Oct 2027 | Trial primary completion date: Feb 2026 --> Oct 2026
Trial completion date • Trial primary completion date
|
KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • FLT3 (Fms-related tyrosine kinase 3) • MET (MET proto-oncogene, receptor tyrosine kinase) • NRAS (Neuroblastoma RAS viral oncogene homolog) • KIT (KIT proto-oncogene, receptor tyrosine kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK2 (Neurotrophic tyrosine kinase, receptor, type 2) • HRAS (Harvey rat sarcoma viral oncogene homolog) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • NF1 (Neurofibromin 1) • AXL (AXL Receptor Tyrosine Kinase) • CCND1 (Cyclin D1) • CDK4 (Cyclin-dependent kinase 4) • PTPN11 (Protein Tyrosine Phosphatase Non-Receptor Type 11) • SMAD4 (SMAD family member 4) • RAF1 (Raf-1 Proto-Oncogene Serine/Threonine Kinase) • FLT1 (Fms-related tyrosine kinase 1) • CDK6 (Cyclin-dependent kinase 6) • CCND3 (Cyclin D3) • TYRO3 (TYRO3 Protein Tyrosine Kinase) • NTRK (Neurotrophic receptor tyrosine kinase)
|
BRAF mutation • NRAS mutation • BRAF V600 • KIT mutation • CDKN2A deletion • HRAS mutation • KRAS G12 • PDGFRA mutation • KRAS amplification • NRAS G12
|
Mekinist (trametinib) • Tafinlar (dabrafenib) • Alecensa (alectinib) • Cabometyx (cabozantinib tablet) • Stivarga (regorafenib) • Kisqali (ribociclib) • Ayvakit (avapritinib) • siremadlin (HDM201)