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DRUG CLASS:

cRAF inhibitor

1d
Defactinib, Avutometinib and Nivolumab for the Treatment of Anti-PD1 Refractory LKB1-Mutant Advanced Non-Small Cell Lung Cancer (clinicaltrials.gov)
P2, N=50, Recruiting, Emory University | Trial completion date: Sep 2028 --> Sep 2029 | Trial primary completion date: Mar 2028 --> Mar 2029
Trial completion date • Trial primary completion date • IO biomarker
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KRAS (KRAS proto-oncogene GTPase) • STK11 (Serine/threonine kinase 11)
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KRAS G12C • KRAS G12
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Opdivo (nivolumab) • Avmapki (avutometinib) • Fakzynja (defactinib) • ABP 206 (nivolumab biosimilar)
2d
PRAME-Positive Eruptive Melanocytic Nevi in the Setting of BRAF-Inhibitors. (PubMed, J Cutan Pathol)
We report here a patient on encorafenib who developed numerous new pigmented lesions within 3 weeks of therapy...This case underscores that BRAF inhibition may enhance PRAME expression in benign melanocytic nevi, potentially through mechanisms involving mitogen-activated protein kinase (MAPK) activation, altered Erk phosphorylation, or disruption of retinoic acid (RA) signaling. This case also brings awareness to the potential of medication-induced PRAME expression and encourages both dermatologists and dermatopathologists to avoid overdiagnosis as PRAME continues to gain prominence as a diagnostic biomarker.
Journal
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PRAME (Preferentially Expressed Antigen In Melanoma)
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Braftovi (encorafenib)
11d
Targeting the energy metabolism of melanoma cells: FX-11 acts as a mitochondrial uncoupler. (PubMed, Eur J Pharmacol)
In a compound screen on melanoma cells, we identified FX-11 as one of the compounds inhibiting the growth of sensitive and Encorafenib/Binimetinib-resistant 624Mel and Wm3248 melanoma cells. Taken together, we provide evidence that FX-11 inhibits the growth of melanoma cells, including drug-resistant ones, through an AMPK-dependent mechanism by acting as a mitochondrial uncoupler. Our data do not support that FX-11 acts as an LDH inhibitor.
Journal
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EIF4EBP1 (Eukaryotic translation initiation factor 4E binding protein 1)
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Mektovi (binimetinib) • Braftovi (encorafenib)
12d
Health-related Quality of Life with Encorafenib plus Binimetinib for BRAFV600E Thyroid Cancer. (PubMed, Eur Thyroid J)
Combination therapy of encorafenib plus binimetinib for unresectable BRAF V600-mutated thyroid cancer was associated with generally maintained HR-QoL. Considering the efficacy and safety data from the trial, the regimen may provide clinical benefits while maintaining HR-QoL.
Journal • HEOR
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BRAF (B-raf proto-oncogene)
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BRAF V600E • BRAF V600
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Mektovi (binimetinib) • Braftovi (encorafenib)
13d
Enrollment open
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BRAF V600E • BRAF V600
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Avastin (bevacizumab) • Erbitux (cetuximab) • Braftovi (encorafenib)
13d
BECOME-MB: Binimetinib Encorafenib Pembrolizumab +/- Stereotactic Radiosurgery in BRAFV600 Melanoma With Brain Metastasis (clinicaltrials.gov)
P2, N=10, Active, not recruiting, UNICANCER | Trial completion date: Apr 2029 --> Mar 2026 | Trial primary completion date: Apr 2025 --> Mar 2026
Trial completion date • Trial primary completion date
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BRAF (B-raf proto-oncogene)
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BRAF V600E • BRAF V600 • BRAF V600K
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Keytruda (pembrolizumab) • Mektovi (binimetinib) • Braftovi (encorafenib)
14d
S2107: Testing the Addition of Nivolumab to Standard Treatment for Patients With Metastatic or Unresectable Colorectal Cancer That Have a BRAF Mutation (clinicaltrials.gov)
P2, N=84, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Feb 2026 --> Sep 2026 | Trial primary completion date: Feb 2026 --> Sep 2026
Trial completion date • Trial primary completion date
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BRAF (B-raf proto-oncogene) • MSI (Microsatellite instability) • MLH1 (MutL homolog 1) • MSH6 (MutS homolog 6) • MSH2 (MutS Homolog 2)
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BRAF V600E • BRAF V600
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Opdivo (nivolumab) • Erbitux (cetuximab) • Braftovi (encorafenib) • ABP 206 (nivolumab biosimilar)
26d
Combinatorial treatment with donafenib and quercetin suppresses lipid metabolism in HepG2 cells by targeting the CREB1/DRP1/SREBP1 axis. (PubMed, Transl Cancer Res)
These findings indicate that the combination of QUE and DON exerts its antitumor effects by inhibiting the CREB1/DRP1/SREBP1 axis mediated lipid metabolism pathway in HepG2 cells. This offers a novel potential approach for enhancing the therapeutic efficacy of DON in the treatment of HCC.
Journal
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CREB1 (CAMP Responsive Element Binding Protein 1)
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Zepsun (donafenib)
26d
Study of Efficacy and Safety of LXH254 Combinations in Patients With Previously Treated Unresectable or Metastatic Melanoma (clinicaltrials.gov)
P2, N=134, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Mar 2026 --> Feb 2027 | Trial primary completion date: Mar 2026 --> Feb 2027
Trial completion date • Trial primary completion date
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BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
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NRAS mutation • BRAF V600
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Mekinist (trametinib) • Kisqali (ribociclib) • naporafenib (ERAS-254) • rineterkib (LTT462)