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- | RAF265 / Novartis
Journal: A Drug Repositioning Approach Reveals Ergotamine May Be a Potential Drug for the Treatment of Alzheimer's Disease. (Pubmed Central) - Sep 13, 2024
In further analysis by molecular dynamics simulations, both drugs exhibited reasonable stability. Our work indicated that ergotamine and RAF-265 may be potential candidates for treating AD.
- | RAF265 / Novartis
Journal: Identification of Collagen-Suppressive Agents in Keloidal Fibroblasts Using a High-Content, Phenotype-Based Drug Screen. (Pubmed Central) - Feb 2, 2024
Our work indicated that ergotamine and RAF-265 may be potential candidates for treating AD. The most collagen suppressive agents were CGP60474 (
- Mekinist (trametinib) / Novartis, BeiGene, naporafenib (ERAS-254) / Erasca, RAF265 / Novartis
MAPK pathway alterations as a targetable vulnerability in bladder cancer. (Level 1, West Hall; Poster Bd # K16) - Dec 13, 2023 - Abstract #ASCOGU2024ASCO_GU_627;
We tested the activity of a RAF inhibitors in BC cell lines with RAF1 amplifications and NRAS mutations and found that MAPK pathway-altered models displayed increased sensitivity to RAF inhibition compared to MAPK-unaltered models. We further showed this sensitivity in vivo with RAF1-amplified mouse xenografts and elucidated the synergistic effect of concurrent RAF and MEK inhibition.
- | RAF265 / Novartis
Journal: An open source plant kinase chemogenomics set. (Pubmed Central) - Dec 1, 2022
Compound RAF265 (CHIR-265), previously shown to bind the human kinase BRAF (B-Raf proto-oncogene, serine/threonine kinase), also binds to nine highly conserved rice kinases tested. The binding of human and rice kinases to the same compound suggests that human kinase inhibitor sets will be useful for dissecting the function of plant kinases.
- | RAF265 / Novartis
Journal: Small-Molecule RAF265 as an Antiviral Therapy Acts against PEDV Infection. (Pubmed Central) - Oct 28, 2022
RAF265 also presented potent inhibitory activity against viral infection by SARS-CoV-2-pp and SARS-CoV-pp. The present work may provide a starting point for further progress toward the development of antiviral strategies effective against coronavirus PEDV.
- | RAF265 / Novartis
Journal: Small Molecule RAF265 as an Antiviral Therapy Acts Against HSV-1 by Regulating Cytoskeleton Rearrangement and Cellular Translation Machinery. (Pubmed Central) - Oct 18, 2022
RAF265 mediated cytoskeleton rearrangement and targeted the host cell's translation machinery, which suggests that the antiviral activity of RAF265 may be attributed to a dual inhibition strategy. This work offers a starting point for further advances toward clinical development of antivirals against HSV-1.
- | Zelboraf (vemurafenib) / Roche
Journal: B-Raf inhibitor vemurafenib counteracts sulfur mustard-induced epidermal impairment through MAPK/ERK signaling. (Pubmed Central) - Jan 7, 2022
Furthermore, vemurafenib partially improved cutaneous damage in a mouse ear vesicant model. Collectively, our results provide evidence that the B-Raf inhibitor vemurafenib is a potential therapeutic agent against SM injury, and oncogenic B-Raf might be an exciting new therapeutic target following exposure to mustard vesicating agents.
- | RAF265 / Novartis
Phase classification, Metastases: CHIR-265-MEL01: A Study to Evaluate RAF265, an Oral Drug Administered to Subjects With Locally Advanced or Metastatic Melanoma (clinicaltrials.gov) - Sep 2, 2020
P1/2, N=104, Completed, Sponsor: Novartis Pharmaceuticals
Collectively, our results provide evidence that the B-Raf inhibitor vemurafenib is a potential therapeutic agent against SM injury, and oncogenic B-Raf might be an exciting new therapeutic target following exposure to mustard vesicating agents. Phase classification: P2 --> P1/2
- | Biomarker, Preclinical, Journal: Therapeutic potential of combined BRAF/MEK blockade in BRAF-wild type preclinical tumor models. (Pubmed Central) - May 11, 2019
Overall, our data indicate that RAF inhibition-induced paradoxical MAPK activation could be exploited for therapeutic purposes by simultaneously targeting both RAF and MEK (and potentially EGFR family members) in appropriate molecular contexts. KRAS mutation per se does not effectively predict therapeutic synergism and other biomarkers need to be developed to identify patients potentially deriving benefit from combined BRAF/MEK targeting.
- | RAF265 / Novartis, Germanin (suramin) / Optimum Therapeutics
Journal: New tools for evaluating protein tyrosine sulphation: Tyrosyl Protein Sulphotransferases (TPSTs) are novel targets for RAF protein kinase inhibitors. (Pubmed Central) - Apr 5, 2019
By screening the Published Kinase Inhibitor Set (PKIS), we identified oxindole-based inhibitors of the Ser/Thr kinase RAF as low micromolar inhibitors of TPST1 and TPST2. Interestingly, unrelated RAF inhibitors, exemplified by the dual BRAF/VEGFR2 inhibitor RAF265, were also TPST inhibitors in vitro We propose that target-validated protein kinase inhibitors could be repurposed, or redesigned, as more-specific TPST inhibitors to help evaluate the sulphotyrosyl proteome. Finally, we speculate that mechanistic inhibition of cellular tyrosine sulphation might be relevant to some of the phenotypes observed in cells exposed to anionic TPST ligands and RAF protein kinase inhibitors.
- | RAF265 / Novartis
Biomarker, Clinical, P1 data, Journal, IO biomarker: A first-in-human phase I, multicenter, open-label, dose-escalation study of the oral RAF/VEGFR-2 inhibitor (RAF265) in locally advanced or metastatic melanoma independent from BRAF mutation status. (Pubmed Central) - Apr 24, 2018
Antitumor activity occurred in patients with BRAF-mutant and BRAF-WT disease. Despite low activity at tolerable doses, this study provides a framework for the development of pan-RAF inhibitors and modulators of angiogenesis for the treatment of melanoma.
- Mektovi (binimetinib) / Ono Pharma, Pierre Fabre, Pfizer
Trial completion, Metastases: MEK162 and RAF265 in Adult Patients With Advanced Solid Tumors Harboring RAS or BRAFV600E Mutations (clinicaltrials.gov) - Dec 20, 2017
P1, N=69, Completed, Sponsor: Novartis Pharmaceuticals
Despite low activity at tolerable doses, this study provides a framework for the development of pan-RAF inhibitors and modulators of angiogenesis for the treatment of melanoma. Active, not recruiting --> Completed
- || RAF265 / Novartis
Trial primary completion date, Metastases: CHIR-265-MEL01: A Study to Evaluate RAF265, an Oral Drug Administered to Subjects With Locally Advanced or Metastatic Melanoma (clinicaltrials.gov) - Jun 26, 2014
P2, N=104, Completed, Sponsor: Novartis Pharmaceuticals
Active, not recruiting --> Completed Trial primary completion date: Jul 2014 --> Nov 2013
- |||| RAF265 / Novartis
Trial completion, Trial primary completion date, Metastases: CHIR-265-MEL01: A Study to Evaluate RAF265, an Oral Drug Administered to Subjects With Locally Advanced or Metastatic Melanoma (clinicaltrials.gov) - Jun 26, 2014
P2, N=104, Completed, Sponsor: Novartis Pharmaceuticals
Trial primary completion date: Jul 2014 --> Nov 2013 Active, not recruiting --> Completed | Trial primary completion date: Jul 2014 --> Nov 2013
- ||| RAF265 / Novartis
Enrollment change, Metastases: CHIR-265-MEL01: A Study to Evaluate RAF265, an Oral Drug Administered to Subjects With Locally Advanced or Metastatic Melanoma (clinicaltrials.gov) - Oct 17, 2013
P2, N=104, Active, not recruiting, Sponsor: Novartis Pharmaceuticals
Active, not recruiting --> Completed | Trial primary completion date: Jul 2014 --> Nov 2013 N=170 --> 104
- ||| RAF265 / Novartis
Enrollment closed, Metastases: CHIR-265-MEL01: A Study to Evaluate RAF265, an Oral Drug Administered to Subjects With Locally Advanced or Metastatic Melanoma (clinicaltrials.gov) - Mar 18, 2012
P2, N=104, Active, not recruiting, Sponsor: Novartis Pharmaceuticals
N=170 --> 104 Recruiting --> Active, not recruiting