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    DRUG:

    RAF265

    i
    Other names: RAF265, CHIR-265
    Company:
    Novartis
    Drug class:
    BRAF inhibitor, VEGFR-2 inhibitor
    Related drugs:
    8d
    Targeting USP10/SCD1 axis by RAF265 suppresses lipogenesis and induced ferroptosis in head and neck squamous cell carcinoma. (PubMed, Cell Death Discov)
    Notably, we discover that RAF265, a compound already approved by the FDA, effectively inhibits USP10 activity, leading to decreased SCD1 expression and lipogenesis, which then suppresses tumor growth and enhances ferroptosis in both in vitro and in vivo models of HNSCC. Collectively, these results underscore the critical role of the E2F4/USP10/SCD1 pathway in modulating ferroptosis and driving HNSCC progression, suggesting that targeting this axis with RAF265 may offer a promising strategy for therapeutic intervention in this malignancy.
    Journal
    |
    SCD (Stearoyl-CoA Desaturase) • USP1 (Ubiquitin Specific Peptidase 1)
    |
    RAF265
    almost6years
    CHIR-265-MEL01: A Study to Evaluate RAF265, an Oral Drug Administered to Subjects With Locally Advanced or Metastatic Melanoma (clinicaltrials.gov)
    P1/2, N=104, Completed, Novartis Pharmaceuticals | Phase classification: P2 --> P1/2
    Clinical • Phase classification
    |
    BRAF (B-raf proto-oncogene)
    |
    BRAF mutation
    |
    RAF265
    over8years
    MEK162 and RAF265 in Adult Patients With Advanced Solid Tumors Harboring RAS or BRAFV600E Mutations (clinicaltrials.gov)
    P1, N=69, Completed, Novartis Pharmaceuticals | Active, not recruiting --> Completed
    Clinical • Trial completion
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    BRAF V600E • KRAS mutation • NRAS mutation • BRAF V600
    |
    Mektovi (binimetinib) • RAF265