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    DRUG CLASS:

    RAF kinase inhibitor

    Related drugs:
    6d
    Stereotactic Body Radiotherapy Plus FAK and RAF/MEK Inhibition in Advanced Pancreatic Adenocarcinoma (clinicaltrials.gov)
    P2, N=36, Recruiting, Washington University School of Medicine | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Avmapki (avutometinib) • Fakzynja (defactinib)
    1m
    FRAME: Phase I Trial of Defactinib and VS-6766. (clinicaltrials.gov)
    P1, N=87, Active, not recruiting, Institute of Cancer Research, United Kingdom | Trial completion date: Oct 2023 --> Oct 2026
    Trial completion date
    |
    KRAS (KRAS proto-oncogene GTPase) • RAS (Rat Sarcoma Virus)
    |
    KRAS mutation • RAS mutation • KRAS G12
    |
    Avmapki (avutometinib) • Fakzynja (defactinib)
    3ms
    DDU RAF/MEK: Phase I Trial of VS-6766 Alone and in Combination With Everolimus (clinicaltrials.gov)
    P1, N=104, Completed, Royal Marsden NHS Foundation Trust | Active, not recruiting --> Completed | Trial completion date: Jun 2025 --> Oct 2025 | Trial primary completion date: Jun 2025 --> Oct 2025
    Trial completion • Trial completion date • Trial primary completion date
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    KRAS mutation • BRAF mutation • NRAS mutation • RAS mutation
    |
    everolimus • Avmapki (avutometinib)
    4ms
    Stereotactic Body Radiotherapy Plus FAK and RAF/MEK Inhibition in Advanced Pancreatic Adenocarcinoma (clinicaltrials.gov)
    P2, N=36, Not yet recruiting, Washington University School of Medicine
    New P2 trial
    |
    Avmapki (avutometinib) • Fakzynja (defactinib)
    4ms
    RAMP201J: A Study of Avutometinib + Defactinib in Recurrent Low-Grade Serous Ovarian Cancer in Japanese Patients (clinicaltrials.gov)
    P2, N=16, Active, not recruiting, Verastem, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    Avmapki (avutometinib) • Fakzynja (defactinib)
    7ms
    Advances in artificial intelligence for spatial transcriptomics in cancer: Special focus on Yin Yang 1 (YY1) and Raf kinase inhibitor protein (RKIP). (PubMed, Biochim Biophys Acta Rev Cancer)
    Additionally, exploring unsupervised learning approaches like clustering and dimensionality reduction methods (PCA, t-SNE, UMAP) allows us to see hidden structures in ST data that may be overlooked. This review discusses recent tools and techniques that have been introduced within the last few years, underlining the transformation brought into ST by ML, AI, and statistical methods that provide new insight into oncogenic drivers such as YY1 and RKIP, cancer heterogeneity, and avenues for personalized medicine approaches in cancer treatment.
    Review • Journal
    |
    YY1 (YY1 Transcription Factor)
    11ms
    DDU RAF/MEK: Phase I Trial of VS-6766 Alone and in Combination With Everolimus (clinicaltrials.gov)
    P1, N=104, Active, not recruiting, Royal Marsden NHS Foundation Trust | Recruiting --> Active, not recruiting | Trial completion date: May 2024 --> Jun 2025 | Trial primary completion date: May 2024 --> Jun 2025
    Enrollment closed • Trial completion date • Trial primary completion date
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    KRAS mutation • BRAF mutation • NRAS mutation • RAS mutation
    |
    everolimus • Avmapki (avutometinib)
    over1year
    RAMP201J: A Study of Avutometinib + Defactinib in Recurrent Low-Grade Serous Ovarian Cancer in Japanese Patients (clinicaltrials.gov)
    P2, N=15, Recruiting, Verastem, Inc.
    New P2 trial • Combination therapy
    |
    Avmapki (avutometinib) • Fakzynja (defactinib)
    almost2years
    Cross-Talks between Raf Kinase Inhibitor Protein and Programmed Cell Death Ligand 1 Expressions in Cancer: Role in Immune Evasion and Therapeutic Implications. (PubMed, Cells)
    Bioinformatic analyses in various human cancers demonstrated the inverse relationship between PD-L1 and RKIP expressions and their prognostic roles. Therefore, we suspect that the direct upregulation of RKIP and/or the use of targeted RKIP inducers in combination with ICIs could result in a more targeted anti-tumor immune response-addressing the therapeutic challenges related to PD-1/PD-L1 monotherapy alone.
    Review • Journal • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • CD8 (cluster of differentiation 8) • IFNG (Interferon, gamma) • PD-L2 (Programmed Cell Death 1 Ligand 2) • SOX2 • IL1B (Interleukin 1, beta) • YY1 (YY1 Transcription Factor)
    almost2years
    ALDH1A1 confers resistance to RAF/MEK inhibitors in melanoma cells by maintaining stemness phenotype and activating PI3K/AKT signaling. (PubMed, Biochem Pharmacol)
    Consistently, pharmacological inhibition of ALDH1A1 activity downregulated the activation of AKT and partially recovered responsiveness to vemurafenib and trametinib. We propose ALDH1A1 as a new potential target for treating melanoma resistant to MAPK/ERK inhibitors.
    Journal
    |
    ALDH1A1 (Aldehyde Dehydrogenase 1 Family Member A1)
    |
    BRAF mutation
    |
    Mekinist (trametinib) • Zelboraf (vemurafenib)
    2years
    ENGOT-ov60: A Study of Avutometinib (VS-6766) v. Avutometinib (VS-6766) + Defactinib in Recurrent Low-Grade Serous Ovarian Cancer With and Without a KRAS Mutation (clinicaltrials.gov)
    P2, N=225, Active, not recruiting, Verastem, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed • Combination therapy
    |
    Avmapki (avutometinib) • Fakzynja (defactinib)
    2years
    Sorafenib in Treating Patients With Metastatic Breast Cancer (clinicaltrials.gov)
    P2, N=23, Completed, National Cancer Institute (NCI) | N=42 --> 23
    Enrollment change • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive • HER-2 amplification
    |
    sorafenib