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    DRUG CLASS:

    MEK1 inhibitor

    Related drugs:
    6d
    TUPELO: Evaluate REC-4881 in Participants With Familial Adenomatous Polyposis (FAP) (clinicaltrials.gov)
    P1/2, N=67, Recruiting, Recursion Pharmaceuticals Inc. | Trial completion date: Jul 2026 --> Sep 2027 | Trial primary completion date: Jul 2026 --> Jun 2027
    Trial completion date • Trial primary completion date
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    APC (APC Regulator Of WNT Signaling Pathway)
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    REC-4881
    7d
    Dual RAF inhibition outperforms RAF-MEK combinations for suppressing ERK signaling in KRAS mutant cells. (PubMed, NPJ Syst Biol Appl)
    KSR1 knockdown did not substantially affect ppERK responses to Type I½ RAF inhibitor (Encorafenib) in both cell types, whereas ppERK sensitivity slightly decreased for Type II RAFi (TAK-632) in MCF7 cells, aligning with simulations. The efficacy of MEKi (Cobimetinib) slightly increased in MCF7 cells following KSR1 knockdown but slightly decreased in PSN1 cells where higher MEKi concentrations were required to suppress ERK signaling, as predicted by the model. Our computational models predict, and experiments validate that in RAS-mutant cells, two conformation-specific RAF inhibitors used in combination suppress the ERK pathway more effectively than a combination of MEK and RAF inhibitors irrespective of KSR1 levels.
    Journal
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    KRAS (KRAS proto-oncogene GTPase)
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    KRAS mutation • KRAS wild-type • RAS mutation • KRAS G12R
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    Cotellic (cobimetinib) • Braftovi (encorafenib) • TAK‐632
    15d
    Testing the Combination of APG-1252 (Pelcitoclax) and Cobimetinib in Recurrent Ovarian and Endometrial Cancers (clinicaltrials.gov)
    P1, N=42, Active, not recruiting, National Cancer Institute (NCI) | Recruiting --> Active, not recruiting
    Enrollment closed
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    BRAF (B-raf proto-oncogene)
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    Cotellic (cobimetinib) • pelcitoclax (APG-1252)
    16d
    Evaluation of TQ-B3234 Capsules in Patients With Symptomatic, Non-Surgical Type 1 Neurofibromatosis-Associated Plexiform Neurofibromas (clinicaltrials.gov)
    P3, N=177, Recruiting, Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open
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    NF1 (Neurofibromin 1)
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    TQ-B3234
    24d
    STEP-WISE COMBINATION OF OBINUTUZUMAB, VEMURAFENIB AND COBIMETINIB IN PATIENTS WITH HAIRY CELL LEUKEMIA (HCL) PREVIOUSLY TREATED WITH PURINE ANALOGS OR UNFIT FOR CHEMOTHERAPY: A PHASE-2, SINGLE-ARMS, ITALIAN, MULTICENTER STUDY (HCL-PG04) (2024-520121-36-00)
    P1/2, N=50, Recruiting, Universita' Degli Studi Di Perugia | Not yet recruiting --> Recruiting
    Enrollment open
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    BRAF (B-raf proto-oncogene) • IL2RA (Interleukin 2 receptor, alpha) • ANXA1 (Annexin A1) • ITGAE (Integrin Subunit Alpha E) • ITGAX (Integrin Subunit Alpha X) • ISG20 (Interferon Stimulated Exonuclease Gene 20)
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    BRAF V600E • BRAF V600
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    Zelboraf (vemurafenib) • Cotellic (cobimetinib) • Gazyva (obinutuzumab)
    1m
    A Study to Evaluate Safety, Pharmacokinetics, and Preliminary Clinical Activity of RO7276389 Alone and in Combination with Cobimetinib in Participants with BRAF-V600 Mutation-Positive Advanced Solid Tumor or BRAF-V600 Mutation-Positive Melanoma with Central Nervous System Metastases (2023-506310-43-00)
    P1, N=70, Completed, F. Hoffmann-La Roche AG | Recruiting --> Completed
    Trial completion
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    BRAF (B-raf proto-oncogene)
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    Cotellic (cobimetinib)
    2ms
    Comparative Proteomic Analysis of the Secretome of Control and BRAF/MEK Inhibitor-Resistant Melanoma Cells. (PubMed, J Proteome Res)
    Therefore, this study aimed to examine the protein composition of the secretome of cells resistant to vemurafenib (a BRAF inhibitor) and cobimetinib (a MEK inhibitor) and to compare it with that of nonresistant cells. Proteins secreted by resistant melanoma cells can undoubtedly influence the surrounding microenvironment in a way that promotes the formation of a pro-tumor niche. Among the proteins secreted in significantly higher amounts by resistant cells (compared to the control group), which may be potential biomarkers or therapeutic targets in melanoma, plasminogen activator inhibitor 1, thymosin beta-4, clusterin, interleukin-6, superoxide dismutase, and selected matrix metalloproteinases can be distinguished.
    Journal
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    IL6 (Interleukin 6) • CLU (Clusterin)
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    Zelboraf (vemurafenib) • Cotellic (cobimetinib)
    2ms
    Modified LCH-III Regimen With or Without Luvometinib for Multisystem Pediatric Langerhans Cell Histiocytosis (clinicaltrials.gov)
    P=N/A, N=120, Recruiting, West China Second University Hospital
    New trial
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    CD20 positive
    |
    vincristine • prednisone • Fu Mai Ning (luvometinib) • mercaptopurine
    2ms
    A Study to Evaluate Safety, Pharmacokinetics, and Preliminary Clinical Activity of RO7276389 Alone and in Combination with Cobimetinib in Participants with BRAF-V600 Mutation-Positive Advanced Solid Tumor or BRAF-V600 Mutation-Positive Melanoma with Central Nervous System Metastases (2023-506310-43-00)
    P1, N=70, Recruiting, F. Hoffmann-La Roche AG | -> Recruiting | Phase classification: PN/A --> P1
    Enrollment open • Phase classification
    |
    BRAF (B-raf proto-oncogene)
    |
    Cotellic (cobimetinib)
    2ms
    Evaluation of TQ-B3234 Capsules in Patients With Symptomatic, Non-Surgical Type 1 Neurofibromatosis-Associated Plexiform Neurofibromas (clinicaltrials.gov)
    P3, N=177, Not yet recruiting, Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
    New P3 trial
    |
    NF1 (Neurofibromin 1)
    |
    TQ-B3234
    2ms
    CONCERTO: Cobimetinib in Newly Diagnosed or HMA-treated CMML Patients With RAS Pathway Mutations (clinicaltrials.gov)
    P2, N=29, Active, not recruiting, University of Utah | Trial primary completion date: Jan 2026 --> Apr 2025
    Trial primary completion date
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • FLT3 (Fms-related tyrosine kinase 3) • ABL1 (ABL proto-oncogene 1) • NRAS (Neuroblastoma RAS viral oncogene homolog) • BCR (BCR Activator Of RhoGEF And GTPase) • NF1 (Neurofibromin 1) • JAK2 (Janus kinase 2) • PTPN11 (Protein Tyrosine Phosphatase Non-Receptor Type 11)
    |
    BRAF mutation
    |
    Cotellic (cobimetinib)
    3ms
    A Study of REC-4881 in Participants With Cancers Which Have an AXIN1 or APC Mutation (clinicaltrials.gov)
    P2, N=18, Terminated, Recursion Pharmaceuticals Inc. | N=60 --> 18 | Trial completion date: Jan 2027 --> Feb 2025 | Active, not recruiting --> Terminated | Trial primary completion date: Jan 2027 --> Feb 2025; Study was terminated due to sponsor decision. This decision was not related to safety concerns.
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date
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    APC (APC Regulator Of WNT Signaling Pathway) • RAS (Rat Sarcoma Virus) • AXIN1 (Axin 1)
    |
    REC-4881