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    DRUG:

    Cotellic (cobimetinib)

    i
    Other names: GDC-0973, RG-7420, XL518, RO 5514041, RG7421, XL-518, R-7421, RO-5514041, GDC 0973, R 7421, GDC0973, R7421, RG 7421, RO5514041, XL 518
    Company:
    Exelixis, Roche
    Drug class:
    MEK1 inhibitor
    Related drugs:
    2d
    Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR) (clinicaltrials.gov)
    P2, N=720, Recruiting, Canadian Cancer Trials Group | Trial primary completion date: Jan 2026 --> Dec 2026
    Trial primary completion date • Tumor mutational burden • Pan tumor
    |
    BRAF (B-raf proto-oncogene)
    |
    Opdivo (nivolumab) • Herceptin (trastuzumab) • Lynparza (olaparib) • Xalkori (crizotinib) • erlotinib • Yervoy (ipilimumab) • Ibrance (palbociclib) • dasatinib • Zelboraf (vemurafenib) • sunitinib • Perjeta (pertuzumab) • Cotellic (cobimetinib) • bosutinib • Tukysa (tucatinib) • temsirolimus • axitinib • Erivedge (vismodegib)
    2d
    Belvarafenib in Combination With Cobimetinib in Patients With Locally Advanced or Metastatic NRAS-Mutant Melanoma (clinicaltrials.gov)
    P2, N=45, Recruiting, Hanmi Pharmaceutical Company Limited
    New P2 trial
    |
    NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation
    |
    Cotellic (cobimetinib) • belvarafenib (RG6185)
    9d
    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
    |
    IL6 (Interleukin 6) • CLU (Clusterin)
    |
    Zelboraf (vemurafenib) • Cotellic (cobimetinib)
    16d
    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)
    22d
    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)
    1m
    A Study to Evaluate the Safety and Activity of Belvarafenib as a Single Agent and in Combination With Either Cobimetinib or Cobimetinib Plus Nivolumab in Patients With NRAS-mutant Advanced Melanoma. (clinicaltrials.gov)
    P1, N=65, Active, not recruiting, Genentech, Inc. | Trial completion date: Dec 2025 --> Jun 2027 | Trial primary completion date: Dec 2025 --> Jun 2027
    Trial completion date • Trial primary completion date • IO biomarker
    |
    NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation
    |
    Opdivo (nivolumab) • Cotellic (cobimetinib) • belvarafenib (RG6185)
    1m
    Phase I study of ABM-1310 as monotherapy and in combination with cobimetinib for BRAF-mutated advanced solid tumors: safety, efficacy, and dose expansion. (PubMed, ESMO Open)
    ABM-1310 showed a favorable safety profile and encouraging intracranial activity. These findings support continued evaluation for CNS tumors and in cancer patients with prior BRAF inhibitor exposure.
    P1 data • Journal • First-in-human
    |
    BRAF (B-raf proto-oncogene)
    |
    BRAF V600E • BRAF mutation
    |
    Cotellic (cobimetinib) • ABM-1310
    1m
    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 | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    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)
    2ms
    IN10018 Monotherapy and Combination Therapy for Metastatic Melanoma (clinicaltrials.gov)
    P1, N=51, Completed, InxMed (Shanghai) Co., Ltd. | Active, not recruiting --> Completed | N=120 --> 51
    Trial completion • Enrollment change
    |
    NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • NRAS Q61 • NRAS G12 • NRAS G13
    |
    Tecentriq (atezolizumab) • Cotellic (cobimetinib) • ifebemtinib (IN10018)
    2ms
    Effects of Vemurafenib ± Cobimetinib on Intratumoral and Host Immunity in Patients With BRAFV600 Mutant Melanoma: Implications for Combination With Immunotherapy. (PubMed, Cancer Med)
    Data from this study provides provocative evidence that, while BRAF+/-MEK inhibitor therapy produces an increase in overall and clonal T cell infiltrates, there is limited evidence for generation of new or persistent tumor immunity. Thus, BRAFi/MEKi therapy may enable tumor-reactive T cells to infiltrate tumors but tumor control does not appear to depend on priming new immune responses.
    Journal • IO biomarker
    |
    CD8 (cluster of differentiation 8) • IFNG (Interferon, gamma) • CD4 (CD4 Molecule)
    |
    BRAF mutation • BRAF V600
    |
    Zelboraf (vemurafenib) • Cotellic (cobimetinib)
    3ms
    Atezolizumab, Cobimetinib, and Eribulin in Treating Patients With Chemotherapy Resistant Metastatic Inflammatory Breast Cancer (clinicaltrials.gov)
    P2, N=37, Active, not recruiting, M.D. Anderson Cancer Center | Trial completion date: Dec 2025 --> Dec 2027 | Trial primary completion date: Dec 2025 --> Dec 2027
    Trial completion date • Trial primary completion date
    |
    PD-L1 (Programmed death ligand 1) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    HER-2 positive
    |
    Tecentriq (atezolizumab) • Cotellic (cobimetinib) • Halaven (eribulin mesylate)
    3ms
    MORPHEUS-EC: A Study of Multiple Immunotherapy-Based Treatment Combinations in Patients With Locally Advanced Unresectable or Metastatic Gastric or Gastroesophageal Junction Cancer (G/GEJ) or Esophageal Cancer (Morpheus-Gastric and Esophageal Cancer) (clinicaltrials.gov)
    P1/2, N=214, Completed, Hoffmann-La Roche | Active, not recruiting --> Completed | N=410 --> 214
    Trial completion • Enrollment change
    |
    HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • TIGIT (T Cell Immunoreceptor With Ig And ITIM Domains 2)
    |
    HER-2 negative • HER-2 expression
    |
    cisplatin • Tecentriq (atezolizumab) • paclitaxel • 5-fluorouracil • Cotellic (cobimetinib) • Cyramza (ramucirumab) • oxaliplatin • leucovorin calcium • tiragolumab (RG6058) • pegvorhyaluronidase alfa (PEGPH20) • Aphexda (motixafortide)