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DRUG CLASS:

MEK1 inhibitor

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
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IL6 (Interleukin 6) • CLU (Clusterin)
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Zelboraf (vemurafenib) • Cotellic (cobimetinib)
11d
New trial
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CD20 positive
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vincristine • prednisone • Fu Mai Ning (luvometinib) • mercaptopurine
16d
Enrollment open • Phase classification
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BRAF (B-raf proto-oncogene)
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Cotellic (cobimetinib)
22d
New P3 trial
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NF1 (Neurofibromin 1)
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TQ-B3234
23d
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
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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)
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BRAF mutation
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Cotellic (cobimetinib)
29d
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)
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REC-4881
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
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NRAS (Neuroblastoma RAS viral oncogene homolog)
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NRAS mutation
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Opdivo (nivolumab) • Cotellic (cobimetinib) • belvarafenib (RG6185)
1m
New P4 trial
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NF1 (Neurofibromin 1)
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Fu Mai Ning (luvometinib)
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
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BRAF (B-raf proto-oncogene)
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BRAF V600E • BRAF mutation
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Cotellic (cobimetinib) • ABM-1310
1m
New trial
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Fu Mai Ning (luvometinib)
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
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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)
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BRAF mutation
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Cotellic (cobimetinib)
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
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CD8 (cluster of differentiation 8) • IFNG (Interferon, gamma) • CD4 (CD4 Molecule)
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BRAF mutation • BRAF V600
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Zelboraf (vemurafenib) • Cotellic (cobimetinib)