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    DRUG CLASS:

    c-MET inhibitor

    Related drugs:
    1d
    COCOON: Enhanced Dermatological Care to Reduce Rash and Paronychia in Epidermal Growth Factor Receptor (EGRF)-Mutated Non-Small Cell Lung Cancer (NSCLC) Treated First-line With Amivantamab Plus Lazertinib (clinicaltrials.gov)
    P2, N=305, Active, not recruiting, Janssen Research & Development, LLC | Recruiting --> Active, not recruiting
    Enrollment closed • Adverse events
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    EGFR (Epidermal growth factor receptor)
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    EGFR L858R • EGFR exon 19 deletion
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    Rybrevant (amivantamab-vmjw) • Lazcluze (lazertinib) • Rybrevant Faspro (amivantamab and hyaluronidase-lpuj) • minocycline
    3d
    Unravelling the human disposition of [14C]-vebreltinib: Faecal recovery of parent drug and a major circulating metabolite defines its mass balance profile. (PubMed, Br J Clin Pharmacol)
    Following oral administration, the predominant radioactive component recovered in faeces was unchanged parent drug. The quantitative metabolic profile confirms significant systemic exposure to the M2 metabolite. These data provide critical insights into the human disposition of vebreltinib, including a MIST assessment, and support its continued clinical development.
    Journal
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    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    vebreltinib (APL-101)
    4d
    MDX-2001-101: Dose Escalation and Dose Expansion Study of MDX2001 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=285, Recruiting, ModeX Therapeutics, An OPKO Health Company | N=115 --> 285
    Enrollment change • First-in-human
    5d
    A Phase IB/II Clinical Study of SHR-9839 for Injection Combined With Other Anti-tumor Therapies in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=156, Recruiting, Shanghai Hengrui Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    carboplatin • paclitaxel • pemetrexed • Ameile (aumolertinib) • AiRuiLi (adebrelimab) • ruzaltatug rezetecan (SHR-A2009) • tizetatug rezetecan (SHR-A1921)
    8d
    Vebreltinib plus EGFR-TKI for EGFR-mutated NSCLC with MET-driven resistance: A real-world study of Chinese patients. (PubMed, Lung Cancer)
    Vebreltinib plus an EGFR-TKI demonstrates favorable efficacy and manageable safety in real-world NSCLC patients with MET-driven resistance, with notable intracranial activity. Immunohistochemistry 3 + may serve as a practical predictive biomarker.
    Journal • Real-world evidence
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    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    EGFR mutation • MET amplification • MET overexpression • MET mutation • MET expression
    |
    vebreltinib (APL-101)
    9d
    Phase I Study of Telisotuzumab Adizutecan (Temab-A, ABBV-400), a Novel c-Met Antibody-Drug Conjugate, in Patients With Late-Line Colorectal Cancer and Advanced Solid Tumors. (PubMed, J Clin Oncol)
    Temab-A at 2.4 mg/kg once every 3 weeks has a tolerable and manageable safety profile, with promising antitumor activity.
    P1 data • Journal • First-in-human
    |
    BRAF (B-raf proto-oncogene) • MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    BRAF wild-type
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    telisotuzumab adizutecan (ABBV-400) • telisotuzumab (h224G11)
    10d
    Association of MUC3A P258S mutation with advanced phase CML structural and in silico insights. (PubMed, Funct Integr Genomics)
    Collectively, these findings suggest that MUC3A P258S acts as a potential candidate biomarker of CML progression and influences therapeutic response, highlighting Capmatinib and related inhibitors as candidates for drug repurposing in hematological malignancies. To our knowledge, this is the first report implicating MUC3A in leukemia biology, extending its role beyond epithelial cancers.
    Journal
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    ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
    |
    Tabrecta (capmatinib)
    12d
    Knockdown of FAXDC2 promotes cell proliferation, migration, invasion and EMT in HepG2 cells by upregulating c-Met and its phosphorylation. (PubMed, Mol Biol Rep)
    FAXDC2 acts as a tumor suppressor in HCC, and its knockdown promotes cell proliferation, migration, invasion, and EMT via upregulating c-Met expression and enhancing its phosphorylation in HepG2 cells. Therefore, the FAXDC2/c-Met axis may serve as a noval potential therapeutic target for HCC intervention.
    Journal
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    MET expression
    |
    Tepmetko (tepotinib)
    16d
    POTENT - Tepotinib in Combination With Pembrolizumab in NSCLC (clinicaltrials.gov)
    P1, N=19, Active, not recruiting, Institute of Cancer Research, United Kingdom | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    MET exon 14 mutation • MET mutation
    |
    Keytruda (pembrolizumab) • Tepmetko (tepotinib)
    17d
    Vebreltinib Plus Chemotherapy as First-line Treatment for MET-overexpressing NSCLC (clinicaltrials.gov)
    P2, N=19, Not yet recruiting, Shanghai Chest Hospital
    New P2 trial
    |
    KRAS (KRAS proto-oncogene GTPase) • ALK (Anaplastic lymphoma kinase) • MET (MET proto-oncogene, receptor tyrosine kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    KRAS G12C • MET amplification • ALK rearrangement • MET exon 14 mutation • MET overexpression • ROS1 rearrangement • MET mutation • KRAS G12 • ALK negative
    |
    vebreltinib (APL-101)
    18d
    An exploratory clinical study on pierced-therapy +/- radiotherapy for refractory gliomas (ChiCTR2600120358)
    P=N/A, N=29, Fudan University Shanghai Cancer Center; Fudan University Shanghai Cancer Center
    New trial
    |
    Avastin (bevacizumab) • vebreltinib (APL-101)