^
    Contact us  to learn more about
    our Premium Content:  News alerts, weekly reports and conference planners
    DRUG:

    vebreltinib (APL-101)

    i
    Other names: APL-101, PLB-1001, CBI-3103, PLB1001, CBT 101, CBT-101, APL101
    Company:
    Apollomics, Avistone Biotech, LaunXP Biomedical
    Drug class:
    c-MET inhibitor
    Related drugs:
    9d
    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
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    vebreltinib (APL-101)
    14d
    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
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    EGFR mutation • MET amplification • MET overexpression • MET mutation • MET expression
    |
    vebreltinib (APL-101)
    23d
    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)
    24d
    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)
    24d
    A clinical trial of Vebreltinib plus Andamertinib in NSCLC with MET overexpression following EGFR-TKI (ChiCTR2600117889)
    P2, N=37, Zhongshan Hospital, Fudan University; Zhongshan Hospital, Fudan University
    New P2 trial
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    EGFR mutation • MET overexpression
    |
    vebreltinib (APL-101) • andamertinib (PLB1004)
    2ms
    Vebreltinib for Previously Treated Astrocytoma, IDH-Mutant, Grade 4, and Glioblastoma, IDH Wild-Type with PTPRZ1-MET Fusion Gene: A Multicenter, Phase III Randomized, Open-Label Trial. (PubMed, Cancer Commun (Lond))
    In this multicenter, open-label ZM FUsion GENe (FUGEN) trial, patients with previously treated astrocytoma, IDH-mutant, grade 4, or glioblastoma, IDH wild-type, harboring the ZM fusion were randomized in a 1:1 ratio to receive vebreltinib (300 mg orally twice daily) or control treatment (temozolomide or cisplatin plus etoposide) in 28-d cycles. Vebreltinib significantly improved OS in patients with previously treated high-grade glioma harboring the ZM fusion, particularly in the subgroup with IDH-mutant astrocytoma, and the safety profile was manageable. Trial registration: This study was registered with the Chinese Drug Clinical Trial Registry (ChinaDrugTrials.org.cn) under the identifier, CTR20181664 (registration date: 2018 September 19).
    Clinical • P3 data • Journal
    |
    PTPRZ1 (Protein Tyrosine Phosphatase Receptor Type Z1)
    |
    IDH wild-type
    |
    cisplatin • temozolomide • etoposide IV • vebreltinib (APL-101)
    4ms
    An Open-Label, Single-Center, Multi-Cohort, Phase II Study Evaluating the Safety and Efficacy of Vebreltinib-Based Combination Therapy in Previously Treated Patients with Locally Advanced or Metastatic MET-Overexpressing Non-Small Cell Lung Cancer (ChiCTR2500112942)
    P2, N=52, Not yet recruiting, West China Hospital of Sichuan University; West China Hospital of Sichuan University
    New P2 trial
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • MET (MET proto-oncogene, receptor tyrosine kinase) • RET (Ret Proto-Oncogene) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    BRAF V600E • KRAS mutation • EGFR mutation • BRAF V600 • ALK rearrangement • MET exon 14 mutation • MET overexpression • ALK fusion • RET mutation • ROS1 fusion • ROS1 rearrangement • MET mutation • MET expression • RET rearrangement • NTRK fusion
    |
    docetaxel • Jiataile (sacituzumab tirumotecan) • vebreltinib (APL-101)
    4ms
    A Study of PLB1001 Enteric Capsules in the Treatment of sGBM/IDH Mutant Glioblastoma Patients With the ZM Fusion Gene (FUGEN). (clinicaltrials.gov)
    P2/3, N=84, Active, not recruiting, Beijing Pearl Biotechnology Limited Liability Company | Trial completion date: Dec 2024 --> Dec 2026
    Trial completion date
    |
    cisplatin • temozolomide • etoposide IV • vebreltinib (APL-101)
    4ms
    Safety and Efficacy of Combining APL-101 With Frontline Osimertinib in Patients With EGFR-mutated Metastatic Non-small Cell Lung Cancer (NSCLC) (clinicaltrials.gov)
    P1/2, N=27, Active, not recruiting, Washington University School of Medicine | Recruiting --> Active, not recruiting | Trial completion date: May 2030 --> Dec 2029 | Trial primary completion date: Jun 2027 --> Jan 2027
    Enrollment closed • Trial completion date • Trial primary completion date
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation
    |
    Tagrisso (osimertinib) • vebreltinib (APL-101) • simmitinib (SYHA1817)
    5ms
    Vebreltinib in MET amplification-driven advanced non-small-cell lung cancer (KUNPENG): a single-arm, multi-cohort, multicentre, phase 2 study. (PubMed, Lancet Oncol)
    Vebreltinib showed antitumour activity in patients with MET amplification-driven advanced NSCLC who had previously received chemotherapy or were chemotherapy-naive. Further research is needed to validate these findings.
    P2 data • Journal
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    MET amplification
    |
    vebreltinib (APL-101)