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    DRUG:

    bozitinib (APL-101)

    i
    Other names: PLB1001, CBT 101, CBT-101, APL101, APL-101, PLB-1001, CBI-3103
    Company:
    Apollomics, Avistone Biotech
    Drug class:
    c-MET inhibitor
    Related drugs:
    1m
    Vebreltinib Plus PLB1004 in EGFR-mutated, Advanced NSCLC With MET Amplification or MET Overexpression Following EGFR-TKI (clinicaltrials.gov)
    P1/2, N=156, Recruiting, Avistone Biotechnology Co., Ltd.
    New P1/2 trial
    |
    bozitinib (APL-101) • PLB1004
    3ms
    Evaluationn of Tolerability and Safety of CBT101, an Autologous Natural Killer Cell, in Patients With Solid Cancer (clinicaltrials.gov)
    P1, N=6, Completed, CHABiotech CO., Ltd | Not yet recruiting --> Completed
    Trial completion
    |
    bozitinib (APL-101) • CBT101
    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=22, Recruiting, Washington University School of Medicine | Trial completion date: Sep 2027 --> Sep 2029
    Trial completion date • Metastases
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation
    |
    Tagrisso (osimertinib) • bozitinib (APL-101)
    7ms
    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
    New P2/3 trial
    |
    MET fusion
    |
    cisplatin • temozolomide • etoposide IV • bozitinib (APL-101)
    7ms
    SPARTA: APL-101 Study of Subjects With NSCLC With c-Met EXON 14 Skip Mutations and c-Met Dysregulation Advanced Solid Tumors (clinicaltrials.gov)
    P2, N=497, Recruiting, Apollomics Inc. | Phase classification: P1/2 --> P2 | N=344 --> 497
    Phase classification • Enrollment change • Metastases
    |
    HGF (Hepatocyte growth factor) • PTPRZ1 (Protein Tyrosine Phosphatase Receptor Type Z1)
    |
    EGFR mutation • MET amplification • EGFR wild-type • MET exon 14 mutation • MET overexpression • MET expression • EGFR positive • MET fusion
    |
    bozitinib (APL-101)
    7ms
    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=22, Recruiting, Washington University School of Medicine | Trial completion date: Nov 2026 --> Sep 2027 | Trial primary completion date: Nov 2026 --> Sep 2027
    Trial completion date • Trial primary completion date • Metastases
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation
    |
    Tagrisso (osimertinib) • bozitinib (APL-101)
    8ms
    Treatment sequencing in the VISION study of tepotinib in patients with MET exon 14 ( MET ex14) skipping NSCLC (COSA 2023)
    48 patients received subsequent METi (crizotinib, n=20; capmatinib, n=15; bozitinib, n=4; tepotinib, n=3; amivantamab, n=3; cabozantinib, n=3; other, n=4; different METi in subsequent lines, n=4)... Robust and durable efficacy, particularly in the 1L setting, support early use of tepotinib in the treatment sequence. Almost half of this elderly population received subsequent treatment, higher than the 20%–30% reported for 1L CT/IO IPSOS trial in elderly patients (median age 75). METi treatment sequencing analyses are ongoing.
    Clinical
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    MET exon 14 mutation
    |
    Xalkori (crizotinib) • Cabometyx (cabozantinib tablet) • Rybrevant (amivantamab-vmjw) • Tepmetko (tepotinib) • Tabrecta (capmatinib) • bozitinib (APL-101)
    9ms
    A Confirmatory Clinical Study in NSCLC Patients With MET Exon 14 Mutation (KUNPENG-2) (clinicaltrials.gov)
    P3, N=131, Active, not recruiting, Beijing Pearl Biotechnology Limited Liability Company
    New P3 trial • Metastases
    |
    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • ALK (Anaplastic lymphoma kinase) • MET (MET proto-oncogene, receptor tyrosine kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    ALK rearrangement • EGFR wild-type • MET exon 14 mutation • ROS1 rearrangement • MET mutation
    |
    bozitinib (APL-101)
    9ms
    A Study of PLB1001 in Non-small Cell Lung Cancer With c-Met Dysregulation(KUNPENG) (clinicaltrials.gov)
    P2, N=185, Recruiting, Beijing Pearl Biotechnology Limited Liability Company | Trial primary completion date: Dec 2022 --> Dec 2024
    Trial primary completion date • Metastases
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    bozitinib (APL-101)
    10ms
    Preliminary results of phase II KUNPENG study of vebreltinib in patients (Pts) with advanced NSCLC harboring c-MET alterations (ESMO 2023)
    Most of the TRAEs were grade 1/2. Conclusions Vebreltinib showed promising efficacy and favorable safety in patients with METex14 mutant NSCLC.
    Clinical • P2 data • Metastases
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    MET exon 14 mutation
    |
    bozitinib (APL-101)
    10ms
    Target therapy matched to genomic alterations in patients with recurrent IDH wildtype glioblastoma: A real-life cohort analysis from Veneto Institute of Oncology, Padua (Italy) (ESMO 2023)
    All pts received radiotherapy and temozolomide as first-line...TT was dabrafenib/trametinib (9 pts), larotrectinib (2 pts), erdafitinib (4 pts), entrectinib (1 pt), vebreltinib (2 pts), capmatinib (1 pt), alpelisib (6 pts), ipatasertib+/-atezolizumab (12 pts)...We had a dramatic response to a MET inhibitor. Deeper explorations are needed in targeting FGFR e ROS1.
    Clinical • PD(L)-1 Biomarker
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • FGFR1 (Fibroblast growth factor receptor 1) • NTRK (Neurotrophic receptor tyrosine kinase) • PTPRZ1 (Protein Tyrosine Phosphatase Receptor Type Z1)
    |
    BRAF V600E • PIK3CA mutation • BRAF V600 • MET amplification • FGFR1 amplification • ROS1 fusion • FGFR1 fusion • IDH wild-type • PIK3CA mutation + PTEN mutation • MET fusion • NTRK fusion
    |
    Mekinist (trametinib) • Tecentriq (atezolizumab) • Tafinlar (dabrafenib) • Vitrakvi (larotrectinib) • Rozlytrek (entrectinib) • temozolomide • Piqray (alpelisib) • Balversa (erdafitinib) • ipatasertib (RG7440) • Tabrecta (capmatinib) • bozitinib (APL-101)
    10ms
    Phase I/II Study Exploring Safety and Efficacy of Apl-101 Plus Frontline Osimertinib in EGFR-mutated Metastatic Non-small Cell Lung Cancer (IASLC-WCLC 2023)
    Blood and tumor biopsy are collected at baseline, prior to combination treatment (optional tumor biopsy) and at progression for exploratory analyses to help identify genomic alterations leading to drug tolerance and biomarkers that can predict for benefit of combination therapy. Dose level 1 has been completed with 1 dose-limiting toxicity and dose-level 2 began enrolling in August 2022.
    Clinical • P1/2 data • IO biomarker • Metastases
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation
    |
    Tagrisso (osimertinib) • bozitinib (APL-101)
    10ms
    PTPRZ1-METFUsion GENe (ZM-FUGEN) trial: study protocol for a multicentric, randomized, open-label phase II/III trial. (PubMed, Chin Neurosurg J)
    If proven effective, this targeted multifaceted intervention protocol will be extended for more glioma patients as a protocol to evaluate the safety and efficacy of MET inhibitors.
    P2/3 data • Journal
    |
    PTPRZ1 (Protein Tyrosine Phosphatase Receptor Type Z1)
    |
    MET fusion
    |
    bozitinib (APL-101)
    1year
    Treatment sequencing in the VISION study of tepotinib in patients with MET exon 14 (METex14) skipping NSCLC (ELCC 2023)
    48 pts received subsequent METi (20 crizotinib, 15 capmatinib, 4 bozitinib, 3 tepotinib, 3 amivantamab, 3 cabozantinib, 4 other; 4 pts received different METi in subsequent lines)...Almost half of this elderly population received subsequent Tx, higher than the 20–30% reported for 1L CT/IO IPSOS trial in elderly pts (median age 75). METi Tx sequencing analyses ongoing.
    Clinical
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    MET exon 14 mutation
    |
    Xalkori (crizotinib) • Cabometyx (cabozantinib tablet) • Rybrevant (amivantamab-vmjw) • Tepmetko (tepotinib) • Tabrecta (capmatinib) • bozitinib (APL-101)
    almost2years
    SPARTA: APL-101 Study of Subjects With NSCLC With c-Met EXON 14 Skip Mutations and c-Met Dysregulation Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=344, Recruiting, Apollomics Inc. | N=201 --> 344 | Trial completion date: Dec 2022 --> Nov 2026 | Trial primary completion date: Dec 2022 --> Mar 2026
    Enrollment change • Trial completion date • Trial primary completion date
    |
    EGFR (Epidermal growth factor receptor) • PTPRZ1 (Protein Tyrosine Phosphatase Receptor Type Z1)
    |
    MET amplification • EGFR wild-type • MET exon 14 mutation • MET fusion • MET-H
    |
    bozitinib (APL-101)
    over2years
    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=22, Recruiting, Washington University School of Medicine | Not yet recruiting --> Recruiting
    Enrollment open
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation
    |
    Tagrisso (osimertinib) • bozitinib (APL-101)
    over2years
    MET overexpression contributes to STAT4-PD-L1 signaling activation associated with tumor-associated, macrophages-mediated immunosuppression in primary glioblastomas. (PubMed, J Immunother Cancer)
    These data indicated that the MET-STAT4-PD-L1 axis and tumor-associated macrophages might enforce glioma immune evasion and were associated with poor prognosis in GBM samples, suggesting potential clinical strategies for targeted therapy combined with immunotherapy in patients with primary GBM.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • MET (MET proto-oncogene, receptor tyrosine kinase) • HGF (Hepatocyte growth factor) • STAT4 (Signal Transducer And Activator Of Transcription 4)
    |
    MET overexpression • MET expression
    |
    bozitinib (APL-101)
    over2years
    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=22, Not yet recruiting, Washington University School of Medicine | Trial completion date: Sep 2026 --> Jan 2027 | Initiation date: Nov 2021 --> Mar 2022 | Trial primary completion date: Sep 2026 --> Jan 2027
    Clinical • Trial completion date • Trial initiation date • Trial primary completion date
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation
    |
    Tagrisso (osimertinib) • bozitinib (APL-101)
    3years
    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=22, Not yet recruiting, Washington University School of Medicine
    Clinical • New P1/2 trial
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation
    |
    Tagrisso (osimertinib) • bozitinib (APL-101)
    4years
    [VIRTUAL] A phase I study of cMET inhibitor bozitinib in patients with advanced NSCLC harboring cMET alterations (AACR-I 2020)
    Based on safety profiles, PK and efficacy analyses, 200mg BID was determined to be RP2D. Bozitinib was well-tolerated with manageable safety profiles when administered at RP2D. Preliminary antitumor activity was observed in patients with exon 14 skipping and/or amplification, particularly in those with NGS-identified exon 14 skipping.
    Clinical • P1 data
    |
    MET (MET proto-oncogene, receptor tyrosine kinase) • HGF (Hepatocyte growth factor)
    |
    bozitinib (APL-101)
    over4years
    A Study of PLB1001 in Non-small Cell Lung Cancer With c-Met Dysregulation (clinicaltrials.gov)
    P2, N=185, Recruiting, Beijing Pearl Biotechnology Limited Liability Company
    Clinical • New P2 trial
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    bozitinib (APL-101)