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    DRUG:

    elzovantinib (TPX-0022)

    i
    Other names: TPX-0022, TPX 0022
    Company:
    BMS, ZAI Lab
    Drug class:
    Src kinase inhibitor, c-MET inhibitor, CSF-1R inhibitor
    Related drugs:
    5ms
    Structural insight into the macrocyclic inhibitor TPX-0022 of c-Met and c-Src. (PubMed, Comput Struct Biotechnol J)
    In addition, TPX-0022 exhibited potent activity against the resistance-relevant c-Met L1195F mutant and moderate activity against the c-Met G1163R, F1200I and Y1230H mutants but weak activity against the c-Met D1228N and Y1230C mutants. Overall, our study reveals the structural mechanism underlying the potency and selectivity of TPX-0022 and the ability to overcome acquire resistance mutations and provides insight into the development of selective c-Met macrocyclic inhibitors.
    Journal
    |
    MET (MET proto-oncogene, receptor tyrosine kinase) • CSF1R (Colony stimulating factor 1 receptor)
    |
    MET mutation • MET D1228N • MET F1200I • MET Y1230C • MET Y1230C
    |
    elzovantinib (TPX-0022)
    6ms
    SHIELD-1: Study of TPX-0022 in Patients With Advanced NSCLC, Gastric Cancer or Solid Tumors Harboring Genetic Alterations in MET (clinicaltrials.gov)
    P1/2, N=180, Active, not recruiting, Turning Point Therapeutics, Inc. | Trial completion date: Nov 2023 --> Mar 2025 | Trial primary completion date: Nov 2023 --> Mar 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    MET amplification • MET exon 14 mutation • MET mutation • MET fusion
    |
    elzovantinib (TPX-0022)
    10ms
    SHIELD-1: Study of TPX-0022 in Patients With Advanced NSCLC, Gastric Cancer or Solid Tumors Harboring Genetic Alterations in MET (clinicaltrials.gov)
    P1/2, N=180, Active, not recruiting, Turning Point Therapeutics, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed • Metastases
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    MET amplification • MET exon 14 mutation • MET mutation • MET fusion
    |
    elzovantinib (TPX-0022)
    over1year
    Activating MET Kinase Domain Mutations Define a Novel Targetable Molecular Subtype of Non-small Cell Lung Cancer that is Clinically Sensitive to MET Inhibitor Elzovantinib (TPX-0022) (IASLC-TTLC 2023)
    "CONCLUSION Activating MET TKD mutations without concurrent MET exon 14 mutations were detected in ~ 0.2% of NSCLC, and occur in the absence of other known drivers in a subset of cases. Comprehensive genomic profiling to detect these alterations and guide treatment selection and clinical trial enrollment is warranted."
    Clinical
    |
    EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • MET amplification • EGFR amplification • MET exon 14 mutation • MET H1094Y • MET D1228N • MET F1200I
    |
    elzovantinib (TPX-0022)
    over1year
    SHIELD-1: Study of TPX-0022 in Patients With Advanced NSCLC, Gastric Cancer or Solid Tumors Harboring Genetic Alterations in MET (clinicaltrials.gov)
    P1/2, N=180, Recruiting, Turning Point Therapeutics, Inc. | N=330 --> 180 | Trial primary completion date: Nov 2022 --> Nov 2023
    Enrollment change • Trial primary completion date • Metastases
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    MET amplification • MET exon 14 mutation • MET mutation • MET fusion
    |
    elzovantinib (TPX-0022)
    over1year
    Preliminary interim data of elzovantinib (TPX-0022), a novel inhibitor of MET/SRC/CSF1R, in patients with advanced solid tumors harboring genetic alterations in MET: Update from the Phase 1 SHIELD-1 trial (AACR-NCI-EORTC 2022)
    Elzovantinib, a novel MET/SRC/CSF1R inhibitor, was generally well tolerated with primarily low-grade dizziness, no high-grade edema, and a favorable PK profile. The RP2D is currently under evaluation and updated safety and efficacy data will be available for presentation. A global multi-cohort Phase 2 trial of pts with MET-altered tumors is planned.
    Clinical • P1 data
    |
    MET (MET proto-oncogene, receptor tyrosine kinase) • CSF1R (Colony stimulating factor 1 receptor)
    |
    MET exon 14 mutation
    |
    elzovantinib (TPX-0022)
    2years
    SHIELD-1: Study of TPX-0022 in Patients With Advanced NSCLC, Gastric Cancer or Solid Tumors Harboring Genetic Alterations in MET (clinicaltrials.gov)
    P1/2, N=330, Recruiting, Turning Point Therapeutics, Inc. | Phase classification: P1 --> P1/2 | N=120 --> 330
    Phase classification • Enrollment change
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    MET amplification • MET exon 14 mutation • MET mutation
    |
    elzovantinib (TPX-0022)
    over2years
    [VIRTUAL] Preliminary interim data of elzovantinib (TPX-0022), a novel inhibitor of MET/SRC/CSF1R, in patients with advanced solid tumors harboring genetic alterations in MET: Update from the Phase 1 SHIELD-1 trial (AACR-NCI-EORTC 2021)
    No abstract available
    Clinical • P1 data
    |
    CSF1R (Colony stimulating factor 1 receptor)
    |
    elzovantinib (TPX-0022)
    over3years
    [VIRTUAL] First-in-human safety, pharmacokinetics, and preliminary efficacy of TPX-0022, a novel inhibitor of MET/SRC/CSF1R in patients with advanced solid tumors harboring genetic alterations in MET (AACR-NCI-EORTC 2020)
    TPX-0022 is a novel MET/SRC/CSF1R inhibitor. TPX-0022 was generally well-tolerated. Responses were observed in Δex14 NSCLC and MET amplified GC and CRC.
    Clinical • P1 data • PK/PD data • Late-breaking abstract
    |
    HGF (Hepatocyte growth factor) • CSF1R (Colony stimulating factor 1 receptor)
    |
    MET amplification • MET exon 14 mutation
    |
    elzovantinib (TPX-0022)
    4years
    [VIRTUAL] A phase I, open-label, multicenter, first-in-human study of the safety, tolerability, pharmacokinetics, and antitumor activity of TPX-0022, a novel MET/CSF1R/SRC inhibitor, in patients with advanced solid tumors harboring genetic alterations in MET. (ASCO 2020)
    The study is open and enrolling in the dose escalation portion at the time of submission. Research Funding: Turning Point Therapeutics
    Clinical • P1 data • PK/PD data
    |
    MET (MET proto-oncogene, receptor tyrosine kinase) • HGF (Hepatocyte growth factor) • CSF1R (Colony stimulating factor 1 receptor)
    |
    MET amplification • MET exon 14 mutation
    |
    elzovantinib (TPX-0022)
    over4years
    Phase 1 Study of TPX-0022, a MET/CSF1R/SRC Inhibitor, in Patients With Advanced Solid Tumors Harboring Genetic Alterations in MET (clinicaltrials.gov)
    P1, N=120, Recruiting, Turning Point Therapeutics, Inc. | Initiation date: Dec 2019 --> Aug 2019
    Clinical • Trial initiation date
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    MET amplification • MET exon 14 mutation • MET exon 14 deletion
    |
    elzovantinib (TPX-0022)