^
    4ms
    Ningetinib plus gefitinib in EGFR-mutant non-small-cell lung cancer with MET and AXL dysregulations: A phase 1b clinical trial and biomarker analysis. (PubMed, Lung Cancer)
    This study demonstrates that combined blockade of MET, AXL and EGFR is a feasible strategy for a subset of EGFR-mutant NSCLC.
    P1 data • Journal
    |
    EGFR (Epidermal growth factor receptor) • AXL (AXL Receptor Tyrosine Kinase)
    |
    EGFR mutation • MET amplification • MET overexpression • MET mutation • AXL expression • AXL overexpression
    |
    gefitinib • ningetinib (CT053PTSA)
    over1year
    Preclinical characterization and phase I clinical trial of CT053PTSA targets MET, AXL, and VEGFR2 in patients with advanced solid tumors. (PubMed, Front Immunol)
    In this FIH phase I trial, CT053PTSA was well tolerated and had a satisfactory safety profile. Further trials evaluating the clinical activity of CT053PTSA are ongoing.
    P1 data • Preclinical • Clinical Trial,Phase I • Journal
    |
    FLT3 (Fms-related tyrosine kinase 3) • MET (MET proto-oncogene, receptor tyrosine kinase) • AXL (AXL Receptor Tyrosine Kinase) • KDR (Kinase insert domain receptor) • MERTK (MER Proto-Oncogene, Tyrosine Kinase)
    |
    MET expression • MET-H
    |
    ningetinib (CT053PTSA)
    almost2years
    Ningetinib (CT053PTSA) Plus Gefitinib in Stage IIIB or IV NSCLC Patients With EGFR Mutation and T790M Negative (clinicaltrials.gov)
    P1/2, N=158, Active, not recruiting, Sunshine Lake Pharma Co., Ltd. | Recruiting --> Active, not recruiting | Trial completion date: Nov 2021 --> Jul 2023 | Trial primary completion date: Aug 2021 --> Jul 2023
    Enrollment closed • Trial completion date • Trial primary completion date • Combination therapy
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    EGFR mutation • EGFR T790M negative
    |
    gefitinib • ningetinib (CT053PTSA)
    3years
    A Phase Ib Study of CT053PTSA in Relapsed / Refractory Acute Myeloid Leukemia (AML) (clinicaltrials.gov)
    P1, N=12, Terminated, Sunshine Lake Pharma Co., Ltd. | N=34 --> 12 | Recruiting --> Terminated; Company strategy adjustment
    Clinical • Enrollment change • Trial termination
    |
    FLT3 (Fms-related tyrosine kinase 3)
    |
    ningetinib (CT053PTSA)
    over3years
    Drug interaction of ningetinib and gefitinib involving CYP1A1 and efflux transporters in non-small cell lung cancer patients. (PubMed, Br J Clin Pharmacol)
    The high plasma exposure of M1 in patients was attributed to the inhibition of M1 efflux by ningetinib and its low tissue affinity. When co-administered, gefitinib inhibited the formation of M1, but due to the low metabolic yield of M1 in vivo, the pharmacokinetics of ningetinib was not influenced. Inhibition of CYP1A1 may increase the concentration of ningetinib in target tissues, and the long-term safety and efficacy of ningetinib combined with gefitinib should be evaluated.
    Clinical • Journal
    |
    CYP1A1 (Cytochrome P450 Family 1 Subfamily A Member 1)
    |
    gefitinib • ningetinib (CT053PTSA)
    4years
    [VIRTUAL] A phase Ib study of a novel c-MET, AXL and VEGFR-2 inhibitor ningetinib and gefitinib combination therapy in Chinese EGFR-TKI resistant NSCLC with T790M negative. (ASCO 2020)
    Ningetinib was well tolerated at 30 mg and 40 mg dosage with Gefitinib 250 mg, the RP2D for Ningetinb was 40 mg. This combination therapy showed promising anti-tumor activity in prior EGFR-TKIs acquired resistant NSCLC pts with T790M negative. C-Met GCN was the potential efficacy biomarker.
    P1 data • Combination therapy
    |
    EGFR (Epidermal growth factor receptor) • FLT3 (Fms-related tyrosine kinase 3) • MET (MET proto-oncogene, receptor tyrosine kinase) • AXL (AXL Receptor Tyrosine Kinase) • KDR (Kinase insert domain receptor)
    |
    MET amplification
    |
    gefitinib • ningetinib (CT053PTSA)
    4years
    Ningetinib (CT053PTSA) Plus Gefitinib in Stage IIIB or IV NSCLC Patients With EGFR Mutation and T790M Negative (clinicaltrials.gov)
    P1/2, N=158, Recruiting, Sunshine Lake Pharma Co., Ltd. | N=72 --> 158 | Trial completion date: Nov 2019 --> Nov 2021 | Trial primary completion date: Aug 2019 --> Aug 2021
    Clinical • Enrollment change • Trial completion date • Trial primary completion date • Combination therapy
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    EGFR mutation • EGFR T790M negative
    |
    gefitinib • ningetinib (CT053PTSA)