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    DRUG:

    enbezotinib (TPX-0046)

    i
    Other names: TPX-0046, TPX0046, TPX 0046
    Company:
    BMS
    Drug class:
    Src kinase inhibitor, RET inhibitor
    Related drugs:
    over1year
    Study of TPX-0046, A RET/SRC Inhibitor in Adult Subjects With Advanced Solid Tumors Harboring RET Fusions or Mutations (clinicaltrials.gov)
    P1/2, N=41, Terminated, Turning Point Therapeutics, Inc. | Trial completion date: Nov 2023 --> May 2023 | Active, not recruiting --> Terminated; Adverse change in the risk/benefit.
    Trial completion date • Trial termination • Metastases
    |
    enbezotinib (TPX-0046)
    almost2years
    Precious Gene: The Application of RET-Altered Inhibitors. (PubMed, Molecules)
    Thus, the novel highly potent and RET-specific inhibitors selpercatinib and pralsetinib have been accelerated for approval by the Food and Drug Administration (FDA), and clinical trials of TPX-0046 and zetletinib are underway. It is well tolerated and a potential therapeutic for RET-altered cancers. Thus, we will focus on current state-of-the-art therapeutics with these novel RET inhibitors and show their efficacy and safety in therapy.
    Review • Journal
    |
    RET (Ret Proto-Oncogene)
    |
    RET rearrangement
    |
    Retevmo (selpercatinib) • Gavreto (pralsetinib) • enbezotinib (TPX-0046)
    almost2years
    Study of TPX-0046, A RET/SRC Inhibitor in Adult Subjects With Advanced Solid Tumors Harboring RET Fusions or Mutations (clinicaltrials.gov)
    P1/2, N=462, Active, not recruiting, Turning Point Therapeutics, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed • Metastases
    |
    RET (Ret Proto-Oncogene)
    |
    RET fusion • RET mutation
    |
    enbezotinib (TPX-0046)
    over2years
    Study of TPX-0046, A RET/SRC Inhibitor in Adult Subjects With Advanced Solid Tumors Harboring RET Fusions or Mutations (clinicaltrials.gov)
    P1/2, N=462, Recruiting, Turning Point Therapeutics, Inc. | Trial completion date: Mar 2025 --> Nov 2026 | Trial primary completion date: May 2024 --> Dec 2025
    Trial completion date • Trial primary completion date
    |
    RET (Ret Proto-Oncogene)
    |
    RET fusion • RET mutation
    |
    enbezotinib (TPX-0046)
    over4years
    [VIRTUAL] The next-generation RET inhibitor TPX-0046 is active in drug-resistant and naïve RET-driven cancer models. (ASCO 2020)
    Selective RET inhibitors (selpercatinib/pralsetinib) are active in patients with these cancers; unfortunately, resistance often occurs. TPX-0046 is a unique next-generation RET inhibitor that possesses potent in vitro and in vivo activity against a diverse range of RET alterations, including SFM-mediated resistance. A phase 1/2 trial for RET inhibitor-resistant and naïve RET-driven cancers is on-going (NCT04161391). Research Funding: Turning Point Therapeutics
    Preclinical
    |
    RET (Ret Proto-Oncogene) • KIF5B (Kinesin Family Member 5B) • CCDC6 (Coiled-Coil Domain Containing 6)
    |
    RET fusion • RET mutation • RET C634W
    |
    Retevmo (selpercatinib) • Gavreto (pralsetinib) • enbezotinib (TPX-0046)