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    DRUG:

    TAS0728

    i
    Other names: TAS0728, TAS 0728, TAS-0728, TPC-107, TPC 107, TPC107
    Associations

    News

    Trials
    Company:
    Otsuka
    Drug class:
    HER2 inhibitor
    Related drugs:
    Associations

    News

    Trials
    5ms
    A Study of TAS0728 in Patients With Solid Tumors With HER2 or HER3 Abnormalities (clinicaltrials.gov)
    P1, N=19, Terminated, Taiho Oncology, Inc. | Phase classification: P1/2 --> P1
    Phase classification • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
    |
    TAS0728
    2years
    A Study of TAS0728 in Patients With Solid Tumors With HER2 or HER3 Abnormalities (clinicaltrials.gov)
    P1/2, N=19, Terminated, Taiho Oncology, Inc. | Active, not recruiting --> Terminated; The study was stopped due to unacceptable toxicity during the dose-escalation portion (Phase 1) of the study and did not progress to Phase 2
    Trial termination • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
    |
    HER-2 overexpression • HER-2 amplification • ERBB3 overexpression • ERBB3 mutation
    |
    TAS0728
    almost3years
    A Study of TAS0728 in Patients With Solid Tumors With HER2 or HER3 Abnormalities (clinicaltrials.gov)
    P1/2, N=19, Active, not recruiting, Taiho Oncology, Inc. | Trial completion date: Dec 2021 --> Jun 2022 | Trial primary completion date: Dec 2021 --> Jun 2022
    Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
    |
    HER-2 overexpression • HER-2 amplification • ERBB3 overexpression • ERBB3 mutation
    |
    TAS0728
    3years
    A Study of TAS0728 in Patients With Solid Tumors With HER2 or HER3 Abnormalities (clinicaltrials.gov)
    P1/2, N=19, Active, not recruiting, Taiho Oncology, Inc. | Trial completion date: Aug 2021 --> Dec 2021 | Trial primary completion date: Aug 2021 --> Dec 2021
    Clinical • Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
    |
    HER-2 overexpression • HER-2 amplification • ERBB3 overexpression • ERBB3 mutation
    |
    TAS0728
    over3years
    A first-in-human phase I study of TAS0728, an oral covalent binding inhibitor of HER2, in patients with advanced solid tumors with HER2 or HER3 aberrations. (PubMed, Invest New Drugs)
    The study was stopped due to unacceptable toxicity during the dose-escalation as the overall risk-benefit ratio no longer favored the dose level being tested, therefore the MTD was not determined. ClinicalTrials.gov registration number: https://clinicaltrials.gov/ct2/show/NCT03410927 ; registered on January 25, 2018.
    Clinical • P1 data • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
    |
    HER-2 overexpression • HER-2 amplification • ERBB3 overexpression • ERBB3 mutation
    |
    TAS0728
    over4years
    A Study of TAS0728 in Patients With Solid Tumors With HER2 or HER3 Abnormalities (clinicaltrials.gov)
    P1/2, N=19, Active, not recruiting, Taiho Oncology, Inc. | Trial completion date: Jun 2020 --> Jan 2021 | Trial primary completion date: Jun 2020 --> Jan 2021
    Clinical • Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
    |
    HER-2 overexpression • HER-2 amplification • ERBB3 overexpression • ERBB3 mutation
    |
    TAS0728
    over4years
    Acquired resistance to trastuzumab/pertuzumab or to T-DM1 in vivo can be overcome by HER2 kinase inhibition with TAS0728. (PubMed, Cancer Sci)
    HER2-targeting antibodies (trastuzumab, pertuzumab) and a HER2-directed antibody-drug conjugate (trastuzumab emtansine: T-DM1) are used for the treatment of HER2-overexpressing breast cancer. These results suggest that tumors with acquired resistance to trastuzumab and pertuzumab and to T-DM1 are still dependent on oncogenic HER2-HER3 signaling and are vulnerable to HER2 signal inhibition by TAS0728. These results provide a rationale for TAS0728 therapy for breast cancers that are refractory to established anti-HER2 therapies.
    Preclinical • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
    |
    HER-2 overexpression
    |
    Perjeta (pertuzumab) • Kadcyla (ado-trastuzumab emtansine) • TAS0728
    over4years
    TAS0728, a covalent-binding, HER2-selective kinase inhibitor shows potent antitumor activity in preclinical models. (PubMed, Mol Cancer Ther)
    Taken together, our results demonstrated that TAS0728 may offer a promising therapeutic option with improved efficacy as compared to current HER2 inhibitors for HER2-activated cancers. Assessment of TAS0728 in ongoing clinical trials is awaited (NCT03410927).
    Preclinical • Journal
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR expression
    |
    TAS0728
    almost5years
    A Study of TAS0728 in Patients With Solid Tumors With HER2 or HER3 Abnormalities (clinicaltrials.gov)
    P1/2, N=19, Active, not recruiting, Taiho Oncology, Inc. | Trial completion date: Dec 2019 --> Jun 2020 | Trial primary completion date: Dec 2019 --> Jun 2020
    Clinical • Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
    |
    HER-2 overexpression • HER-2 amplification • ERBB3 overexpression • ERBB3 mutation
    |
    TAS0728