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    DRUG:

    Tukysa (tucatinib)

    i
    Other names: MK7119, ONT380, MK 7119, ONT 380, ARRY-380, ARRY 380, ONT-380, MK-7119, ARRY380
    Company:
    Pfizer
    Drug class:
    HER2 inhibitor
    Related drugs:
    3d
    Harnessing Machine Learning for the Virtual Screening of Natural Compounds as Both EGFR and HER2 Inhibitors in Colorectal Cancer: A Novel Therapeutic Approach. (PubMed, ACS Omega)
    Among these, LTS0131923 demonstrated the highest binding affinity against HER2 (PDB ID: 7MN5), with a binding energy of -11.2 kcal/mol and an inhibition constant of 0.00626 μM, outperforming Tucatinib, a standard CRC treatment. This study reveals the potential of ML-driven approaches to accelerate the discovery of dual-target inhibitors for CRC therapy and highlights Ceratonia siliqua L. as a promising source of bioactive compounds for cancer treatment.
    Journal
    |
    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation
    |
    Tukysa (tucatinib)
    6d
    TRACE: Tucatinib in Patients With Locally Advanced or Metastatic HER2-positive Breast Cancer Who Received at Least Two Prior Anti-HER2 Treatment Regimens. (clinicaltrials.gov)
    P=N/A, N=49, Completed, iOMEDICO AG | Recruiting --> Completed | N=300 --> 49 | Trial completion date: May 2027 --> Jun 2025 | Trial primary completion date: May 2027 --> Jun 2025
    Trial completion • Enrollment change • Trial completion date • Trial primary completion date
    |
    HER-2 positive
    |
    capecitabine • Tukysa (tucatinib)
    7d
    Clinicomics for predicting HER2 expression in metastatic colorectal cancer: a multicenter machine learning analysis on real-world data. (PubMed, Oncology)
    Hb 100 ng/mL, height >160 cm, and the presence of lymph node metastases were associated with HER2 expression and positivity. HER2 testing should be considered mandatory when all these factors are present. The mechanisms linking these four factors to HER2 expression require further investigation.
    Journal • Real-world evidence
    |
    HER-2 (Human epidermal growth factor receptor 2) • CEACAM5 (CEA Cell Adhesion Molecule 5)
    |
    HER-2 positive • HER-2 amplification • HER-2 expression
    |
    Enhertu (fam-trastuzumab deruxtecan-nxki) • Tukysa (tucatinib)
    7d
    Tucatinib, trastuzumab, and capecitabine with stereotactic radiosurgery in patients with brain metastases from HER-2 positive breast cancer (TUTOR): Study protocol for a multicenter phase 1 clinical trial. (PubMed, BMC Cancer)
    This trial has been approved by the Institutional Review Board (IRB) and began patient enrollment in January 2024. The trial will provide insights into the safety and effectiveness of a novel combinatorial therapy for BCBM.
    P1 data • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive
    |
    Herceptin (trastuzumab) • capecitabine • Tukysa (tucatinib)
    10d
    Development of cellular models expressing cynomolgus (Macaca fascicularis) HER2 for the functional evaluation of cross-reactive anti-human HER2 response. (PubMed, Front Pharmacol)
    Our model, based on NIH 3T3 cells, became sensitive to the monoclonal antibody trastuzumab and to the selective HER2 tyrosine kinase inhibitor tucatinib. The results suggest that this model could be a promising tool for preclinical functional cross-reactivity tests of anti-HER2 therapies before in vivo studies.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • ACACA (Acetyl-CoA Carboxylase Alpha)
    |
    HER-2 positive • HER-2 expression
    |
    Herceptin (trastuzumab) • Tukysa (tucatinib)
    21d
    Tucatinib and trastuzumab emtansine for patients with previously treated HER2-positive locally advanced and metastatic breast cancer: primary analysis of the randomized phase III trial HER2CLIMB-02. (PubMed, Ann Oncol)
    The addition of tucatinib to T-DM1 improved PFS in patients with previously treated HER2+ LA/MBC, including patients with BMs, and exhibited a manageable safety profile.
    P3 data • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive • EGFR positive
    |
    Kadcyla (ado-trastuzumab emtansine) • Tukysa (tucatinib)
    22d
    Real World-clinical Outcomes of Tucatinib, Trastuzumab, and Capecitabine Following Trastuzumab Deruxtecan (T-DXd) for the Treatment of HER2-positive Metastatic Breast Cancer. (clinicaltrials.gov)
    P=N/A, N=93, Completed, Pfizer | Active, not recruiting --> Completed
    Trial completion • Real-world evidence
    |
    Enhertu (fam-trastuzumab deruxtecan-nxki) • capecitabine • Tukysa (tucatinib)
    24d
    A Study to Learn More About Tukysa Once it is Out in the Korean Market (clinicaltrials.gov)
    P=N/A, N=600, Not yet recruiting, Pfizer | Trial completion date: Jun 2030 --> May 2029 | Trial primary completion date: Jun 2030 --> May 2029
    Trial completion date • Trial primary completion date
    |
    Tukysa (tucatinib)
    1m
    HERTHENA-Breast-01: Study of Patritumab Deruxtecan With Other Anticancer Agents in Participants With HER2 Positive Breast Cancer That Has Spread and Cannot Be Surgically Removed (MK-1022-009) (clinicaltrials.gov)
    P1/2, N=81, Recruiting, Merck Sharp & Dohme LLC | Trial completion date: Sep 2029 --> Apr 2030 | Trial primary completion date: Sep 2029 --> Apr 2030
    Trial completion date • Trial primary completion date
    |
    Perjeta (pertuzumab) • Tukysa (tucatinib) • patritumab deruxtecan (U3-1402) • Herzuma (trastuzumab-pkrb) • Trazimera (trastuzumab-qyyp)
    1m
    T-DM1 and Tucatinib Compared With T-DM1 Alone in Preventing Relapses in People With High Risk HER2-Positive Breast Cancer, the CompassHER2 RD Trial (clinicaltrials.gov)
    P3, N=1056, Active, not recruiting, Alliance for Clinical Trials in Oncology | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    HER-2 positive • ER positive • HR positive • HR negative • ER negative
    |
    Kadcyla (ado-trastuzumab emtansine) • Tukysa (tucatinib)
    2ms
    SGNTUC 024: Tucatinib Plus Trastuzumab and Oxaliplatin-based Chemotherapy or Pembrolizumab-containing Combinations for HER2+ Gastrointestinal Cancers (clinicaltrials.gov)
    P2, N=40, Active, not recruiting, Seagen, a wholly owned subsidiary of Pfizer | Trial completion date: Sep 2025 --> Dec 2025
    Trial completion date
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    Keytruda (pembrolizumab) • Herceptin (trastuzumab) • 5-fluorouracil • capecitabine • oxaliplatin • Tukysa (tucatinib) • leucovorin calcium
    2ms
    Real-world efficacy of tucatinib in Danish human epidermal growth factor receptor 2-positive metastatic breast cancer. (PubMed, Dan Med J)
    Our results align with data presented from the HER2CLIMB trial. Considerably fewer patients than initially expected have been treated in Denmark.
    Retrospective data • Journal • Real-world evidence
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR positive
    |
    Herceptin (trastuzumab) • capecitabine • Tukysa (tucatinib)