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    DRUG CLASS:

    Nectin-4-targeted peptide-drug conjugate

    Related drugs:
    21d
    Duravelo-1: Study BT8009-100 in Subjects With Nectin-4 Expressing Advanced Malignancies (clinicaltrials.gov)
    P1/2, N=329, Active, not recruiting, BicycleTx Limited | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • ALK (Anaplastic lymphoma kinase) • PGR (Progesterone receptor) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NECTIN4 (Nectin Cell Adhesion Molecule 4)
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    EGFR mutation • ALK fusion
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    Keytruda (pembrolizumab) • zelenectide pevedotin (BT8009)
    29d
    First-in-Human, Phase I/II Dose Escalation and Expansion Study of Zelenectide Pevedotin in Patients With Advanced Solid Tumors: Results From Monotherapy Dose Escalation. (PubMed, J Clin Oncol)
    Zelenectide pevedotin monotherapy demonstrated a generally well-tolerated safety profile and preliminary efficacy, particularly in UC, supporting investigation of UC and non-UC populations in the expansion phase.
    P1/2 data • Journal • First-in-human
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    NECTIN4 (Nectin Cell Adhesion Molecule 4)
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    zelenectide pevedotin (BT8009)
    2ms
    "Precision on Two Wheels"─Structural Refinement of 64Cu- and 68Ga-Labeled Bicyclic Peptides Targeting Nectin-4 for Improved Tumor Imaging: From Preclinical Development to First-in-Human Application. (PubMed, J Med Chem)
    For this purpose, we developed 64Cu- and 68Ga-labeled ligands derived from bicyclic peptide-drug conjugate BT8009...The suitability of the most promising ligand from the preclinical studies, NECT-224, for PET imaging purposes was also demonstrated in a first-in-human application using [68Ga]Ga-NECT-224. The results suggest its further clinical development, but also that of [64Cu]Cu-NECT-224.
    P1 data • Preclinical • Journal • First-in-human
    |
    NECTIN4 (Nectin Cell Adhesion Molecule 4)
    |
    zelenectide pevedotin (BT8009)
    2ms
    Duravelo-1: Study BT8009-100 in Subjects With Nectin-4 Expressing Advanced Malignancies (clinicaltrials.gov)
    P1/2, N=329, Recruiting, BicycleTx Limited | Trial primary completion date: Dec 2026 --> Mar 2026
    Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • ALK (Anaplastic lymphoma kinase) • PGR (Progesterone receptor) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NECTIN4 (Nectin Cell Adhesion Molecule 4)
    |
    EGFR mutation • ALK fusion
    |
    Keytruda (pembrolizumab) • zelenectide pevedotin (BT8009)
    4ms
    Zelenectide Pevedotin in NECTIN4 Amplified Advanced or Metastatic Non-small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=73, Recruiting, BicycleTx Limited | Not yet recruiting --> Recruiting
    Enrollment open
    |
    zelenectide pevedotin (BT8009)
    4ms
    SC-101 in Subjects With Advanced NECTIN4-Amplified Cancers (clinicaltrials.gov)
    P2, N=120, Not yet recruiting, Tianjin ConjuStar Biologics Co., Ltd.
    New P2 trial
    6ms
    Design, synthesis and antitumor evaluation of a novel nectin-4 targeting bicyclic toxin conjugate. (PubMed, Bioorg Med Chem Lett)
    In vivo antiproliferative activity assay results showed that BGC1614 (0.12 μM/kg) exhibited better antiproliferative activity than BT8009 (0.12 μM/kg, inhibition rate (IR) 87.6 %) in PC-3 (human prostate cancer cell) model with IR of 96.3 %, while BGC1614 (0.36 μM/kg) displayed similar inhibition with BT8009 (0.36 μM/kg, IR 72.7 %) in N87 (human gastric cancer cell) model with IR of 70.1 %, demonstrating that BGC1614 exhibited better antitumor effect in the same molar concentration in PC-3 model. In addition, BGC1614 was well-tolerated in efficacious doses in the nude model assays, while the pharmacokinetic (PK) parameters of BGC1614 were comparable to that of BT8009.
    Journal
    |
    NECTIN4 (Nectin Cell Adhesion Molecule 4)
    |
    zelenectide pevedotin (BT8009)
    8ms
    Zelenectide Pevedotin in NECTIN4 Amplified Advanced or Metastatic Non-small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=73, Not yet recruiting, BicycleTx Limited
    New P2 trial
    |
    zelenectide pevedotin (BT8009)
    8ms
    Study SC-101 in Subjects With Advanced Malignancies (clinicaltrials.gov)
    P1, N=100, Recruiting, Tianjin ConjuStar Biologics Co., Ltd. | Trial completion date: Dec 2025 --> Sep 2026 | Trial primary completion date: Jun 2025 --> Mar 2026
    Trial completion date • Trial primary completion date
    9ms
    Study to Assess Clinical Activity of Zelenectide Pevedotin in Participants With Advanced Breast Cancer (clinicaltrials.gov)
    P2, N=66, Recruiting, BicycleTx Limited | Not yet recruiting --> Recruiting
    Enrollment open
    |
    zelenectide pevedotin (BT8009)
    10ms
    Study to Assess Clinical Activity of Zelenectide Pevedotin in Participants With Advanced Breast Cancer (clinicaltrials.gov)
    P2, N=66, Not yet recruiting, BicycleTx Limited
    New P2 trial
    |
    zelenectide pevedotin (BT8009)
    11ms
    The validation and clinical bioanalysis of the Bicycle® Toxin Conjugate zelenectide pevedotin in human plasma. (PubMed, Bioanalysis)
    The Bicycle® toxin conjugate (BTC) zelenectide pevedotin, formerly known as BT8009, is a novel bicyclic peptide targeting the Nectin-4 tumor antigen conjugated to the cytotoxin monomethyl auristatin E (MMAE) via a valine-citrulline cleavable linker...The method was validated according to local standard operating procedures and has met all US Food and Drug Administration and European Medicines Agency regulatory guidance criteria. A bioanalytical method for measuring zelenectide pevedotin in plasma samples was developed and successfully applied in evaluating over 3000 samples from patients in a Phase 1/2 clinical study of zelenectide pevedotin in patients with advanced solid tumors.
    Journal
    |
    NECTIN4 (Nectin Cell Adhesion Molecule 4)
    |
    NECTIN4 expression
    |
    zelenectide pevedotin (BT8009)