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    DRUG CLASS:

    CCR2-targeted antibody-drug conjugate

    Related drugs:
    1m
    Identification of a Novel Linker Enabling the Bioconjugation of a Cyclic Dinucleotide for the STING Antibody-Drug Conjugate TAK-500. (PubMed, Bioconjug Chem)
    The stochastic cysteine conjugation of the dazostinag containing these linkers provided ADC TAK-500 and its mouse surrogate mTAK-500 with DAR = 4. In syngeneic tumor-bearing mouse models, mTAK-500 showed target specific antitumor activity as well as the induction of immune-stimulating cytokines.
    Journal
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    STING (stimulator of interferon response cGAMP interactor 1) • CCR2 (C-C Motif Chemokine Receptor 2)
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    plozalizumab plevistinag (TAK-500) • dazostinag (TAK-676)
    9ms
    A Study of TAK-500 With or Without Pembrolizumab in Adults With Select Locally Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
    P1/2, N=61, Terminated, Takeda | Recruiting --> Terminated | Trial primary completion date: Aug 2026 --> Jan 2025 | N=313 --> 61 | Trial completion date: Aug 2026 --> Jan 2025; Clinical Futility of TAK 500 met. No further development with this compound
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date
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    Keytruda (pembrolizumab) • plozalizumab plevistinag (TAK-500)
    10ms
    Selective STING Activation in Intratumoral Myeloid Cells via CCR2-Directed Antibody Drug Conjugate TAK-500. (PubMed, Cancer Immunol Res)
    Spatially resolved analysis of CCR2 and immune cell markers in the TME of >1,000 primary human tumors showed the CCR2 protein was predominantly expressed in intratumoral myeloid cells. Collectively, these data highlight the clinical potential of delivering a STING agonist to CCR2+ cells.
    Journal
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    STING (stimulator of interferon response cGAMP interactor 1) • CCR2 (C-C Motif Chemokine Receptor 2)
    |
    plozalizumab plevistinag (TAK-500)
    2years
    A Study of TAK-500 With or Without Pembrolizumab in Adults With Select Locally Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
    P1/2, N=313, Recruiting, Takeda | Phase classification: P1a/1b --> P1/2 | N=118 --> 313 | Trial completion date: Mar 2025 --> Aug 2026 | Trial primary completion date: Mar 2025 --> Aug 2026
    Phase classification • Enrollment change • Trial completion date • Trial primary completion date • Combination therapy • Metastases
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    Keytruda (pembrolizumab) • plozalizumab plevistinag (TAK-500)
    over2years
    TAK-500 as a single agent and in combination with pembrolizumab in patients (pts) with advanced solid tumors: Rationale and design of a phase I/II study (ESMO 2023)
    Background TAK-500 is a novel immune-cell-directed antibody drug conjugate comprising the STING agonist TAK-676 conjugated to a human IgG1 anti-C-C chemokine receptor 2 (CCR2) antibody. A single-stage statistical design will be utilized for 3rd-line NS NSCLC and RCC. As of May 2023, 6 sites in the United States are recruiting; the global phase 2 is planned to start in 2024.
    Clinical • P1/2 data • Combination therapy • Metastases
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    CCR2 (C-C Motif Chemokine Receptor 2)
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    Keytruda (pembrolizumab) • plozalizumab plevistinag (TAK-500) • dazostinag (TAK-676)
    over2years
    TAK-500 is a clinical stage immune-cell directed antibody drug conjugate (iADC) inducing STING activation in CCR2-expressing intratumor myeloid cells and favorable immunomodulation (AACR 2023)
    The iADC TAK-500 and mTAK-500 induces CCR2-dependent immune cell activation and anti-tumor effect. CCR2 is highly expressed in intratumor myeloid cells from NSCLC. High CCR2 is associated with enhanced local adaptive immune responses and specific clinical/molecular tumor subsets.
    Clinical • PD(L)-1 Biomarker • IO biomarker • Immunomodulating • Immune cell
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    EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • MSI (Microsatellite instability) • CD8 (cluster of differentiation 8) • STING (stimulator of interferon response cGAMP interactor 1) • CD68 (CD68 Molecule) • ITGAM (Integrin, alpha M) • CCR2 (C-C Motif Chemokine Receptor 2)
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    PD-L1 expression • KRAS mutation • EGFR mutation • PD-L1 overexpression
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    Keytruda (pembrolizumab) • plozalizumab plevistinag (TAK-500)