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    DRUG:

    DS-6157

    i
    Other names: DS-6157, DS-6157a, DNA topoisomerase I inhibitor Exatecan-derivative based ADC, GPR20 ADC
    Company:
    Daiichi Sankyo
    Drug class:
    Topoisomerase I inhibitor, GPR20 -targeted antibody-drug conjugate
    Related drugs:
    9ms
    DS-6157a in Participants With Advanced Gastrointestinal Stromal Tumor (GIST) (clinicaltrials.gov)
    P1, N=34, Terminated, Daiichi Sankyo | Completed --> Terminated; The study was terminated due to a business decision.
    Trial termination • Stroma • Metastases
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • GPR20 (G Protein-Coupled Receptor 20)
    |
    KIT mutation • PDGFRA D842V • PDGFRA mutation
    |
    DS-6157
    1year
    A Phase 1, Multicenter, Open-Label, First-in-Human Study of DS-6157a in Patients With Advanced Gastrointestinal Stromal Tumor. (PubMed, Clin Cancer Res)
    Targeting GPR20 with DS-6157a was tolerated in patients with advanced GIST with tumor shrinkage demonstrated in KIT/PDGFRA wild type GIST. However, the study did not proceed further due to lower efficacy outcomes than anticipated.
    P1 data • Journal • Stroma • Metastases
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • GPR20 (G Protein-Coupled Receptor 20)
    |
    PDGFR wild-type
    |
    DS-6157
    over2years
    DS-6157a in Participants With Advanced Gastrointestinal Stromal Tumor (GIST) (clinicaltrials.gov)
    P1, N=35, Completed, Daiichi Sankyo, Inc. | Active, not recruiting --> Completed
    Trial completion
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • GPR20 (G Protein-Coupled Receptor 20)
    |
    KIT mutation • PDGFRA D842V • PDGFRA mutation
    |
    DS-6157
    3years
    DS-6157a in Participants With Advanced Gastrointestinal Stromal Tumor (GIST) (clinicaltrials.gov)
    P1, N=34, Active, not recruiting, Daiichi Sankyo, Inc. | N=100 --> 34 | Trial completion date: Oct 2024 --> May 2022 | Trial primary completion date: May 2024 --> Jan 2022
    Clinical • Enrollment change • Trial completion date • Trial primary completion date
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • GPR20 (G Protein-Coupled Receptor 20)
    |
    KIT mutation • PDGFRA D842V • PDGFRA mutation
    |
    DS-6157
    over3years
    DS-6157a in Participants With Advanced Gastrointestinal Stromal Tumor (GIST) (clinicaltrials.gov)
    P1, N=100, Active, not recruiting, Daiichi Sankyo, Inc. | Recruiting --> Active, not recruiting
    Clinical • Enrollment closed
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • GPR20 (G Protein-Coupled Receptor 20)
    |
    KIT mutation • PDGFRA D842V • PDGFRA mutation
    |
    DS-6157
    almost4years
    Identification and Therapeutic Targeting of GPR20, Selectively Expressed in Gastrointestinal Stromal Tumors, with DS-6157a, a First-In-Class Antibody-Drug Conjugate. (PubMed, Cancer Discov)
    DS-6157a exhibited GPR20 expression-dependent antitumor activity in GIST xenograft models including a GIST model resistant to imatinib, sunitinib, and regorafenib. Pre-clinical pharmacokinetics and safety profile of DS-6157a support its clinical development as a potential novel GIST therapy in patients with resistance, refractory, or intolerance to approved TKIs.
    Journal
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • GPR20 (G Protein-Coupled Receptor 20)
    |
    KIT mutation • PDGFRA mutation • KIT expression • GPR20 expression
    |
    imatinib • sunitinib • Stivarga (regorafenib) • DS-6157
    over4years
    [VIRTUAL] Therapeutic targeting of GPR20, selectively expressed in gastrointestinal stromal tumor (GIST), with DS-6157a, an antibody-drug conjugate (ADC) (AACR-II 2020)
    In addition, DS-6157a showed antitumor activity in a GIST patient-derived xenograft model that was resistant to imatinib, sunitinib, and regorafenib. In preclinical toxicology studies using rats and cynomolgus monkeys, the pharmacokinetics and safety profile of DS-6157a were favorable at up to 200 mg/kg and 30 mg/kg, respectively. These data support the clinical development of DS-6157a as a potential novel GIST therapy with activity in patients that are resistant, refractory, or intolerant to approved TKIs.
    PARP Biomarker
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • CHEK1 (Checkpoint kinase 1) • GPR20 (G Protein-Coupled Receptor 20)
    |
    PDGFRA mutation • KIT expression • GPR20 expression
    |
    imatinib • sunitinib • Stivarga (regorafenib) • DS-6157
    over4years
    DS-6157a in Participants With Advanced Gastrointestinal Stromal Tumor (GIST) (clinicaltrials.gov)
    P1, N=100, Not yet recruiting, Daiichi Sankyo, Inc. | Trial completion date: Mar 2025 --> Oct 2024 | Trial primary completion date: Mar 2025 --> May 2024
    Clinical • Trial completion date • Trial primary completion date
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • GPR20 (G Protein-Coupled Receptor 20)
    |
    KIT mutation • PDGFRA D842V • PDGFRA mutation
    |
    DS-6157
    over4years
    DS-6157a in Participants With Advanced Gastrointestinal Stromal Tumor (GIST) (clinicaltrials.gov)
    P1, N=100, Recruiting, Daiichi Sankyo, Inc. | Not yet recruiting --> Recruiting
    Clinical • Enrollment open
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • GPR20 (G Protein-Coupled Receptor 20)
    |
    KIT mutation • PDGFRA D842V • PDGFRA mutation
    |
    DS-6157