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    DRUG CLASS:

    GPR20 -targeted antibody-drug conjugate

    Related drugs:
    10ms
    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
    over1year
    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
    almost2years
    The activation mechanism and antibody binding mode for orphan GPR20. (PubMed, Cell Discov)
    We also uncover the molecular interactions between GPR20 and Ab046, which may enable the design of tool antibodies with enhanced affinity or new functionality for GPR20. Furthermore, we report the orthosteric pocket occupied by an unassigned density which might be essential for exploring opportunities for deorphanization.
    Journal
    |
    GPR20 (G Protein-Coupled Receptor 20)
    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
    over3years
    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