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Therapy Name | DS-1001b |
Synonyms | |
Therapy Description |
DS-1001b specifically targets IDH1 mutations, including at amino acid R132, which results in decreased 2HG production and potentially leads to increased differentiation and decreased proliferation of IDH1 mutant cancer cells (PMID: 31727689, PMID: 31406254). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
DS-1001b | DS-1001|DS1001|Safusidenib|AB-218|AB218|AB 218 | IDH1 Inhibitor 8 | DS-1001b specifically targets IDH1 mutations, including at amino acid R132, which results in decreased 2HG production and potentially leads to increased differentiation and decreased proliferation of IDH1 mutant cancer cells (PMID: 31727689, PMID: 31406254). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
IDH1 R132C | Advanced Solid Tumor | predicted - sensitive | DS-1001b | Preclinical - Biochemical | Actionable | In a preclinical study, DS-1001b inhibited IDH1 R132C enzymatic activity in an in vitro assay, and inhibited production of the oncometabolite 2-hydroxyglutarate (2-HG) in transformed human cells expressing IDH1 R132C in culture (PMID: 31727689). | 31727689 |
IDH1 R132L | Advanced Solid Tumor | predicted - sensitive | DS-1001b | Preclinical - Biochemical | Actionable | In a preclinical study, transformed human cells expressing IDH1 R132L demonstrated sensitivity to DS-1001b in culture, resulting in reduced production of the oncometabolite 2-hydroxyglutarate (2-HG) (PMID: 31727689). | 31727689 |
IDH1 R132G | Advanced Solid Tumor | predicted - sensitive | DS-1001b | Preclinical - Biochemical | Actionable | In a preclinical study, transformed human cells expressing IDH1 R132G demonstrated sensitivity to DS-1001b in culture, resulting in reduced production of the oncometabolite 2-hydroxyglutarate (2-HG) (PMID: 31727689). | 31727689 |
IDH1 R132S | Advanced Solid Tumor | predicted - sensitive | DS-1001b | Preclinical - Biochemical | Actionable | In a preclinical study, transformed human cells expressing IDH1 R132S demonstrated sensitivity to DS-1001b in culture, resulting in reduced production of the oncometabolite 2-hydroxyglutarate (2-HG) (PMID: 31727689). | 31727689 |
IDH1 R132H | Advanced Solid Tumor | predicted - sensitive | DS-1001b | Preclinical - Biochemical | Actionable | In a preclinical study, DS-1001b inhibited IDH1 R132H enzymatic activity in an in vitro assay, and inhibited production of the oncometabolite 2-hydroxyglutarate (2-HG) in transformed human cells expressing IDH1 R132H in culture (PMID: 31727689). | 31727689 |
IDH1 R132H | glioblastoma | sensitive | DS-1001b | Preclinical - Pdx | Actionable | In a preclinical study, treatment with DS-1001b inhibited subcutaneous and intracranial tumor growth in a patient-derived xenograft (PDX) model of glioblastoma harboring IDH1 R132H, and also demonstrated reduced levels of the oncometabolite 2-hydroxyglutarate (2-HG) within tumors and plasma and increased expression of the astrocyte differentiation marker glial fibrillary acidic protein in tumor cells (PMID: 31727689). | 31727689 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT05303519 | Phase II | DS-1001b | Safusidenib Phase 2 Study in IDH1 Mutant Glioma | Recruiting | USA | 0 |
NCT05577416 | Phase I | DS-1001b | A Study of AB-218 in Patients With IDH1 Mutated Low Grade Glioma (AB-218-IIT-201) | Recruiting | AUS | 0 |