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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).

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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).

Filtering

  • Case insensitive filtering will display rows if any text in any cell matches the filter term
  • Use simple literal full or partial string matches
  • Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
  • Filtering will only apply to rows that are already loaded on the page. Filtering has no impact on query parameters.
  • Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")

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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

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  • Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")

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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


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