Therapy Detail
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| Therapy Name | BAY1436032 |
| Synonyms | |
| Therapy Description |
BAY1436032 inhibits mutant IDH1, resulting in decreased levels of (R)-2-hydroxyglutarate (R-2HG) and leading to reduced proliferation and increased differentiation of IDH1-mutant tumor cells (PMID: 28232670, PMID: 32733012). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| BAY1436032 | BAY-1436032|BAY 1436032 | IDH1 Inhibitor 8 | BAY1436032 inhibits mutant IDH1, resulting in decreased levels of (R)-2-hydroxyglutarate (R-2HG) and leading to reduced proliferation and increased differentiation of IDH1-mutant tumor cells (PMID: 28232670, PMID: 32733012). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| IDH1 R132H IDH1 T313I | leukemia | predicted - resistant | BAY1436032 | Preclinical - Biochemical | Actionable | In a preclinical study, BAY1436032 did not inhibit R-2HG production in a leukemia cell line expressing IDH1 R132H and T313I in culture (PMID: 36222845). | 36222845 |
| IDH1 R132C | acute myeloid leukemia | sensitive | BAY1436032 | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, BAY1436032 decreased R-2HG levels and inhibited growth of primary acute myeloid leukemia (AML) cells harboring IDH1 R132C in culture, and decreased blast number and increased survival of two AML patient-derived xenograft (PDX) models, one which harbored additional alterations in FLT3, NPM1, and NRAS and one which harbored a KMT2A (MLL) alteration (PMID: 28232670). | 28232670 |
| IDH1 R132S | acute myeloid leukemia | sensitive | BAY1436032 | Preclinical - Patient cell culture | Actionable | In a preclinical study, BAY1436032 decreased (R)-2-hydroxyglutarate (R-2HG) levels, and inhibited growth and increased differentiation of patient-derived acute myeloid leukemia cells harboring IDH1 R132S in culture (PMID: 28232670). | 28232670 |
| IDH1 R132G | acute myeloid leukemia | sensitive | BAY1436032 | Preclinical - Patient cell culture | Actionable | In a preclinical study, BAY1436032 decreased (R)-2-hydroxyglutarate (R-2HG) levels and increased differentiation of patient-derived acute myeloid leukemia cells harboring IDH1 R132G in culture (PMID: 28232670). | 28232670 |
| IDH1 R132X | acute myeloid leukemia | no benefit | BAY1436032 | Phase I | Actionable | In a Phase I trial, treatment with BAY1436032 in acute myeloid leukemia patients harboring an IDH1 R132X mutation demonstrated safety and resulted in an overall response rate of 15% (4/27), including one complete remission, one partial remission, and morphologic leukemia-free state in two patients, stable disease in 67% (18/27), and a median overall survival of 6.6 months, however, due to low response rates for all doses, further clinical development was not supported (PMID: 32733012; NCT03127735). | 32733012 |
| IDH1 R132H | acute myeloid leukemia | sensitive | BAY1436032 | Preclinical - Patient cell culture | Actionable | In a preclinical study, BAY1436032 decreased (R)-2-hydroxyglutarate (R-2HG) levels, and inhibited growth and increased differentiation of patient-derived acute myeloid leukemia cells harboring IDH1 R132H in culture (PMID: 28232670). | 28232670 |
| IDH1 R132H IDH1 H315D | leukemia | predicted - resistant | BAY1436032 | Preclinical - Biochemical | Actionable | In a preclinical study, BAY1436032 did not inhibit R-2HG production in a leukemia cell line expressing IDH1 R132H and H315D in culture (PMID: 36222845). | 36222845 |
| IDH1 R132L | acute myeloid leukemia | sensitive | BAY1436032 | Preclinical - Patient cell culture | Actionable | In a preclinical study, BAY1436032 decreased (R)-2-hydroxyglutarate (R-2HG) levels, and inhibited growth and increased differentiation of patient-derived acute myeloid leukemia cells harboring IDH1 R132L in culture (PMID: 28232670). | 28232670 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT02746081 | Phase I | BAY1436032 | Phase I Study of BAY1436032 in IDH1-mutant Advanced Solid Tumors | Active, not recruiting | USA | DEU | 2 |
| NCT03127735 | Phase I | BAY1436032 | BAY1436032 in Patients With Mutant IDH1(mIDH1) Advanced Acute Myeloid Leukemia (AML) | Completed | USA | DEU | 0 |
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