Therapy Detail
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| Therapy Name | AGI-5198 + Talazoparib |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| AGI-5198 | AG5198|AGI 5198|IDH-C35 | IDH1 Inhibitor 8 | AGI-5198 is a selective inhibitor of mutant forms of IDH1, which decreases production of R-2HG, potentially leading to reduced growth of IDH1-mutant tumor cells (PMID: 23558169, PMID: 26368816, PMID: 31151327). | |
| Talazoparib | Talzenna | BMN673 | PARP Inhibitor (Pan) 30 | Talzenna (talazoparib) is an inhibitor of PARP1 and PARP2, which prevents the DNA repair of single strand DNA breaks, thus causing the accumulation of DNA strand breaks, genomic instability and apoptosis, and leads to lethality in homologous recombination repair deficient cells (PMID: 28242752). Talzenna (talazoparib) is FDA approved for use in patients with ERBB2 (HER2)-negative breast cancer harboring deleterious or suspected deleterious germline BRCA mutations, and in combination with Xtandi (enzalutamide) in patients with homologous recombination repair gene (ATM, ATR, BRCA1/2, CDK12, CHEK2, FANCA, MLH1, MRE11A, NBN, PALB2, or RAD51C)-mutated metastatic castration-resistant prostate cancer (FDA.gov). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| IDH1 R132H | Advanced Solid Tumor | decreased response | AGI-5198 + Talazoparib | Preclinical - Cell culture | Actionable | In a preclinical study, AGI-5198 reverted the sensitivity of transformed cells over expressing IDH1 R132H to Talzenna (talazoparib)-induced growth inhibition in culture (PMID: 28148839). | 28148839 |
| IDH1 R132C | sarcoma | decreased response | AGI-5198 + Talazoparib | Preclinical - Cell culture | Actionable | In a preclinical study, AGI-5198 reverted the sensitivity of sarcoma cells harboring IDH1 R132C to Talzenna (talazoparib)-induced growth inhibition in culture (PMID: 28148839). | 28148839 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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