Table 2.
IDH mutations inhibitors and clinical trials.
| Compound | Drug Name | Route | Target | Clinical Trials and Preclinical Studies | References |
|---|---|---|---|---|---|
| AGI-5198 | Oral | IDH1mut R132H | Phase 3 clinical trial (NCT03173248) in IDH mutated AML | ||
| Delays growth and promotes differentiation in IDH1 mutated glioma cells | [117,135] | ||||
| AG-120 | Ivosidenib | Oral | IDH1mut R132H and R132C | Phase 1 clinical trial (NCT03343197) in patients with recurrent, non-enhancing IDH1 mutated low grade glioma | [137] |
| (FDA-approved) | Phase 1 clinical trial (NCT02073994) in IDH1 mutated advanced solid tumors, including glioma | ||||
| AG-221 | Enasidenib | Oral | IDH2mut R140Q and R172K | Phase 1/2 clinical trial (NCT02273739) in adults with IDH2 mutated advanced solid tumors, including glioma | |
| (FDA-approved) | |||||
| DS-1001b | Oral | IDH1mutations | Phase 1 clinical trial (NCT03030066) in patients with gene IDH1 mutated gliomas | [134] | |
| Phase 2 clinical trial (NCT04458272) in patients with chemo- and radiotherapy-naive IDH1 mutated WHO grade II glioma | |||||
| BAY1436032 | Oral | pan IDH1 mutations | Phase 1 clinical trial (NCT02746081) in IDH1 mutated advanced solid tumors, including glioma | [140] | |
| (R132H, R132C, R132G, R132L, and R132S) | |||||
| AG-881 | Vorasidenib | Oral | IDH1/2 mutation | Phase 1 clinical trial (NCT02481154) in patients with IDH1 or IDH2 mutated advanced solid tumors, including gliomas | [143] |
| (IDH1mut R132H, R132C, R132G, R132L, and R132S) | Phase 1 clinical trial (NCT03343197) in patients with recurrent, non-enhancing IDH1 mutated low grade glioma | ||||
| (IDH2mut R140Q and R172K) | Phase 3 clinical trial (NCT04164901) in patients with residual or recurrent grade 2 IDH1 or IDH2 mutated glioma | [144] | |||
| AGI-6780 | IDH2 mut R140Q | Reverses IDH2 R140Q induced histone hypermethylation expression in IDH2 mutated AML cell model | [145] | ||
| MRK-A | IDH1mut R132H and R132C | Show survival benefit in IDH1 mutated patient-derived cells xenograft model | [146] | ||
| FT-2102 | Olutasidenib | Oral | Phase 1 dose escalation study in patients with IDH1 mutated AML or MDS | [147] | |
| HMS-101 | IDH1mut R132C | In vitro and in vivo in IDH1 mutated AML | [148] | ||
| IDH305 | Oral | IDH1mut R132H and R132C | Phase 1 clinical trial (NCT02381886) in patients with IDH1R132 mutated advanced malignancies, including glioma | [149] | |
Clinical trial information was collected and organized from clinicaltrials.gov.