Table 3.
Development of IDH Mutant Inhibitors for Cancer Treatment.
| Inhibitors | Targets | Cancers with IDH mutation | R & D status | Clinical trial identifiers |
|---|---|---|---|---|
|
AG-221
(FDA approved) |
IDH2 mutant | Glioma Angioimmunoblastic T-cell lymphoma Cholangiocarcinoma Chondrosarcoma MDS AML |
Phase 1/2 Phase 1/2 Phase 1/2 Phase 1/2 Phase 3 Phase 3 |
NCT02273739 NCT02273739 NCT02273739 NCT02273739 NCT03839771 NCT03839771 |
|
AG-120
(FDA approved) |
IDH1 mutant | AML Glioma Chondrosarcoma MDS Chondrosarcoma Cholangiocarcinoma |
Phase 3 Phase 2 Phase 2 Phase 2 Phase 2 Phase 3 |
NCT03839771 NCT04056910 NCT04278781 NCT04044209 NCT04278781 NCT02989857 |
| AG-881 | IDH1/IDH2 mutant | AML Glioma |
Phase 1 Phase 3 |
NCT02492737 NCT04164901 |
| IDH305 | IDH1 mutant | AML Glioma MDS |
Phase 1 Phase 2 Phase 1 |
NCT02826642 NCT02977689 NCT02381886 |
| BAY1436032 | IDH1 mutant | Solid Tumors AML |
Phase 1 Phase 1 |
NCT02746081 NCT03127735 |
| FT-2102 | IDH1 mutant | AML MDS Glioma Chondrosarcoma |
Phase 1/2 Phase 1/2 Phase 1/2 Phase 1/2 |
NCT04013880 NCT04013880 NCT03684811 NCT03684811 |
| AGI-5198 | IDH1 mutant | Glioma | Preclinical | / |
| AGI-6780 | IDH2 mutant | AML | Preclinical | / |
| MRK-A | IDH1 mutant | Glioma | Preclinical | / |
| GSK321 | IDH1 mutant | AML | Preclinical | / |
| GSK864 | IDH1 mutant | AML Glioma |
Preclinical | / |