Review Article
Activators and Inhibitors of NRF2: A Review of Their Potential for Clinical Development
Table 4
Selected KEAP1-independent activators of NRF2.
| | Compound | Mechanism of action | Disease | Clinical trial | ClinicalTrials.gov identifier |
| Tideglusib
| GSK-3 inhibition | Autism spectrum disorders | Phase II | NCT02586935 | | Myotonic dystrophy 1 | Phase II | NCT02858908 | | Alzheimer’s disease | Phase II | NCT01350362 |
| Nordihydroguaiaretic acid (NDGA)
| GSK-3 inhibition | Prostate cancer | Phase II | NCT00678015 | | Phase I | NCT00313534 | | Brain and central nervous system tumors | Phase I/II | NCT00404248 |
| Terameprocol (NDGA derivative)
| GSK-3 inhibition | High-grade glioma | Phase I | NCT02575794 | Leukemias
Acute myeloid leukemia (AML)
Acute lymphocytic leukemia (ALL) | Phase I | NCT00664677 | Refractory solid tumors
Lymphoma | Phase I | NCT00664586 |
| Enzastaurin
| GSK-3 inhibition | Diffuse large B cell lymphoma | Phase III | NCT03263026 | Solid tumor
Lymphoma, malignant | Phase I | NCT01432951 |
| LS-102
| HRD1 inhibition | — | — | No clinical trials available |
| Rapamycin
| p62/SQSTM1 activation | Diabetes mellitus, type 1 | Phase III | NCT01060605 | | Systemic lupus erythematosus (SLE) | Phase II | NCT00779194 | | Autosomal dominant polycystic kidney disease | Phase II/III | NCT00920309 |
| HPP-4382
| BACH1 inhibition | — | — | No clinical trials available |
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