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 |