Table 1.
Small molecule inhibitors, mechanism, clinical targets, delivery, and status in clinical application
| Inhibitors | Mechanism | Target | Delivery | Clinical status |
|---|---|---|---|---|
| CX-4945 |
CK2 inhibitor |
Lung, myeloma |
Oral, IV |
Phase 1/2 |
| EW-7195 |
TGFβ Inhibitor |
Breast, Lung metastases |
Orally available |
Phase 1 Clinical Trial |
| EW-7203 |
TGFβ 1 and 2 receptor kinase inhibitor |
Breast, Lung metastases |
IV |
Pre-Clinical |
| EW-7197 |
TGFβ 1 and 2 receptor kinase inhibitor |
Breast, Lung metastases |
IV |
Pre-Clinical |
| IN-1130 |
TGFβ 1 and 2 receptor kinase inhibitor |
Breast, Lung metastases |
IV |
Pre-Clinical |
| SB-431542 |
Inhibition of ATP binding to ALK5 kinase |
Glioma |
IV |
Pre-Clinical |
| SD-208 |
TGFβ 1 receptor kinase inhibitor |
Metastatic breast cancer |
IV |
Pre-Clinical |
| SD-093 |
TGFβ 1 receptor kinase inhibitor |
Metastatic breast cancer |
IV |
Pre-Clinical |
| LY-2152799 |
TGFβ 1 receptor kinase antagonist |
Breast, Myelodysplastic syndromes, Hepatocellular Carcinoma, Pancreatic Cancer, Malignant Glioma |
Orally available |
Clinical trial: Phase 2/3; Phase 2; Phase 1b/2; Phase 1b/2a |
| LGK974 |
Porcupine inhibitor (Wnt signaling) |
Breast |
Orally available |
Phase 1 Clinical Trial |
| CWP232291 |
Wnt signaling inhibitor |
Hematologic malignancies (AML) |
Oral, IV |
Phase 1 Clinical Trial |
| MK-0752 | ϒ-secretase inhibitor | Cranial tumors, solid tumors | Oral, IV | Phase 1/2 Clinical Trial |