Table 1 Small molecule inhibitors, mechanism, clinical targets, delivery, and status in clinical application
From: Novel clinical therapeutics targeting the epithelial to mesenchymal transition
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 | γ-secretase inhibitor | Cranial tumors, solid tumors | Oral, IV | Phase 1/2 Clinical Trial |