Vactosertib (Not yet branded)

Other Medications

US Experimental EU Experimental ES Not available Oral 2 Clinical Trials
TGF-β receptor I (ALK5)

Description

Vactosertib is a small molecule inhibitor of transforming growth factor beta (TGF- ) receptor I that blocks TGF-? signaling pathways. In colorectal cancer treatment, it is being combined with natural killer (NK) cell therapy and interleukin-2 to enhance immune system function against tumors. The drug targets the immunosuppressive effects of TGF-? that often allow cancer cells to evade immune detection and destruction.

Mechanism of Action

Vactosertib selectively inhibits TGF-? receptor I (ALK5) kinase activity, preventing the phosphorylation and activation of SMAD2 and SMAD3 transcription factors. By blocking this pathway, the drug reduces TGF- -mediated immunosuppression in the tumor microenvironment, potentially allowing enhanced NK cell and T-cell anti-tumor activity.

Molecular Targets

Side Effects

Fatigue Nausea Diarrhea Skin rash Decreased appetite Elevated liver enzymes Low blood cell counts Joint pain

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT05400122 Phase 1
Suspended
Natural Killer (NK) Cells in Combination With Interleukin-2 (IL-2) and Transforming Growth Factor Beta (TGFbeta) Receptor I Inhibitor Vactosertib in Cancer
United States
NCT03844750 Phase 2
Terminated
Preoperative Immunotherapy (Pembrolizumab) for Patients With Colorectal Cancer and Resectable Hepatic Metastases
United States