vactosertib

Vactosertib is an orally bioavailable, potent, and selective small molecule inhibitor of the serine/threonine kinase transforming growth factor beta type I receptor (TGFBR1), also known as activin receptor-like kinase 5 (ALK5). By blocking TGFBR1-mediated signaling, vactosertib suppresses tumor growth in TGFBR1-overexpressing tumor cells and modulates the tumor microenvironment by reducing immunosuppression. It promotes immune cell-mediated cancer cell killing, inhibits metastasis and angiogenesis, and reduces cancer stem cell proliferation. Vactosertib is being developed primarily for various cancers including colorectal cancer, gastric cancer, multiple myeloma, non-small cell lung cancer, pancreatic cancer, fibroma, osteosarcoma, bladder cancer, and myelodysplastic syndromes. It has orphan drug status for osteosarcoma and pancreatic/gastric cancers. Developers include MedPacto, AstraZeneca, and Merck & Co.

Other names

vactosertib1352608-82-2