SB273005 is an orally active and potent nonpeptide integrin αvβ3 antagonist that inhibits αvβ3 and αvβ5 and reduces the production of Th2 cells and the cytokine IL-10 in pregnant mice.

αvβ5 receptor:0.3 nM, αvβ3 receptor:1.2 nM

In vitro, SB273005 inhibits human osteoclast-mediated bone resorption with IC50 of 11 nM. [1] In blood containing MDA-MB-231 cells, a combination of SB273005 and lamifiban inhibits tumor cell adhesion to vascular extracellular matrix (ECM). [3]

In rat models of bone resorption and osteoporosis, SB273005 (30 mg/kg, p.o.) inhibits the parathyroid hormone-stimulated calcemic response, and inhibits bone loss. [1] In rat with adjuvant-induced arthritis, SB273005 (60 mg/kg, p.o.) significantly reduces the symptoms of adjuvant-induced arthritis. [2] SB273005 (1000 mg/kg/day, p.o.) causes acute, transient necrosis of vascular smooth muscle cell (VSMC) in aorta and renal arteries of mice. [4] In pregnant mice, SB273005 reverses the reduction of Th1 cell-produced IL-2 levels and the increase of Th2 cell-derived IL-10 levels. [5]