Zotarolimus

Zotarolimus (ABT-578) is a derivative of Rapamycin (HY-10219), with anti-proliferative activity. Zotarolimus is an immunosuppressant. Zotarolimus is developed specifically for local delivery from stents for the prevention of coronary artery restenosis^[1][2]. In Vitro:Zotarolimus (0.01-1000 nM) potently inhibits the binding of an ascomycin derivative to immobilized FKBP12 in a concentration-dependent manner with an IC₅₀ value of 2.57 nM in the FKBP binding affinity assay^[1].
Zotarolimus (0.01-1000 nM; 2 days) inhibits Concanavalin A-induced human and rat T cells proliferation in a concentration-dependent manner with IC₅₀ values of 7.0 nM and 1337 nM, respectively^[1].
Zotarolimus (v0.01-1000 nM; 2 days) inhibits human coronary artery smooth muscle cell proliferation in a concentration-dependent manner with an IC₅₀ value of 0.8 nM^[1].
In Vivo:Zotarolimus (0.1-10 mg/kg; oral administration; on days 1, 4, 5, 6, and 7) inhibits the rat adjuvant-induced delayed-type hypersensitivity (DTH) response in a dose-dependent manner with an ED₅₀ value of 1.72 mg/kg/day in the rat adjuvant DTH model^[1].
Zotarolimus (0.1-10 mg/kg; oral administration; once daily; for 13 days) inhibits the rat experimental autoimmune encephalomyelitis (EAE) in a dose - dependent manner with an ED₅₀ value of 1.17 mg/kg/day in the rat EAE model^[1].
Zotarolimus (0.1-10 mg/kg; oral administration; once daily; for 13 days) shows a dose-related delay in cardiac allograft rejection with an ED₅₀ value of 3.71 mg/kg/day in the rat cardiac allograft rejection model^[1].