Fradafiban is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM.
Fradafiban is a nonpeptide mimetic of the arginine-glycine-aspartic acid recognition sequence. Fradafiban binds with high affinity and selectivity to the human platelet GP IIb/IIIa complex and potently inhibits human platelet aggregation in vitro. Fradafiban reversibly binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM[1].
Fradafiban has only very limited oral activity probably due to its high polarity and thus poor absorption after oral ingestion[1].
[1]. Müller TH, et al. Profound and sustained inhibition of platelet aggregation by Fradafiban, a nonpeptide platelet glycoprotein IIb/IIIa antagonist, and its orally active prodrug, Lefradafiban, in men. Circulation. 1997 Aug 19;96(4):1130-8.