Drug intelligence / Profile preview

RPR128515

Development stage
Discontinued
Lead developer
Sanofi
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
01

Overview

RPR128515 is an experimental small molecule inhibitor belonging to the class of biphenyl derivatives. It was designed as a synthetic serine protease inhibitor and has been specifically characterized as a potent and selective inhibitor of Factor Xa, a key enzyme in the coagulation cascade. The compound contains structural features such as benzamidine and biphenyl moieties that enable it to bind in a canonical fashion to the active site of serine proteases like trypsin and Factor Xa. RPR128515 has not been approved for clinical use or advanced beyond preclinical/early experimental stages[1][5][4]. Its primary development focus was anticoagulation via inhibition of Factor Xa.

Other names
methyl (2R,3R)-3-({4-[3-(aminomethyl)phenyl]phenyl}formamido)-2-[(3-carbamimidoylphenyl)methyl]butanoate3-[(3'-aminomethyl-biphenyl-4-carbonyl)-amino]-2-(3-carbamimidoyl-benzyl)-butyric acid methyl ester
02

Targets

F10 (Factor Xa)

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