Drug intelligence / Profile preview

α-NAPAP

Development stage
Unknown
Lead developer
Pentapharm
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

α-NAPAP (alpha-NAPAP) is a highly potent, selective, and competitive small-molecule direct thrombin inhibitor. It reversibly binds to the active site of thrombin, mimicking the basic amino acid residues (arginine and lysine) typically cleaved by trypsin-like serine proteases. In preclinical research, α-NAPAP is widely utilized as an anticoagulant and neuroprotective agent. It has been shown to significantly reduce brain edema, blood-brain barrier breakdown, and seizure activity in animal models of status epilepticus, traumatic brain injury, and intracerebral hemorrhage by blocking thrombin-mediated activation of protease-activated receptor 1 (PAR1).

Brand names
Pefabloc TH
Other names
alpha-NAPAPN-alpha-(2-naphthalenesulfonylglycyl)-4-amidino-D,L-phenylalaninepiperidideN-alpha-(2-naphthalenesulfonylglycyl)-4-amidino-DL-phenylalaninepiperidideNAPAPNα-(2-naphthalenesulfonylglycyl)-4-amidino-D,L-phenylalaninepiperidideNα-(2-naphthalenesulfonylglycyl)-4-amidino-DL-phenylalaninepiperidideThrombstopThromstop
02

Targets

F2 (Thrombin)

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