BM121307

BM121307 is a guanylate cyclase activator that was in phase I development for the treatment of ischaemic heart disorders. The research has been discontinued.

Signaling Pathways >> GPCR/G Protein >> Guanylate Cyclase

Research Areas >> Cardiovascular Disease

The elimination of BM121307 and its metabolites via urine and feces amount to 76.5% after oral application, and to 80.7% of the applied dose after intravenous application. The major amount of radioactivity is eliminated via urine (69.4% and 73.6% of the dose, respectively), whereas the fecal elimination is found to be negligible. Investigations of the urinary samples show that the drug is metabolized to a high percentage trans-N-(4-Hydroxycyclohexyl) acetamide is the main metabolite; 73% of the radioactive compounds (after p.o.-administration and 69% after intravenous application could be identified as the alcohol of BM121307; the amounts of the drug totaled 9% and 13%, respectively[1].

Dogs[1] The biotransformation of BM121307 in the dog is examined after oral and intravenous administration. For that purpose, the organic nitrate is synthesized as radioactive [14C]- and as [13C]-labeled compounds. The defined isotopic mixture is administered to the dogs. Within the examined period of 168 h, the elimination of BM121307 is measured[1].

[1]. Zell C, et al. Biotransformation of the organic nitrate trans-N-(4-nitroxycyclohexyl)acetamide in dogs. Arzneimittelforschung. 1994 Sep;44(9):1021-8.

Lificiguat | Linaclotide | Cinaciguat | BAY 41-2272 | Vericiguat | Nelociguat