Disease relevance of Fasidotril

• Cardiac hypertrophy was significantly attenuated by fasidotril for the three infarct sizes [1].
• Effect of long-term therapy with fasidotril, a mixed inhibitor of neprilysin and angiotensin-converting enzyme (ACE), on survival of rats after myocardial infarction [1].
• Phase II trials to investigate the potential of fasidotril for the treatment of hypertension and CHF had commenced by the late 1990s, and were ongoing in July 2003 in the US and Europe [2].

High impact information on Fasidotril

• Mixed inhibitors of angiotensin-converting enzyme (EC 3.4.15.1) and enkephalinase (EC 3.4.24.11): rational design, properties, and potential cardiovascular applications of glycopril and alatriopril [3].
• Fasidotril therapy had no significant effects on arterial blood pressure and heart rate [1].
• METHODS: The effects of long-term therapy with fasidotril, a mixed NEP/ACE inhibitor, were assessed in rats submitted to coronary artery ligation [1].
• Plasma renin was increased by 36-fold after captopril but only by 1.6-fold after alatriopril, a difference that presumably reflects the inhibition of renal renin secretion by endogenous ANF after alatriopril [4].
• At a dose of 30 mg/kg p.o., ecadotril, the orally active prodrug of (S)-thiorphan, decreased the systolic blood pressure in conscious TGR by 22 mmHg for 6 h, whereas alatriopril (100 mg/kg p.o.) also reduced the systolic pressure in these rats with a maximal reduction of 22 mmHg [5].

Gene context of Fasidotril

• Fasidotril is a related compound which has special interest as an equipotent dual inhibitor of NEP and ACE (EC 3.4.15.1) [6].

Analytical, diagnostic and therapeutic context of Fasidotril

• Twenty-four hours after ligation, 172 rats were assigned to either placebo or fasidotril therapy (180 mg/kg/day, orally) for 40 weeks [1].

References