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Chemical Compound Review

Monopril     (2S,4R)-4-cyclohexyl-1-[2- [(2-methyl-1...

Synonyms: Acecor, Fosenopril, Staril, fosinopril, Monopril (TN), ...
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Disease relevance of fosinopril


High impact information on fosinopril


Chemical compound and disease context of fosinopril


Biological context of fosinopril


Anatomical context of fosinopril

  • In addition, fosinopril inhibited CuSO4-induced oxidation of LDL that was obtained from the aortas of the treated mice, as shown by an 18% and 37% reduction in the LDL content of lipid peroxides and hydroperoxy-cholesterol linoleate, respectively, compared with the placebo-treated mice (P < 0.01) [14].
  • In the present study, we extended our investigations into mechanisms of cytotoxicity, using rat hepatocyte cultures, to captopril and three recently marketed ACEIs: fosinopril, lisinopril and quinapril [11].
  • Compared with controls, fosinopril reduced the number of intimal macrophage-foam cells/mm2, foam cell size and the fatty streak area by 85%, 38% and 90%, respectively [15].
  • It is concluded that skeletal muscle vascular responsiveness to sympathetic nervous activity is unchanged after exercise or during ACE inhibition with fosinopril [16].
  • The objective of this study was to delineate the transepithelial transport mechanisms of fosinopril in cultured cell lines expressing the intestinal and renal peptide transporters [17].

Associations of fosinopril with other chemical compounds


Gene context of fosinopril

  • Only one ACE inhibitor, fosinopril, has been shown to be effective in normalizing ET-1 levels in clinically relevant situations, such as the long-term study of patients with CHF [22].
  • The aim of this study is to investigate the effect of low doses of fosinopril, a converting enzyme inhibitor, on the development of atherosclerosis in LDL-receptor-deficient mice [23].
  • Finally, fosinopril downregulated STAT3 activation and ED-1 influx, which are effects that may attenuate renal damage in this model [24].
  • Fosinopril decreases levels of soluble vascular cell adhesion molecule-1 in borderline hypertensive type II diabetic patients with microalbuminuria [25].
  • Taken as a whole, our findings demonstrate that fosinopril is transported intact by PEPT2 and PEPT1, with high-affinity and by a proton-coupled, saturable process [17].

Analytical, diagnostic and therapeutic context of fosinopril

  • DESIGN: A randomized, placebo-controlled, double-blind study of 12 weeks, followed by 23 weeks of an open-label trial using fosinopril [26].
  • Restenosis rates according to the National Heart, Lung, and Blood Institute criterion 4 (loss of > or = 50% of the initial gain [primary end point]) were 45.7% and 40.7% in the fosinopril and control groups, respectively (not significant) [2].
  • CONCLUSIONS: Administration of fosinopril in a dose of 40 mg daily during 6 months after PTCA does not prevent restenosis and has no effect on overall clinical outcome [2].
  • The in vivo selective inhibitory potency of single oral doses of 10 mg omapatrilat and 20 mg fosinopril were investigated in a double-blind, placebo-controlled, cross-over study in 9 mildly sodium-depleted normotensive subjects [27].
  • Fosinopril was well tolerated in clinical trials in patients with heart failure [28].


  1. Angiotensin-converting enzyme inhibition prolongs survival and modifies the transition to heart failure in rats with pressure overload hypertrophy due to ascending aortic stenosis. Weinberg, E.O., Schoen, F.J., George, D., Kagaya, Y., Douglas, P.S., Litwin, S.E., Schunkert, H., Benedict, C.R., Lorell, B.H. Circulation (1994) [Pubmed]
  2. Angiotensin-converting enzyme inhibition with fosinopril sodium in the prevention of restenosis after coronary angioplasty. Desmet, W., Vrolix, M., De Scheerder, I., Van Lierde, J., Willems, J.L., Piessens, J. Circulation (1994) [Pubmed]
  3. Long-term angiotensin-converting enzyme inhibition with fosinopril improves depressed responsiveness to Ca2+ in myocytes from aortic-banded rats. Kagaya, Y., Hajjar, R.J., Gwathmey, J.K., Barry, W.H., Lorell, B.H. Circulation (1996) [Pubmed]
  4. Angiotensin-converting enzyme inhibition and the progression of congestive cardiomyopathy. Effects on left ventricular and myocyte structure and function. Spinale, F.G., Holzgrefe, H.H., Mukherjee, R., Hird, R.B., Walker, J.D., Arnim-Barker, A., Powell, J.R., Koster, W.H. Circulation (1995) [Pubmed]
  5. Immediate and short-term cardiovascular effects of fosinopril, a new angiotensin-converting enzyme inhibitor, in patients with essential hypertension. Oren, S., Messerli, F.H., Grossman, E., Garavaglia, G.E., Frohlich, E.D. J. Am. Coll. Cardiol. (1991) [Pubmed]
  6. Inhibition of angiotensin type 1 receptor prevents decline of glucose transporter (GLUT4) in diabetic rat heart. Hoenack, C., Roesen, P. Diabetes (1996) [Pubmed]
  7. Vasopeptidase inhibition attenuates the progression of renal injury in subtotal nephrectomized rats. Cao, Z., Burrell, L.M., Tikkanen, I., Bonnet, F., Cooper, M.E., Gilbert, R.E. Kidney Int. (2001) [Pubmed]
  8. Comparison of the steady-state pharmacokinetics of fosinopril, lisinopril and enalapril in patients with chronic renal insufficiency. Sica, D.A., Cutler, R.E., Parmer, R.J., Ford, N.F. Clinical pharmacokinetics. (1991) [Pubmed]
  9. Additive antiproteinuric effect of combined ACE inhibition and angiotensin II receptor blockade. Ferrari, P., Marti, H.P., Pfister, M., Frey, F.J. J. Hypertens. (2002) [Pubmed]
  10. Role of angiotensin II in hyperinsulinemia-induced hypertension in rats. Fang, T.C., Huang, W.C. J. Hypertens. (1998) [Pubmed]
  11. Comparative cytotoxicity of angiotensin-converting enzyme inhibitors in cultured rat hepatocytes. Jurima-Romet, M., Huang, H.S. Biochem. Pharmacol. (1993) [Pubmed]
  12. Pharmacokinetics of fosinopril. Shahinfar, S., Shaw, W.C. Clin. Pharmacol. Ther. (1992) [Pubmed]
  13. Fosinopril attenuates clinical deterioration and improves exercise tolerance in patients with heart failure. Fosinopril Efficacy/Safety Trial (FEST) Study Group. Erhardt, L., MacLean, A., Ilgenfritz, J., Gelperin, K., Blumenthal, M. Eur. Heart J. (1995) [Pubmed]
  14. The angiotensin-converting enzyme inhibitor, fosinopril, and the angiotensin II receptor antagonist, losartan, inhibit LDL oxidation and attenuate atherosclerosis independent of lowering blood pressure in apolipoprotein E deficient mice. Hayek, T., Attias, J., Coleman, R., Brodsky, S., Smith, J., Breslow, J.L., Keidar, S. Cardiovasc. Res. (1999) [Pubmed]
  15. Inhibitors of angiotensin converting enzyme decrease early atherosclerosis in hyperlipidemic hamsters. Fosinopril reduces plasma cholesterol and captopril inhibits macrophage-foam cell accumulation independently of blood pressure and plasma lipids. Kowala, M.C., Grove, R.I., Aberg, G. Atherosclerosis (1994) [Pubmed]
  16. Unchanged neurogenic vasoconstrictor response after exercise during angiotensin converting enzyme inhibition with fosinopril. Beaulieu, M., Lacourcière, Y., Cléroux, J. Am. J. Hypertens. (1994) [Pubmed]
  17. Mechanism of intestinal absorption and renal reabsorption of an orally active ace inhibitor: uptake and transport of fosinopril in cell cultures. Shu, C., Shen, H., Hopfer, U., Smith, D.E. Drug Metab. Dispos. (2001) [Pubmed]
  18. Physiologic consequences of vasopeptidase inhibition in humans: effect of sodium intake. Azizi, M., Lamarre-Cliche, M., Labatide-Alanore, A., Bissery, A., Guyene, T.T., Ménard, J. J. Am. Soc. Nephrol. (2002) [Pubmed]
  19. Different effects of fosinopril and atenolol on wave reflections in hypertensive patients. Chen, C.H., Ting, C.T., Lin, S.J., Hsu, T.L., Yin, F.C., Siu, C.O., Chou, P., Wang, S.P., Chang, M.S. Hypertension (1995) [Pubmed]
  20. Combination of fosinopril and pravastatin decreases platelet response to thrombin receptor agonist in monkeys. Hale, L.P., Craver, K.T., Berrier, A.M., Sheffield, M.V., Case, L.D., Owen, J. Arterioscler. Thromb. Vasc. Biol. (1998) [Pubmed]
  21. Angiotensin converting enzyme inhibition improves cardiac neuronal uptake of noradrenaline in spontaneously hypertensive rats. Raasch, W., Betge, S., Dendorfer, A., Bartels, T., Dominiak, P. J. Hypertens. (2001) [Pubmed]
  22. Neurohormonal markers of clinical outcome in cardiovascular disease: is endothelin the best one? Monge, J.C. J. Cardiovasc. Pharmacol. (1998) [Pubmed]
  23. The effect of renin-angiotensin axis inhibition on early atherogenesis in LDL-receptor-deficient mice. Sharabi, Y., Grossman, E., Sherer, Y., Shaish, A., Levkovitz, H., Bitzur, R., Harats, D. Pathobiology (2000) [Pubmed]
  24. Expression and activation of STAT3 in chronic proliferative immune complex glomerulonephritis and the effect of fosinopril. Zhang, W., Chen, X., Shi, S., Wei, R., Wang, J., Yamanaka, N., Hong, Q. Nephrol. Dial. Transplant. (2005) [Pubmed]
  25. Fosinopril decreases levels of soluble vascular cell adhesion molecule-1 in borderline hypertensive type II diabetic patients with microalbuminuria. Gasic, S., Wagner, O.F., Fasching, P., Ludwig, C., Veitl, M., Kapiotis, S., Jilma, B. Am. J. Hypertens. (1999) [Pubmed]
  26. Improvement of lipid abnormalities associated with proteinuria using fosinopril, an angiotensin-converting enzyme inhibitor. Keilani, T., Schlueter, W.A., Levin, M.L., Batlle, D.C. Ann. Intern. Med. (1993) [Pubmed]
  27. In vitro and in vivo inhibition of the 2 active sites of ACE by omapatrilat, a vasopeptidase inhibitor. Azizi, M., Massien, C., Michaud, A., Corvol, P. Hypertension (2000) [Pubmed]
  28. Fosinopril. A review of its pharmacology and clinical efficacy in the management of heart failure. Davis, R., Coukell, A., McTavish, D. Drugs (1997) [Pubmed]
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