Carperitide

Description

Carperitide is the α-human atrial natriuretic peptide (α-hANP) produced by recombinant technology. It was introduced in Japan as a treatment for acute congestive heart failure (CHF). In dogs with CHF, carperitide significantly reduced the elevated left ventricular end-diastolic pressure and the index of myocardial oxygen consumption (systolic blood pressure x heart rate). In a clinical trial, carperitide was effective in improving hemodynamics and symptoms in 60% of patients with acute CHF. Carperitide was reported to be well tolerated with no significant adverse effects clinically. A beneficial effect on hemodynamics has been reported in chronic heart failure patients. Carperitide is also in clinical trials for maintenance of blood pressure during surgical operations.

Description

Atrial natriuretic peptide (ANP) is an endogenous peptide generated by proteolysis of prepro-ANP that is secreted by cardiomyocytes in the heart. It has effects on the renal and cardiovascular systems that decrease vasoconstriction, inhibit renin secretion, and increase sodium excretion. Human ANP binds to ANP receptors on cultured vascular smooth muscle cells (VSMCs) with a K_d value of approximately 1-2 nM and increases cGMP levels in a dose-dependent manner. It relaxes potassium-induced contraction of isolated canine renal arterial strips when used at concentrations of 10 and 100 ng/ml and dilates renal arteries in anesthetized dogs when used at doses ranging from 10 to 100 ng/kg. In a rat model of heart failure following experimental autoimmune myocarditis, human ANP, via osmotic mini pump for 28 days, decreases cardiomyocyte size as well as the amount of cardiac fibrosis and left ventricular remodeling. ANP (1-28) (human) is a 28 amino acid peptide corresponding to the human protein sequence.

Originator

Suntory (Japan)

Uses

Treatment of decompensated congestive heart failure.

Definition

ChEBI: Carperitide is a polypeptide.

brand name

Daiichi Suntory, Japan.

References

[1] T.GEOFFREY FLYNN  Adolfo J de B  Mercedes L de Bold. The amino acid sequence of an atrial peptide with potent diuretic and natriuretic properties[J]. Biochemical and biophysical research communications, 1983, 117 3: Pages 859-865. DOI: 10.1016/0006-291x(83)91675-3
[2] MAACK T. Role of atrial natriuretic factor in volume control[J]. Kidney international, 1996, 49 6: Pages 1732-1737. DOI: 10.1038/ki.1996.257
[3] YUKIO HIRATA. Specific receptors for atrial natriuretic factor (ANF) in cultured vascular smooth muscle cells of rat aorta[J]. Biochemical and biophysical research communications, 1984, 125 2: Pages 562-568. DOI: 10.1016/0006-291x(84)90576-x
[4] T. ISHIHARA. Vasodilatory and diuretic actions of α-human atrial natriuretic polypeptide (α-hANP)[J]. Life sciences, 1985, 36 12: Pages 1205-1215. DOI: 10.1016/0024-3205(85)90239-5
[5] KOMEI TANAKA. Long-term carperitide treatment attenuates left ventricular remodeling in rats with heart failure after autoimmune myocarditis.[J]. Journal of Cardiovascular Pharmacology, 2009: 232-239. DOI: 10.1097/fjc.0b013e3181b0cf50