Angiotensin (1-7)
Overview
Angiotensin (1-7) is a seven-amino acid peptide component of the renin-angiotensin system formed through cleavage of angiotensin II by ACE2 or from angiotensin I by endopeptidases. It binds to the Mas receptor to produce vasodilation, anti-proliferative, anti-fibrotic, and anti-inflammatory effects that generally oppose the actions of angiotensin II. This counter-regulatory arm of the renin-angiotensin system represents a therapeutic target in hypertension, heart failure, and renal disease.
Key Research Findings
Preclinical studies have demonstrated that angiotensin (1-7) reduces blood pressure, attenuates cardiac remodeling, and improves endothelial function in animal models of cardiovascular disease. Clinical development has been limited by the peptide's short half-life, though modified analogues and oral formulations are under investigation without published phase 3 trial results.
Subcutaneous injection, Intravenous, Oral
Investigational
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Eptifibatide (Integrilin)
FDA ApprovedA synthetic cyclic heptapeptide modeled after the KGD (Lys-Gly-Asp) disintegrin sequence found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarius barbouri). Eptifibatide is a potent, reversible glycoprotein IIb/IIIa receptor antagonist that blocks the final common pathway of platelet aggregation by preventing fibrinogen and von Willebrand factor binding to activated platelets.
Nesiritide (Natrecor)
FDA ApprovedA recombinant form of human B-type natriuretic peptide (BNP), a 32-amino acid peptide naturally produced by ventricular cardiomyocytes in response to volume overload and wall stress. Nesiritide binds natriuretic peptide receptor A (NPR-A), activating guanylyl cyclase and increasing intracellular cGMP to produce venous, arterial, and coronary vasodilation, natriuresis, and suppression of the renin-angiotensin-aldosterone and sympathetic nervous systems.
Angiotensin II (Giapreza)
FDA ApprovedA synthetic form of the endogenous octapeptide angiotensin II, the primary effector of the renin-angiotensin system. Angiotensin II acts on AT1 receptors on vascular smooth muscle to produce potent vasoconstriction, and on the adrenal cortex to stimulate aldosterone release. Exogenous administration raises blood pressure in vasodilatory shock refractory to conventional vasopressors by restoring vascular tone through a mechanism complementary to catecholamine vasopressors.
Serelaxin (Relaxin-2)
InvestigationalSerelaxin is a recombinant form of human relaxin-2, a naturally occurring peptide hormone composed of two chains linked by disulfide bonds. It acts via the relaxin family peptide receptor 1 (RXFP1) to promote vasodilation, inhibit fibrosis, and modulate hemodynamics. The therapeutic rationale targets acute heart failure by improving renal perfusion and reducing vascular resistance.