RAAS-Acting Peptides
13 compounds in this family, each with its recorded mechanism, routes of administration, safety notes and references to published literature.
- AclerastideAclerastide (also known as DSC127, C21, or NorLeu3‑angiotensin (1‑7)) is an investigational peptide analogue of the renin‑angiotensin system being evaluated for the treatment of diabetic foot ulcers. Early pre‑clinical work suggested it could speed wound closure, and it entered Phase III trials as a topical agent, although later data indicated a lack of efficacy.
- Angiotensin 1-7Angiotensin‑(1‑7) is a heptapeptide fragment of the renin‑angiotensin system that belongs to the alternative, protective arm of the pathway. It is generated primarily by ACE2‑mediated cleavage of angiotensin II and acts through the Mas receptor to oppose many actions of the classical Ang II‑AT1 axis. Research is exploring its role in blood‑pressure regulation, vascular remodeling, and organ protection, but it remains an investigational compound without approved therapeutic indications.
- Angiotensin IIAngiotensin II (Giapreza) is a synthetic human angiotensin II approved for vasodilatory shock. It acts on AT1 receptors to produce potent vasoconstriction, raising mean arterial pressure in catecholamine-refractory septic or other distributive shock states.
- AngiotensinamideAngiotensinamide is a synthetic peptide analogue of angiotensin II, studied primarily in laboratory settings. It acts as an agonist at angiotensin receptors, producing vasoconstriction, blood‑pressure elevation, and a strong thirst‑stimulating (dipsogenic) response in animal models. Research has examined its pharmacology, structure‑activity relationships, and, more recently, its potential as a scaffold for SARS‑CoV‑2 main protease inhibition.
- DitekirenDitekiren (also known as Ro 42‑5892) is a synthetic pseudo‑hexapeptide that acts as a potent inhibitor of renin, the enzyme that initiates the renin‑angiotensin system. Developed as a research‑stage antihypertensive agent, it has been evaluated in animal models and in early human studies, but it has not received regulatory approval for clinical use.
- EnalaprilEnalapril is a prescription ACE‑inhibitor prodrug used to lower blood pressure and improve outcomes in heart failure with reduced ejection fraction. It is administered orally or intravenously, and after conversion to the active metabolite enalaprilat it blocks the angiotensin‑converting enzyme, reducing vasoconstriction and aldosterone‑mediated fluid retention. Clinical research includes heart‑failure survival trials and a postpartum hypertension review, where it was compared with other antihypertensives.
- EnalaprilatEnalaprilat is the active, intravenously administered dipeptide metabolite of the oral ACE inhibitor enalapril. It belongs to the RAAS‑acting peptide family and is approved for use in hypertensive emergencies, acute heart‑failure states, and as an after‑load reducer in critical care. The compound is delivered by IV infusion and is employed when rapid blood‑pressure control is required, especially in patients at risk of cerebral hypoperfusion.
- EnalkirenEnalkiren is a synthetic dipeptide that directly inhibits renin, the enzyme that initiates the renin‑angiotensin‑aldosterone system. Developed as a research‑only agent, it has been investigated intravenously in healthy volunteers, hypertensive patients, and those with congestive heart failure. The compound lowers plasma renin activity and angiotensin II, producing dose‑dependent reductions in systolic and diastolic blood pressure that persist for many hours after infusion.
- LisinoprilLisinopril is an orally administered, prescription‑only angiotensin‑converting‑enzyme (ACE) inhibitor approved for the treatment of hypertension, chronic heart failure, and post‑myocardial‑infarction care. By blocking ACE, it diminishes angiotensin II production, leading to vasodilation and reduced blood‑volume retention. It is a widely used member of the RAAS‑acting peptide family and is taken once daily.
- N-(1-carboxy-3-phenylpropyl)phenylalanyl-alpha-asparagineEnalapril diacid is the active diacid form of the ACE‑inhibitor enalapril. It belongs to the RAAS‑acting peptide family and is prescribed to lower elevated blood pressure by blocking the conversion of angiotensin I to the vasoconstrictor angiotensin II. The compound can be given intravenously or taken orally.
- SaralasinSaralasin is a synthetic peptide that blocks the angiotensin II type 1 (AT1) receptor. Developed as an intravenous agent, it was investigated for acute blood‑pressure reduction in essential hypertension and for haemodynamic improvement in congestive heart failure. Although it demonstrated efficacy in early clinical studies, the compound was later withdrawn and is now used only as a research tool to probe the renin‑angiotensin system.
- SpiraprilSpirapril is an orally administered, pro‑drug angiotensin‑converting enzyme (ACE) inhibitor approved for the treatment of mild‑to‑moderate essential hypertension. After ingestion it is converted to the active metabolite spiraprilat, which lowers blood pressure by reducing angiotensin II formation. Clinical studies have shown it provides roughly 10 mmHg reductions in diastolic pressure and is comparable to other ACE inhibitors such as enalapril.
- TerlakirenTerlakiren is a synthetic peptidomimetic that was developed as an oral renin inhibitor for hypertension. Early pre‑clinical work showed it could be absorbed when taken by mouth and lower blood pressure in several animal species. The compound was later withdrawn from development and has not been approved for any therapeutic use. Recent computational screens have also highlighted it as a potential inhibitor of the SARS‑CoV‑2 main protease, although no laboratory confirmation exists.