Angiotensin 1-7

Summary

Angiotensin 1-7 (Ang-(1-7)) is an endogenous heptapeptide of the renin-angiotensin system that counterbalances the classical Angiotensin II/AT1R axis via Mas receptor activation. It promotes vasodilation, reduces oxidative stress and inflammation, improves insulin sensitivity, and has cardioprotective and renoprotective properties. It is under active clinical investigation for conditions including heart failure, COVID-19-related lung injury, cancer, and metabolic disorders.

Mechanism of Action

Endogenous heptapeptide formed primarily by ACE2-mediated cleavage of Angiotensin II (or by neprilysin/ACE2 from Angiotensin I). Acts as an agonist at the Mas receptor (MasR/MAS1), producing vasodilation, anti-inflammatory, anti-fibrotic, and anti-proliferative effects that generally oppose the vasoconstrictive and pro-fibrotic actions of Angiotensin II. Also interacts with AT2 receptors and bradykinin B2 receptors.

Routes of Administration

Goals & Uses

• COVID-19 / Acute Lung InjuryPulmonary / Infectious DiseaseModerate
• Anti-cancer / Tumor SuppressionOncologyLow
• Renoprotection / Chronic Kidney DiseaseRenalModerate
• Hematopoietic RecoveryHematologyModerate
• Metabolic / Insulin SensitizationMetabolicLow
• Cardioprotection / Heart failureCardiovascularModerate

Contraindications

• PregnancyPopulationHighPotential fetal risk or insufficient safety data
• Hypersensitivity to Angiotensin 1-7 or excipientsAllergy / ImmunologicHigh
• Severe hypotensionCardiovascularHigh

Adverse Effects

• Injection site reactionsLocalCommon
• HypotensionCardiovascularUncommonLow blood pressure
• FlushingVascularUncommonWarmth and redness of the skin
• BradycardiaCardiovascularRare

Drug Interactions

• Antihypertensive agentsModerate
• Angiotensin II Receptor Blockers (ARBs, e.g., losartan)Moderate
• NSAIDsLowMay increase renal risk in susceptible patients
• ACE Inhibitors (e.g., enalapril, lisinopril)Moderate

Population Constraints

• Patients with baseline hypotensionCardiovascularRelative
• Severe renal impairmentOrgan ImpairmentRelative
• Pediatric patientsAgeRelative
• Pregnant womenReproductiveRelative

Regulatory Status

• European UnionInvestigationalClinical trials registered and ongoing; not approved for any indication by EMA.
• United StatesInvestigationalMultiple IND applications filed; Phase I/II trials conducted for COVID-19, myelosuppression, and cardiovascular indications. TXA127 (cyclic form) received Orphan Drug Designation for sickle cell disease.
• United KingdomInvestigationalNo MHRA approval; research and clinical trial context only.

Not approved by FDA, EMA, or other major regulatory bodies for any indication. Multiple clinical trials (Phase I/II) are ongoing or completed. Cyclic forms and analogs (e.g., cyclic Ang-(1-7), TXA127) are being developed to improve bioavailability and half-life.

Evidence & Sources

No sources recorded yet.