Endothelin and Vasoactive Peptides
9 compounds in this family, each with its recorded mechanism, routes of administration, safety notes and references to published literature.
- AviptadilAviptadil is a synthetic analogue of vasoactive intestinal peptide (VIP) developed as an investigational drug. It has been explored for several pulmonary and vascular conditions, including pulmonary arterial hypertension, acute respiratory distress syndrome (ARDS), and COVID‑19‑related hypoxaemic respiratory failure, as well as in early studies for erectile dysfunction. The compound is administered by inhalation, intravenous infusion, or subcutaneous injection, but it remains unapproved for any indication.
- BQ-123BQ-123 is a cyclic pentapeptide that selectively blocks endothelin‑A (ET_A) receptors. It is used primarily as a research tool to probe the role of endothelin‑1 in vascular tone, cardiac remodeling, and pregnancy‑related hypertension. The compound is administered intravenously or intracoronarily in experimental settings and has not received regulatory approval for therapeutic use.
- BQ-788BQ-788 is a synthetic peptide that selectively blocks endothelin‑B (ET_B) receptors. It is employed as a research tool to dissect the role of ET_B‑mediated signalling in vascular tone, bronchoconstriction, cell growth and inflammation. The compound is not approved for therapeutic use and is administered intravenously or by other experimental routes in animal and human studies.
- BradykininBradykinin is a nine‑amino‑acid vasoactive peptide that modulates blood‑vessel tone, renal function and inflammatory responses. In humans it is generated from high‑molecular‑weight kininogen and acts primarily through G‑protein‑coupled B1 and B2 receptors, producing vasodilation, increased vascular permeability and pain. Excessive bradykinin activity underlies several forms of angioedema, especially hereditary angioedema (HAE) and ACE‑inhibitor‑induced swelling.
- Endothelin-1Endothelin‑1 (ET‑1) is a 21‑amino‑acid vasoactive peptide that acts as a powerful vasoconstrictor and bronchoconstrictor. It is investigated in research settings for its role in ocular diseases such as diabetic retinopathy and glaucoma, in migraine pathophysiology, and in airway hyper‑reactivity. Elevated circulating or ocular ET‑1 levels have been reported in several clinical conditions, prompting interest in its use as a biomarker or therapeutic target, although no approved drug formulations exist.
- IcatibantIcatibant (brand name Firazyr) is a synthetic peptide that blocks the bradykinin B2 receptor. It is prescribed for acute attacks of bradykinin‑mediated angioedema, including hereditary angioedema (HAE), acquired angioedema, and angioedema linked to ACE‑inhibitor therapy. By preventing bradykinin from binding its receptor, icatibant reduces the swelling that can threaten the airway and cause painful facial or intestinal edema.
- LabradimilLabradimil is an investigational nine‑amino‑acid peptide that acts as a selective agonist of the bradykinin B2 receptor. It is being studied as a blood‑brain barrier (BBB) modulator that transiently opens tight junctions to improve delivery of co‑administered drugs, particularly chemotherapeutics, into malignant brain tumours.
- OlcegepantOlcegepant is an investigational small‑molecule peptide‑mimetic that blocks the calcitonin gene‑related peptide (CGRP) receptor. Developed for acute migraine treatment, it is administered intravenously in research settings. Early clinical trials and a network meta‑analysis have shown it to be highly effective at relieving migraine pain within two hours, positioning it among the most potent CGRP antagonists studied to date.
- SovateltideSovateltide (Tycamzzi™) is a synthetic peptide that selectively activates endothelin‑B (ET_B) receptors. It is approved in India for the treatment of acute cerebral ischemic stroke when administered within 24 hours of symptom onset. The drug is given intravenously and is intended to improve neurological recovery after stroke.