Source: FDA label
| Molecular formula | C52H74N16O15S2 |
|---|---|
| Molecular weight | 1227.4 g/mol |
| Registered trials | 130 |
| PubChem CID | 72081 |
| Drug class | Vasopressin Receptor Agonist [EPC] |
| Brand names | Terlivaz |
Boxed warning: The FDA label for this compound includes a boxed warning, the FDA's strongest safety warning. See the full prescribing information for details.
Mechanism of Action
12.1 Mechanism of Action Terlipressin is a synthetic vasopressin analogue with twice the selectivity for vasopressin V 1 receptors versus V 2 receptors. Terlipressin acts as both a prodrug for lysine-vasopressin, as well as having pharmacologic activity on its own. Terlipressin is thought to increase renal blood flow in patients with hepatorenal syndrome by reducing portal hypertension and blood circulation in portal vessels and increasing effective arterial volume and mean arterial pressure (MA
Key takeaways
- Terlipressin, sold as Terlivaz, is FDA-approved to improve kidney function in adults with hepatorenal syndrome with rapid kidney decline.
- It carries a boxed warning.
- It works as a vasopressin V1 receptor agonist, narrowing portal blood vessels and raising arterial pressure.
- More than 130 clinical trials have studied terlipressin, including head-to-head comparisons with other vasopressor therapies.
- The most frequently reported issue in adverse event data is treatment not working as intended, followed by ascites and kidney related complications.
What terlipressin is
Terlipressin is a synthetic analogue of vasopressin, a hormone the body uses to regulate blood vessel tone. It has about twice the selectivity for V1 receptors compared to V2 receptors. It acts both as a direct agonist and as a prodrug that converts into lysine-vasopressin in the body. This dual action is believed to increase blood flow to the kidneys by reducing pressure in the portal vein and raising mean arterial pressure.
What terlipressin is approved for
Under the brand name Terlivaz, terlipressin is approved to improve kidney function in adults with hepatorenal syndrome accompanied by a rapid drop in kidney function. The label notes that patients with a serum creatinine above 5 mg/dL are unlikely to see benefit from treatment. Terlipressin carries a boxed warning, meaning the FDA requires prominent safety information on the label.
What the evidence shows
Terlipressin has been studied in more than 130 registered clinical trials. A completed Phase 3 trial compared terlipressin against noradrenaline for hepatorenal syndrome. A separate Phase 2/3 trial comparing terlipressin plus albumin against midodrine plus octreotide for the same condition was terminated before completion. Newer trials continue to examine terlipressin's effects on portal pressure, including one currently recruiting patients undergoing liver transplantation.
Reported side effects
Adverse event reports for terlipressin are led by cases where the drug was described as ineffective (40 reports), followed by ascites (21) and renal impairment (19). Cardiac and systemic concerns also appear, including QT prolongation on electrocardiogram (17) and multiple organ dysfunction syndrome (17), alongside diarrhoea (16). A number of reports also flag off-label use or use in an unapproved indication (17 each). These figures reflect the number of reports submitted, not confirmed rates or proof that terlipressin caused the event.
FAQ
What is terlipressin used for?
Terlipressin, marketed as Terlivaz, is approved to improve kidney function in adults with hepatorenal syndrome who have a rapid decline in kidney function. It is not expected to help patients whose serum creatinine is already above 5 mg/dL.
How does terlipressin work?
Terlipressin is a synthetic version of vasopressin that preferentially activates V1 receptors over V2 receptors. This narrows blood vessels in the portal circulation and raises arterial pressure, which is thought to improve blood flow to the kidneys.
Does terlipressin have a boxed warning?
Yes, terlipressin's FDA label includes a boxed warning, which highlights safety information the agency considers especially important for prescribers and patients to know.
What are the most commonly reported side effects of terlipressin?
Adverse event reports most often describe the drug being ineffective, along with ascites, renal impairment, QT prolongation, and diarrhoea. These are counts of submitted reports, not confirmed side effect rates, so they do not prove terlipressin caused each event.
Has terlipressin been studied in clinical trials?
Yes, terlipressin has been evaluated in more than 130 registered clinical trials. These include completed Phase 3 comparisons with other vasopressor treatments for hepatorenal syndrome and ongoing studies in liver transplant settings.
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Content is editorial information, not medical advice. Talk to your doctor before any treatment decision.
Sources: DailyMed label (Terlivaz) ClinicalTrials.gov FDA FAERS PubChem
Updated 2026-08-03