What it is
Terlipressin is a twelve-amino-acid peptide drug built on lysine vasopressin — the version of the water-and-blood-pressure hormone that carries lysine instead of arginine at position 8. The Terlivaz label's chemical name, N-triglycyl-8-lysine-vasopressin, describes it exactly:
- three glycines added to the front;
- the nine-residue vasopressin ring and tail behind them, with a disulfide bond between the two cysteines;
- an amide cap at the end.
It weighs 1,227.38 as the free base. Each Terlivaz vial holds 0.85 mg terlipressin, equal to 1 mg of the acetate salt.
How it works
The label calls terlipressin both a prodrug and a drug. The body clips the three glycines off, releasing lysine vasopressin slowly, but terlipressin also acts on its own. It is about twice as selective for V1 receptors — which tighten blood vessels — as for V2 receptors, which control water handling in the kidney.
In hepatorenal syndrome the kidneys fail because of advanced liver disease rather than kidney damage. The label states terlipressin is thought to increase kidney blood flow by reducing portal hypertension — high pressure in the veins that drain the gut into the liver — and blood circulation in those vessels, while increasing effective arterial volume and mean arterial pressure. The label measured the effect directly: after one dose, mean arterial pressure rose by an estimated maximum of 16.2 mmHg and heart rate fell by 10.6 beats a minute, peaking at 1.2 to 2 hours.
| Measure (label, steady state, 1 mg acetate) | Terlipressin | Lysine vasopressin |
|---|---|---|
| Median peak level | 70.5 ng/mL | 1.2 ng/mL |
| Median 24-hour exposure (AUC) | 123 ng·h/mL | 11.2 ng·h/mL |
What the trial showed
Approval rests on CONFIRM (NCT02770716), a double-blind, placebo-controlled trial in 300 adults with cirrhosis and rapidly worsening hepatorenal syndrome, randomised 2:1. Both groups received albumin.
| Endpoint (label) | Terlipressin (199) | Placebo (101) | p |
|---|---|---|---|
| Verified HRS reversal (primary) | 29.1% | 15.8% | 0.012 |
| HRS reversal | 31.7% | 15.8% | 0.003 |
| Reversal without recurrence by day 30 | 24.1% | 15.8% | 0.092 |
The last row is the one most often left out: the difference in reversal that held for 30 days did not reach statistical significance. Median treatment lasted five days.
Safety
The label carries a boxed warning for serious or fatal respiratory failure, with higher risk in people with fluid overload or grade 3 acute-on-chronic liver failure. It requires oxygen saturation to be checked before the first dose and monitored continuously throughout. In CONFIRM:
| Reaction | Terlipressin (200) | Placebo (99) |
|---|---|---|
| Abdominal pain | 19.5% | 6.1% |
| Nausea | 16.0% | 10.1% |
| Respiratory failure | 15.5% | 7.1% |
| Diarrhoea | 13.0% | 7.1% |
| Ischaemia-related events | 4.5% | 0% |
Treatment was stopped for adverse events in 12.0% on terlipressin and 5.1% on placebo.
Where it stands
Drugs@FDA lists one terlipressin application on 2026-10-02: Terlivaz, NDA 022231, held by Mallinckrodt and approved 2022-09-14, with no generic. PubMed returns 1,396 records, 145 tagged as randomised controlled trials. It is a hospital drug given as an intravenous injection; the label sets dose changes by the day-4 creatinine result and caps treatment at 14 days.
Related reading
Terlipressin is the third vasopressin-family molecule in this library, after the hormone vasopressin and the kidney-targeted copy desmopressin. The library's sibling hormone oxytocin differs from vasopressin at two positions.