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RenalFDA Approved

Terlipressin

Overview

A synthetic vasopressin analog and prodrug that is cleaved by endopeptidases to release lysine-vasopressin. Terlipressin has greater V1a receptor selectivity than vasopressin, producing splanchnic vasoconstriction that reduces portal pressure and redistributes blood flow to the kidneys. This mechanism addresses the pathophysiology of hepatorenal syndrome (HRS) by counteracting the splanchnic vasodilation that drives renal hypoperfusion.

Key Research Findings

FDA-approved in 2022 (Terlivaz) for hepatorenal syndrome type 1. CONFIRM trial demonstrated significant improvement in renal function (verified HRS reversal in 32% vs. 17% with placebo) without the need for renal replacement therapy (Wong et al., NEJM, 2021). Previously approved in Europe and Asia for variceal bleeding and hepatorenal syndrome. Risk of respiratory failure prompted a boxed warning in the FDA label.

Route of Administration

Intravenous

Regulatory Status

FDA Approved

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Related Peptides

Vasopressin (ADH)

FDA Approved

A nine-amino acid cyclic peptide hormone (arginine vasopressin) produced in the hypothalamus and released from the posterior pituitary. Vasopressin acts on V1a receptors (vascular smooth muscle vasoconstriction), V1b receptors (ACTH release from pituitary), and V2 receptors (aquaporin-2 insertion in renal collecting ducts for water reabsorption). It is essential for body water homeostasis and hemodynamic stability.

Desmopressin (DDAVP)

FDA Approved

A synthetic analog of vasopressin with enhanced V2 receptor selectivity and minimal V1a vasopressor activity. Desmopressin has a deaminated cysteine at position 1 and D-arginine at position 8, increasing its antidiuretic potency 10-fold while largely eliminating the hypertensive effects of native vasopressin. Its prolonged half-life of 2-4 hours (vs. 10-20 minutes for vasopressin) allows convenient dosing for chronic conditions.