Drug intelligence / Profile preview

terlipressin

Development stage
Approved
Lead developer
Mallinckrodt
Modality
Peptides, Small Molecules
Administration
Intravenous
01

Overview

Terlipressin is a synthetic peptide analog of vasopressin with high selectivity for the vasopressin V1 receptor. After intravenous administration, it is enzymatically cleaved to release lysine vasopressin slowly, resulting in prolonged activity. Terlipressin acts primarily as a potent vasoconstrictor on vascular smooth muscle cells via V1 receptors, leading to reduced portal venous pressure and decreased splanchnic blood flow. It is used mainly for the treatment of complications related to portal hypertension (such as acute variceal bleeding) and hepatorenal syndrome (HRS), particularly type 1 HRS in patients with advanced liver disease. The drug improves renal function by reversing renal hypoperfusion and has been shown to increase mean arterial pressure and urine output while reducing serum creatinine levels[2][5][7]. Originally developed by Ferring Pharmaceuticals, terlipressin has been approved in many countries since 1981; Mallinckrodt received FDA approval for its use in the United States under the brand name Terlivaz for improving kidney function in adults with HRS[3].

Brand names
GlypressinTerlivaz可利新
Other names
特利加压素N-α-三甘氨酰-8-赖氨酸-加压素
02

Targets

AVPR1A (Arginine vasopressin receptor 1A)

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