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Description

Terlipressin (Glypressin) is indicated for the treatment of bleeding oesophageal varices and in some countries for the treatment of hepatorenal syndrome type 1. It is a prodrug and is converted to the lysine vasopressin in the circulation after the N-triglycyl residue is cleaved by endothelial peptidases. This results in a ‘slow release’ of the vasoactive lysine vasopressin. Terlipressin exerts its action by activating V1a, V1b and V2 vasopressin receptors. On September 14, 2022, the FDA granted approval to terlipressin (Terlivaz) for the treatment of adults hospitalized with hepatorenal syndrome with rapid reduction in kidney function (HRS-1). Prior to the approval, no approved treatment for this condition existed in the United States.

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
852.0 nM [Ki]
1115.0 nM [Ki]
1580.0 nM [Ki]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
TERLIVAZ
Primary
GLYPRESSIN

Cmax

ValueDoseCo-administeredAnalytePopulation
70.5 ng/mL
1 mg 4 times / day multiple, intravenous
TERLIPRESSIN plasma
Homo sapiens
1.16 ng/mL
1 mg 4 times / day multiple, intravenous
LYPRESSIN plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
123 ng × h/mL
1 mg 4 times / day multiple, intravenous
TERLIPRESSIN plasma
Homo sapiens
11.2 ng × h/mL
1 mg 4 times / day multiple, intravenous
LYPRESSIN plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
0.9 h
1 mg 4 times / day multiple, intravenous
TERLIPRESSIN plasma
Homo sapiens
3 h
1 mg 4 times / day multiple, intravenous
LYPRESSIN plasma
Homo sapiens

Doses

AEs

Drug as perpetrator​

Drug as victim

PubMed

Sample Use Guides

In Vivo Use Guide
Recommended Dosage Regimen: (2.2) • Days 1 to 3 administer TERLIVAZ 0.85 mg (1 vial) intravenously every 6 hours. • Day 4: Assess serum creatinine (SCr) versus baseline. • If SCr has decreased by at least 30% from baseline, continue TERLIVAZ 0.85 mg (1 vial) intravenously every 6 hours. • If SCr has decreased by less than 30% from baseline, dose may be increased to TERLIVAZ 1.7 mg (2 vials) intravenously every 6 hours.
Route of Administration: Intravenous
In Vitro Use Guide
Terlipressin also non-selectively interacted with all the vasopressin receptors but with an affinity reduced by at least 710 folds (Ki in nM: 852 for hV1A-R; 1115 for hV1B-R; and 1580 for hV2-R)
Substance Class Protein
Protein Sub Type
Sequence Type COMPLETE
Record UNII
7Z5X49W53P
Record Status Validated (UNII)
Record Version
Subunit 0