DIQTA 1.0: Drug-Induced QT Prolongation Atlas

TOLVAPTAN

Classification:Ambiguous

Severity Score:1.0

CLINICAL PHARMACOLOGY
Pharmacodynamics
In a parallel-arm, double-blind (for tolvaptan and placebo), placebo- and positive-controlled, multiple dose study of the effect of tolvaptan on the QTc interval, 172 healthy subjects were randomized to tolvaptan 30 mg, tolvaptan 300 mg, placebo, or moxifloxacin 400 mg once daily. At both the 30 mg and 300 mg doses, no significant effect of administering tolvaptan on the QTc interval was detected on Day 1 and Day 5. At the 300 mg dose, peak tolvaptan plasma concentrations were approximately 4-fold higher than the peak concentrations following a 30 mg dose. Moxifloxacin increased the QT interval by 12 ms at 2 hours after dosing on Day 1 and 17 ms at 1 hour after dosing on Day 5, indicating that the study was adequately designed and conducted to detect tolvaptan’s effect on the QT interval, had an effect been present.

Current Drug

Other Drugs

QT Prolongation

24088

Other ADRs

18229

38363358

Odds Ratio = 0.35

ATC Code(s):

Active Ingredient:TOLVAPTAN

Active Ingredient UNII:21G72T1950

Drugbank ID:DB06212

PubChem Compound:443894

PharmGKB:

CAS Number:150683-30-0

Dosage Form(s):tablet

Route(s) Of Administrator:oral

Daily Dose:

Chemical Structure:

SMILE Code:
CC1=CC=CC=C1C(=O)NC1=CC(C)=C(C=C1)C(=O)N1CCC[C@@H](O)C2=C1C=CC(Cl)=C2

[Diezi Léonore,Renard Delphine,Rothuizen Laura E,Livio Françoise]
Rev Med Suisse,2014 Jan 15;10(412-413):119-22. PMID: 24558915