DIQTA 1.0: Drug-Induced QT Prolongation Atlas

APALUTAMIDE

DIR Classification Postmarketing Surveillance Drug Property Information Reference

DIR Classification

Classification:Ambiguous

Severity Score:1.0

Description in Drug Labeling: View Full Labeling: SPL in DailyMed | PDF

CLINICAL PHARMACOLOGY
Pharmacodynamics
Cardiac Electrophysiology
The effect of apalutamide 240 mg once daily on the QTc interval was assessed in an open-label, uncontrolled, multi-center, single-arm dedicated QT study in 45 patients with CRPC. The maximum mean QTcF change from baseline was 12.4 ms (2-sided 90% upper CI: 16.0 ms). An exposure-QT analysis suggested a concentration-dependent increase in QTcF for apalutamide and its active metabolite.

Postmarketing Surveillance

Contingency Table:

Current Drug

Other Drugs

QT Prolongation

24087

Other ADRs

4551

38377036

Odds Ratio = 1.751

Drug Property Information

ATC Code(s):

L02BB05 - apalutamide

L02BB - Anti-androgens
L02B - HORMONE ANTAGONISTS AND RELATED AGENTS
L02 - ENDOCRINE THERAPY
L - ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Active Ingredient:Apalutamide

Active Ingredient UNII:4T36H88UA7

Drugbank ID:DB11901

PubChem Compound:24872560

CTD ID:C572045

PharmGKB:

CAS Number:956104-40-8

Dosage Form(s):tablet, film coated

Route(s) Of Administrator:oral

Daily Dose:

240.0 mg/day L02BB05

Chemical Structure:

SMILE Code:
CNC(=O)C1=CC=C(C=C1F)N1C(=S)N(C(=O)C11CCC1)C1=CC(=C(N=C1)C#N)C(F)(F)F

Reference

1: An open-label, multicenter, phase Ib study investigating the effect of apalutamide on ventricular repolarization in men with castration-resistant prostate cancer.

[Belderbos Bodine P S I,de Wit Ronald,Chien Caly,Mitselos Anna,Hellemans Peter,Jiao James,Yu Margaret K,Attard Gerhardt,Bulat Iurie,Edenfield W Jeffrey,Saad Fred]
Cancer Chemother Pharmacol,2018 Sep;82(3):457-468. PMID: 29974203

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