DIQTA 1.0: Drug-Induced QT Prolongation Atlas

ROLAPITANT

DIR Classification Postmarketing Surveillance Drug Property Information Reference

DIR Classification

Classification:Most-DIQT concern

Severity Score:4.0

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

WARNINGS AND PRECAUTIONS
Interaction with CYP2D6 Substrates
Narrow Therapeutic Index Drugs (Thioridazine and Pimozide)
VARUBI is contraindicated in patients taking CYP2D6 substrates with a narrow therapeutic index such as thioridazine and pimozide. Increased plasma concentrations of thioridazine and pimozide are associated with serious and/or life-threatening events of QT prolongation and Torsades de Pointes [see CONTRAINDICATIONS (4)].
DRUG INTERACTIONS
CONTRAINDICATIONS
VARUBI is contraindicated in patients taking CYP2D6 substrates with a narrow therapeutic index, such as thioridazine and pimozide. VARUBI can significantly increase the plasma concentrations of thioridazine and pimozide, which may result in QT prolongation and Torsades de Pointes [see WARNINGS AND PRECAUTIONS (5.1)].
CLINICAL PHARMACOLOGY
Pharmacodynamics
Cardiac Electrophysiology
At an oral dose of 720 mg (4 times the recommended oral dose), VARUBI does not prolong the QT interval to any clinically relevant extent.

Postmarketing Surveillance

Contingency Table:

Current Drug

Other Drugs

QT Prolongation

24092

Other ADRs

38381587

Odds Ratio = N/A

Drug Property Information

ATC Code(s):

A04AD14 - rolapitant

A04AD - Other antiemetics
A04A - ANTIEMETICS AND ANTINAUSEANTS
A04 - ANTIEMETICS AND ANTINAUSEANTS
A - ALIMENTARY TRACT AND METABOLISM

Active Ingredient:ROLAPITANT HYDROCHLORIDE

Active Ingredient UNII:57O5S1QSAQ

Drugbank ID:DB09291

PubChem Compound:10311306

CTD ID:C578834

PharmGKB:

CAS Number:552292-08-7

Dosage Form(s):tablet

Route(s) Of Administrator:oral

Daily Dose:

180.0 mg/day A04AD14

Chemical Structure:

SMILE Code:
C[C@@H](OC[C@]1(CC[C@]2(CCC(=O)N2)CN1)C1=CC=CC=C1)C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F

Reference

1: Drugs for preventing postoperative nausea and vomiting in adults after general anaesthesia: a network meta-analysis.

[Weibel Stephanie,Rücker Gerta,Eberhart Leopold Hj,Pace Nathan L,Hartl Hannah M,Jordan Olivia L,Mayer Debora,Riemer Manuel,Schaefer Maximilian S,Raj Diana,Backhaus Insa,Helf Antonia,Schlesinger Tobias,Kienbaum Peter,Kranke Peter]
Cochrane Database Syst Rev,2020 Oct 19;10:CD012859. PMID: 33075160

2: A Phase 1 Assessment of the QT Interval in Healthy Adults Following Exposure to Rolapitant, a Cancer Supportive Care Antiemetic.

[Wang Xiaodong,Zhang Zhi-Yi,Wang Jing,Kansra Vikram]
Clin Pharmacol Drug Dev,2019 Jul;8(5):603-611. PMID: 30256537

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