DIQTA 1.0: Drug-Induced QT Prolongation Atlas

NELFINAVIR MESYLATE

DIR Classification Postmarketing Surveillance Drug Property Information Reference

DIR Classification

Classification:Moderate-DIQT concern

Severity Score:3.0

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

DRUG INTERACTIONS
ADVERSE REACTIONS
Postmarketing Experience
The following adverse reactions have been identified during post-approval use of VIRACEPT. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Cardiovascular System: QTc prolongation, torsades de pointes.
CLINICAL PHARMACOLOGY
Pharmacodynamics
Effects on Electrocardiogram
The effect of Viracept at the recommended dose of 1250 mg twice daily on the QTcF interval administered with a low fat meal (20% fat) was evaluated in a randomized, placebo and active (moxifloxacin 400 mg once daily) controlled, crossover study in 66 healthy subjects. The maximum mean time-matched (95% upper confidence bound) differences in QTcF interval from placebo after baseline-correction was below 10 milliseconds, the threshold of clinical concern. This finding was unchanged when a single supratherapeutic dose of Viracept 3125 mg was administered following a 3-day administration of Viracept 1250 mg twice daily. The exposure at 3125 mg was 1.4-fold that at 1250 mg. The dose of 3125 mg in this study did not achieve the anticipated exposures in patients taking a high fat meal (50% fat) or with concomitant administration of drugs that could increase nelfinavir exposure [see PHARMACOKINETICS (12.3)].
No subject in any group had an increase in QTcF of ≥60 milliseconds from baseline. No subject experienced an interval exceeding the potentially clinically relevant threshold of 500 milliseconds.

Postmarketing Surveillance

Contingency Table:

Current Drug

Other Drugs

QT Prolongation

24081

Other ADRs

2208

38379379

Odds Ratio = 7.94

Drug Property Information

ATC Code(s):

J05AE04 - nelfinavir mesylate

J05AE - Protease inhibitors
J05A - DIRECT ACTING ANTIVIRALS
J05 - ANTIVIRALS FOR SYSTEMIC USE
J - ANTIINFECTIVES FOR SYSTEMIC USE

Active Ingredient:NELFINAVIR MESYLATE

Active Ingredient UNII:98D603VP8V

Drugbank ID:DB00220

PubChem Compound:64143

CTD ID:D019888

PharmGKB:PA450606

CAS Number:159989-64-7

Dosage Form(s):tablet, film coated

Route(s) Of Administrator:oral

Daily Dose:

2250.0 mg/day J05AE04

Chemical Structure:

SMILE Code:
[H][C@@]12CCCC[C@]1([H])CN(C[C@@H](O)[C@H](CSC1=CC=CC=C1)NC(=O)C1=C(C)C(O)=CC=C1)[C@@H](C2)C(=O)NC(C)(C)C

Reference

N/A