DIQTA 1.0: Drug-Induced QT Prolongation Atlas

BINIMETINIB

DIR Classification Postmarketing Surveillance Drug Property Information Reference

DIR Classification

Classification:Moderate-DIQT concern

Severity Score:2.0

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

DOSAGE AND ADMINISTRATION
Dosage Modifications for Adverse Reactions
Dose modification of MEKTOVI when administered with encorafenib is not recommended for the following adverse reactions: palmar-plantar erythrodysesthesia syndrome (PPES), non-cutaneous RAS mutation-positive malignancies, and QTc prolongation.
ADVERSE REACTIONS
The COLUMBUS trial [see CLINICAL STUDIES (14)] excluded patients with a history of Gilbert's syndrome, abnormal left ventricular ejection fraction, prolonged QTc (> 480 msec), uncontrolled hypertension, and history or current evidence of retinal vein occlusion. The median duration of exposure was 11.8 months for patients treated with MEKTOVI in combination with encorafenib and 6.2 months for patients treated with vemurafenib.
CLINICAL PHARMACOLOGY
Pharmacodynamics
Cardiac Electrophysiology
Following MEKTOVI 45 mg twice daily, no clinically meaningful QT prolongation was observed.

Postmarketing Surveillance

Contingency Table:

Current Drug

Other Drugs

QT Prolongation

24084

Other ADRs

6101

38375486

Odds Ratio = 2.09

Drug Property Information

ATC Code(s):

L01EE03 - binimetinib

L01EE0 -
L01EE -
L01E -
L01 - ANTINEOPLASTIC AGENTS
L - ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Active Ingredient:BINIMETINIB

Active Ingredient UNII:181R97MR71

Drugbank ID:DB11967

PubChem Compound:10288191

CTD ID:C581313

PharmGKB:PA166179867

CAS Number:606143-89-9

Dosage Form(s):tablet, film coated

Route(s) Of Administrator:oral

Daily Dose:

Chemical Structure:

SMILE Code:
CN1C=NC2=C(F)C(NC3=CC=C(Br)C=C3F)=C(C=C12)C(=O)NOCCO

Reference

1: Cardiovascular Adverse Events Associated With BRAF and MEK Inhibitors: A Systematic Review and Meta-analysis.

[Mincu Raluca I,Mahabadi Amir A,Michel Lars,Mrotzek Simone M,Schadendorf Dirk,Rassaf Tienush,Totzeck Matthias]
JAMA Netw Open,2019 Aug 2;2(8):e198890. PMID: 31397860

2: Tolerability of BRAF/MEK inhibitor combinations: adverse event evaluation and management.

[Heinzerling Lucie,Eigentler Thomas K,Fluck Michael,Hassel Jessica C,Heller-Schenck Daniela,Leipe Jan,Pauschinger Matthias,Vogel Arndt,Zimmer Lisa,Gutzmer Ralf]
ESMO Open,2019 May 23;4(3):e000491. PMID: 31231568

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