DIQTA 1.0: Drug-Induced QT Prolongation Atlas

CABOZANTINIB

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
The exposure-response or safety relationship for cabozantinib is unknown.
Cardiac Electrophysiology
The effect of cabozantinib on QTc interval was evaluated in a randomized, double-blinded, placebo-controlled trial in patients with medullary thyroid cancer administered a cabozantinib capsule formulation. A mean increase in QTcF of 10 - 15 ms was observed at 4 weeks after initiation. A concentration-QTc relationship could not be definitively established. Changes in cardiac wave form morphology or new rhythms were not observed. No patients in this study had a confirmed QTcF > 500 ms nor did any patients in METEOR, CABOSUN, or CELESTIAL.

Postmarketing Surveillance

Contingency Table:

Current Drug

Other Drugs

QT Prolongation

24083

Other ADRs

49734

38331853

Odds Ratio = 0.289

Drug Property Information

ATC Code(s):

L01EX07 - cabozantinib

L01EX -
L01E -
L01 - ANTINEOPLASTIC AGENTS
L - ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Active Ingredient:cabozantinib s-malate

Active Ingredient UNII:DR7ST46X58

Drugbank ID:DB08875

PubChem Compound:25102847

CTD ID: C558660

PharmGKB:

CAS Number:849217-68-1

Dosage Form(s):tablet

Route(s) Of Administrator:oral

Daily Dose:

Chemical Structure:

SMILE Code:
COC1=CC2=C(C=C1OC)C(OC1=CC=C(NC(=O)C3(CC3)C(=O)NC3=CC=C(F)C=C3)C=C1)=CC=N2

Reference

1: Comparative efficacy and safety of tyrosine kinase inhibitors for thyroid cancer: a systematic review and meta-analysis.

[Oba Takaaki,Chino Tatsunori,Soma Ai,Shimizu Tadafumi,Ono Mayu,Ito Tokiko,Kanai Toshiharu,Maeno Kazuma,Ito Ken-Ichi]
Endocr J,2020 Dec 28;67(12):1215-1226. PMID: 32814730

2: Management of treatment-related toxicities in advanced medullary thyroid cancer.

[Brose Marcia S,Bible Keith C,Chow Laura Q M,Gilbert Jill,Grande Carolyn,Worden Francis,Haddad Robert]
Cancer Treat Rev,2018 May;66:64-73. PMID: 29704768

3: Update on Cardiovascular Safety of Tyrosine Kinase Inhibitors: With a Special Focus on QT Interval, Left Ventricular Dysfunction and Overall Risk/Benefit.

[Shah Rashmi R,Morganroth Joel]
Drug Saf,2015 Aug;38(8):693-710. PMID: 26008987

4: QTc interval prolongation with vascular endothelial growth factor receptor tyrosine kinase inhibitors.

[Ghatalia P,Je Y,Kaymakcalan M D,Sonpavde G,Choueiri T K]
Br J Cancer,2015 Jan 20;112(2):296-305. PMID: 25349964

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