Drug/Small Molecule:
etoricoxib

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB has no annotated drug labels with pharmacogenomic information for this drug/small molecule. If you know of a drug label with PGx, send us a message.

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • MK-663
  • etoricoxib
Trade Names
  • Algix
  • Arcoxia
  • Nucoxia
  • Tauxib
Brand Mixture Names

PharmGKB Accession Id:
PA164776853

Description

Etoricoxib is a new COX-2 selective inhibitor. Current therapeutic indications are: treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout. Like any other COX-2 selective inhibitor, Etoricoxib selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2). This reduces the generation of prostaglandins (PGs) from arachidonic acid.

Source: Drug Bank

Indication

For the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Like any other COX-2 selective inhibitor Etoricoxib selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2). This reduces prostaglandins (PGs) generation from arachidonic acid.

Source: Drug Bank

Pharmacology

Etoricoxib is a COX-2 selective inhibitor (approximately 106 times more selective for COX-2 inhibition over COX-1). Currently it is approved in more than 60 countries worldwide but not in the US, where the Food and Drug Administration (FDA) require additional safety and efficacy data for etoricoxib before it will issue approval.

Source: Drug Bank

Food Interaction

Take without regard to meals.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic, primarily via CYP3A4.

Source: Drug Bank

Protein Binding

92%

Source: Drug Bank

Absorption

Bioavailability is 100% following oral administration.

Source: Drug Bank

Half-Life

22 hours

Source: Drug Bank

Toxicity

This reduced activity is the cause of reduced gastrointestinal toxicity, as demonstrated in several large clinical trials performed with different COXIB (see below links on NEJM and The Lancet). Some clinical trials and meta-analysis showed that treatment with COXIB lead to increased incidence of cardiovascular adverse events compared to placebo

Source: Drug Bank

Chemical Properties

Chemical Formula

C18H15ClN2O2S

Source: Drug Bank

Isomeric SMILES

CC1=NC=C(C=C1)C2=C(C=C(C=N2)Cl)C3=CC=C(C=C3)S(=O)(=O)C

Source: Drug Bank

CC1=CC=C(C=N1)C1=NC=C(Cl)C=C1C1=CC=C(C=C1)S(C)(=O)=O

Source: Drug Bank

Canonical SMILES

CC1=NC=C(C=C1)C1=C(C=C(Cl)C=N1)C1=CC=C(C=C1)S(C)(=O)=O

Source: Drug Bank

Average Molecular Weight

358.842

Source: Drug Bank

Monoisotopic Molecular Weight

358.054276131

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

EvidenceGene
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PTGS2

Drug Targets

Gene Description
PTGS2 (source: Drug Bank)

Drug Interactions

Drug Description
etoricoxib Etoricoxib increases the levels of ethinyl estradiol (source: Drug Bank)
acenocoumarol Etoricoxib may increase the anticoagulant effect of acenocoumarol. (source: Drug Bank)
anisindione Etoricoxib may increase the anticoagulant effect of anisindione. (source: Drug Bank)
dicumarol Etoricoxib may increase the anticoagulant effect of dicumarol. (source: Drug Bank)
lithium Etoricoxib increases serum levels of lithium (source: Drug Bank)
rifampin Rifampin reduces levels and efficacy of etoricoxib (source: Drug Bank)
warfarin Etoricoxib may increase the anticoagulant effect of warfarin. (source: Drug Bank)
etoricoxib Etoricoxib increases serum levels of lithium (source: Drug Bank)
etoricoxib Rifampin reduces levels and efficacy of etoricoxib (source: Drug Bank)
No related diseases are available

Publications related to etoricoxib: 1

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for PTGS2. Pharmacogenetics and genomics. 2010. Thorn Caroline F, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01628
PDB:
5CH
ChEBI:
6339
KEGG Compound:
C11718
KEGG Drug:
D03710
PubChem Compound:
123619
PubChem Substance:
13883
46504505
BindingDB:
50072064
ChemSpider:
110209
HET:
5CH
Therapeutic Targets Database:
DAP000738

Clinical Trials

These are trials that mention etoricoxib and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.