Drug/Small Molecule:
formoterol

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.

Links to Unannotated Labels

These links are to labels associated with formoterol that have not been annotated by PharmGKB.

  1. DailyMed - DrugLabel PA166105024

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?

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No Clinical Annotations available VA
rs1042713 148206440G>A, 148206440G>G, 46A>A, 46A>G, 46G>A, 5285A>A, 5285A>G, 9369367G>A, 9369367G>G, ADRB2:16Arg>Gly, ADRB2:Arg16Gly, ADRB2:Gly16Arg, Arg16, Arg16=
G > A
Missense
Arg16Gly
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Formoterol fumarate
  • Formoterolum [INN-Latin]
  • formoterol
Trade Names
  • Foradil
  • Foradile
  • Oxeze Turbuhaler
  • Oxeze Turbuhaler Foradil
  • Oxis
Brand Mixture Names

PharmGKB Accession Id:
PA134687907

Description

Formoterol is a long-acting (12 hours) beta2-agonist used in the management of asthma and/or chronic obstructive pulmonary disease (COPD). Inhaled formoterol works like other beta2-agonists, causing bronchodilatation through relaxation of the smooth muscle in the airway so as to treat the exacerbation of asthma.

Source: Drug Bank

Indication

For use as long-term maintenance treatment of asthma in patients 6 years of age and older with reversible obstructive airways disease, including patients with symptoms of nocturnal asthma, who are using optimal corticosteroid treatment and experiencing regular or frequent breakthrough symptoms requiring use of a short-acting bronchodilator. Not indicated for asthma that can be successfully managed with occasional use of an inhaled, short-acting beta2-adrenergic agonist. Also used for the prevention of exercise-induced bronchospasm, as well as long-term treatment of bronchospasm associated with COPD.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

The pharmacologic effects of beta2-adrenoceptor agonist drugs, including formoterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3', 5'-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibits the release of pro-inflammatory mast-cell mediators such as histamine and leukotrienes. Formoterol also inhibits histamine-induced plasma albumin extravasation in anesthetized guinea pigs and inhibits allergen-induced eosinophil influx in dogs with airway hyper-responsiveness. The relevance of these in vitro and animal findings to humans is unknown.

Source: Drug Bank

Pharmacology

Formoterol is a long-acting selective beta2-adrenergic receptor agonist (beta2-agonist). Inhaled formoterol fumarate acts locally in the lung as a bronchodilator. In vitro studies have shown that formoterol has more than 200-fold greater agonist activity at beta2-receptors than at beta1- receptors. Although beta2-receptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-receptors are the predominant receptors in the heart, there are also beta2-receptors in the human heart comprising 10%-50% of the total beta-adrenergic receptors. The precise function of these receptors has not been established, but they raise the possibility that even highly selective beta2- agonists may have cardiac effects.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Metabolized primarily by direct glucuronidation at either the phenolic or aliphatic hydroxyl group and O-demethylation followed by glucuronide conjugation at either phenolic hydroxyl groups. Minor pathways involve sulfate conjugation of formoterol and deformylation followed by sulfate conjugation. The most prominent pathway involves direct conjugation at the phenolic hydroxyl group. The second major pathway involves O-demethylation followed by conjugation at the phenolic 2'-hydroxyl group. Four cytochrome P450 isozymes (CYP2D6, CYP2C19, CYP2C9 and CYP2A6) are involved in the O-demethylation of formoterol.

Source: Drug Bank

Protein Binding

The binding of formoterol to human plasma proteins in vitro was 61%-64% at concentrations from 0.1 to 100 ng/mL. Binding to human serum albumin in vitro was 31%-38% over a range of 5 to 500 ng/mL. The concentrations of formoterol used to assess the plasma protein binding were higher than those achieved in plasma following inhalation of a single 120 microg dose.

Source: Drug Bank

Absorption

Rapidly absorbed into plasma following administration by oral inhalation. It is likely that the majority of the inhaled formoterol delivered is swallowed and then absorbed from the gastrointestinal tract.

Source: Drug Bank

Half-Life

10 hours

Source: Drug Bank

Toxicity

An overdosage is likely to lead to effects that are typical of beta2-adrenergic stimulants: nausea, vomiting, headache, tremor, somnolence, palpitations, tachycardia, ventricular arrhythmias, metabolic acidosis, hypokalemia, hyperglycemia.

Source: Drug Bank

Clearance

Source: Drug Bank

Route of Elimination

Following inhalation of a 12 mcg or 24 mcg dose by 16 patients with asthma, about 10% and 15%-18% of the total dose was excreted in the urine as unchanged formoterol and direct conjugates of formoterol, respectively.

Source: Drug Bank

Chemical Properties

Chemical Formula

C19H24N2O4

Source: Drug Bank

Isomeric SMILES

C[C@H](CC1=CC=C(C=C1)OC)NC[C@H](C2=CC(=C(C=C2)O)NC=O)O

Source: Drug Bank

COC1=CC=C(CC(C)NCC(O)C2=CC(NC=O)=C(O)C=C2)C=C1

Source: Drug Bank

Canonical SMILES

COC1=CC=C(CC(C)NCC(O)C2=CC(NC=O)=C(O)C=C2)C=C1

Source: Drug Bank

Average Molecular Weight

344.4049

Source: Drug Bank

Monoisotopic Molecular Weight

344.173607266

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Beta-agonist/Beta-blocker Pathway, Pharmacodynamics
    Simplified pharmacodynamic pathway of drug action on beta 2 adrenergic receptor in a stylized airway cell.
  1. Sympathetic Nerve Pathway (Neuroeffector Junction)
    Simplified diagram of a sympathetic neuroeffector junction displaying genes which may be involved.

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this drug. To report a pathway, click here.

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 VA No VIP available PW
ADRB2

Drug Targets

Gene Description
ADRB2 (source: Drug Bank)

Drug Interactions

Drug Description
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
acebutolol Antagonism (source: Drug Bank)
acebutolol Antagonism (source: Drug Bank)
atenolol Antagonism (source: Drug Bank)
atenolol Antagonism (source: Drug Bank)
betaxolol Antagonism (source: Drug Bank)
betaxolol Antagonism (source: Drug Bank)
bevantolol Antagonism (source: Drug Bank)
bisoprolol Antagonism (source: Drug Bank)
bisoprolol Antagonism (source: Drug Bank)
carteolol Antagonism (source: Drug Bank)
carvedilol Antagonism (source: Drug Bank)
carvedilol Antagonism (source: Drug Bank)
esmolol Antagonism (source: Drug Bank)
esmolol Antagonism (source: Drug Bank)
labetalol Antagonism (source: Drug Bank)
metoprolol Antagonism (source: Drug Bank)
metoprolol Antagonism (source: Drug Bank)
nadolol Antagonism (source: Drug Bank)
nadolol Antagonism (source: Drug Bank)
oxprenolol Antagonism (source: Drug Bank)
oxprenolol Antagonism (source: Drug Bank)
penbutolol Antagonism (source: Drug Bank)
pindolol Antagonism (source: Drug Bank)
pindolol Antagonism (source: Drug Bank)
practolol Antagonism (source: Drug Bank)
propranolol Antagonism (source: Drug Bank)
propranolol Antagonism (source: Drug Bank)
sotalol Antagonism (source: Drug Bank)
sotalol Antagonism (source: Drug Bank)
timolol Antagonism (source: Drug Bank)
timolol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)
formoterol Antagonism (source: Drug Bank)

Curated Information ?

EvidenceDisease
No Dosing Guideline available DL No Clinical Annotation available VA No VIP available No VIP available
Asthma

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
May Prevent
Contraindicated With

Publications related to formoterol: 2

No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Effect of ADRB2 polymorphisms on response to longacting beta2-agonist therapy: a pharmacogenetic analysis of two randomised studies. Lancet. 2007. Bleecker Eugene R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The Ile164 beta(2)-adrenoceptor polymorphism alters salmeterol exosite binding and conventional agonist coupling to G(s). European journal of pharmacology. 2001. Green S A, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0085-1402-01
DrugBank:
DB00983
KEGG Compound:
C07805
PubChem Compound:
3410
PubChem Substance:
10007
46507099
Drugs Product Database (DPD):
2237225
ChemSpider:
3292
Therapeutic Targets Database:
DAP000247
FDA Drug Label at DailyMed:
7b9da867-04ad-4ace-a889-9f4ff8bec47b

Clinical Trials

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

Common Searches

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