Drug/Small Molecule:
eltrombopag

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 gathers information regarding PGx on FDA drug labels from the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels", and from FDA-approved FDA and EMA-approved (European Medicines Agency) EMA labels brought to our attention. Excerpts from the label and downloadable highlighted label PDFs are manually curated by PharmGKB.

Please note that some drugs may have been removed from or added to the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels" without our knowledge. We periodically check the table for additions to this table and update PharmGKB accordingly.

There is currently no such list for European drug labels - we are working with the EMA to establish a list of European Public Assessment Reports (EPAR)s that contain PGx information. We are constructing this list by initially searching for drugs for which we have PGx-containing FDA drug labels - of these 44 EMA EPARs were identified and are being curated for pgx information.

We welcome any information regarding drug labels containing PGx information approved by the FDA, EMA or other Medicine Agencies around the world - please contact feedback.



last updated 10/25/2013

FDA Label for eltrombopag and F5, SERPINC1

This label is on the FDA Biomarker List
Actionable PGx

Summary

The FDA-approved drug label for eltrombopag (PROMACTA) notes that patients taking the drug have an increased risk of thromboembolism if they have antithrombin III deficiency (SERPINC1) or Factor V Leiden (F5).

Annotation

Eltrombopag olamine (PROMACTA) is a thrombopoietin receptor agonist indicated for the treatment of thrombocytopenia. The FDA-approved drug label cautions that patients taking eltrombopag have an increased risk for thromboembolism if they have known risk factors such as Factor V Leiden or antithrombin III deficiency (ATIII). These risk factors are listed as biomarkers (FV and SERPINC1, respectively) on the FDA Pharmacogenomic Biomarkers in Drug Labels table.

Excerpt from the eltrombopag (PROMACTA) drug label:

Consider the potential for an increased risk of thromboembolism when administering PROMACTA to patients with known risk factors for thromboembolism (e.g., Factor V Leiden, ATIII deficiency, antiphospholipid syndrome, chronic liver disease)

Note that Factor V Leiden is a polymorphism resulting in an Arg to Gln substitution at position 506 in the Factor V heavy chain (rs6025)

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the eltrombopag drug label.

*Disclaimer: The contents of this page have not been endorsed by the FDA and are the sole responsibility of PharmGKB.

Full label available at DailyMed

Genes and/or phenotypes found in this label

  • ABCG2
    • Drug interactions section, Clinical pharmacology section
    • source: FDA Label
  • CYP1A2
    • Drug interactions section, metabolism/PK
    • source: FDA Label
  • CYP2C19
    • Clinical pharmacology section
    • source: FDA Label
  • CYP2C8
    • Drug interactions section, metabolism/PK
    • source: FDA Label
  • CYP2C9
    • Drug interactions section
    • source: FDA Label
  • CYP3A4
    • Clinical pharmacology section
    • source: FDA Label
  • F5
    • Warnings and precautions section, toxicity
    • source: FDA Label
  • SERPINC1
    • Warnings and precautions section, toxicity
    • source: FDA Label
  • SLCO1B1
    • Drug interactions section, Clinical pharmacology section
    • source: FDA Label
  • UGT1A1
    • Drug interactions section
    • source: FDA Label
  • UGT1A3
    • Drug interactions section
    • source: FDA Label
  • UGT1A4
    • Drug interactions section
    • source: FDA Label
  • UGT1A6
    • Drug interactions section
    • source: FDA Label
  • UGT1A9
    • Drug interactions section
    • source: FDA Label
  • UGT2B15
    • Drug interactions section
    • source: FDA Label
  • UGT2B7
    • Drug interactions section
    • source: FDA Label

last updated 10/25/2013

European Medicines Agency (EMA) Label for eltrombopag and F5, SERPINC1

Actionable PGx

Summary

The EMA European Public Assessment Report (EPAR) highlights that caution should be taken when administering eltrombopag in patients with known risk factors for thromboembolism, including Factor V Leiden (F5 gene) and ATIII deficiency (SERPINC1 gene).

Annotation

Excerpt from the Eltrombopag (Revolade) EPAR:

"Thrombotic/Thromboembolic complications Thrombotic/Thromboembolic complications may occur in patients with ITP. Platelet counts above the normal range present a theoretical risk of thrombotic/thromboembolic complications. In eltrombopag clinical trials in ITP thromboembolic events were observed at low and normal platelet counts. Caution should be used when administering eltrombopag to patients with known risk factors for thromboembolism including but not limited to inherited (e.g. Factor V Leiden) or acquired risk factors (e.g. ATIII deficiency, antiphospholipid syndrome), advanced age, patients with prolonged periods of immobilisation, malignancies, contraceptives and hormone replacement therapy, surgery/trauma, obesity and smoking. Platelet counts should be closely monitored and consideration given to reducing the dose or discontinuing eltrombopag treatment if the platelet count exceeds the target levels (see section 4.2). The risk-benefit balance should be considered in patients at risk of thromboembolic events (TEEs) of any aetiology."

This information is highlighted in the following sections: Special warnings and precautions for use, key elements to be included in educational material.

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the Eltrombopag EMA drug label.

*Disclaimer: The contents of this page have not been endorsed by the EMA and are the sole responsibility of PharmGKB.


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
  • Eltrombopag olamine
Trade Names
  • Promacta
  • Revolade
Brand Mixture Names

PharmGKB Accession Id:
PA165981594

Indication

Eltrombopag is a thrombopoietin receptor agonist indicated for the treatment of thrombocytopenia in patients with chronic immune (idiopathic) thrombocytopenia (ITP) who have had an insufficient response to corticosteroids, immunoglobulins, or splenectomy (excerpt from drug label).

Source: PharmGKB

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Chemical Properties

Chemical Formula

C29H36N6O6

Source: PubChem Compound

Canonical SMILES

CC1=C(C=C(C=C1)N2C(=O)C(=C(N2)C)N/N=C/3\C=CC=C(C3=O)C4=CC(=CC=C4)C(=O)O)C.C(CO)N.C(CO)N

Source: PubChem Compound

Average Molecular Weight

564.63274

Source: PubChem Compound

Monoisotopic Molecular Weight

564.269633

Source: PubChem Compound

IUPAC Names

  • 2-aminoethanol; 3-[(5E)-5-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]hydrazinylidene]-6-oxocyclohexa-1,3-dien-1-yl]benzoic acid

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 ?

No related drugs are available.
No related diseases are available

LinkOuts

PubChem Compound:
9915926

Clinical Trials

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

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