Drug/Small Molecule:
interferon alfa-2a, recombinant

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 annotates drug labels containing pharmacogenetic information approved by the US Food and Drug Administration (FDA), European Medicines Agency (EMA) and the Pharmaceuticals and Medical Devices Agency, Japan (PMDA). PharmGKB annotations provide a brief summary of the PGx in the label, an excerpt from the label and a downloadable highlighted label PDF file. A list of genes and phenotypes found within the label is mapped to label section headers and listed at the end of each annotation. PharmGKB also attempts to interpret the level of action implied in each label with the "PGx Level" tag.

Sources:

  • FDA Information is gathered from the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels" and from FDA-approved labels brought to our attention. Please note that drugs may be removed from or added to the FDA's Table without our knowledge. We periodically check the Table for changes and update PharmGKB accordingly. Drugs listed on the Table to our knowledge are tagged with the Biomarker icon. A drug label that has been removed from the Table will not have the Biomarker icon but will continue to have an annotation on PharmGKB stating the label has been removed from the FDA's Table. We acquire label PDF files from DailyMed.
  • EMA European Public Assessment Reports (EPARs) that contain PGx information were identified from [Article:24433361] and also by searching for drugs for which we have PGx-containing FDA drug labels.

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



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

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

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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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.

List of all variant annotations for interferon alfa-2a, recombinant

Gene ? Variant?
(142)
Alternate Names ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA VA HLA-B *44:02:01:01 N/A N/A N/A
No VIP available No Clinical Annotations available VA
rs12979860 12007005C>T, 39738787C>T
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs179008 10785421A>C, 10785421A>T, 12903659A>C, 12903659A>T, 130A>C, 130A>T, 23458A>C, 23458A>T, 32A>C, 32A>T, Gln11Leu, Gln11Pro
A > T
A > C
Missense
Gln11Leu
Gln11Pro
No VIP available No Clinical Annotations available VA
rs187238 -368G>C, 112034988C>G, 15597404C>G, 4853G>C
C > G
5' Flanking
No VIP available No Clinical Annotations available VA
rs1946518 -838A>C, 112035458T>G, 15597874T>G, 4383A>C
T > G
5' Flanking
No VIP available No Clinical Annotations available VA
rs8099917 12011383T>G, 39743165T>G
T > G
Not Available
No VIP available CA VA
rs9657182 27623994C>T, 39765848C>T
C > T
Not Available
No VIP available CA VA
rs9939609 46-23525T>A, 53820527T>A, 7434726T>A, 87653T>A, FTO:c.46-23525A>T
T > A
Intronic
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 142

Overview

Generic Names
  • Interferon alfa-2a
  • Oral interferon alfa
  • rIFN-alpha-2a
Trade Names
  • Roferon A (Hoffmann-La Roche Inc)
  • Veldona (Amarillo Biosciences)
Brand Mixture Names

PharmGKB Accession Id:
PA164779048

Description

Interferon a (human leukocyte protein moiety reduced). A type I interferon consisting of 165 amino acid residues with lysine in position 23. This protein is produced by recombinant DNA technology and resembles interferon secreted by leukocytes. It is used extensively as an antiviral or antineoplastic agent. An oral form is being developed by Amarillo Biosciences.

Source: Drug Bank

Indication

For the treatment of chronic hepatitis C, hairy cell leukemia, AIDS-related Kaposi's sarcoma, and chronic myelogenous leukemia. Also for the treatment of oral warts arising from HIV infection.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Interferon alpha binds to type I interferon receptors (IFNAR1 and IFNAR2c) which, upon dimerization, activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers and activators of transcription)which dimerize and activate multiple (~100) immunomodulatory and antiviral proteins. Interferon alpha binds less stably to type I interferon receptors than interferon beta.

Source: Drug Bank

Pharmacology

Upregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Interferon alpha also induce the synthesis of several key antiviral mediators, including 2'-5' oligoadenylate synthetase (2'-5' A synthetase) and protein kinase R.

Source: Drug Bank

Food Interaction

Avoid alcohol.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Absorption

Absorption is high (greater than 80%) when administered intramuscularly or subcutaneously.

Source: Drug Bank

Half-Life

The IM half-life of interferon alfa-2a is 6 hours to 8 hours; the half-life for IV infusion is 3.7 hours to 8.5 hours (mean 5.1 hours).

Source: Drug Bank

Toxicity

Interferon alfa-2 may cause serious adverse effects such as anemia; autoimmune diseases, including vasculitis, arthritis, hemolytic anemia, and erythematosus syndrome; cardiotoxicity; hepatotoxicity; hyperthyroidism or hypothyroidism; transient ischemic attacks; leukopenia; neurotoxicity; peripheral neuropathy; and thrombocytopenia. Some lesser side effects that may not need medical attention include blurred vision, change in taste or metallic taste, cold sores or stomatitis, diarrhea, dizziness, dry mouth, dry skin or itching, flu-like syndrome, increased sweating, leg cramps, loss of appetite, nausea or vomiting, skin rash, unusual tiredness, weight loss, and partial loss of hair.

Source: Drug Bank

Clearance

Source: Drug Bank

Route of Elimination

Alpha-interferons are totally filtered through the glomeruli and undergo rapid proteolytic degradation during tubular reabsorption, rendering a negligible reappearance of intact alfa interferon in the systemic circulation.

Source: Drug Bank

Volume of Distribution

Source: Drug Bank

Chemical Properties

Chemical Formula

C860H1353N227O255S9

Source: Drug Bank

Canonical SMILES

Not Available

Source: Drug Bank

Average Molecular Weight

19241.1000

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 ?

Drug Targets

Gene Description
IFNAR1 (source: Drug Bank)
IFNAR2 (source: Drug Bank)

Drug Interactions

Drug Description
aminophylline Interferon increases the effect and toxicity of theophylline (source: Drug Bank)
dyphylline Interferon increases the effect and toxicity of theophylline (source: Drug Bank)
oxtriphylline Interferon increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Interferon increases the effect and toxicity of theophylline (source: Drug Bank)

Curated Information ?

Publications related to interferon alfa-2a, recombinant: 11

No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
IFNL3 polymorphisms predict response to therapy in chronic hepatitis C genotype 2/3 infection. Journal of hepatology. 2014. Eslam Mohammed, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Strong prediction of virological response to combination therapy by IL28B gene variants rs12979860 and rs8099917 in chronic hepatitis C genotype 4. Liver international : official journal of the International Association for the Study of the Liver. 2014. Ragheb Mostafa M, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
FTO rs9939609 polymorphism is associated with metabolic disturbances and response to HCV therapy in HIV/HCV-coinfected patients. BMC medicine. 2014. Pineda-Tenor Daniel, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Association of a polymorphism in the indoleamine- 2,3-dioxygenase gene and interferon-alpha-induced depression in patients with chronic hepatitis C. Molecular psychiatry. 2011. Smith A K, 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
Genomics and drug response. The New England journal of medicine. 2011. Wang Liewei, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Toll-like receptor 7 rs179008/Gln11Leu gene variants in chronic hepatitis C virus infection. Journal of medical virology. 2010. Askar Eva, 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
Genome-wide association of IL28B with response to pegylated interferon-alpha and ribavirin therapy for chronic hepatitis C. Nature genetics. 2009. Tanaka Yasuhito, 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
IL28B is associated with response to chronic hepatitis C interferon-alpha and ribavirin therapy. Nature genetics. 2009. Suppiah Vijayaprakash, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Interleukin 18 promoter variants (-137G>C and -607C>A) in patients with chronic hepatitis C: association with treatment response. Journal of clinical immunology. 2009. Haas Stephan L, 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
Genetic variation in IL28B predicts hepatitis C treatment-induced viral clearance. Nature. 2009. Ge Dongliang, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
HLA class I B44 is associated with sustained response to interferon + ribavirin therapy in patients with chronic hepatitis C. The American journal of gastroenterology. 2003. Romero-Gómez Manuel, et al. PubMed

LinkOuts

GenBank:
J00207
UniProtKB:
IFNA2_HUMAN (P01563)
National Drug Code Directory:
0004-2015-09
DrugBank:
DB00034
Drugs Product Database (DPD):
2217066
Therapeutic Targets Database:
DAP000801
FDA Drug Label at DailyMed:
4c918b02-f158-4f7c-8ecc-fd49574ec228

Clinical Trials

These are trials that mention interferon alfa-2a, recombinant and are related to either pharmacogenetics or pharmacogenomics.

No trials found.

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