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Identification
- Summary
Peginterferon alfa-2a is a modified form of recombinant human interferon used to stimulate the innate antiviral response in the treatment of hepatitis B and C viruses.
- Brand Names
- Pegasys
- Generic Name
- Peginterferon alfa-2a
- DrugBank Accession Number
- DB00008
- Background
Peginterferon alfa-2a is a form of recombinant interferon used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States, and affecting 72% of all chronic HCV patients 3. Treatment options for chronic Hepatitis C have advanced significantly since 2011, with the development of Direct Acting Antivirals (DAAs) resulting in less use of Peginterferon alfa-2a. Peginterferon alfa-2a is derived from the alfa-2a moeity of recombinant human interferon and acts by binding to human type 1 interferon receptors. Activation and dimerization of this receptor induces the body's innate antiviral response by activating the janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway. Use of Peginterferon alfa-2a is associated with a wide range of severe adverse effects including the aggravation and development of endocrine and autoimmune disorders, retinopathies, cardiovascular and neuropsychiatric complications, and increased risk of hepatic decompensation in patients with cirrhosis. The use of Peginterferon alfa-2a has largely declined since newer interferon-free antiviral therapies have been developed.
In a joint recommendation published in 2016, the American Association for the Study of Liver Diseases (AASLD) and the Infectious Diseases Society of America (IDSA) no longer recommend Peginterferon alfa-2a for the treatment of Hepatitis C 1. Peginterferon alfa-2a was used alongside Ribavirin with the intent to cure, or achieve a sustained virologic response (SVR), after 48 weeks of therapy. SVR and eradication of HCV infection is associated with significant long-term health benefits including reduced liver-related damage, improved quality of life, reduced incidence of Hepatocellular Carcinoma, and reduced all-cause mortality 2.
Peginterferon alfa-2a is available as a fixed dose injector (tradename Pegasys) used for the treatment of chronic Hepatitis C. Approved in 2002 by the FDA, Pegasys is indicated for the treatment of HCV with Ribavirin or other antiviral drugs Label. When combined together, Peginterferon alfa-2a and Ribavirin have been shown to achieve a SVR between 36% for genotype 1 and 59% for genotypes 2-6 after 48 weeks of treatment.
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Interferons - Protein Structure
- Protein Chemical Formula
- Not Available
- Protein Average Weight
- 60000.0 Da
- Sequences
>Peginterferon alfa-2a sequence CDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMI QQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVR KYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE
Download FASTA Format- Synonyms
- PEG-IFN alfa-2A
- PEG-Interferon alfa-2A
- Peginterferon alfa-2a
- Pegylated Interfeaon alfa-2A
- Pegylated interferon alfa-2a
- Pegylated interferon alpha-2a
- Pegylated-interferon alfa 2a
- External IDs
- RO 25-8310/000
- RO-25-8310/000
- RO-258310000
Pharmacology
- Indication
Peginterferon alfa-2a is indicated for the treatment of HCV in combination with other antiviral drugs in patients over 5 years of age with compensated liver disease Label. May be used as a monotherapy in patients with contraindications to or significant intolerance to other anti-viral therapies.
Peginterferon alfa-2a is also indicated as a monotherapy for adult patients with HBeAg positive and HBeAg negative chronic hepatitis B infection who have compensated liver disease and evidence of viral replication and liver inflammation Label.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Chronic hepatitis c virus (hcv) infection •••••••••••• ••••• ••••••••••• ••••• ••••••• ••••••••• Treatment of Chronic hepatitis c virus (hcv) infection •••••••••••• ••••• ••••••••••• ••••• •••••••• •••••••••••••••• •• ••••••••••• •• ••••• ••••••• ••••••••• Used in combination to treat Chronic hepatitis c virus (hcv) infection Regimen in combination with: Ribavirin (DB00811) •••••••••••• ••••••••• ••••••••••• ••••• ••••••• ••••••••• Treatment of Hbeag positive chronic hepatitis b •••••••••••• ••••••••• •••••••••• •• ••••• ••••••• •••••••••••••••• •••••• ••••• •••••••••••• ••••••••••••• ••••••••• Treatment of Hepatitis b chronic infection •••••••••••• ••••• ••••••••••• ••••• •••••••• ••••• ••••••••••• ••••••••• - Contraindications & Blackbox Warnings
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Peginterferon alfa-2a induces the body's innate antiviral response Label.
- Mechanism of action
Peginterferon alfa-2a is derived from recombinant human interferon's alfa-2a moeity Label. It binds to and activates human type 1 interferon receptors causing them to dimerize. This activates the JAK/STAT pathway. Activation of the JAK/STAT pathway increases expression of multiple genes in multiple tissues involved in the innate antiviral response.
Target Actions Organism AInterferon alpha/beta receptor 2 agonistHumans AInterferon alpha/beta receptor 1 agonistHumans - Absorption
Peginterferon alfa-2a reaches peak plasma concentration 72-96 hours after subcutaneous administration Label. Trough concentrations at week 48 are approximately 2 fold higher than week 1. The peak to trough ratio at week 48 is 2.
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
The mean terminal half-life of peginterferon alfa-2a is 164 in a range of 84-353 hours Label.
- Clearance
The mean systemic clearance of peginterferon alfa-2a is 94 milliliters per hour Label.
- Adverse Effects
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Peginterferon alfa-2a may manifest neuropsychiatric complications include suicide, suicidal ideation, homicidal ideation, depression, relapse of drug addiction, and drug overdose Label. Hypertension, supraventricular arrhythmias, chest pain, and myocardial infarction have been observed in patients using Peginterferon alfa-2a. Peginterferon alfa-2a may produce myelosuppression as well as the development or aggravation of autoimmune disorders including myositis, hepatitis, thrombotic thrombocytopenic purpura, idiopathic thrombocytopenic purpura, psoriasis, rheumatoid arthritis, interstitial nephritis, thyroiditis, and systemic lupus erythematosus. Peginterferon alfa-2a causes or aggravates hypothyroidism and hyperthyroidism. Hyperglycemia, hypoglycemia, and diabetes mellitus have been observed to develop in patients treated with Peginterferon alfa-2a. Peginterferon alfa-2a may decrease or produce loss of vision, retinopathy including macular edema, retinal artery or vein thrombosis, retinal hemorrhages and cotton wool spots, optic neuritis, papilledema and serous retinal detachment. Peginterferon mayy be related to increased ischemic and hemorrhagic cerebrovascular events. Patients with cirrhosis on Peginterferon alfa-2a are at risk of hepatic decompensation. Dyspnea, pulmonary infiltrates, pneumonia, bronchiolitis obliterans, interstitial pneumonitis, pulmonary hypertension and sarcoidosis may be induced or aggravated by Peginterferon alfa-2a. Serious and severe infections (bacterial, viral, or fungal) have been reported during treatment with Peginterferon alfa-2a. Ulcerative and hemorrhagic/ischemic colitis have been observed within 12 weeks of starting Peginterferon alfa-2a treatment. Pancreatitis and peripheral nephropathy have also been reported. Peginterferon alfa-2a is associated with growth inhibition in pediatric patients. Use of Peginterferon alfa-2a while pregant may result in delopmental abnormalities or death of the fetus.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details Interferon lambda-3 --- (T;T) / (C;T) / (G;G) / (G;T) C > T Effect Directly Studied Patients with this genotype in IFNL3 have a reduced likelihood of achieving sustained virologic response to peginterferon alfa-2a therapy. Details
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbatacept The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Abatacept. Abciximab The risk or severity of bleeding can be increased when Abciximab is combined with Peginterferon alfa-2a. Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Peginterferon alfa-2a. Acetaminophen The metabolism of Acetaminophen can be decreased when combined with Peginterferon alfa-2a. Acetyldigitoxin Acetyldigitoxin may decrease the cardiotoxic activities of Peginterferon alfa-2a. - Food Interactions
- Drink plenty of fluids.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Pegasys Injection, solution 180 μg Subcutaneous Pharmaand Gmb H 2016-09-08 Not applicable EU 
Pegasys Injection, solution 180 μg Subcutaneous Pharmaand Gmb H 2016-09-08 Not applicable EU Pegasys Injection, solution 180 μg Subcutaneous Pharmaand Gmb H 2016-09-08 Not applicable EU Pegasys Injection, solution 135 μg Subcutaneous Pharmaand Gmb H 2016-09-08 Not applicable EU Pegasys Injection, solution 135 μg Subcutaneous Pharmaand Gmb H 2016-09-08 Not applicable EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Pegasys Rbv Peginterferon alfa-2a (180 mcg / mL) + Ribavirin (200 mg / tab) Solution; Tablet Oral; Subcutaneous Hoffmann La Roche 2004-05-26 2018-07-10 Canada 
Pegasys Rbv Peginterferon alfa-2a (180 mcg / 0.5 mL) + Ribavirin (200 mg / tab) Solution; Tablet Oral; Subcutaneous Hoffmann La Roche 2004-05-26 2018-07-10 Canada
Categories
- ATC Codes
- L03AB11 — Peginterferon alfa-2a
- L03AB — Interferons
- L03A — IMMUNOSTIMULANTS
- L03 — IMMUNOSTIMULANTS
- L — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
- Drug Categories
- Adjuvants, Immunologic
- Alcohols
- Alfa Interferons
- Amino Acids, Peptides, and Proteins
- Anti-Infective Agents
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Antiviral Agents
- Biological Factors
- Cardiotoxic antineoplastic agents
- Compounds used in a research, industrial, or household setting
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 Enzyme Inhibitors
- Cytokines
- Drug Carriers
- Ethylene Glycols
- Glycols
- Hepatotoxic Agents
- Immunosuppressive Agents
- Intercellular Signaling Peptides and Proteins
- Interferon alpha
- Interferon Type I
- Interferons
- Macromolecular Substances
- Myelosuppressive Agents
- Narrow Therapeutic Index Drugs
- Pegylated agents
- Peptides
- Polymers
- Proteins
- Treatments for Hepatitis C
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- Q46947FE7K
- CAS number
- 198153-51-4
References
- General References
- Bagaglio S, Uberti-Foppa C, Morsica G: Resistance Mechanisms in Hepatitis C Virus: implications for Direct-Acting Antiviral Use. Drugs. 2017 May 12. doi: 10.1007/s40265-017-0753-x. [Article]
- Myers RP, Shah H, Burak KW, Cooper C, Feld JJ: An update on the management of chronic hepatitis C: 2015 Consensus guidelines from the Canadian Association for the Study of the Liver. Can J Gastroenterol Hepatol. 2015 Jan-Feb;29(1):19-34. Epub 2015 Jan 13. [Article]
- American Association for the Study of Liver Diseases; Infectious Diseases Society of America. HCV guidance. http://hcvguidelines.org. Accessed June 12, 2017. [Link]
- External Links
- UniProt
- P01563
- Genbank
- J00207
- PubChem Substance
- 46504860
- 120608
- ChEMBL
- CHEMBL1201560
- Therapeutic Targets Database
- DAP001278
- PharmGKB
- PA164749390
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Peginterferon_alfa-2a
- FDA label
- Download (1.13 MB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Active Not Recruiting Not Available Antiviral Treatment / Chronic Hepatitis B Infection / Fatty Liver Disease 1 somestatus stop reason just information to hide Not Available Available Not Available Cirrhosis of the Liver / Decompensated Cirrhosis / Hepatic Ascites / Hepatocellular Carcinoma / Varices, Esophageal / Viral Hepatitis B / Viral Hepatitis D 1 somestatus stop reason just information to hide Not Available Completed Not Available Chronic Fatigue Syndrome/ Myalgic Encephalitis (CFS/ME) / Chronic Hepatitis C Virus (HCV) Infection / Cognitive Dysfunctions / Major Depressive Disorder (MDD) 1 somestatus stop reason just information to hide Not Available Completed Not Available Chronic Hepatitis B Infection 6 somestatus stop reason just information to hide Not Available Completed Not Available Chronic Hepatitis C Virus (HCV) Infection 17 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- F Hoffmann La Roche Ltd.
- F Hoffmann-La Roche Ltd.
- Dosage Forms
Form Route Strength Injection Subcutaneous 135 mcg Injection Subcutaneous 180 mcg Injection, solution Subcutaneous 135 μg Injection, solution Subcutaneous 135 MCG Injection, solution Subcutaneous 135 ug/0.5mL Injection, solution Subcutaneous 180 ug/1mL Injection, solution Subcutaneous 180 ug/0.5mL Injection, solution Subcutaneous 180 mcg/ml Injection, solution Subcutaneous 180 μg Injection, solution Subcutaneous 180 MCG Injection, solution Subcutaneous 90 μg Solution Subcutaneous 0.135 mg Solution Subcutaneous 180 mcg / mL Solution Subcutaneous 180 mcg / 0.5 mL Injection Subcutaneous 135 mcg/0.5ml Injection Subcutaneous 180 mcg/0.5ml Solution; tablet Oral; Subcutaneous Injection, solution Subcutaneous 135 mcg/0.5ml Injection, solution Subcutaneous 180 mcg/0.5ml - Prices
Unit description Cost Unit Pegasys (1 Kit = Four 180 mcg/ml Vials Prefilled Syringes) Box 2634.53USD box Pegasys 180 mcg/0.5 ml conv.pk 2533.2USD each Pegasys 180 mcg/ml vial 642.64USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2172664 No 2000-10-03 2016-03-26 Canada CA2203480 No 2009-06-30 2017-04-23 Canada
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 61 °C Beldarrain, A. et al., Biochemistry 38:7865-7873 (1999) isoelectric point 5.99 Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Together with IFNAR1, forms the heterodimeric receptor for type I interferons (including interferons alpha, beta, epsilon, omega and kappa) (PubMed:10049744, PubMed:10556041, PubMed:21854986, PubMed:26424569, PubMed:28165510, PubMed:32972995, PubMed:7665574, PubMed:7759950, PubMed:8181059, PubMed:8798579, PubMed:8969169). Type I interferon binding activates the JAK-STAT signaling cascade, resulting in transcriptional activation or repression of interferon-regulated genes that encode the effectors of the interferon response (PubMed:10049744, PubMed:17517919, PubMed:21854986, PubMed:26424569, PubMed:28165510, PubMed:32972995, PubMed:7665574, PubMed:7759950, PubMed:8181059, PubMed:8798579, PubMed:8969169). Mechanistically, type I interferon-binding brings the IFNAR1 and IFNAR2 subunits into close proximity with one another, driving their associated Janus kinases (JAKs) (TYK2 bound to IFNAR1 and JAK1 bound to IFNAR2) to cross-phosphorylate one another (PubMed:10556041, PubMed:11682488, PubMed:12105218, PubMed:21854986, PubMed:32972995). The activated kinases phosphorylate specific tyrosine residues on the intracellular domains of IFNAR1 and IFNAR2, forming docking sites for the STAT transcription factors (STAT1, STAT2 and STAT) (PubMed:11682488, PubMed:12105218, PubMed:21854986, PubMed:32972995). STAT proteins are then phosphorylated by the JAKs, promoting their translocation into the nucleus to regulate expression of interferon-regulated genes (PubMed:12105218, PubMed:28165510, PubMed:9121453)
- Specific Function
- Cytokine binding
- Gene Name
- IFNAR2
- Uniprot ID
- P48551
- Uniprot Name
- Interferon alpha/beta receptor 2
- Molecular Weight
- 57758.24 Da
References
- Dhalluin C, Ross A, Huber W, Gerber P, Brugger D, Gsell B, Senn H: Structural, kinetic, and thermodynamic analysis of the binding of the 40 kDa PEG-interferon-alpha2a and its individual positional isomers to the extracellular domain of the receptor IFNAR2. Bioconjug Chem. 2005 May-Jun;16(3):518-27. [Article]
- Yano H, Ogasawara S, Momosaki S, Akiba J, Kojiro S, Fukahori S, Ishizaki H, Kuratomi K, Basaki Y, Oie S, Kuwano M, Kojiro M: Growth inhibitory effects of pegylated IFN alpha-2b on human liver cancer cells in vitro and in vivo. Liver Int. 2006 Oct;26(8):964-75. [Article]
- Ishii K, Shinohara M, Sawa M, Kogame M, Higami K, Sano M, Morita T, Sumino Y: Interferon alpha receptor 2 expression by peripheral blood monocytes in patients with a high viral load of hepatitis C virus genotype 1 showing substitution of amino Acid 70 in the core region. Intervirology. 2010;53(2):105-10. doi: 10.1159/000264200. Epub 2009 Dec 3. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Together with IFNAR2, forms the heterodimeric receptor for type I interferons (including interferons alpha, beta, epsilon, omega and kappa) (PubMed:10049744, PubMed:14532120, PubMed:15337770, PubMed:2153461, PubMed:21854986, PubMed:24075985, PubMed:31270247, PubMed:33252644, PubMed:35442418, PubMed:7813427). Type I interferon binding activates the JAK-STAT signaling cascade, resulting in transcriptional activation or repression of interferon-regulated genes that encode the effectors of the interferon response (PubMed:10049744, PubMed:21854986, PubMed:7665574). Mechanistically, type I interferon-binding brings the IFNAR1 and IFNAR2 subunits into close proximity with one another, driving their associated Janus kinases (JAKs) (TYK2 bound to IFNAR1 and JAK1 bound to IFNAR2) to cross-phosphorylate one another (PubMed:21854986, PubMed:32972995, PubMed:7665574, PubMed:7813427). The activated kinases phosphorylate specific tyrosine residues on the intracellular domains of IFNAR1 and IFNAR2, forming docking sites for the STAT transcription factors (PubMed:21854986, PubMed:32972995, PubMed:7526154, PubMed:7665574, PubMed:7813427). STAT proteins are then phosphorylated by the JAKs, promoting their translocation into the nucleus to regulate expression of interferon-regulated genes (PubMed:19561067, PubMed:21854986, PubMed:32972995, PubMed:7665574, PubMed:7813427, PubMed:9121453). Can also act independently of IFNAR2: form an active IFNB1 receptor by itself and activate a signaling cascade that does not involve activation of the JAK-STAT pathway (By similarity)
- Specific Function
- Cytokine binding
- Gene Name
- IFNAR1
- Uniprot ID
- P17181
- Uniprot Name
- Interferon alpha/beta receptor 1
- Molecular Weight
- 63524.81 Da
References
- Dhalluin C, Ross A, Huber W, Gerber P, Brugger D, Gsell B, Senn H: Structural, kinetic, and thermodynamic analysis of the binding of the 40 kDa PEG-interferon-alpha2a and its individual positional isomers to the extracellular domain of the receptor IFNAR2. Bioconjug Chem. 2005 May-Jun;16(3):518-27. [Article]
- Yano H, Ogasawara S, Momosaki S, Akiba J, Kojiro S, Fukahori S, Ishizaki H, Kuratomi K, Basaki Y, Oie S, Kuwano M, Kojiro M: Growth inhibitory effects of pegylated IFN alpha-2b on human liver cancer cells in vitro and in vivo. Liver Int. 2006 Oct;26(8):964-75. [Article]
- Ishii K, Shinohara M, Sawa M, Kogame M, Higami K, Sano M, Morita T, Sumino Y: Interferon alpha receptor 2 expression by peripheral blood monocytes in patients with a high viral load of hepatitis C virus genotype 1 showing substitution of amino Acid 70 in the core region. Intervirology. 2010;53(2):105-10. doi: 10.1159/000264200. Epub 2009 Dec 3. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:19965576, PubMed:9435160). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:19965576, PubMed:9435160). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:11555828, PubMed:12865317). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2 (PubMed:11555828, PubMed:12865317). Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). May act as a major enzyme for all-trans retinoic acid biosynthesis in the liver. Catalyzes two successive oxidative transformation of all-trans retinol to all-trans retinal and then to the active form all-trans retinoic acid (PubMed:10681376). Primarily catalyzes stereoselective epoxidation of the last double bond of polyunsaturated fatty acids (PUFA), displaying a strong preference for the (R,S) stereoisomer (PubMed:19965576). Catalyzes bisallylic hydroxylation and omega-1 hydroxylation of PUFA (PubMed:9435160). May also participate in eicosanoids metabolism by converting hydroperoxide species into oxo metabolites (lipoxygenase-like reaction, NADPH-independent) (PubMed:21068195). Plays a role in the oxidative metabolism of xenobiotics. Catalyzes the N-hydroxylation of heterocyclic amines and the O-deethylation of phenacetin (PubMed:14725854). Metabolizes caffeine via N3-demethylation (Probable)
- Specific Function
- Aromatase activity
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58406.915 Da
References
- Begre S, von Bardeleben U, Ladewig D, Jaquet-Rochat S, Cosendai-Savary L, Golay KP, Kosel M, Baumann P, Eap CB: Paroxetine increases steady-state concentrations of (R)-methadone in CYP2D6 extensive but not poor metabolizers. J Clin Psychopharmacol. 2002 Apr;22(2):211-5. [Article]
- Peg-interferon FDA label [File]
Drug created at June 13, 2005 13:24 / Updated at September 15, 2024 21:55