Identification
NameInterferon Alfa-2b, Recombinant
Accession NumberDB00105  (BTD00066, BIOD00066, DB05600)
TypeBiotech
GroupsApproved
Description

Interferon alpha 2b (human leukocyte clone hif-sn 206 protein moiety reduced). A type I interferon consisting of 165 amino acid residues with arginine 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.

Protein structureDb00105
Related Articles
Protein chemical formulaC860H1353N229O255S9
Protein average weight19271.0 Da
Sequences
>DB00105 sequence
CDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMI
QQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMNEDSILAVR
KYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE
Download FASTA Format
Synonyms
Interferon alfa-2b
Interferon α-2b
Intron (Interferon α2b)
Intron A
Intron A (Interferon α2b)
rIFN-alpha-2b
External IDs 99210-65-8 / Sch 30500 / YM 14090
Product Ingredients Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Intron AKitMerck Sharp & Dohme Limited1986-06-04Not applicableUs
Intron AInjection, solution19.2 ug/.5mLIntralesional; Intramuscular; SubcutaneousMerck Sharp & Dohme Limited1986-06-04Not applicableUs
Intron AKitMerck Sharp & Dohme Limited2014-08-11Not applicableUs
Intron ASolution6000000 unitIntramuscular; Intravenous; SubcutaneousMerck Ltd.1998-12-10Not applicableCanada
Intron ALiquid25000000 unitSubcutaneousMerck Ltd.1999-09-23Not applicableCanada
Intron AKitMerck Sharp & Dohme Limited1986-06-04Not applicableUs
Intron AInjection, solution11.6 ug/.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1986-06-04Not applicableUs
Intron AKitMerck Sharp & Dohme Limited2014-08-11Not applicableUs
Intron ASolution10000000 unitIntramuscular; Intravenous; SubcutaneousMerck Ltd.1998-12-10Not applicableCanada
Intron ALiquid50000000 unitSubcutaneousMerck Ltd.1999-09-23Not applicableCanada
Intron AKitMerck Sharp & Dohme Limited1986-06-04Not applicableUs
Intron AKitMerck Sharp & Dohme Limited2014-08-11Not applicableUs
Intron ALiquid15000000 unitSubcutaneousMerck Ltd.1999-09-23Not applicableCanada
Intron A - Liq 5000000iu/mlLiquid5000000 unitIntralesional; Intramuscular; SubcutaneousSchering Plough (Brinny) Co.1997-09-252001-07-18Canada
Intron A Inj 10000000unit/vialLiquid10000000 unitSubcutaneousAvondale (Brinny) Chemical Company1986-12-311999-07-22Canada
Intron A Inj 3000000unit/vialLiquid3000000 unitSubcutaneousAvondale (Brinny) Chemical Company1986-12-311999-07-22Canada
Intron A Inj 5000000unit/vialLiquid5000000 unitSubcutaneousAvondale (Brinny) Chemical Company1986-12-311999-07-22Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
LocteronNot Available
Brand mixtures
NameLabellerIngredients
Intron AMerck Ltd.
Intron A - Kit (pws+diluent) 3000000iu/vialSchering Plough (Brinny) Co.
Intron A - Kit (pws+diluent) 5000000iu/vialSchering Plough (Brinny) Co.
Rebetron Ready To Use Solution (albumin(human)free) (6000000 Iu/ml and 200mg Capsules)Schering Plough
Rebetron Solution (albumin (human) Free) (18 Miu Multi-dose Pen / 200mg Capsules)Schering Plough
Categories
UNII43K1W2T1M6
CAS number98530-12-2
Pharmacology
Indication

For the treatment of hairy cell leukemia, malignant melanoma, and AIDS-related Kaposi's sarcoma.

Structured Indications
Pharmacodynamics

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.

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.

TargetKindPharmacological actionActionsOrganismUniProt ID
Interferon alpha/beta receptor 2Proteinyes
binder
HumanP48551 details
Interferon alpha/beta receptor 1Proteinyes
binder
HumanP17181 details
Related Articles
Absorption

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

Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half life

The elimination half-life following both intramuscular and subcutaneous injections was approximately 2 to 3 hours. The elimination half-life was approximately 2 hours following intravenous injection.

ClearanceNot Available
Toxicity

There is limited experience with overdosage. Postmarketing surveillance includes reports of patients receiving a single dose as great as 10 times the recommended dose. In general, the primary effects of an overdose are consistent with the effects seen with therapeutic doses of interferon alfa-2b. Hepatic enzyme abnormalities, renal failure, hemorrhage, and myocardial infarction have been reported with single administration overdoses and/or with longer durations of treatment than prescribed. Toxic effects after ingestion of interferon alfa-2b are not expected because interferons are poorly absorbed orally.

Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
AldesleukinThe risk or severity of adverse effects can be increased when Interferon Alfa-2b, Recombinant is combined with Aldesleukin.Approved
Ambroxol acefyllinateThe metabolism of Ambroxol acefyllinate can be decreased when combined with Interferon Alfa-2b, Recombinant.Experimental
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Interferon Alfa-2b, Recombinant.Approved
DyphyllineThe metabolism of Dyphylline can be decreased when combined with Interferon Alfa-2b, Recombinant.Approved
MethadoneThe serum concentration of Methadone can be increased when it is combined with Interferon Alfa-2b, Recombinant.Approved
RibavirinThe risk or severity of adverse effects can be increased when Interferon Alfa-2b, Recombinant is combined with Ribavirin.Approved
TelbivudineThe risk or severity of adverse effects can be increased when Interferon Alfa-2b, Recombinant is combined with Telbivudine.Approved, Investigational
TheophyllineThe metabolism of Theophylline can be decreased when combined with Interferon Alfa-2b, Recombinant.Approved
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Interferon Alfa-2b, Recombinant.Approved
ZidovudineThe risk or severity of adverse effects can be increased when Interferon Alfa-2b, Recombinant is combined with Zidovudine.Approved
Food Interactions
  • Avoid alcohol.
References
Synthesis ReferenceNot Available
General References
  1. Radhakrishnan R, Walter LJ, Hruza A, Reichert P, Trotta PP, Nagabhushan TL, Walter MR: Zinc mediated dimer of human interferon-alpha 2b revealed by X-ray crystallography. Structure. 1996 Dec 15;4(12):1453-63. [PubMed:8994971 ]
External Links
ATC CodesL03AB05 — Interferon alfa-2b
AHFS Codes
  • 08:18.20
PDB Entries
FDA labelDownload (3.52 MB)
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentMelanoma2
1CompletedNot AvailableChronic Hepatitis C Infection1
1CompletedTreatmentAdult Solid Neoplasm1
1CompletedTreatmentBladder Cancers / Urethral Cancer1
1CompletedTreatmentCancer, Advanced / Tumors, Solid1
1CompletedTreatmentChronic Hepatitis C Infection / Human Immunodeficiency Virus (HIV) Infections1
1CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Kaposi s Sarcoma (KS)1
1CompletedTreatmentMelanoma2
1CompletedTreatmentRecurrent Melanoma / Recurrent Renal Cell Cancer / Stage III Melanoma / Stage IV Melanoma / Stage IV Renal Cell Cancer1
1RecruitingTreatmentSolid Cancers1
1, 2Active Not RecruitingTreatmentMelanoma1
1, 2CompletedTreatmentChronic Hepatitis C Virus Infection / Genotype 1 / Relapses / Treatment-Experienced Patients1
1, 2CompletedTreatmentMelanoma1
1, 2CompletedTreatmentRecurrent Ovarian Cancer1
1, 2RecruitingTreatmentBreastcancer / Neoplasms, Breast1
1, 2RecruitingTreatmentCarcinoma, Colorectal / Colorectal Cancers / Colorectal Tumors / Neoplasms, Colorectal1
1, 2RecruitingTreatmentMalignant Neoplasm of Pancreas Metastatic to Peritoneal Surface / Malignant Peritoneal Mesothelioma / Peritoneal Carcinomatosis1
1, 2TerminatedTreatmentMalignant Lymphomas / Precancerous/Nonmalignant Condition1
1, 2TerminatedTreatmentRenal Cell Adenocarcinoma1
1, 2WithdrawnTreatmentMelanoma1
2Active Not RecruitingTreatmentCiliary Body and Choroid Melanoma, Medium/Large Size / Ciliary Body and Choroid Melanoma, Small Size / Iris Melanoma / Recurrent Intraocular Melanoma1
2Active Not RecruitingTreatmentCutaneous Melanoma / Metastatic Melanoma1
2Active Not RecruitingTreatmentRecurrent Melanoma / Stage IIIA Skin Melanoma / Stage IIIB Skin Melanoma / Stage IIIC Skin Melanoma / Stage IV Skin Melanoma1
2CompletedTreatmentChronic Hepatitis C Infection1
2CompletedTreatmentClear Cell Renal Cell Carcinoma / Recurrent Renal Cell Cancer / Stage III Renal Cell Cancer / Stage IV Renal Cell Cancer1
2CompletedTreatmentClear Cell Renal Cell Carcinoma / Renal Cell Carcinoma Recurrent / Stage IV Renal Cell Cancer1
2CompletedTreatmentHepatitis C, Chronic1
2CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Kaposi s Sarcoma (KS)1
2CompletedTreatmentLeukemias1
2CompletedTreatmentLeukemias / Malignant Lymphomas / Unspecified Childhood Solid Tumor, Protocol Specific1
2CompletedTreatmentMalignant Neoplasm of Pancreas1
2CompletedTreatmentRecurrent Melanoma / Stage IV Melanoma1
2CompletedTreatmentRecurrent Renal Cell Cancer / Stage IV Renal Cell Cancer1
2CompletedTreatmentRefractory Multiple Myeloma / Stage I Multiple Myeloma / Stage II Multiple Myeloma / Stage III Multiple Myeloma1
2CompletedTreatmentRenal Cell Adenocarcinoma / Stage IV Renal Cell Cancer1
2RecruitingTreatmentMucosal Melanoma1
2TerminatedTreatmentClear Cell Renal Cell Carcinoma / Papillary Renal Cell Carcinoma / Recurrent Renal Cell Cancer / Stage III Renal Cell Cancer / Stage IV Renal Cell Cancer1
2TerminatedTreatmentLeukemias1
2TerminatedTreatmentMycosis Fungoides (MF) / Neoplasms, Hematologic / T-Cell Lymphomas1
2TerminatedTreatmentRecurrent Grade 1 Follicular Lymphoma / Recurrent Grade 2 Follicular Lymphoma1
2TerminatedTreatmentRenal Cell Adenocarcinoma1
2Unknown StatusTreatmentMetastatic Renal Cell Carcinoma1
2WithdrawnTreatmentCancer, Advanced / Tumors, Solid1
2WithdrawnTreatmentMalignant Melanoma / Melanoma1
2, 3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection1
3Active Not RecruitingTreatmentNeuroendocrine Carcinomas1
3Active Not RecruitingTreatmentRecurrent Melanoma / Stage IIIB Skin Melanoma / Stage IIIC Skin Melanoma / Stage IV Skin Melanoma1
3CompletedTreatmentLeukemia,Myeloid, Chronic1
3CompletedTreatmentMalignant Melanoma / Recurrent Melanoma1
3CompletedTreatmentMelanoma / Neoplasms Metastasis1
3CompletedTreatmentMelanoma / Skin Cancers1
3CompletedTreatmentStage I Multiple Myeloma / Stage II Multiple Myeloma / Stage III Multiple Myeloma1
3RecruitingTreatmentAnaplastic Astrocytoma (AA) / Anaplastic Oligoastrocytoma / Glioblastomas1
3RecruitingTreatmentMetastatic Non-Cutaneous Melanoma / Non-Cutaneous Melanoma / Recurrent Melanoma of the Skin / Recurrent Non-Cutaneous Melanoma / Stage III Mucosal Melanoma of the Head and Neck / Stage III Mucosal Melanoma of the Head and Neck AJCC v7 / Stage IIIA Skin Melanoma / Stage IIIB Skin Melanoma / Stage IIIC Skin Melanoma / Stage IV Skin Melanoma / Stage IVA Mucosal Melanoma of the Head and Neck / Stage IVA Mucosal Melanoma of the Head and Neck AJCC v7 / Stage IVB Mucosal Melanoma of the Head and Neck / Stage IVB Mucosal Melanoma of the Head and Neck AJCC v7 / Stage IVC Mucosal Melanoma of the Head and Neck / Stage IVC Mucosal Melanoma of the Head and Neck AJCC v7 / Stages III Skin Melanoma1
3TerminatedTreatmentHuman Immunodeficiency Virus (HIV) Infections1
3TerminatedTreatmentMelanoma (Skin)1
3WithdrawnTreatmentGastro-intestinal Neuroendocrine Tumors1
3WithdrawnTreatmentHypertrophic Scars / Minor burns1
4Active Not RecruitingTreatmentConjunctival Intraepithelial Neoplasia / Corneal Intraepithelial Neoplasia1
4Active Not RecruitingTreatmentHepatitis B,Chronic1
4RecruitingTreatmentLymphoma, T-Cell, Cutaneous / Mycosis Fungoides (MF)1
Not AvailableActive Not RecruitingTreatmentStage IA Skin Melanoma / Stage IB Skin Melanoma / Stage IIA Skin Melanoma / Stage IIB Skin Melanoma / Stage IIC Skin Melanoma / Stage IIIA Skin Melanoma / Stage IIIB Skin Melanoma / Stage IIIC Skin Melanoma / Stage IV Skin Melanoma1
Not AvailableCompletedNot AvailableMelanoma2
Not AvailableCompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Progressive Multifocal Leukoencephalopathy1
Not AvailableRecruitingTreatmentLeukemias1
Not AvailableTerminatedNot AvailableChronic Hepatitis C Infection / Hepatitis C, Chronic1
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, solutionIntralesional; Intramuscular; Subcutaneous19.2 ug/.5mL
Injection, solutionIntramuscular; Subcutaneous11.6 ug/.5mL
Kit
Kit; liquid; powder, for solutionIntralesional; Intramuscular; Intravenous; Subcutaneous
LiquidSubcutaneous15000000 unit
LiquidSubcutaneous25000000 unit
LiquidSubcutaneous50000000 unit
Liquid; powder, for solutionIntralesional; Intramuscular; Intravenous; Subcutaneous
SolutionIntramuscular; Intravenous; Subcutaneous10000000 unit
SolutionIntramuscular; Intravenous; Subcutaneous6000000 unit
Liquid; powder, for solutionIntralesional; Intramuscular; Subcutaneous
LiquidIntralesional; Intramuscular; Subcutaneous5000000 unit
LiquidSubcutaneous10000000 unit
LiquidSubcutaneous3000000 unit
LiquidSubcutaneous5000000 unit
Capsule; kit; liquidOral; Subcutaneous
Prices
Unit descriptionCostUnit
Intron-A 10000000 unit/0.2ml Kit (each Box Contains One 6 Dose 1.5ml Pen)1110.84USD box
Intron a 10 million unit pen1068.12USD pen
Intron-A 5000000 unit/0.2ml Kit Box683.34USD box
Intron a 5 million unit/ml pen657.06USD pen
Intron a 3 million unit/ml pen394.21USD pen
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1341567 No2008-02-192025-02-19Canada
CA2201749 No1999-06-152015-10-10Canada
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point (°C)61 °CBeldarrain, A. et al., Biochemistry 38:7865-7873 (1999)
hydrophobicity-0.339Not Available
isoelectric point5.99Not Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
binder
General Function:
Type i interferon receptor activity
Specific Function:
Associates with IFNAR1 to form the type I interferon receptor. Receptor for interferons alpha and beta. Involved in IFN-mediated STAT1, STAT2 and STAT3 activation. Isoform 1 and isoform 2 are directly involved in signal transduction due to their association with the TYR kinase, JAK1. Isoform 3 is a potent inhibitor of type I IFN receptor activity.
Gene Name:
IFNAR2
Uniprot ID:
P48551
Uniprot Name:
Interferon alpha/beta receptor 2
Molecular Weight:
57758.24 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Eid P, Tovey MG: Characterization of a domain of a human type I interferon receptor protein involved in ligand binding. J Interferon Cytokine Res. 1995 Mar;15(3):205-11. [PubMed:7584665 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
binder
General Function:
Type i interferon receptor activity
Specific Function:
Associates with IFNAR2 to form the type I interferon receptor. Receptor for interferons alpha and beta. Binding to type I IFNs triggers tyrosine phosphorylation of a number of proteins including JAKs, TYK2, STAT proteins and IFNR alpha- and beta-subunits themselves. Can also transduce IFNB signals without the help of IFNAR2, and not activating the Jak-STAT pathway.
Gene Name:
IFNAR1
Uniprot ID:
P17181
Uniprot Name:
Interferon alpha/beta receptor 1
Molecular Weight:
63524.81 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Khine AA, Lingwood CA: Functional significance of globotriaosyl ceramide in interferon-alpha(2)/type 1 interferon receptor-mediated antiviral activity. J Cell Physiol. 2000 Jan;182(1):97-108. [PubMed:10567921 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Uniprot Name:
Cytochrome P450 1A2
Molecular Weight:
58293.76 Da
Drug created on June 13, 2005 07:24 / Updated on June 26, 2017 20:37