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Identification
NameThyrotropin Alfa
Accession NumberDB00024  (BTD00020, BIOD00020)
TypeBiotech
GroupsApproved, Vet Approved
Description

Thyrotropin alfa is a recombinant form of thyroid stimulating hormone used in performing certain tests in patients who have or have had thyroid cancer. It is also used along with a radioactive agent to destroy remaining thyroid tissue in certain patients who have had their thyroid gland removed because of thyroid cancer. It is a heterodimeric glycoprotein comprised of two non-covalently linked subunits, an alpha subunit of 92 amino acid residues containing two N-linked glycosylation sites and a beta subunit of 112 residues containing one N-linked glycosylation site. The alpha subunit is nearly identical to that of human chorionic gonadotropin (hCG), luteinizing hormone (LH), and follicle-stimulating hormone (FSH). The alpha subunit is thought to be the effector region responsible for stimulation of adenylate cyclase (involved the generation of cAMP). The beta subunit (TSHB) is unique to TSH, and therefore determines its receptor specificity. The amino acid sequence of thyrotropin alfa is identical to that of human pituitary thyroid stimulating hormone.

Protein structureDb00024
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Protein chemical formulaC975H1513N267O304S26
Protein average weight22672.9 Da
Sequences
>Alpha chain
APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCC
VAKSYNRVTVMGGFKVENHTACHCSTCYYHKS
>Beta chain
FCIPTEYTMHIERRECAYCLTINTTICAGYCMTRDINGKLFLPKYALSQDVCTYRDFIYR
TVEIPGCPLHVAPYFSYPVALSCKCGKCNTDYSDCIHEAIKTNYCTKPQKSY
Download FASTA Format
Synonyms
rTSH
Thyroid stimulating hormone
Thyrotrophin-alfa
Thyrotrophin-alpha
Thyrotropin
Thyrotropin-a
Thyrotropin-alpha
Thytrophin
TSH
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Thyrogeninjection, powder, for solution.9 mg/mLintramuscularGenzyme Corporation1998-11-302016-04-05Us
Thyrogenpowder for solution0.9 mgintramuscularGenzyme Canada A Division Of Sanofi Aventis Canada Inc2002-08-12Not applicableCanada
ThyrogenkitGenzyme Corporation1998-11-302016-04-05Us
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII02KSI6Z9AK
CAS number194100-83-9
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
Pharmacology
IndicationFor detection of residueal or recurrent thyroid cancer
PharmacodynamicsBinding of thyrotropin alfa to TSH receptors on normal thyroid epithelial cells or on well-differentiated thyroid cancer tissue stimulates iodine uptake and organification. Thyrogen is an exogenous source of human TSH that offers an additional diagnostic tool in the follow-up of patients with a history of well-differentiated thyroid cancer.
Mechanism of actionThyrotropin Alfa binds to the thyrotropin receptors found on any residual thyroid cells or tissues. This stimulates radioactive iodine uptake for better radiodiagnostic imaging.
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AbsorptionTime to peak: Median: 10 hours (range: 3-24 hours) After a single intramuscular injection of 0.9 mg of thyrotropin alfa: Cmax= 116+38mU/L, Tmax=22+8.5 hours. AUC=5088+1728 mU·hr/L.
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationkidney and liver
Half life25 ± 10 hours
ClearanceNot Available
ToxicityNo difference in efficacy and toxicity between adult and geriatric patients. No studies in lactating women, pregnant women and pediatrics. Cautionary administration is advised.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
Manufacturers
  • Sanofi aventis us llc
  • Genzyme corp
Packagers
Dosage forms
FormRouteStrength
Injection, powder, for solutionintramuscular.9 mg/mL
Kit
Powder for solutionintramuscular0.9 mg
Prices
Unit descriptionCostUnit
Thyrogen 1.1 mg vial1196.4USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5840566 No1995-11-242015-11-24Us
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point55 °CNot Available
hydrophobicity-0.330Not Available
isoelectric point7.50Not Available
References
Synthesis Reference

19366632

General References
  1. Lexicomp
    #Product label
External Links
ATC CodesH01AB01V04CJ01
AHFS Codes
  • 36:60.00
PDB Entries
FDA labelDownload (2.27 MB)
MSDSNot Available
Interactions
Drug InteractionsNo interactions found.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Thyroid-stimulating hormone receptor activity
Specific Function:
Receptor for thyrothropin. Plays a central role in controlling thyroid cell metabolism. The activity of this receptor is mediated by G proteins which activate adenylate cyclase. Also acts as a receptor for thyrostimulin (GPA2+GPB5).
Gene Name:
TSHR
Uniprot ID:
P16473
Molecular Weight:
86828.965 Da
References
  1. Szkudlinski MW: Recombinant human thyrotropins of the twenty-first century. Expert Opin Pharmacother. 2004 Dec;5(12):2435-40. [PubMed:15571461 ]
  2. Conway GS: Clinical manifestations of genetic defects affecting gonadotrophins and their receptors. Clin Endocrinol (Oxf). 1996 Dec;45(6):657-63. [PubMed:9039330 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
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Drug created on June 13, 2005 07:24 / Updated on May 02, 2016 15:21