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Identification
NameLutropin alfa
Accession NumberDB00044  (BTD00056, BIOD00056)
TypeBiotech
GroupsApproved
Description

Lutropin alfa is a recombinant human luteinizing hormone produced in yeast with 2 subunits, alpha = 92 residues, beta = 121 residues. It is a heterodimeric glycoprotein. Each monomeric unit is a glycoprotein molecule. In females, an acute rise of LH (“LH surge”) triggers ovulation and the development of the corpus luteum. In males, it stimulates Leydig cell production of testosterone. Lutropin alfa was the first and only recombinant human form of luteinizing hormone (LH) developed for use in the stimulation of follicular development.

Protein structureDb00044
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Protein chemical formulaC1014H1609N287O294S27
Protein average weight30000.0 Da
Sequences
>Alpha Chain
APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCC
VAKSYNRVTVMGGFKVENHTACHCSTCYYHKS
>Beta Chain (LH)
SREPLRPWCHPINAILAVEKEGCPVCITVNTTICAGYCPTMMRVLQAVLPPLPQVVCTYR
DVRFESIRLPGCPRGVDPVVSFPVALSCRCGPCRRSTSDCGGPKDHPLTCDHPQLSGLLF
L
Download FASTA Format
Synonyms
ICSH
Insterstiial cell-stimulating hormone
LH
LH-B
LSH- beta
LSH-B
Luteinizing hormone
Luteinizing hormone beta subunit
Lutrophin
Lutropin alpha
Lutropin beta chain precursor
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Luverispowder for solution75 unitsubcutaneousEmd Serono A Division Of Emd Inc Canada2005-06-28Not applicableCanada
Luverissolution450 unitsubcutaneousEmd Serono A Division Of Emd Inc CanadaNot applicableNot applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
Humegon Inj 75 I.U.Organon Canada Ltd Ltee
Pergonal 75 I.U.Emd Serono A Division Of Emd Inc Canada
PergoverisEmd Serono A Division Of Emd Inc Canada
SaltsNot Available
Categories
UNII3JGY52XJNA
CAS number152923-57-4
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 treatment of infertility in women with hypothalamic or pituitary insufficiency (hypogonadotropic hypogonadism) and profound LH deficiency (LH <1.2 international units [IU]/L)
PharmacodynamicsUsed to facilitate female conception, lutropin alfa performs the same actions as luteinizing hormone (LH), which is normally produced in the pituitary gland. Lutropin is usually given in combination with follitropin alfa. Together they stimulate the development of a follicle to prepare the reproductive tract for implementation and pregnancy. Lutropin alfa also stimulates the theca cells to produce androgens and the secretion of estradiol by the follicles. Lutropin alfa and follitropin alfa are discontinued once ultrasound assessment and serum estradiol concentrations show sufficient follicular maturation. hCG is then administered to complete follicular maturation and induce ovulation. In females, a LH surge about halfway through the menstrual cycle triggers the onset of ovulation. Lutropin alfa substitutes for endogenous LH and induces rupture of the preovulatory ovarian follicle and oocyte expulsion. Lutropin alfa induces and maintains the corpus luteum, which then secretes progesterone.
Mechanism of actionLuteinizing hormone binds to a receptor shared with the human chorionic gonadotropin hormone (hCG) on the ovarian theca (and granulosa) cells and testicular Leydig cells. This LH/CG transmembrane receptor is a member of the super-family of G protein-coupled receptors. Adenylate cyclase then activates many other pathways leading to steroid hormone production and other follicle maturation processes.
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AbsorptionMean absolute bioavailability is 56%, following sub-Q administration, maximum serum concentrations reached after 4–16 hours. Time to peak, serum: 9 hours
Volume of distribution

The steady state volume of distribution is around 10-14 L.

Protein bindingNot Available
Metabolism

<5% of dose excreted renally as unchanged drug.

Route of eliminationTotal body clearance is approximately 2 to 3 L/h with less than 5 percent of the dose being excreted unchanged renally.
Half lifeBiphasic; terminal half-life is approximately 18 hours.
Clearance
  • 2 – 3 L/h [healthy female following subcutaneous administration]
ToxicityLutropin alfa is not indicated for people under 16 and over 60, pregnant and lactating women, patients with uncontrolled thyroid and adrenal failure, patients with active, untreated tumours of the hypothalamus and pituitary gland, and in any patient with a condition that makes a normal pregnancy possible such as primary ovarian failure or fibroid tumors of the uterus.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
Manufacturers
  • Emd serono inc
Packagers
Dosage forms
FormRouteStrength
Liquid; powder for solutionintramuscular
Powder for solutionsubcutaneous75 unit
Solutionsubcutaneous450 unit
Powder for solutionintramuscular
Kit; powder for solutionsubcutaneous
Prices
Unit descriptionCostUnit
Luveris 75 unit vial38.88USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5767251 No1995-06-162015-06-16Us
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point55 °CForastieri, H., Ingham, K.C. J. Biol. Chem. 257:7976-7981 (1982)
hydrophobicity-0.063Not Available
isoelectric point8.44Not Available
References
Synthesis ReferenceNot Available
General References
  1. Blanchard J: Gastrointestinal absorption. I. Mechanisms. Am J Pharm Sci Support Public Health. 1975 Sep-Oct;147(5):135-46. [PubMed:3972 ]
  2. Louvet JP, Harman SM, Ross GT: Effects of human chorionic gonadotropin, human interstitial cell stimulating hormone and human follicle-stimulating hormone on ovarian weights in estrogen-primed hypophysectomized immature female rats. Endocrinology. 1975 May;96(5):1179-86. [PubMed:1122882 ]
  3. Nielsen MS, Barton SD, Hatasaka HH, Stanford JB: Comparison of several one-step home urinary luteinizing hormone detection test kits to OvuQuick. Fertil Steril. 2001 Aug;76(2):384-7. [PubMed:11476792 ]
  4. Gibreel A, Bhattacharya S: Recombinant follitropin alfa/lutropin alfa in fertility treatment. Biologics. 2010 Feb 4;4:5-17. [PubMed:20161981 ]
  5. Dhillon S, Keating GM: Lutropin alfa. Drugs. 2008;68(11):1529-40. [PubMed:18627209 ]
  6. Link [Link]
External Links
ATC CodesG03GA07
AHFS Codes
  • 68:18.00
PDB Entries
FDA labelDownload (218 KB)
MSDSNot Available
Interactions
Drug InteractionsNo interactions found.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Luteinizing hormone receptor activity
Specific Function:
Receptor for lutropin-choriogonadotropic hormone. The activity of this receptor is mediated by G proteins which activate adenylate cyclase.
Gene Name:
LHCGR
Uniprot ID:
P22888
Molecular Weight:
78642.01 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. Gibreel A, Bhattacharya S: Recombinant follitropin alfa/lutropin alfa in fertility treatment. Biologics. 2010 Feb 4;4:5-17. [PubMed:20161981 ]
  4. 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 March 14, 2016 09:57