DrugBank: Lutropin alfa (DB00044)

targets (1)

Identification

Name

Lutropin alfa

Accession Number

DB00044 (BIOD00056, BTD00056)

Type

biotech

Groups

approved

Description

Recombinant human luteinizing hormone produced in yeast with 2 subunits, alpha = 92 residues, beta = 121 residues

Protein structure

Protein chemical formula

C₁₀₁₄H₁₆₀₉N₂₈₇O₂₉₄S₂₇

Protein average weight

23390.3000

Sequences

>AlphaChain
APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCC
VAKSYNRVTVMGGFKVENHTACHCSTCYYHKS

>BetaChain (LH)
SREPLRPWCHPINAILAVEKEGCPVCITVNTTICAGYCPTMMRVLQAVLPPLPQVVCTYR
DVRFESIRLPGCPRGVDPVVSFPVALSCRCGPCRRSTSDCGGPKDHPLTCDHPQLSGLLF
L

FASTA

Synonyms

LH-B
LSH- beta
LSH-B
Luteinizing hormone beta subunit
Lutropin beta chain precursor

Brand names

Luveris (Serono)

Brand name mixtures

Not Available

Categories

Fertility Agents

CAS number

152923-57-4

Taxonomy

Kingdom

Not Available

Classes

Not Available

Substructures

Not Available

Pharmacology

Indication

For treatment of female infertility

Pharmacodynamics

Used 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. In females, a LH surge about halfway through the menstrual cycle triggers the onset of ovulation. LH also induces the ovulated follicle to become a corpus luteum, which then secretes progesterone.

Mechanism of action

Binds to the luteinizing hormone receptor which then activates adenylate cylcase through G protein mediation. Adenylate cyclase then activates many other pathways leading to steroid hormone production and other follicle maturation processes.

Absorption

Not Available

Volume of distribution

10 L

Protein binding

Not Available

Metabolism

Route of elimination

Total body clearance is approximately 2 to 3 L/h with less than 5 percent of the dose being excreted unchanged renally.

Half life

4.4 hours (mammalian reticulocytes, in vitro)

Clearance

2 – 3 L/h [healthy female following subcutaneous administration]

Toxicity

Not Available

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacoeconomics

Manufacturers

Emd serono inc

Packagers

Dosage forms

Form	Route	Strength
Powder, for solution	Subcutaneous

Prices

Unit description	Cost	Unit
Luveris 75 unit vial	38.88 USD	vial

Patents

Country	Patent Number	Approved	Expires
United States	5767251	1995-06-16	2015-06-16

Properties

State

liquid

Melting point

55 oC (Forastieri, H., Ingham, K.C. J. Biol. Chem. 257:7976-7981 (1982))

Experimental Properties

Property	Value	Source
hydrophobicity	-0.063	PhysProp
isoelectric point	8.44	Various sources

References

Synthesis Reference

Not Available

General Reference

Blanchard J: Gastrointestinal absorption. I. Mechanisms. Am J Pharm Sci Support Public Health. 1975 Sep-Oct;147(5):135-46. Pubmed
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
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
Gibreel A, Bhattacharya S: Recombinant follitropin alfa/lutropin alfa in fertility treatment. Biologics. 2010 Feb 4;4:5-17. Pubmed

External Links

Resource	Link
UniProt	P01229
Genbank	X00264
PharmGKB	PA10306
Drug Product Database	2269066
Drugs.com	http://www.drugs.com/cdi/lutropin-alfa.html
Wikipedia	http://en.wikipedia.org/wiki/Lutropin_alfa

ATC Codes

G03GA07

AHFS Codes

68:18.00

PDB Entries

Not Available

FDA label

show (218 KB)

MSDS

Not Available

Interactions

Drug Interactions

Drug	Interaction

Food Interactions

Not Available

Targets
1. Lutropin-choriogonadotropic hormone receptor Pharmacological action: yes Actions: agonist Receptor for lutropin-choriogonadotropic hormone. The activity of this receptor is mediated by G proteins which activate adenylate cyclase Organism class: human UniProt ID: P22888 Gene: LHCGR Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References: Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed 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 Gibreel A, Bhattacharya S: Recombinant follitropin alfa/lutropin alfa in fertility treatment. Biologics. 2010 Feb 4;4:5-17. Pubmed Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

Targets

1. Lutropin-choriogonadotropic hormone receptor

Pharmacological action: yes
Actions: agonist

Receptor for lutropin-choriogonadotropic hormone. The activity of this receptor is mediated by G proteins which activate adenylate cyclase

Organism class: human
UniProt ID: P22888 Link_out

Gene: LHCGR Link_out

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
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
Gibreel A, Bhattacharya S: Recombinant follitropin alfa/lutropin alfa in fertility treatment. Biologics. 2010 Feb 4;4:5-17. Pubmed
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

Comments

Drug created on June 13, 2005 07:24 / Updated on August 04, 2011 22:55

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.