|Accession Number||DB00044 (BTD00056, BIOD00056)|
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 chemical formula||C1014H1609N287O294S27|
|Protein average weight||30000.0 Da|
>Alpha Chain APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCC VAKSYNRVTVMGGFKVENHTACHCSTCYYHKS
>Beta Chain (LH) SREPLRPWCHPINAILAVEKEGCPVCITVNTTICAGYCPTMMRVLQAVLPPLPQVVCTYR DVRFESIRLPGCPRGVDPVVSFPVALSCRCGPCRRSTSDCGGPKDHPLTCDHPQLSGLLF LDownload FASTA Format
|External IDs||Not Available|
|Product Ingredients||Not Available|
|Approved Prescription Products|
|Approved Generic Prescription Products||Not Available|
|Approved Over the Counter Products||Not Available|
|Unapproved/Other Products||Not Available|
|International Brands||Not Available|
For treatment of infertility in women with hypothalamic or pituitary insufficiency (hypogonadotropic hypogonadism) and profound LH deficiency (LH <1.2 international units [IU]/L)
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. 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 action|
Luteinizing 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.
Mean 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 binding||Not Available|
<5% of dose excreted renally as unchanged drug.
|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.
Biphasic; terminal half-life is approximately 18 hours.
Lutropin 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.
|Pharmacogenomic Effects/ADRs||Not Available|
|Drug Interactions||No interactions found.|
|Food Interactions||Not Available|
|Synthesis Reference||Not Available|
|ATC Codes||G03GA07 — Lutropin alfa|
|FDA label||Download (218 KB)|
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
|Super Class||Organic Acids|
|Class||Carboxylic Acids and Derivatives|
|Sub Class||Amino Acids, Peptides, and Analogues|
|Alternative Parents||Not Available|
|Molecular Framework||Not Available|
|External Descriptors||Not Available|
- Pharmacological action
- 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:
- Uniprot ID:
- Uniprot Name:
- Lutropin-choriogonadotropic hormone receptor
- Molecular Weight:
- 78642.01 Da
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- Gibreel A, Bhattacharya S: Recombinant follitropin alfa/lutropin alfa in fertility treatment. Biologics. 2010 Feb 4;4:5-17. [PubMed:20161981 ]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]