Lutropin alfa

Identification

Summary

Lutropin alfa is a form of recombinant human luteinizing hormone used to treat female infertility due to hypothalamic or pituitary insufficiency, or due to profound luteinizing hormone deficiency.

Brand Names

Luveris, Pergoveris

Generic Name

Lutropin alfa

DrugBank Accession Number

DB00044

Background

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 made up of monomeric units. Lutropin alfa was the first and only recombinant human form of luteinizing hormone (LH) developed for use in the stimulation of follicular development. Its pharmacological action mimics the biological activity of endogenous LH; an acute rise of LH, or LH surge, in females triggers ovulation and the development of the corpous luteum. In males, LH stimulates Leydig cell to produce testosterone.

Type

Biotech

Groups

Approved

Biologic Classification

Protein Based Therapies
Hormones

Protein Structure

Protein Chemical Formula: C₁₀₁₄H₁₆₀₉N₂₈₇O₂₉₄S₂₇
Protein Average Weight: 30000.0 Da

Sequences

>Alpha Chain
APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCC
VAKSYNRVTVMGGFKVENHTACHCSTCYYHKS

>Beta Chain (LH)
SREPLRPWCHPINAILAVEKEGCPVCITVNTTICAGYCPTMMRVLQAVLPPLPQVVCTYR
DVRFESIRLPGCPRGVDPVVSFPVALSCRCGPCRRSTSDCGGPKDHPLTCDHPQLSGLLF
L

Download FASTA Format

Synonyms

Lutropin alfa
Lutropin alpha
Lutropina alfa

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Pharmacology

Indication

For treatment of infertility in women with hypothalamic or pituitary insufficiency (hypogonadotropic hypogonadism) and profound LH deficiency (LH <1.2 international units [IU]/L)

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Contraindications & Blackbox Warnings

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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. 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.

Target	Actions	Organism
ALutropin-choriogonadotropic hormone receptor	agonist	Humans

Absorption

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

Metabolism

<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.

Half-life

Biphasic; terminal half-life is approximately 18 hours.

Clearance

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

Adverse Effects

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Toxicity

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.

Pathways

Not Available

Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">

Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">: This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
No interactions found.
Food Interactions: No interactions found.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Luveris	Injection, powder, for solution	75 IU	Subcutaneous	Merck Europe B.V.	2021-02-11	Not applicable
Luveris	Injection, powder, for solution	75 IU	Subcutaneous	Merck Europe B.V.	2021-02-11	Not applicable
Luveris	Powder, for solution	75 unit / vial	Subcutaneous	Emd Serono, A Division Of Emd Inc., Canada	2005-06-28	Not applicable
Luveris	Injection, powder, for solution	75 IU	Subcutaneous	Merck Europe B.V.	2021-02-11	Not applicable
Luveris	Injection, powder, for solution	75 IU	Subcutaneous	Merck Europe B.V.	2021-02-11	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Pergoveris	Lutropin alfa (75 IU) + Follitropin (150 IU)	Injection, powder, for solution	Subcutaneous	Merck Europe B.V.	2016-09-20	Not applicable
PERGOVERIS	Lutropin alfa (150 UI) + Follitropin (300 UI)	Injection, solution	Subcutaneous	Merck Europe B.V.	2018-08-31	Not applicable
PERGOVERIS	Lutropin alfa (75 UI) + Follitropin (150 UI)	Powder	Parenteral; Subcutaneous	Merck Europe B.V.	2014-07-08	Not applicable
Pergoveris	Lutropin alfa (150 unit / 0.48 mL) + Follitropin (300 unit / 0.48 mL)	Solution	Subcutaneous	Emd Serono, A Division Of Emd Inc., Canada	2021-10-21	Not applicable
Pergoveris	Lutropin alfa (450 IU) + Follitropin (900 IU)	Injection, solution	Subcutaneous	Merck Europe B.V.	2020-12-21	Not applicable

Chemical Identifiers

UNII: 3JGY52XJNA
CAS number: 152923-57-4

References

General References

Blanchard J: Gastrointestinal absorption. I. Mechanisms. Am J Pharm Sci Support Public Health. 1975 Sep-Oct;147(5):135-46. [Article]
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. [Article]
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. [Article]
Gibreel A, Bhattacharya S: Recombinant follitropin alfa/lutropin alfa in fertility treatment. Biologics. 2010 Feb 4;4:5-17. [Article]
Dhillon S, Keating GM: Lutropin alfa. Drugs. 2008;68(11):1529-40. [Article]

External Links

UniProt: P01229
Genbank: X00264
PubChem Substance: 46507624
RxNav: 388084
ChEMBL: CHEMBL1201419
Therapeutic Targets Database: DAP001103
PharmGKB: PA164750539
Drugs.com: Drugs.com Drug Page
Wikipedia: Luteinizing_hormone

FDA label

Download (218 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Completed	Prevention	Infertility	1
4	Completed	Treatment	Female Infertility	1
4	Completed	Treatment	In Vitro Fertilization (IVF) / Infertility	1
4	Completed	Treatment	Infertility	2
4	Completed	Treatment	Infertility / Progesterone Levels	1

Pharmacoeconomics

Manufacturers

Emd serono inc

Packagers

EMD Canada Inc.
Merck Serono SPA

Dosage Forms

Form	Route	Strength
Solution	Parenteral	75 UI
Injection, powder, for solution	Parenteral; Subcutaneous	75 IU/ML
Injection, solution	Subcutaneous	450 UI
Kit	Subcutaneous	82.5 [iU]/1mL
Powder, for solution	Subcutaneous	75 unit / vial
Solution	Subcutaneous	450 unit / 0.72 mL
Injection, powder, for solution		75 iu/1vial
Injection, powder, lyophilized, for solution	Subcutaneous
Injection, solution	Subcutaneous	75 iu
Injection, powder, for solution	Subcutaneous	75 iu
Injection, powder, for solution	Subcutaneous
Kit; powder, for solution	Subcutaneous
Powder	Parenteral; Subcutaneous
Solution	Subcutaneous
Injection	Subcutaneous
Injection, powder, for solution	Subcutaneous	150 IU
Injection, solution	Subcutaneous

Prices

Unit description	Cost	Unit
Luveris 75 unit vial	38.88USD	vial

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US5767251	No	1998-06-16	2015-06-16

Properties

State

Liquid

Experimental Properties

Property	Value	Source
melting point (°C)	55 °C	Forastieri, H., Ingham, K.C. J. Biol. Chem. 257:7976-7981 (1982)
hydrophobicity	-0.063	Not Available
isoelectric point	8.44	Not Available

Targets

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Details1. Lutropin-choriogonadotropic hormone receptor

Kind: Protein
Organism: Humans
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
Uniprot Name: Lutropin-choriogonadotropic hormone receptor
Molecular Weight: 78642.01 Da

References

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

Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55

Lutropin alfa

Identification

Pharmacology

Interactions

Products

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Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

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References