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
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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- 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 agonistHumans - 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
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- 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
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Luveris Injection, powder, for solution 75 IU Subcutaneous Merck Europe B.V. 2021-02-11 Not applicable EU Luveris Injection, powder, for solution 75 IU Subcutaneous Merck Europe B.V. 2021-02-11 Not applicable EU Luveris Powder, for solution 75 unit / vial Subcutaneous Emd Serono, A Division Of Emd Inc., Canada 2005-06-28 Not applicable Canada Luveris Injection, powder, for solution 75 IU Subcutaneous Merck Europe B.V. 2021-02-11 Not applicable EU Luveris Injection, powder, for solution 75 IU Subcutaneous Merck Europe B.V. 2021-02-11 Not applicable EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Pergoveris Lutropin alfa (75 IU) + Follitropin (150 IU) Injection, powder, for solution Subcutaneous Merck Europe B.V. 2016-09-20 Not applicable EU PERGOVERIS Lutropin alfa (150 UI) + Follitropin (300 UI) Injection, solution Subcutaneous Merck Europe B.V. 2018-08-31 Not applicable Italy PERGOVERIS Lutropin alfa (75 UI) + Follitropin (150 UI) Powder Parenteral; Subcutaneous Merck Europe B.V. 2014-07-08 Not applicable Italy 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 Canada Pergoveris Lutropin alfa (450 IU) + Follitropin (900 IU) Injection, solution Subcutaneous Merck Europe B.V. 2020-12-21 Not applicable EU
Categories
- ATC Codes
- G03GA07 — Lutropin alfa
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
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
- 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 US
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
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- 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