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Showing drug card for Lutropin alfa (DB00044)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-02-19 16:03:19
Primary Accession Number DB00044
Secondary Accession Number
  • BIOD00056
  • BTD00056
Name Lutropin alfa
Drug Type
  • Approved
  • Biotech
Description Recombinant human luteinizing hormone produced in yeast with 2 subunits, alpha = 92 residues, beta = 121 residues
Synonyms
  1. LH-B
  2. LSH- beta
  3. LSH-B
  4. Luteinizing hormone beta subunit
  5. Lutropin beta chain precursor
Brand Names
  1. Luveris (Serono)
Brand Mixtures Not Available
Chemical IUPAC Name Human luteinizing hormone
Chemical Formula C1014H1609N287O294S27
Chemical Structure Structure
Protein Sequence(s) >AlphaChain 
APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCC
VAKSYNRVTVMGGFKVENHTACHCSTCYYHKS

>BetaChain (LH) 
SREPLRPWCHPINAILAVEKEGCPVCITVNTTICAGYCPTMMRVLQAVLPPLPQVVCTYR
DVRFESIRLPGCPRGVDPVVSFPVALSCRCGPCRRSTSDCGGPKDHPLTCDHPQLSGLLF
L
CAS Registry Number 152923-57-4
InChI Identifier Not Available
InChI Key Not Available
KEGG Drug Not Available
KEGG Compound Not Available
PubChem Compound Not Available
PubChem Substance Not Available
ChEBI ID Not Available
PharmGKB ID PA10306 Link Image
HET ID Not Available
GenBank ID X00264 Link Image
Drug ID Number [DIN] 02269066 Link Image
RxList Link Not Available
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Lutropin_alfa Link Image
FDA Label
Material Safety Data Sheet (MSDS) Not Available
Synthesis Reference Not Available
Average Molecular Weight 23390.3000
Monoisotopic Molecular Weight Not Available
State Liquid
Melting Point 55 oC (Forastieri, H., Ingham, K.C. J. Biol. Chem. 257:7976-7981 (1982))
Experimental Water Solubility Not Available Source: PhysProp
Predicted Water Solubility Not Available Calculated using ALOGPS
Experimental LogP/Hydrophobicity -0.063 Source: PhysProp
Predicted LogP Not Available Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS Not Available Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point 8.44
Mass Spectrum Not Available
MOL File Not Available
SDF File Not Available
PDB File Not Available
Experimental PDB ID Not Available
Isomeric SMILES Not Available
Canonical SMILES Not Available
Drug Category
  • Fertility Agents
ATC Codes
AHFS Codes
  • 68:18.00
Indication For treatment of female infertility
Pharmacology 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
Toxicity Not Available
Protein Binding Not Available
Biotransformation Not Available
Half Life 4.4 hours (mammalian reticulocytes, in vitro)
Dosage Forms
Form Route
Powder, for solution Subcutaneous
Patient Information Not Available
Contraindications Not Available
Interactions Not Available
Drug Interactions Not Available
Food Interactions Not Available
Pathways Not Available
General References
  1. 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 Link Image]
  2. 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 Link Image]
  3. Blanchard J: Gastrointestinal absorption. I. Mechanisms. Am J Pharm Sci Support Public Health. 1975 Sep-Oct;147(5):135-46. [PubMed Link Image]
  4. Drugs.com Link Image
  5. Wikipedia Link Image
Organisms Affected
  • Humans and other mammals
Targets
  1. Lutropin-choriogonadotropic hormone receptor
Drug Target 1 [top]
Target 1 ID 148
Target 1 Name Lutropin-choriogonadotropic hormone receptor
Target 1 Synonyms
  1. LH/CG-R
  2. LHR
  3. LSH- R
  4. Luteinizing hormone receptor
  5. Lutropin-choriogonadotropic hormone receptor precursor
Target 1 Gene Name LHCGR
Target 1 Protein Sequence >Lutropin-choriogonadotropic hormone receptor precursor 
MKQRFSALQLLKLLLLLQPPLPRALREALCPEPCNCVPDGALRCPGPTAGLTRLSLAYLP
VKVIPSQAFRGLNEVIKIEISQIDSLERIEANAFDNLLNLSEILIQNTKNLRYIEPGAFI
NLPRLKYLSICNTGIRKFPDVTKVFSSESNFILEICDNLHITTIPGNAFQGMNNESVTLK
LYGNGFEEVQSHAFNGTTLTSLELKENVHLEKMHNGAFRGATGPKTLDISSTKLQALPSY
GLESIQRLIATSSYSLKKLPSRETFVNLLEATLTYPSHCCAFRNLPTKEQNFSHSISENF
SKQCESTVRKVSNKTLYSSMLAESELSGWDYEYGFCLPKTPRCAPEPDAFNPCEDIMGYD
FLRVLIWLINILAIMGNMTVLFVLLTSRYKLTVPRFLMCNLSFADFCMGLYLLLIASVDS
QTKGQYYNHAIDWQTGSGCSTAGFFTVFASELSVYTLTVITLERWHTITYAIHLDQKLRL
RHAILIMLGGWLFSSLIAMLPLVGVSNYMKVSICFPMDVETTLSQVYILTILILNVVAFF
IICACYIKIYFAVRNPELMATNKDTKIAKKMAILIFTDFTCMAPISFFAISAAFKVPLIT
VTNSKVLLVLFYPINSCANPFLYAIFTKTFQRDFFLLLSKFGCCKRRAELYRRKDFSAYT
SNCKNGFTGSNKPSQSTLKLSTLHCQGTALLDKTRYTEC
Target 1 Number of Residues 710
Target 1 Molecular Weight 78617
Target 1 Theoretical pI 8.58
Target 1 GO Classification
Function
lutropin-choriogonadotropic hormone receptor activity
protein-hormone receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 1 General Function Involved in rhodopsin-like receptor activity
Target 1 Specific Function Receptor for lutropin-choriogonadotropic hormone. The activity of this receptor is mediated by G proteins which activate adenylate cyclase
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • 1-26
Target 1 Transmembrane Regions
  • 364-385
  • 396-416
  • 440-462
  • 483-505
  • 526-549
  • 571-594
  • 606-627
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 903746 Link Image
Target 1 UniProtKB/Swiss-Prot ID P22888 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name LSHR_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >2058 bp 
ATGAAGCAGCGGTTCTCGCCGCTGCAGCTGCTGAAGCTGCTGCTGCTGCTGCAGGCGCCG
CTGCCACGAGCGCTGCGCAGGCTCTGCCCTGAGCCCTGCAACTGCGTGCCCGACGGCGCC
CTGCGTGCCCCGGCCCCACGGCCGTCCACTCGACTATCACTTGCCTACCTCCCTGTCAAA
GTGATCCCATCTCAAAGTTTCAGAGGACTTAATGAGGTCATAAAAATTGAAATCTCTCAG
ATTGATTCCCTGGAAAGGATAGAAGCTAATGCCTTTGACAACCTCCTCAATTTGTCTGAA
ATACTGATCCAGAACACCAAAAATCTGAGATACATTGAGCCCGGAGCATTTATAAATCTT
CCCCGATTAAAATACTTGAGCATCTGTAACACAGGCATCAGAAAGTTTCCAGATGTTACG
AAGGTCTTCTCCTCTGAATCAAATTTCATTCTGGAAATTTGTGATAACTTACACATAACC
ACCATACCAGGAAATGCTTTTCAAGGGATGAATAATGAATCTGTAACACTCAAACTATAT
GGAAATGGATTTGAAGAAGTACAAAGTCATGCATTCAATGGGACGACACTGACTTCACTG
GAGCTAAAGGAAAACGTACATCTGGAGAAGATGCACAATGGAGCCTTCCGTGGGGCCACA
GGGCCGAAAACCTTGGATATTTCTTCCACCAAATTGCAGGCCCTGCCGAGCTATGGCCTA
GAGTCCATTCAGAGGCTAATTGCCACGTCATCCTATTCTCTAAAAAAATTGCCATCAAAA
CAAACATTTGTCAATCTCCTGAGGGCCACGCTTCATTACCCCAGCCACTGCTGTGCATTT
AGAAACTTGCCAACGAAAGAGCTAAACTTCTCACATTCCATTTCTGAAAACTTTTCCAAA
CAATGTGAAAGCACAGTAAGGAAAAGTGAACTGAGTGGCTGGGACTATGAATATGGTTTC
TGCTTACCCAAGACACCCCGATGTGCTCCTGAACCAGATGCTTTTAATCCCTGTGAAGAC
ATTATGGGCTATGACTTCCTTAGGGTCCTGATTTGGCTGATTAATATTCTAGCCATCATG
GGAAACATGACTGTTCTTTTTGTTCTCCTGACAAGTCGTTACAAACTTACAGTGCCTCGT
TTTCTCATGTGCAATCTCTCCTTTGCAGACTTTTGCATGGGGCTCTATCTGCTGCTCATA
GCCTCAGTTGATTCCCAAACCAAGGGCCAGTACTATAACCATGCCATAGACTGGCAGACA
GGGAGTGGGTGCAGCACTGCTGGCTTTTTCACTGTATTAGCAAGTGAACTTTCTGTCTAC
ACCCTCACCGTCATCACTCTAGAAAGATGGCACACCATCACCTATGCTATTCACCTGGAC
CAAAAGCTGCGATTAAGACATGCCATTCTGATTATGCTTGGAGGCTGGCTCTTTTCTTCT
CTAATTGCTATGTTGCCCCTTGTCGGGGTCAGCAATTACATGAAGGTCAGTATTTGCTTC
CCCATGGATGTGGAAACCACTCTCTCACAAGTCTATATATTAACCATCCTGATTCTCAAT
GTGGTGGCCTTCTTAATAATTTGTGCTTGCTACATTAAAATTTATTTTGCAGTTCGAAAC
CCAGAATTAATGGCTACCAATAAAGATACAAAGATTGCTAAGAAAATGGCAATCCTCATC
TTCACCGATTTTACCTGCATGGCACCTATCTCTTTTTTTGCCATCTCAGCTGCCTTCAAA
GTACCTCTTATCACAGTAACCAACTCTAAAGTTTTACTGGTTCTTTTTTATCCCATCAAT
TCTTGTGCCAATCCATTTCTGTATGCAATATTCACTAAGACATTCCAAAGAGATTTCTTT
CTTTTGCTGAGCAAATTTGGCTGCTGTAAACGTCGGGCTGATCCTCTTTATAGAAGGAAA
GATTTTTCAGCTTACACCTCCAACTGCAAAAATGGCTTCACTGGATCAAATAAGCCTTCT
CAATCCACCTTGAAGTTGTCCACATTGCACTGTCAAGGTACAGCTCTCCTAGACAAGACT
CGCTACACAGAGTGTTAA
Target 1 GenBank Gene ID
Target 1 GeneCard ID LHCGR Link Image
Target 1 GenAtlas ID LHCGR Link Image
Target 1 HGNC ID HGNC:6585 Link Image
Target 1 Chromosome Location 2
Target 1 Locus 2p21
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Liu G, Duranteau L, Carel JC, Monroe J, Doyle DA, Shenker A: Leydig-cell tumors caused by an activating mutation of the gene encoding the luteinizing hormone receptor. N Engl J Med. 1999 Dec 2;341(23):1731-6. [PubMed Link Image]
  2. Jia XC, Oikawa M, Bo M, Tanaka T, Ny T, Boime I, Hsueh AJ: Expression of human luteinizing hormone (LH) receptor: interaction with LH and chorionic gonadotropin from human but not equine, rat, and ovine species. Mol Endocrinol. 1991 Jun;5(6):759-68. [PubMed Link Image]
  3. Minegishi T, Nakamura K, Takakura Y, Miyamoto K, Hasegawa Y, Ibuki Y, Igarashi M, Minegish T [corrected to Minegishi T: Cloning and sequencing of human LH/hCG receptor cDNA. Biochem Biophys Res Commun. 1990 Nov 15;172(3):1049-54. [PubMed Link Image]
  4. Frazier AL, Robbins LS, Stork PJ, Sprengel R, Segaloff DL, Cone RD: Isolation of TSH and LH/CG receptor cDNAs from human thyroid: regulation by tissue specific splicing. Mol Endocrinol. 1990 Aug;4(8):1264-76. [PubMed Link Image]
  5. Atger M, Misrahi M, Sar S, Le Flem L, Dessen P, Milgrom E: Structure of the human luteinizing hormone-choriogonadotropin receptor gene: unusual promoter and 5' non-coding regions. Mol Cell Endocrinol. 1995 Jun;111(2):113-23. [PubMed Link Image]
  6. Latronico AC, Anasti J, Arnhold IJ, Mendonca BB, Domenice S, Albano MC, Zachman K, Wajchenberg BL, Tsigos C: A novel mutation of the luteinizing hormone receptor gene causing male gonadotropin-independent precocious puberty. J Clin Endocrinol Metab. 1995 Aug;80(8):2490-4. [PubMed Link Image]
  7. Shenker A, Laue L, Kosugi S, Merendino JJ Jr, Minegishi T, Cutler GB Jr: A constitutively activating mutation of the luteinizing hormone receptor in familial male precocious puberty. Nature. 1993 Oct 14;365(6447):652-4. [PubMed Link Image]
  8. Yano K, Saji M, Hidaka A, Moriya N, Okuno A, Kohn LD, Cutler GB Jr: A new constitutively activating point mutation in the luteinizing hormone/choriogonadotropin receptor gene in cases of male-limited precocious puberty. J Clin Endocrinol Metab. 1995 Apr;80(4):1162-8. [PubMed Link Image]
  9. Kremer H, Kraaij R, Toledo SP, Post M, Fridman JB, Hayashida CY, van Reen M, Milgrom E, Ropers HH, Mariman E, et al.: Male pseudohermaphroditism due to a homozygous missense mutation of the luteinizing hormone receptor gene. Nat Genet. 1995 Feb;9(2):160-4. [PubMed Link Image]
  10. Kosugi S, Van Dop C, Geffner ME, Rabl W, Carel JC, Chaussain JL, Mori T, Merendino JJ Jr, Shenker A: Characterization of heterogeneous mutations causing constitutive activation of the luteinizing hormone receptor in familial male precocious puberty. Hum Mol Genet. 1995 Feb;4(2):183-8. [PubMed Link Image]
  11. 8281137 Kremer H, Mariman E, Otten BJ, Moll GW Jr, Stoelinga GB, Wit JM, Jansen M, Drop SL, Faas B, Ropers HH, et al.: Cosegregation of missense mutations of the luteinizing hormone receptor gene with familial male-limited precocious puberty. Hum Mol Genet. 1993 Nov;2(11):1779-83.
  12. 8559204 Latronico AC, Anasti J, Arnhold IJ, Rapaport R, Mendonca BB, Bloise W, Castro M, Tsigos C, Chrousos GP: Brief report: testicular and ovarian resistance to luteinizing hormone caused by inactivating mutations of the luteinizing hormone-receptor gene. N Engl J Med. 1996 Feb 22;334(8):507-12.
  13. 8747461 Jiang X, Dreano M, Buckler DR, Cheng S, Ythier A, Wu H, Hendrickson WA, el Tayar N: Structural predictions for the ligand-binding region of glycoprotein hormone receptors and the nature of hormone-receptor interactions. Structure. 1995 Dec 15;3(12):1341-53.
  14. 8829636 Cocco S, Meloni A, Marini MG, Cao A, Moi P: A missense (T577I) mutation in the luteinizing hormone receptor gene associated with familial male-limited precocious puberty. Hum Mutat. 1996;7(2):164-6.
  15. 8929952 Evans BA, Bowen DJ, Smith PJ, Clayton PE, Gregory JW: A new point mutation in the luteinising hormone receptor gene in familial and sporadic male limited precocious puberty: genotype does not always correlate with phenotype. J Med Genet. 1996 Feb;33(2):143-7.
  16. 9215288 Misrahi M, Meduri G, Pissard S, Bouvattier C, Beau I, Loosfelt H, Jolivet A, Rappaport R, Milgrom E, Bougneres P: Comparison of immunocytochemical and molecular features with the phenotype in a case of incomplete male pseudohermaphroditism associated with a mutation of the luteinizing hormone receptor. J Clin Endocrinol Metab. 1997 Jul;82(7):2159-65.
  17. 9467560 Gromoll J, Partsch CJ, Simoni M, Nordhoff V, Sippell WG, Nieschlag E, Saxena BB: A mutation in the first transmembrane domain of the lutropin receptor causes male precocious puberty. J Clin Endocrinol Metab. 1998 Feb;83(2):476-80.
  18. 9514160 Latronico AC, Chai Y, Arnhold IJ, Liu X, Mendonca BB, Segaloff DL: A homozygous microdeletion in helix 7 of the luteinizing hormone receptor associated with familial testicular and ovarian resistance is due to both decreased cell surface expression and impaired effector activation by the cell surface receptor. Mol Endocrinol. 1998 Mar;12(3):442-50.
  19. 9626144 Stavrou SS, Zhu YS, Cai LQ, Katz MD, Herrera C, Defillo-Ricart M, Imperato-McGinley J: A novel mutation of the human luteinizing hormone receptor in 46XY and 46XX sisters. J Clin Endocrinol Metab. 1998 Jun;83(6):2091-8.
  20. 9626653 Martens JW, Verhoef-Post M, Abelin N, Ezabella M, Toledo SP, Brunner HG, Themmen AP: A homozygous mutation in the luteinizing hormone receptor causes partial Leydig cell hypoplasia: correlation between receptor activity and phenotype. Mol Endocrinol. 1998 Jun;12(6):775-84.
  21. 9661624 Latronico AC, Abell AN, Arnhold IJ, Liu X, Lins TS, Brito VN, Billerbeck AE, Segaloff DL, Mendonca BB: A unique constitutively activating mutation in third transmembrane helix of luteinizing hormone receptor causes sporadic male gonadotropin-independent precocious puberty. J Clin Endocrinol Metab. 1998 Jul;83(7):2435-40.
  22. 9851790 Rodien P, Cetani F, Costagliola S, Tonacchera M, Duprez L, Minegishi T, Govaerts C, Vassart G: Evidences for an allelic variant of the human LC/CG receptor rather than a gene duplication: functional comparison of wild-type and variant receptors. J Clin Endocrinol Metab. 1998 Dec;83(12):4431-4.
  23. 9858858 Tsai-Morris CH, Geng Y, Buczko E, Dehejia A, Dufau ML: Genomic distribution and gonadal mRNA expression of two human luteinizing hormone receptor exon 1 sequences in random populations. Hum Hered. 1999 Jan;49(1):48-51.
Target 1 Drug References
  1. 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 Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]

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.