histrelin: gonadotropin releasing hormone agonist
histrelin : An oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, 1-benzyl-D-histidyl, leucyl, arginyl, and N-ethylprolinamide residues joined in sequence. It is a synthetic nonapeptide analogue of gonadotropin-releasing hormone, and is used as a subcutaneous hydrogel implant (particularly as the diacetate salt) for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.
ID Source | ID |
---|---|
PubMed CID | 25077993 |
CHEMBL ID | 1201255 |
CHEBI ID | 5739 |
SCHEMBL ID | 17881 |
SCHEMBL ID | 19409305 |
SCHEMBL ID | 19712198 |
SCHEMBL ID | 22288995 |
MeSH ID | M0093413 |
Synonym |
---|
orf-17070 |
histrelina [spanish] |
vantaas |
histreline [french] |
rwj 17070 |
((imbl)-d-his(sub 6),pro(sub 9)-net)lhrh |
supprelin |
histrelinum [latin] |
5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-n(sup tau)-benzyl-d-histidyl-l-leucyl-l-arginyl-n-ethyl-l-prolinamide |
orf 17070 |
histrelin [usan:inn] |
brn 4290557 |
NCGC00181758-01 |
histrelin |
76712-82-8 |
D02369 |
histrelin (usan/inn) |
CHEMBL1201255 |
rwj-17070 |
chebi:5739 , |
orf 17070rwj 17070 |
histrelinum |
histrelina |
histreline |
hsdb 7657 |
h50h3s3w74 , |
unii-h50h3s3w74 |
5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-1-benzyl-d-histidyl-l-leucyl-l-arginyl-n-ethyl-l-prolinamide |
l-pyroglutamyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-d-n(im)-benzyl-histidyl-l-leucyl-l-arginyl-l-proline ethylamide |
5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-n(tau)-benzyl-d-histidyl-l-leucyl-l-arginyl-n-ethyl-l-prolinamide |
gtpl3884 |
SCHEMBL17881 |
DTXSID50227543 , |
histrelin [inn] |
histrelin [hsdb] |
histrelin [mi] |
histrelin [mart.] |
5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-nt-benzyl-d-histidyl-l-leucyl-l-arginyl-n-ethyl-l-prolinamide |
histrelin [vandf] |
histrelin [who-dd] |
histrelin [usan] |
SCHEMBL19409305 |
SCHEMBL19712198 |
AKOS030573448 |
5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-ntau-benzyl-d-histidyl-l-leucyl-l-arginyl-n-ethyl-l-prolinamide |
l-pyroglutamyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-d-nim-benzyl-histidyl-l-leucyl-l-arginyl-l-proline ethylamide |
Q5871149 |
(des-gly10,d-his(bzl)6,pro-nhet9)-lhrh |
SCHEMBL22288995 |
supprelin lasupprelin la |
des-gly10,(d-his(bzl)6)-lh-rh*ethylamide |
l-prolinamide, 5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-1-(phenylmethyl)-d-histidyl-l-leucyl-l-arginyl-n-ethyl- |
HY-P0056 |
CS-0015085 |
ibhpe-lhrh |
l02ae05 |
lhrh, histidyl(imbzl)(6)-n-ethylprolinamide(9)-des-glycinamide(10)- |
5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-n(sup tau)- benzyl-d-histidyl-l-leucyl-l-arginyl-n-ethyl-l-prolinamide |
imbzl-his(6), pro(9)-net-gnrh |
gnrh, his(imbzl)(6)-n-et-pronh2(9)- |
6-his(imbzl)-9-n-et-pronh2-10-des-glynh2-lhrh |
luteinizing hormone-releasing factor (pig), 6-(1-(phenylmethyl)-d- histidine)-9-(n-ethyl-l-prolinamide)-10-deglycinamide- |
histrelin (mart.) |
dtxcid00150034 |
lhrh, his(imbzl)(6)-n-et-pronh2(9)- |
histrelinum (latin) |
Histrelin is a gonadotrophin-releasing hormone agonist available in a diffusion-controlled reservoir drug delivery system for subcutaneous implantation. The histrelin implant is a new treatment that provides a continuous slow release of the GnRHa Histrelin.
Excerpt | Reference | Relevance |
---|---|---|
"Histrelin is a gonadotropin-releasing hormone agonist available in a diffusion-controlled reservoir drug delivery system for subcutaneous implantation. " | ( Histrelin: in advanced prostate cancer. Deeks, ED, 2010) | 3.25 |
"Histrelin is a luteinising hormone-releasing hormone agonist (LHRH)." | ( Histrelin Hydrogel Implant--Valera: Histrelin implant, LHRH-Hydrogel implant, RL 0903, SPD 424. , 2005) | 2.49 |
"The histrelin implant is a new treatment that provides a continuous slow release of the GnRHa histrelin." | ( Efficacy and safety of histrelin subdermal implant in children with central precocious puberty: a multicenter trial. Clarke, W; Eugster, EA; Flood, L; Gray, W; Kletter, GB; Lee, PA; Neely, EK; Reiter, EO; Saenger, P; Shulman, D; Silverman, L; Tierney, D, 2007) | 1.13 |
"Histrelin is a synthetic gonadotrophin-releasing hormone (GnRH) agonist which, when administered over a prolonged period, suppresses the release of gonadotrophins from the anterior pituitary. " | ( Histrelin. A review of its pharmacological properties and therapeutic role in central precocious puberty. Barradell, LB; McTavish, D, 1993) | 3.17 |
Excerpt | Reference | Relevance |
---|---|---|
"The histrelin implant has been used to treat central precocious puberty (CPP) for more than 15Â years. " | ( Long-term experience with the use of a single histrelin implant beyond one year in patients with central precocious puberty. Eckert, GJ; Eugster, EA; Ray, LA, 2023) | 1.73 |
Excerpt | Reference | Relevance |
---|---|---|
"Treatment with histrelin microcapsules (300 micrograms peptide/kg) prevented any increase in LH secretion in response to a GnRH challenge 3 days later, indicating a direct action of histrelin on the pituitary gland.(ABSTRACT TRUNCATED AT 250 WORDS)" | ( Effects of a sustained release formulation of the gonadotrophin-releasing hormone agonist histrelin on serum concentrations of gonadotrophins and oestradiol, and ovarian LH/human chorionic gonadotrophin receptor content in the rat. Demarest, KT; Ericson, E; Gunnet, JW; Hahn, DW; McGuire, JL, 1991) | 0.84 |
Excerpt | Reference | Relevance |
---|---|---|
" Additionally, the implant was safe and well tolerated." | ( Efficacy and safety of histrelin subdermal implant in patients with advanced prostate cancer. Schlegel, PN, 2006) | 0.64 |
" No significant adverse events occurred." | ( Efficacy and safety of histrelin subdermal implant in children with central precocious puberty: a multicenter trial. Clarke, W; Eugster, EA; Flood, L; Gray, W; Kletter, GB; Lee, PA; Neely, EK; Reiter, EO; Saenger, P; Shulman, D; Silverman, L; Tierney, D, 2007) | 0.65 |
Excerpt | Reference | Relevance |
---|---|---|
" Testosterone suppression was the primary pharmacodynamic endpoint, with treatment success defined as serum testosterone less than 50 ng/dL." | ( An evaluation of the pharmacokinetics and pharmacodynamics of the histrelin implant for the palliative treatment of prostate cancer. Dineen, MK; Kuzma, P; Pentikis, HS; Tierney, DS, 2005) | 0.57 |
Excerpt | Relevance | Reference |
---|---|---|
" Adjustments in dosage or route of administration were sometimes needed." | ( A gonadotropin releasing hormone analogue prevents cyclical attacks of porphyria. Anderson, KE; Bardin, CW; Kappas, A; Spitz, IM, 1990) | 0.28 |
" This study was designed to further compare gonadotrophin responses to GnRH agonist stimulation within and between individual patients in a dose-response manner." | ( Pituitary responsiveness to gonadotrophin-releasing hormone agonist stimulation: a dose-response comparison of luteinizing hormone/follicle-stimulating hormone secretion in women with polycystic ovary syndrome and normal women. Chang, RJ; Cheung, AP, 1995) | 0.29 |
Role | Description |
---|---|
antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
gonadotropin releasing hormone agonist | Any drug which binds to gonadotropin-releasing hormone receptors and triggers a response. |
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Class | Description |
---|---|
oligopeptide | A peptide containing a relatively small number of amino acids. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 24 (26.97) | 18.7374 |
1990's | 19 (21.35) | 18.2507 |
2000's | 14 (15.73) | 29.6817 |
2010's | 25 (28.09) | 24.3611 |
2020's | 7 (7.87) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (57.79) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 13 (13.98%) | 5.53% |
Reviews | 10 (10.75%) | 6.00% |
Case Studies | 7 (7.53%) | 4.05% |
Observational | 1 (1.08%) | 0.25% |
Other | 62 (66.67%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |