Page last updated: 2024-11-13

histrelin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

histrelin: gonadotropin releasing hormone agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

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. [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]

Cross-References

ID SourceID
PubMed CID25077993
CHEMBL ID1201255
CHEBI ID5739
SCHEMBL ID17881
SCHEMBL ID19409305
SCHEMBL ID19712198
SCHEMBL ID22288995
MeSH IDM0093413

Synonyms (66)

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)

Research Excerpts

Overview

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.

ExcerptReferenceRelevance
"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

Effects

ExcerptReferenceRelevance
"The histrelin implant has been used to treat central precocious puberty (CPP) for more than 15 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

Treatment

ExcerptReferenceRelevance
"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

Toxicity

ExcerptReferenceRelevance
" 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

Pharmacokinetics

ExcerptReferenceRelevance
" 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

Dosage Studied

ExcerptRelevanceReference
" 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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
gonadotropin releasing hormone agonistAny 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]

Drug Classes (1)

ClassDescription
oligopeptideA 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]

Research

Studies (89)

TimeframeStudies, This Drug (%)All Drugs %
pre-199024 (26.97)18.7374
1990's19 (21.35)18.2507
2000's14 (15.73)29.6817
2010's25 (28.09)24.3611
2020's7 (7.87)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 57.79

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.

MetricThis Compound (vs All)
Research Demand Index57.79 (24.57)
Research Supply Index4.67 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index93.84 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (57.79)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials13 (13.98%)5.53%
Reviews10 (10.75%)6.00%
Case Studies7 (7.53%)4.05%
Observational1 (1.08%)0.25%
Other62 (66.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]