Page last updated: 2024-11-13

deslorelin

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

Description

deslorelin: Ovuplant is tradename for a short-term-release implant containing deslorelin acetate; RN given refers to D-isomer; RN for cpd without isomeric designation not avail 12/90 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID25077495
CHEMBL ID2365665
CHEBI ID177570
SCHEMBL ID59413
SCHEMBL ID19409316
MeSH IDM0182319

Synonyms (67)

Synonym
CHEBI:177570
somagard
d-trp-lhrh-pea
lhrh-t
(d-trp(sup 6)-pro(sup 9))-lhrh ethylamide
(d-trp6,pro9-nhet)lh-rh
(de-gly10,d-trp6,pro-nhet)-lh-rh
deslorelinum [inn-latin]
(des-gly10(d-tro6)-lh-rh ethylamide
deslorelina [inn-spanish]
5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-d-tryptophyl-l-leucyl-l-arginyl-n-ethyl-l-prolinamide
d-trp(sup 6)-pro(sup 9)-n-ethylamide-lhrh
d-trp lhrh-pea
(d-trp(sub 6)-pro(sup 9)-net)-gnrh
(d-trp6,des-gly-nh210)-lh-rh ethylamide
h 4065
desloreline [inn-french]
bachem 9022
gnrh (d-trp6,pro9-net)
(d-trp6,des-gly10)-lh-rh ethylamide
57773-65-6
deslorelin (usan/inn)
D03694
deslorelin
NCGC00167516-01
NCGC00167516-02
NCGC00167516-03
lhrh, des-glycyl(10)-tryptophyl(6)-ethylamide-
lhrh, des-gly(10)-trp(6)-ethylamide-
deslorelina
gnrh, des-gly(10)-trp(6)-ethylamide-
tkg3i66tve ,
6-trp-9-n-et-pro-10-des-glynh2-lhrh
deslorelin [usan:inn:ban]
gnrh, trp(6)-n-et-pronh2(9)-
unii-tkg3i66tve
des-gly-10-trp-6-ethylamide-lhrh
lhrh, tryptophyl(6)-n-ethylprolinamide(9)-des-glycinamide(10)-
deslorelinum
desloreline
lhrh, trp(6)-n-et-pronh2(9)-
CHEMBL2365665
bdbm84726
AKOS015994649
deslorelin [who-dd]
deslorelin [mi]
deslorelin [usan]
deslorelin [mart.]
(d-trp(sup 6),des-gly(sup 10))-lh-rh ethylamide
deslorelin [inn]
SCHEMBL59413
HS-2009
DTXSID2048323 ,
gtpl9343
CS-5746
HY-12556
[des-gly10, d-trp6]-lh-rh ethylamide, >=97% (hplc)
SCHEMBL19409316
Q5264591
DB11510
6-d-phenylalanine-9-(n-ethyl-l-prolinamide)-
deslorelinum (inn-latin)
deslorelin (mart.)
dtxcid0028298
desloreline (inn-french)
deslorelina (inn-spanish)
AC-8917

Research Excerpts

Overview

Deslorelin acetate is a gonadotropin-releasing hormone agonist formulated in a controlled-release subcutaneous implant. Deslorelin is an alternative to current therapies and castration.

ExcerptReferenceRelevance
"Deslorelin acetate is a gonadotropin-releasing hormone agonist formulated in a controlled-release subcutaneous implant and designed for reversible suppression of testosterone production in dogs. "( Effect of a subcutaneous implant of deslorelin acetate on serum testosterone concentrations in male Hermann's (Testudo hermanni sp.) and Greek (Testudo graeca sp.) tortoises.
Andolfatto, A; Esposito, S; Ferro, A; Pisu, MC; Probo, M; Veronesi, MC, 2023
)
2.63
"Deslorelin implantation is a management option that is safe, affordable, and appears effective for sexually intact male keeshonden with hair cycle arrest."( Deslorelin Implant Treatment for Hair Cycle Arrest (Alopecia X) in Two Intact Male Keeshonden.
Layne, EA; Richmond, RV,
)
2.3
"Deslorelin acetate is a GnRH agonist used for contraception in dogs. "( Deslorelin implants in pre-pubertal female dogs: short- and long-term effects on the genital tract.
Cristarella, S; Macrì, F; Marino, G; Pagano, G; Quartuccio, M; Rizzo, S; Taormina, A; Zanghì, A, 2014
)
3.29
"Deslorelin is an alternative to current therapies and castration."( Deslorelin for the treatment of hair cycle arrest in intact male dogs.
Abramo, F; Albanese, F; Fracassi, F; Malerba, E; Miragliotta, V, 2014
)
2.57
"Deslorelin is a useful and reversible contraceptive for P. "( Preliminary evaluation of deslorelin, a GnRH agonist for contraception of the captive variable flying fox Pteropus hypomelanus.
Heard, DJ; LeBlanc, D; Metrione, LC; Penfold, LM; Verstegen, JP; Walsh, AL, 2008
)
2.09
"Deslorelin was found to be an effective contraceptive in sea otters and was found to be reversible documented by a live birth following treatment, however the duration of suppression in females was much longer than expected with a 6-month and a 1-year implant lasting between 3 and 4 years in females."( Preliminary findings of fecal gonadal hormone concentrations in six captive sea otters (Enhydra lutris) after deslorelin implantation.
Belting, T; Boutelle, SM; Fisher, G; Larson, S; Rifenbury, K,
)
1.06

Effects

ExcerptReferenceRelevance
"Deslorelin implants have been widely available in Europe since 2008."( Semen quality and interval to sterility in tom cats treated with a 9.4 mg deslorelin implant.
Baldan, A; Milani, C; Mollo, A; Righetti, C; Romagnoli, S; Stelletta, C, 2017
)
1.41

Actions

ExcerptReferenceRelevance
"Deslorelin induced an increase in plasma concentrations of LH within 2 h (p < 0.001); LH remained greater (p < 0.05) for heifers treated with deslorelin for 48 h, but from Day 4 to 28 of treatment, LH in treated and control heifers did not differ."( Pituitary function, ovarian follicular growth, and plasma concentrations of 17 beta-estradiol and progesterone in prepubertal heifers during and after treatment with the luteinizing hormone-releasing hormone agonist deslorelin.
Bergfeld, EG; D'Occhio, MJ; Kinder, JE, 1996
)
1.2

Treatment

Deslorelin treatment caused retardation of testicular growth and reduced the serum FSH and testosterone concentrations between 12 and 24 mo of age. In Deslorelin-treated dogs, plasma concentrations of LH and testosterone were undetectable after 21 and 27 days.

ExcerptReferenceRelevance
"In deslorelin-treated and control dogs, its expression was either low or frequently below the detection limit."( Expression of GnRH receptor in the canine corpus luteum, and luteal function following deslorelin acetate-induced puberty delay.
Aslan, S; Boos, A; Gram, A; Kaya, D; Kowalewski, MP; Kuru, M; Schäfer-Somi, S, 2017
)
1.19
"Deslorelin treatment had no discernible effect on body weight."( Inhibition of the reproductive system by deslorelin in male and female pigeons (Columba livia).
Blackberry, MA; Cowan, ML; Doneley, RJ; Johnston, SD; Martin, GB; Monks, DJ, 2014
)
1.39
"One deslorelin-treated female showed an oestrous response and another showed clinical signs of pyometra after the implants."( Long-term-release GnRH agonists postpone puberty in domestic cats.
Barbeito, C; Corrada, Y; Diaz, JD; Gobello, C; Risso, A, 2012
)
0.86
"Deslorelin-treated mares had fewer ovarian follicles >20 mm in diameter 16 days after treatment than hCG-treated mares (P < 0.01)."( Effects of deslorelin or hCG administration on reproductive performance in first postpartum estrus mares.
Blanchar, TL; Brinsko, SP; Rigby, SL, 2002
)
1.43
"In Deslorelin-treated dogs, plasma concentrations of LH and testosterone were undetectable after 21 and 27 days, testicular volume fell to 35% of pretreatment values after 14 weeks and no ejaculates could be obtained after 6 weeks."( Use of a new drug delivery formulation of the gonadotrophin-releasing hormone analogue Deslorelin for reversible long-term contraception in male dogs.
Blackberry, MA; Cummins, JM; Junaidi, A; Martin, GB; Trigg, TE; Williamson, PE, 2003
)
1.06
"Deslorelin treatment caused retardation of testicular growth and reduced the serum FSH and testosterone concentrations between 12 and 24 mo of age."( Chronic treatment of male tammar wallabies with deslorelin implants during pouch life: effects on development, puberty, and reproduction in adulthood.
Cooper, DW; Eckery, DC; Herbert, CA; Trigg, TE, 2007
)
1.32
"In 1 Deslorelin-treated cow, the FWDF regressed, and a second-wave dominant follicle ovulated, while 2 other Deslorelin cows failed to ovulate until after Day 36."( Influence of deslorelin (GnRH-agonist) implant on plasma progesterone, first wave dominant follicle and pregnancy in dairy cattle.
Ambrose, JD; Binelli, M; Diaz, T; Moreira, F; Pires, MF; Thatcher, WW, 1998
)
1.12
"Treatment with Deslorelin increased Day 45 pregnancy rates in cows as compared to untreated controls."( Effect of chronic administration of a gonadotropin-releasing agonist on luteal function and pregnancy rates in dairy cattle.
Davis, TL; Willmore, A, 2019
)
0.85
"Treatment with Deslorelin during postpartum (1) suppressed follicular development, (2) enhanced physical involution of the uterus, (3) increased tone of the uterine wall, (4) delayed first ovulation and reduced responsiveness to a synchronization of ovulation protocol."( Use of increasing doses of a degradable Deslorelin implant to enhance uterine involution in postpartum lactating dairy cows.
Bilby, TR; de Sá, MJ; Lopez, M; Risco, CA; Silvestre, FT; Thatcher, WW, 2009
)
0.96
"Treatment with deslorelin did not affect reactivation of a dormant blastocyst and subsequent birth in 4/8 animals, but post-partum mating was inhibited in these animals."( Effect of deslorelin implants on follicular development, parturition and post-partum oestrus in the tammar wallaby (Macropus eugenii).
Cooper, DW; Herbert, CA; Trigg, TE, 2004
)
1.07
"Treatment with deslorelin STI reduced the time interval to ovulation significantly from 69.5 +/- 25.48 h to 42.7 +/- 12.35 h (p < 0.001)."( Acceleration and timing of fertile ovulation in cyclic mares with a deslorelin implant.
Gånheim, A; Jöchle, W, 1995
)
0.87
"Treatment with deslorelin induced an acute increase in plasma concentrations of immunoactive and bioactive LH, which remained increased over 7 d of observation."( Controlled, reversible suppression of estrous cycles in beef heifers and cows using agonists of gonadotropin-releasing hormone.
Aspden, WJ; D'Occhio, MJ; Whyte, TR, 1996
)
0.63
"Treatment with deslorelin desensitized the pituitary in heifer calves and altered patterns of LH and estradiol secretion."( Influence of the luteinizing hormone-releasing hormone agonist, deslorelin, on patterns of estradiol-17 beta and luteinizing hormone secretion, ovarian follicular responses to superstimulation with follicle-stimulating hormone, and recovery and in vitro d
Aspden, WJ; Bergfeld, EG; D'Occhio, MJ; Earl, CR; Fitzpatrick, LA; Kinder, JE; Maclellan, LJ; Trigg, TE; Walsh, J, 1997
)
0.88
"Treatment with deslorelin initially stimulated oestradiol release, which accompanied treatment-induced ovulations."( Efficacy of the GnRH analogue deslorelin for suppression of oestrous cycles in cats.
Asa, CS; Bauman, JE; Jöchle, W; Munson, L; Trigg, TE, 2001
)
0.94

Bioavailability

ExcerptReferenceRelevance
" Due to the peptide nature of the synthetic analogues oral administration and potential gastrointestinal enzymatic degradation poor bioavailability results necessitating a parenteral delivery system."( GnRH analogues--agonists and antagonists.
Padula, AM, 2005
)
0.33

Dosage Studied

The present experiment characterized the pituitary responsiveness to exogenous GnRH in the first 10 d after ovulation following commercially available deslorelin acetate implantation. The study was conducted to determine if Deslorelin, a potent gonadotropin releasing hormone analogue, would stimulate an ovulatory-like LH surge in the pig.

ExcerptRelevanceReference
" A significant dose-response relationship was observed, with mean +/- SD estradiol levels of 16."( Use of an ultrasensitive recombinant cell bioassay to determine estrogen levels in girls with precocious puberty treated with a luteinizing hormone-releasing hormone agonist.
Barnes, KM; Baron, J; Cutler, GB; Klein, KO; Pescovitz, OH, 1998
)
0.3
" A dose-response study was conducted to determine if Deslorelin, a potent gonadotropin releasing hormone analogue, delivered via the SABER system, a biodegradable controlled release system, would stimulate an ovulatory-like LH surge in the pig."( Luteinizing hormone response to controlled-release deslorelin in estradiol benzoate primed ovariectomized gilts.
Barb, CR; Burns, PJ; Gibson, JW; Kraeling, RR; Rampacek, GB; Simon, B; Sullivan, SA; Thompson, DL, 2000
)
0.81
"The present experiment characterized the pituitary responsiveness to exogenous GnRH in the first 10 d after ovulation following commercially available deslorelin acetate implantation at the normal dosage for hastening ovulation in mares."( Pituitary responsiveness to GnRH in mares following deslorelin acetate implantation to hasten ovulation.
Cartmill, JA; Johnson, CA; Thompson, DL, 2002
)
0.76
" There was a dose-response in some of these early aspects of the hormone profiles."( Dose-response studies for pituitary and testicular function in male dogs treated with the GnRH superagonist, deslorelin.
Blackberry, MA; Cummins, JM; Junaidi, A; Martin, GB; Trigg, TE; Williamson, PE, 2009
)
0.57
" Further studies with a higher dosage of deslorelin acetate are needed to draw conclusions on its contraceptive effect."( Effects of deslorelin acetate on plasma testosterone concentrations in captive yellow-bellied sliders (Trachemys scripta sp.).
Göritz, F; Hermes, R; Loucachevsky, T; Monge, E; Potier, R; Risi, E; Rochel, D, 2017
)
1.11
" There was a dose-response effect on duration rather than magnitude of effect, with high-dose devils remaining suppressed for longer than low-dose animals."( Contraceptive efficacy and dose-response effects of the gonadotrophin-releasing hormone (GnRH) agonist deslorelin in Tasmanian devils (Sarcophilus harrisii).
Cope, HR; Herbert, CA; Hobbs, R; Hogg, CJ; Izzard, S; Keeley, T; Peck, S; White, PJ; Yeen-Yap, W, 2019
)
0.73
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
phosphopantetheinyl transferaseBacillus subtilisPotency50.11870.141337.9142100.0000AID1490
USP1 protein, partialHomo sapiens (human)Potency56.23410.031637.5844354.8130AID504865
GLS proteinHomo sapiens (human)Potency12.58930.35487.935539.8107AID624170
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency39.81070.354828.065989.1251AID504847
huntingtin isoform 2Homo sapiens (human)Potency7.94330.000618.41981,122.0200AID1688
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency16.80370.00798.23321,122.0200AID2546; AID2551
gemininHomo sapiens (human)Potency18.67740.004611.374133.4983AID624296; AID624297
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency13.45910.005612.367736.1254AID624032; AID624044
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gonadotropin-releasing hormone receptorRattus norvegicus (Norway rat)Ki99,999,998,430,674,940.00000.00383.51866.5000AID102938
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID16102Clearance in rat after iv dose (100 ug/kg)1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists.
AID1145197Induction of luteinizing hormone release in ovariectomized estrogen/progesterone-treated rat at 100 ng, sc measured after 15 mins to 60 hrs post dose by RIA relative to LH-RH1976Journal of medicinal chemistry, Mar, Volume: 19, Issue:3
Analogs of luteinizing hormone-releasing hormone with increased biological activity produced by D-amino acid substitutions in position 6.
AID102938In vitro binding affinity for rat pituitary LHRH receptor, activity is expressed as pKI value1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists.
AID1145199Induction of FSH release in ovariectomized estrogen/progesterone-treated rat at 100 ng, sc measured after 15 mins to 60 hrs post dose by RIA relative to LH-RH1976Journal of medicinal chemistry, Mar, Volume: 19, Issue:3
Analogs of luteinizing hormone-releasing hormone with increased biological activity produced by D-amino acid substitutions in position 6.
AID197342Tested in vitro for LH release from cultured rat pituitary cells, activity is expressed as pD2 value1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists.
AID1346002Human GnRH1 receptor (Gonadotrophin-releasing hormone receptors)2016British journal of pharmacology, Jan, Volume: 173, Issue:1
Characterization of 12 GnRH peptide agonists - a kinetic perspective.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (277)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (0.36)18.7374
1990's41 (14.80)18.2507
2000's93 (33.57)29.6817
2010's119 (42.96)24.3611
2020's23 (8.30)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 58.35

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 Index58.35 (24.57)
Research Supply Index5.83 (2.92)
Research Growth Index6.62 (4.65)
Search Engine Demand Index92.92 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (58.35)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials57 (20.21%)5.53%
Reviews13 (4.61%)6.00%
Case Studies15 (5.32%)4.05%
Observational0 (0.00%)0.25%
Other197 (69.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Biomarkers, Breast Density And Risk Reduction Perspectives In BRCA Carriers [NCT00080756]Phase 211 participants (Actual)Interventional2004-03-11Active, not recruiting
A Double-Blind, Randomized, Placebo-Controlled Clinical Trial of Luteinizing Hormone-Releasing Hormone Analog (LHRHa) in Pubertal Patients With Extreme Short Stature [NCT00001190]Phase 250 participants Interventional1983-11-30Completed
Spironolactone and Testolactone Treatment of Boys With Familial Isosexual Precocious Puberty [NCT00001202]Phase 280 participants Interventional1985-01-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]