Page last updated: 2024-11-12

iturelix

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

Description

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

Cross-References

ID SourceID
PubMed CID16130938
CHEMBL ID3989438
SCHEMBL ID1649367
MeSH IDM0159739

Synonyms (34)

Synonym
orf 23541
brn 4866881
d-alaninamide, n-acetyl-3-(naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-n(sup 6)-3-pyridinylcarbonyl)-l-lysyl-n(sup 6)-(3-pyridinylcarbonyl)-d-lysyl-l-leucyl-n(sup 6)-(1-methylethyl)-l-lysyl-l-prolyl-
d-alaninamide, n-acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-n6-(3-pyridinylcarbonyl)-l-lysyl-n6-(3-pyridinylcarbonyl)-d-lysyl-l-leucyl-n6-(1-methylethyl)-l-lysyl-l-prolyl-
(n-acetyl-3-(naphhalen-2-yl)-d-alanyl)-p-chloro-d-phenylalanyl-3-(3-pyridyl)-d-alanyl-l-seryl-n(sup 6)-nicotinyl-l-lysyl-n(sup 6)-nicotinyl-d-lysyl-l-leucyl-n(sup 6)-isopropyl-l-lysyl-l-prolyl-d-alaninamide
d-alaninamide, n-acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-n(sup 6)-(3-pyridinylcarbonyl)-l-lysyl-n(sup 6)-(3-pyridinylcarbonyl)-d-lysyl-l-leucyl-n(sup 6)-(1-methylethyl)-l-lysyl-l-prolyl-
nal-lys-gnrh
iturelix
orf-23541
antide
112568-12-4
n-ac-nal(1)-4-cl-phe(2)-pal(3)-ser(4)-nic-lys(5)-nic-lys(6)-leu(7)-i-lys(8)-pro(9)-ala(10)-nh2
nal-lys-gnrhant
orf-32541
unii-94055uoq3y
94055uoq3y ,
iturelix [usan:inn]
AKOS015896023
iturelix [usan]
iturelix [who-dd]
nal-lys anatagonist
iturelix [inn]
d 21074
gtpl3854
SCHEMBL1649367
antide acetate
n-acetyl-3-(2-naphthyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridyl)-d-alanyl-l-seryl-n6-nicotinoyl-l-lysyl-n6-nicotinoyl-d-lysyl-l-leucyl-n6-isopropyl-l-lysyl-l-prolyl-d-alaninamide
Q27888363
CHEMBL3989438
CS-0012410
HY-P0013
d-alaninamide, n-acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-n6-(3-pyridinylcarbonyl)-l-lysyl-n6-(3-pyridinylcarbonyl)-d-lysyl-l-leucyl-n6-(1-meth ylethyl)-l-lysyl-l-prolyl-
DTXSID201033848
AC-8912

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"0 mg/kg; n = 2), peripheral antide levels followed a similar pharmacokinetic profile and declined slowly."( Inhibition of pituitary gonadotropin secretion by the gonadotropin-releasing hormone antagonist antide. II. Development of an in vitro bioassay for characterization of pharmacokinetics and pharmacodynamics of antide in circulation.
Danforth, DR; Gordon, K; Hodgen, GD; Leal, JA; Williams, RF, 1991
)
0.28

Compound-Compound Interactions

ExcerptReferenceRelevance
" Here, the developmental potential of embryos produced from animals treated with r-hFSH alone or in combination with r-hLH was evaluated."( Developmental potential of embryos produced by in-vitro fertilization from gonadotrophin-releasing hormone antagonist-treated macaques stimulated with recombinant human follicle stimulating hormone alone or in combination with luteinizing hormone.
Hutchison, JS; Stouffer, RL; Weston, AM; Wolf, DP; Zelinski-Wooten, MB, 1996
)
0.29

Bioavailability

ExcerptReferenceRelevance
" The bioavailability of antide almost doubled after dilution in larger volumes."( Dose-finding study of daily gonadotropin-releasing hormone (GnRH) antagonist for the prevention of premature luteinizing hormone surges in IVF/ICSI patients: antide and hormone levels.
Homburg, R; Hompes, PG; Huirne, JA; Lambalk, CB; McDonnell, J; Schats, R; Schoemaker, J; van Loenen, AC, 2004
)
0.32
" In vivo studies demonstrated a relative bioavailability of 34."( The use of thiolated polymers as carrier matrix in oral peptide delivery--proof of concept.
Bernkop-Schnürch, A; D'Antonio, M; Del Curto, MD; Esposito, P; Guggi, D; Huck, C; Kahlbacher, H; Pinter, Y; Schmerold, I; Schöffmann, G; Schuh, M, 2005
)
0.33

Dosage Studied

ExcerptRelevanceReference
" Preincubation of pituitary cells with antide for 6-48 h before GnRH exposure shifted the dose-response curve to the left; the maximally effective dose was 10(-8) M; the ED50 was 10(-10) M antide after 48-h preincubation."( Inhibition of pituitary gonadotropin secretion by the gonadotropin-releasing hormone antagonist antide. I. In vitro studies on mechanism of action.
Danforth, DR; Gordon, K; Hodgen, GD; Williams, RF, 1991
)
0.28
" In conclusion, at a dosage sufficient to suppress reproductive cyclicity (and elicit the regression of endometriosis), Antide also caused long term follicular atresia and infertility."( Follicular atresia and infertility in rats treated with a gonadotropin-releasing hormone antagonist.
Bertero, MC; Lyon, BP; Muse, KN; Sharpe, KL; Vernon, MW, 1990
)
0.28
"The dose-response effects of a single administration of Nal-Lys-GnRHant (antagonist) on serum LH and FSH concentrations were compared to the effects of Nal-Glu-GnRHant in monkeys."( Prolonged duration of gonadotropin inhibition by a third generation GnRH antagonist.
Danforth, DR; Gordon, K; Hodgen, GD; Leal, JA; Williams, RF, 1988
)
0.27
"83 microgram/kg leuprolide acetate (LA) on a 12-hour dosing schedule."( Evaluation of the impact of concurrent gonadotropin-releasing hormone (GnRH) antagonist administration on GnRH agonist-induced gonadotrope desensitization.
Carey, KD; Illions, EH; Navot, D; Scott, RT, 1995
)
0.29
" Following an initial dose-response trial, queens were assigned to one of four treatments: (1) antide, two 6 mg/kg injections 15 days apart (n = 8 cats); (2) levonorgestrel, six silastic rods (36 mg levonorgestrel/rod) implanted for 30 days (n = 8); (3) control injections (n = 5); and (4) control implants (n = 5)."( Short term suppression of follicular recruitment and spontaneous ovulation in the cat using levonorgestrel versus a GnRH antagonist.
Brown, JL; Howard, JG; Ottinger, MA; Pelican, KM; Wildt, DE, 2005
)
0.33
"A dose-response study was made of the broad-spectrum gonadal steroid agonist tibolone (TBL) on lordosis behavior in estradiol benzoate (EB: 5 µg) primed rats."( Tibolone facilitates lordosis behavior through estrogen, progestin, and GnRH-1 receptors in estrogen-primed rats.
Domínguez-Ordoñez, R; García-Juárez, M; González-Flores, O; Lima-Hernández, FJ; Montes-Narváez, O; Pfaus, JG, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID1346002Human GnRH1 receptor (Gonadotrophin-releasing hormone receptors)2002Endocrinology, Mar, Volume: 143, Issue:3
GnRH and GnRH receptor genes in the human genome.
AID1346002Human GnRH1 receptor (Gonadotrophin-releasing hormone receptors)1991Biochemical and biophysical research communications, Apr-15, Volume: 176, Issue:1
Gonadotropin releasing hormone antagonists: novel structures incorporating N omega-cyano modified guanidine moieties.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (141)

TimeframeStudies, This Drug (%)All Drugs %
pre-19906 (4.26)18.7374
1990's60 (42.55)18.2507
2000's54 (38.30)29.6817
2010's18 (12.77)24.3611
2020's3 (2.13)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (3.97%)5.53%
Reviews3 (1.99%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other142 (94.04%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]