Page last updated: 2024-11-12

antarelix

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

Description

antarelix: a synthetic decapeptide, water-soluble LHRH antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID16135076
MeSH IDM0224142

Synonyms (21)

Synonym
teverelix [inn]
n-acetyl-3-(2-naphthyl)-d-alanyl-p-chloro-d-phenylalanyl-3-(3-pyridyl)-d-alanyl-l-seryl-l-tyrosyl-n(sup 6)-carbamoyl-d-lysyl-l-leucyl-n(sup 6)-isopropyl-l-lysyl-l-prolyl-d-alaninamide
151272-78-5
unii-d19v7048jk
d19v7048jk ,
d 23234
d-23234
ac-d-nal-d-cpa-d-pal-ser-tyr-d-hci-leu-lys(ipr)-pro-d-ala-nh2
ep 24332
ep-24332
teverelix
d-alaninamide, n-acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-l-tyrosyl-n6-(aminocarbonyl)-d-lysyl-l-leucyl-n6-(1-methylethyl)-l-lysyl-l-prolyl-
antarelix
DB05624
Q27275967
CS-0025196
n-acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-l-tyrosyl-n6-(aminocarbonyl)-d-lysyl-l-leucyl-n6-(1-methylethyl)-l-lysyl-l-prolyl-d-alaninamide
n-acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-l-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-l-tyrosyl-n6-(aminocarbonyl)-d-lysyl-l-leucyl-n6-(1-methylethyl)-l-lysyl-l-prolyl-d-alaninamide
HY-105173
DTXSID301033772
AKOS040749635

Research Excerpts

Treatment

ExcerptReferenceRelevance
"Antarelix treatment significantly reduced the percentage of follicles > 2.00 mm in diameter in RF+ but not in R+2 ewes."( Effects of the Booroola Fec gene on ovarian follicular populations in superovulated Romanov ewes pretreated with a GnRH antagonist.
Cognié, Y; Dufour, JJ; Mariana, JC; Mermillod, P; Romain, RF, 2000
)
1.03

Pharmacokinetics

ExcerptReferenceRelevance
"A procedure for the radioimmunoassay (RIA) of Antarelix (teverelix) in plasma has been developed for the pharmacokinetic study of this potent LHRH antagonist in dogs."( Radioimmunoassay of Antarelix, a luteinizing hormone releasing-hormone antagonist, in plasma and its application for pharmacokinetic study in dogs.
Adam, A; Boutignon, F; Deghenghi, R; Lenaerts, V; Ong, H; Rondeau, JJ; Sorensen, S; Wüthrich, P, 1996
)
0.88
"0 ng/mL (5 mg teverelix) and tmax occurred between 1 and 4 hours after dosing."( Pituitary and gonadal endocrine effects and pharmacokinetics of the novel luteinizing hormone-releasing hormone antagonist teverelix in healthy men--a first-dose-in-humans study.
Engel, J; Erb, K; Hermann, R; Pechstein, B; Schueler, A, 2000
)
0.31
" All 3 pharmacodynamic end points (luteinizing hormone, follicle-stimulating hormone, and total testosterone) showed reductions that were more prolonged following the 90 mg IM administration compared to 90 mg SC administration."( Pharmacokinetic, Safety, and Pharmacodynamic Properties of Teverelix Trifluoroacetate, a Novel Gonadotropin-Releasing Hormone Antagonist, in Healthy Adult Subjects.
Godsafe, Z; Larsen, F; MacLean, CM; Soto-Forte, P, 2022
)
0.72

Dosage Studied

ExcerptRelevanceReference
" After 5 mg teverelix, testosterone suppression <1 ng/mL started a median of 12 hours after dosing and lasted for a median of 33 hours."( Pituitary and gonadal endocrine effects and pharmacokinetics of the novel luteinizing hormone-releasing hormone antagonist teverelix in healthy men--a first-dose-in-humans study.
Engel, J; Erb, K; Hermann, R; Pechstein, B; Schueler, A, 2000
)
0.31
" The dosage of Antarelix was increased to 5 mg for each injection in EXP III (n = 6)."( Gonadotropin release in periovulatory heifers after GnRH analogs measured by two types of immunoassays.
Bambang Poernomo, S; Becker, F; Bellmann, A; Kanitz, W; Nürnberg, G; Rehfeldt, C; Schneider, F, 2002
)
0.67
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (43)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's14 (32.56)18.2507
2000's27 (62.79)29.6817
2010's1 (2.33)24.3611
2020's1 (2.33)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 (%)
Trials2 (4.35%)5.53%
Reviews3 (6.52%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other41 (89.13%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase I, Open-label, Single Centre Study Investigating the PK, Safety and PD of a Single Dose of Teverelix TFA, a GnRH Antagonist, Via s.c. or i.m. Route of Administration in Healthy Male Volunteers [NCT03781947]Phase 148 participants (Actual)Interventional2018-11-19Completed
An Adaptive Phase 2, Open-Label, Multicentre Study Investigating the Pharmacokinetics, Pharmacodynamics, Efficacy and Safety of Teverelix Trifluoroacetate, a GnRH Antagonist, in Participants With Advanced Prostate Cancer [NCT04693507]Phase 250 participants (Actual)Interventional2021-03-04Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]