PMID- 34448368
OWN - NLM
STAT- MEDLINE
DCOM- 20220404
LR  - 20220531
IS  - 2160-7648 (Electronic)
IS  - 2160-763X (Linking)
VI  - 11
IP  - 2
DP  - 2022 Feb
TI  - Pharmacokinetic, Safety, and Pharmacodynamic Properties of Teverelix 
      Trifluoroacetate, a Novel Gonadotropin-Releasing Hormone Antagonist, in Healthy 
      Adult Subjects.
PG  - 257-269
LID - 10.1002/cpdd.1008 [doi]
AB  - Teverelix trifluoroacetate is a decapeptide, gonadotropin-releasing hormone 
      antagonist that binds competitively and reversibly to gonadotropin-releasing 
      hormone receptors in the pituitary gland, resulting in immediate suppression of 
      luteinizing hormone and follicle-stimulating hormone, which in turn causes a very 
      rapid decrease in testosterone production in the Leydig cells of the testes in 
      men and in estradiol in the ovaries in women. This phase 1 clinical study was an 
      open-label, parallel-design, single-center, single-dose study in older, healthy 
      male subjects. Following injection, teverelix is released into the systemic 
      circulation in a biphasic manner. An initial rapid phase is followed by a 
      slow-release phase thought to be due to the formation of a depot, which limits 
      the diffusion of teverelix into the blood. The release characteristics differ 
      significantly for the subcutaneous (SC) and intramuscular (IM) routes. Teverelix 
      maximum concentration and exposure increased in an approximately 
      dose-proportional manner across the 60 to 120 mg SC doses. 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.
CI  - (c) 2021, The American College of Clinical Pharmacology.
FAU - MacLean, Carol M
AU  - MacLean CM
AD  - Antev Ltd, London, UK.
FAU - Godsafe, Zona
AU  - Godsafe Z
AD  - Antev Ltd, London, UK.
FAU - Soto-Forte, Pablo
AU  - Soto-Forte P
AD  - PAREXEL Early Phase Clinical Unit, Northwick Park Hospital, Harrow, UK.
FAU - Larsen, Finn
AU  - Larsen F
AD  - Antev Ltd, London, UK.
LA  - eng
PT  - Clinical Trial, Phase I
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20210826
PL  - United States
TA  - Clin Pharmacol Drug Dev
JT  - Clinical pharmacology in drug development
JID - 101572899
RN  - 0 (Hormone Antagonists)
RN  - 0 (Oligopeptides)
RN  - 33515-09-2 (Gonadotropin-Releasing Hormone)
RN  - D19V7048JK (antarelix)
RN  - E5R8Z4G708 (Trifluoroacetic Acid)
SB  - IM
MH  - Aged
MH  - Gonadotropin-Releasing Hormone
MH  - *Hormone Antagonists/adverse effects
MH  - Humans
MH  - Male
MH  - *Oligopeptides/adverse effects
MH  - Trifluoroacetic Acid
OTO - NOTNLM
OT  - BPH
OT  - CV safety
OT  - GnRH antagonist
OT  - endometriosis
OT  - local tolerability
OT  - long-acting injectable
OT  - pharmacodynamic
OT  - pharmacokinetic
OT  - prostate cancer
OT  - uterine fibroids
EDAT- 2021/08/28 06:00
MHDA- 2022/04/05 06:00
CRDT- 2021/08/27 07:22
PHST- 2021/05/17 00:00 [received]
PHST- 2021/07/22 00:00 [accepted]
PHST- 2021/08/28 06:00 [pubmed]
PHST- 2022/04/05 06:00 [medline]
PHST- 2021/08/27 07:22 [entrez]
AID - 10.1002/cpdd.1008 [doi]
PST - ppublish
SO  - Clin Pharmacol Drug Dev. 2022 Feb;11(2):257-269. doi: 10.1002/cpdd.1008. Epub 
      2021 Aug 26.