Radioimmunoassay of meterelin and pharmacokinetics after single injection and implant administration in dogs.

  title={Radioimmunoassay of meterelin and pharmacokinetics after single injection and implant administration in dogs.},
  author={E. Hudon and J. Rondeau and V. Lenaerts and P. W{\"u}rthrich and F. Boutignon and R. Deghenghi and S. Marleau and N. Yamaguchi and A. Adam and H. Ong},
  journal={Journal of pharmaceutical sciences},
  volume={86 2},
A sensitive and specific radioimmunoassay for a novel luteinizing-hormone-releasing-hormone (LHRH) agonist, [2-Me-D-Trp6, DesGly10]LHRH ethylamide (meterelin), was developed for documenting the pharmacokinetic parameters of this peptide following its intravenous (iv) and subcutaneous (sc) administration in dogs. The assay was also used for monitoring meterelin in plasma following its release from d,l-lactide-glycolide implants in the same species. Rabbit antisera generated against [DespyroGlu1… Expand
2 Citations
Population Pharmacokinetic/ Pharmacodynamic Modeling of Cetrorelix, a Novel LH-RH Antagonist, and Testosterone in Rats and Dogs
A population pharmacokinetic model was developed to explain the dissolution rate limited absorption from the injection site of cetrorelix and the suppression of testosterone. Expand
Pharmacodynamics of a long acting depot preparation of avorelin in patients with prostate cancer. Avorelin Study Group.
Subcutaneous depot formulations of avorelin were well tolerated and had protracted inhibitory effects on pituitary gonadotropin secretion in patients with prostate cancer, and could be the first luteinizing hormone-releasing hormone agonist formulation to be administered at 6-month intervals. Expand


Radioimmunoassay of [d-Trp6]-luteinizing hormone-releasing hormone: its application to animal pharmacokinetic studies after single injection and long-acting formulation administration
A sensitive radioimmunoassay (RIA) for [D-Trp6]-luteinizing hormone-releasing hormone (LHRH) has been developed and will be particularly useful for the evaluation of long-acting formulations in patients with advanced prostate cancer. Expand
Radioimmunoassay for 6-D-tryptophan analog of luteinizing hormone-releasing hormone: measurement of serum levels after administration of long-acting microcapsule formulations.
A sensitive and specific radioimmunoassay for [6-D-tryptophan]luteinizing hormone-releasing hormone [( D-Trp6]LH-RH) was developed and used for following the rate of liberation from a long-acting delivery system based on a microcapsule formulation, permitting the study of blood levels of the analog after single injections into normal men and after once-a-month administration of microcapsules to rats. Expand
Radioimmunoassay of an analog of luteinizing hormone-releasing hormone, [D-Ser(tBu)]6des-Gly-NH2(10) ethylamide (Buserelin).
Results indicate that this method for radioimmunoassay of buserelin is suitable for analyzing the pharmacokinetics and bioavailability of buSErelin in man. Expand
Pharmacokinetics and endocrine effects of slow release formulations of LHRH analogues
Results on the controlled release of an L HRH antagonist from biodegradable microparticles in rats with DMBA-induced mammary tumours indicate that tumour suppression by LHRH antagonists is well tolerated and highly effective. Expand
Radioimmunoassay of 5-androstene-3β,17β-diol in plasma and in breast cyst fluid
Abstract A simple and reliable radioimmunoassay for the determination of 5-androstene-3β,17β-diol in peripheral plasma and in breast cyst fluid, after a chromatography on Celite microcolumn has beenExpand
Disposition of nafarelin acetate, a potent agonist of luteinizing hormone-releasing hormone, in rats and rhesus monkeys.
This work has studied the distribution and excretion of radiolabeled nafarelin acetate administered iv to rats and rhesus monkeys and has compared the pharmacokinetics to LHRH in these two species and found that of the 13 tissues assayed, highest concentrations of radioactivity were observed in the kidneys, liver, and intestine. Expand
Subcutaneous administration of gonadotropin-releasing hormone: absorption kinetics and gonadotropin responses.
It is concluded that sc GnRH administration results in pulsatile plasma GnRH and gonadotropin responses, the latter resembling those seen after iv GnRH. Expand
Model of the distribution and metabolism of the gonadotropin-releasing hormone (GnRH) agonist [D-Trp6,Des-Gly-NH2(10)]GnRH ethylamide in man.
The plasma dynamics of GnRH ethylamide in men are at least 10 times slower than those reported for the natural GnRH, thus indicating the relevance of its clinical use in suppressive therapy of LH secretion. Expand
Metabolic clearance and plasma half-disappearance time of D-TRP6 and exogenous luteinizing hormone-releasing hormone.
Findings indicated that the enhanced bioactivity of D-Trp6 LRH is in part due to a decreased rate of degradation. Expand
A new extra long acting depot preparation of the LHRH analogue Zoladex®. First endocrinological and pharmacokinetic data in patients with advanced prostate cancer
Taking into account social and psychological factors, patients with advanced prostate carcinoma will soon be able to be treated with a longer acting LHRH depot formulation every 3 months an alternative of the 1-month depot now widely used clinically. Expand