Antide bioavailability: single dose administration for suppression of testosterone and inhibin in male monkeys.
The pharmacokinetics and pharmacodynamics of a single sc injection of Antide on testosterone (T) and inhibin secretion in intact male cynomolgus monkeys were examined. Fifteen primates were randomized to three groups receiving: propylene glycol and water vehicle, 3 mg/kg Antide, and 10 mg/kg of Antide. Antide at the 10 mg/kg dose caused long-term suppression of T ranging from 24-56 days. At the 3 mg/kg dose, suppression of T was of shorter duration. Serum Antide levels were significantly greater in the 10 mg/kg group than the 3 mg/kg group (p less than 0.02), both initially and through 35 days post-treatment. The duration of testosterone inhibition and sustained Antide levels were significantly correlated (p less than 0.01). Inhibin concentrations followed the same general pattern as testosterone reaching a nadir on day 21 post-treatment before subsequent recovery. The prolonged suppressive effect of Antide on T without detectable side effects makes this compound an excellent candidate for clinical evaluation.
Edelstein
M C
MC
Jones Institute for Reproductive Medicine, Department of Obstetrics and Gynecology, Eastern Virginia Medical School, Norfolk 23510.
Gordon
K
K
Williams
R F
RF
Danforth
D R
DR
Winters
S J
SJ
Hodgen
G D
GD
D000818:Animals; D001682:Biological Availability; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D007265:Inhibins / Q000097:blood / Q000378:metabolism*; D007279:Injections, Subcutaneous; D008252:Macaca fascicularis; D008297:Male; D009842:Oligopeptides / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D011863:Radioimmunoassay; D011869:Radioligand Assay; D013739:Testosterone / Q000097:blood / Q000378:metabolism*; D013997:Time Factors
D009842:Oligopeptides; D013739:Testosterone; D007265:Inhibins; C057022:iturelix