Abstract
The behaviour of [DesGly10, D-Ser(t-Bu)]6]-GnRH EA (HOE 766) has been studied in plasma and urine after intranasal (IN,200 ug) or subcutaneous (SC,10 ug/kg) administrations . A RIA for HOE 766 and its metabolites has been developed using 125I-[DesGly10, DTrp6]-GnRH EA (Gift of Dr. J. Rivier) as tracer and an antiserum to HOE 766 (gift of Dr. H. Fraser). Crossreaction with native GnRH was only 1.7 %. Sensitivity was 1 pg/tube. In 6 male adolescents, mean plasma HOE 766 concentration (±SE) was 0.46±0.08 , 0.50±0.10, 0.28±0.04, 0.24±0.04, 0.13±0.03, and 0.08 ±0.02 ng/ml, 30, 60, 90, 120 and 180 min. after IN administration. Urine excretion of HOE 766 metabolites was 9.4±2.0 ug/4h. There was a good correlation between plasma and urine levels (r=0.92). In the same 6 volunteers, plasma HOE 766 levels were 21.2±3.0, 25.9±0.8, 21.2 ±0.9, 17.1±0.7, 12.8±1.1, 8.9±0.4, and 5.9±0.8, 20, 40, 60, 120, 180 and 240 min. after the SC injection. In two girls with precocious puberty followed during 3 months with IN treatment, urine excretion of HOE 766 was in good correlation with the degree of inhibition of E2 and of LH and FSH responses to GnRH. The monitoring of HOE 766 metabolites in the urine thus appears to be helpful for the evaluation of the intranasal therapy of precocious puberty with GnRH analog.
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Reznik, Y., Winiger, B., Aubert, M. et al. Pharmacodynamics of (DesGly10,D-Ser(t-Bu))6−GnKH EA in 6 normal volunteers and in 2 girls with Precocious Puberty. Pediatr Res 18, 1210 (1984). https://doi.org/10.1203/00006450-198411000-00056
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DOI: https://doi.org/10.1203/00006450-198411000-00056
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