Pharmacokinetics of Gonadotropin-Releasing Hormone and Its Analogs

Handelsman, David J.; Swerdloff, Ronald S.

doi:10.1210/edrv-7-1-95

Cited by 90 publications

(31 citation statements)

References 94 publications

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“…Different stimulation protocols have been suggested as GnRH agonist and GnRH antagonist but still there is no consensus as to which protocol is best for patients with PCOS. 22,23 The objective of the current study was to compare fixed GnRH antagonist protocol in relation to GnRH agonist long luteal protocol in PCO infertile patients undergoing ICSI.…”

Section: Discussionmentioning

confidence: 99%

“…20,21 Gonadotrophin-releasing hormone (GnRH) antagonist is being increasingly used in COS for IVF from late 1990s. 22,23 GnRH antagonists do not require long desensitization as in agonist protocol and induce rapid reduction in the level of follicle stimulating hormone (FSH) and luteinizing hormone (LH) without initial flair up thus ensuring a short and simple IVF cycle and better patient compliance. Although there was initial reports that antagonist cycles were associated with lower on-going pregnancy rate when compared to long agonist cycles.…”

Section: Introductionmentioning

confidence: 99%

“…Although there was initial reports that antagonist cycles were associated with lower on-going pregnancy rate when compared to long agonist cycles. [22][23] In our study we use fixed antagonist protocol as there was a trend toward a higher pregnancy rate with fixed antagonist protocol compared with the flexible antagonist protocol.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Fixed gonadotropin-releasing hormone antagonist protocol versus gonadotropin-releasing hormone agonist long protocol in patients with polycystic ovary syndrome treated for intracytoplasmic sperm injection cycles

Khalifa

Orief

Said

et al. 2016

Int J Reprod Contracept Obstet Gynecol

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Fixed gonadotropin-releasing hormone antagonist protocol versus gonadotropin-releasing hormone agonist long protocol in patients with polycystic ovary syndrome treated for intracytoplasmic sperm injection cycles

Khalifa

Orief

Said

et al. 2016

Int J Reprod Contracept Obstet Gynecol

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“…These analogues are distributed into the extracellular space and metabolized by digestive enzymes and kidney. It is believed that LHRH analogues are predominantly cleared by the kidney due to rapid and extensive renal uptake following IV administration (Handelsman and Swerdloff, 1986). All commercial analogues of LHRH are administered through parenteral routes including subcutaneous and intramuscular (Beyer et al, 2011;Padula, 2005).…”

Section: Introductionmentioning

confidence: 99%

In vivo pharmacological evaluation of a lactose-conjugated luteinizing hormone releasing hormone analogue

Moradi

Varamini

Steyn

et al. 2015

International Journal of Pharmaceutics

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Abstract:In the current study, the efficacy and pharmacokinetic profile of lactose-conjugated luteinizing hormone releasing hormone (LHRH) was examined following oral administration in male rats. A rapid and sensitive liquid chromatography/mass spectrometry technique was developed and applied for measuring the concentration of lactose[Q 1 ][w 6 ]LHRH (compound 1) in rat plasma in order to allow measurement of pharmacokinetic parameters. LH release was evaluated using a sandwich ELISA. Maximum serum concentration (Cmax= 0.11 µg/ml) was reached at 2 h (Tmax) following oral administration of the compound at 10 mg/kg. The half-life was determined to be 2.6 h. The absolute bioavailability of the orally administered compound was found to be 14%, which was a remarkable improvement compared to zero-tolow oral bioavailability of the native peptide. Compound 1 was effective in stimulating LH release at 20 mg/kg after oral administration. The method was validated at a linear range of 0.01-20.0 µg/ml and a correlation coefficient of r 2 ≥0.999. The accuracy and precision values showed the reliability and reproducibility of the method for evaluation of the pharmacokinetic parameters. These findings showed that the lactose derivative of LHRH has a therapeutic potential to be further developed as an orally active therapeutics for the treatment of hormone-dependent diseases.

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“…Numerous analogs have been developed mainly to overcome the very short half-life of GnRH (7,8) and to enhance its affinity for the GnRH receptor (9). These GnRH analogs suppress the growth of various tumor cells in vitro and in vivo.…”

mentioning

confidence: 99%

Adenocarcinoma Cells Are Targeted by the New GnRH-PE66 Chimeric Toxin through Specific Gonadotropin-releasing Hormone Binding Sites

Nechushtan

Yarkoni

Marianovsky

et al. 1997

Journal of Biological Chemistry

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Luteinizing hormone-releasing hormone, also termed gonadotropin-releasing hormone (GnRH), accounts for the hypothalamic-pituitary gonadal control of human reproduction. The involvement of GnRH has been demonstrated in several carcinomas of hormone-responsive tissues. Exploiting this common feature, we constructed a Pseudomonas exotoxin (PE)-based chimeric toxin (GnRH-PE 66 ) aimed at targeting those cancer cells bearing GnRH binding sites. We report here the strong growth inhibition and killing of a surprisingly wide variety of cancers, confined to the adenocarcinoma type. These cancer cells arising from hormone-responsive tissues, as well as non-responsive ones, express specific GnRH binding sites as indicated by the marked killing of ovarian, breast, endometrial, cervical, colon, lung, hepatic, and renal adenocarcinoma. This cytotoxicity is specific as it could be blocked upon addition of excess GnRH. The specificity of GnRH-PE 66 chimeric toxin was also confirmed by GnRH binding assays, and its ability to prevent the formation of colon cancer xenografts in nude mice is presented. Although the functional role of specific GnRH binding sites in human carcinomas remains obscure, GnRH-PE 66 displays considerable targeting potential and its use as a therapeutic agent for cancer should be considered.

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Pharmacokinetics of Gonadotropin-Releasing Hormone and Its Analogs

Cited by 90 publications

References 94 publications

Fixed gonadotropin-releasing hormone antagonist protocol versus gonadotropin-releasing hormone agonist long protocol in patients with polycystic ovary syndrome treated for intracytoplasmic sperm injection cycles

Fixed gonadotropin-releasing hormone antagonist protocol versus gonadotropin-releasing hormone agonist long protocol in patients with polycystic ovary syndrome treated for intracytoplasmic sperm injection cycles

In vivo pharmacological evaluation of a lactose-conjugated luteinizing hormone releasing hormone analogue

Adenocarcinoma Cells Are Targeted by the New GnRH-PE66 Chimeric Toxin through Specific Gonadotropin-releasing Hormone Binding Sites

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