Clinical use of GnRH analogues

Kiesel, L.; Rody, Achim; Greb, Robert R.; Szilágyi, András

doi:10.1046/j.1365-2265.2002.01291.x

Cited by 83 publications

(63 citation statements)

References 81 publications

(82 reference statements)

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“…Analogues that capitalize on both mechanisms have been highly effective in suppressing the serum levels of gonadotrophins and steroid hormone production, provoking a chemical castration (Cusan et al 1979, Conn & Crowley 1991, Filicori 1994, Emons et al 1997, Ulloa-Aguirre & Timossi 2000, Kiesel et al 2002, Chabbert-Buffet et al 2003. Nevertheless, complete and prolonged suppression of gonadotrophin secretion and gonadal steroids by GnRH analogues frequently results in symptoms of oestrogen deficiency (DeFazio et al 1983, Matta et al 1987, Johansen et al 1988, Tummon et al 1988, Conn & Crowley 1991, Fogelman 1992, Pierce et al 2000.…”

Section: Introductionmentioning

confidence: 99%

“…The ability to suppress reproductive function by the continuous stimulation of the GnRHR by agonists (desensitization), or through continuous occupancy of the GnRHR with antagonists, has led to the development of GnRH agonists and antagonists currently employed as key therapeutic agents in a number of diseases, including cancer (Conn & Crowley 1991, Filicori 1994, Emons et al 1997, Kiesel et al 2002, Chabbert-Buffet et al 2003. Analogues that capitalize on both mechanisms have been highly effective in suppressing the serum levels of gonadotrophins and steroid hormone production, provoking a chemical castration (Cusan et al 1979, Conn & Crowley 1991, Filicori 1994, Emons et al 1997, Ulloa-Aguirre & Timossi 2000, Kiesel et al 2002, Chabbert-Buffet et al 2003.…”

Section: Introductionmentioning

confidence: 99%

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Identification of new gonadotrophin-releasing hormone partial agonists

Leaños‐Miranda

Ulloa‐Aguirre²,

Cervini³

et al. 2006

Journal of Endocrinology

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GnRH agonists or antagonists are currently utilized as therapeutic agents in a number of diseases. A side-effect of prolonged treatment with GnRH analogues is hypoestrogenism. In this study, we tested the in vitro potency of different GnRH analogues originally found to be partial agonists (i.e. analogues with decreased efficacy for activating or stimulating their cognate receptor) as well as novel analogues, to identify compounds that might potentially be useful for partial blockade of gonadotrophin release.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Identification of new gonadotrophin-releasing hormone partial agonists

Leaños‐Miranda

Ulloa‐Aguirre²,

Cervini³

et al. 2006

Journal of Endocrinology

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“…Email: deepakpharmatech @ gmail.com Deslorelin is a luteinizing hormone releasing hormone (LHRH)/Gonadotropin releasing hormone (GnRH) analogue which is 144 times more potent than the native LHRH/GnRH (Suprelorin, 2010). It is used to treat prostate cancer, endometriosis, uterine fibroids, precocious puberty and breast cancer (Kiesel et al, 2002). Treatment with GnRH or its agonists require long term therapy primarily by parenteral route (i.v., s.c. or i.m.)…”

Section: * Corresponding Authormentioning

confidence: 99%

“…It is used to treat prostate cancer, endometriosis, uterine fibroids, precocious puberty and breast cancer (Kiesel et al, 2002). Treatment with GnRH or its agonists require long term therapy primarily by parenteral route (i.v., s.c. or i.m.…”

Section: Introductionmentioning

confidence: 99%

Development and optimization of in-situ forming microparticles for long term controlled delivery of deslorelin acetate

Kapoor¹,

Katare²,

Kaurav³

et al. 2018

J App Pharm Sci

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Deslorelin is a nonapeptide analogue of the natural gonadotropin releasing hormone or luteinizing hormone releasing hormone used to treat prostate cancer, endometriosis and uterine fibroids. In-situ forming microparticles were developed for deslorelin using smart, biodegradable polymer i.e. PLGA. Response surface, I-optimal design were used to design, formulate and characterize different formulations of deslorelin. To determine the optimized formulation, numerical and graphical optimization techniques were employed. The resulting optimized formulation was evaluated for other physicochemical parameters viz., rheology, particle size distribution, surface morphology of the particles, peptide conformation stability in the formulation and stability study at different environmental conditions. It was concluded that the optimized deslorelin acetate ISFM formulation effectively extended the peptide release for 30 days while maintaining its conformational stability during the period of study. The optimized ISFM formulation was found to be stable at 5°C ± 2°C and 25°C ± 2°C during 6 months stability studies. Key words:PLGA, Implants, Optimal Design, Peptide and Protein Delivery. INTRODUCTIONUnlike conventional small molecules, therapeutic proteins are difficult to be administered orally because they are liable to degradation by the harsh gastric environment, hepatic metabolism and short half-lives thereby necessitating frequent administration of high doses by parenteral route (Cleland et al., 2001;Fu et al., 2000;Robinson and Talmadge, 2002). This may lead to major compliance issues in case of geriatric and pediatric patients on replacement therapy. To improve the patient compliance and convenience, prefilled syringes, needleless injectors, auto injectors, pen devices and syringe injectors have been introduced in the market (Arslanoglu et al., 2000;Oberye et al., 2000). However, even these modified and improved versions have their own limitations like higher cost and complex manufacturing process. Moreover, they do not address the requirement for decrease in the dosing frequency. * Corresponding AuthorDeepak N Kapoor, School of Pharmaceutical Sciences, Shoolini University of Biotechnology and Management Sciences, Solan-173212, H.P., India. Email: deepakpharmatech @ gmail.com Deslorelin is a luteinizing hormone releasing hormone (LHRH)/Gonadotropin releasing hormone (GnRH) analogue which is 144 times more potent than the native LHRH/GnRH (Suprelorin, 2010). It is used to treat prostate cancer, endometriosis, uterine fibroids, precocious puberty and breast cancer (Kiesel et al., 2002). Treatment with GnRH or its agonists require long term therapy primarily by parenteral route (i.v., s.c. or i.m.) since these peptides are vulnerable to gastrointestinal peptidase degradation which makes them inappropriate for oral administration with only 0.1% bioavailability (Conn and Crowley, 1991; Chrisp and Goa, 1990). Intra-nasal administration of deslorelin is also ineffective and inconstant, with only 4 to 21% being available rel...

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“…GnRH analogues are also employed in almost all cycles for IVF treatment to avoid the spontaneous LH surge and loss of oocytes before laproscopic surgery for oocyte retrieval 66 . In all other applications of GnRH analogues, alternative therapeutic approaches are available (for details the reader is referred to a review 67 ).…”

Section: Therapeutic Applications Of Gnrh Analoguesmentioning

confidence: 99%

Current and future applications of GnRH, kisspeptin and neurokinin B analogues

Millar

Newton

2013

Nat Rev Endocrinol

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Reproductive hormones impact on all stages of life from gamete production, fertilisation, fetal development and parturition, neonatal development and puberty through to adulthood and senescence.The reproductive hormone cascade has therefore been the target for the development of numerous drugs which modulate its activity at many levels. As the central regulator of the cascade, gonadotropinreleasing hormone (GnRH) agonists and antagonists have found extensive applications in treating a wide range of hormone-dependent deseases such as precocious puberty, prostate cancer, benign prostatic hyperplasia, endometriosis and uterine fibroids, as well as being an essential component of in vitro fertilisation (IVF) protocols. Recently-discovered neuroendocrine peptides, kisspeptin (KP) and neurokinin B (NKB), have also been identified as therapeutic targets and novel agonists and antagonists are being developed as modulators of the cascade upstream of GnRH. Here we review the development and applications of analogues of the major neuroendocrine peptide regulators of the reproductive hormone cascade, GnRH, KP and NKB.

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Clinical use of GnRH analogues

Cited by 83 publications

References 81 publications

Identification of new gonadotrophin-releasing hormone partial agonists

Identification of new gonadotrophin-releasing hormone partial agonists

Development and optimization of in-situ forming microparticles for long term controlled delivery of deslorelin acetate

Current and future applications of GnRH, kisspeptin and neurokinin B analogues

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