Drug Insight: clinical use of agonists and antagonists of luteinizing-hormone-releasing hormone

  title={Drug Insight: clinical use of agonists and antagonists of luteinizing-hormone-releasing hormone},
  author={J{\"o}rg Bernhard Engel and Andrew V. Schally},
  journal={Nature Clinical Practice Endocrinology \&Metabolism},
  • J. EngelA. Schally
  • Published 1 February 2007
  • Medicine, Biology
  • Nature Clinical Practice Endocrinology &Metabolism
This article reviews the clinical uses of agonists and antagonists of luteinizing-hormone-releasing hormone (LHRH), also known as gonadotropin-releasing hormone. In particular, the state of the art treatment of breast, ovarian and prostate cancer, reproductive disorders, uterine leiomyoma, endometriosis and benign prostatic hypertrophy is reported. Clinical applications of LHRH agonists are based on gradual downregulation of pituitary receptors for LHRH, which leads to inhibition of the… 

Luteinizing Hormone-Releasing Hormone and Its Agonistic, Antagonistic, and Targeted Cytotoxic Analogs in Prostate Cancer

Experimental studies and early clinical trials with targeted cytotoxic L HRH analogs developed recently for targeted chemotherapy of tumors expressing LHRH receptors are described and reviewed.

Analogs of Luteinizing Hormone-Releasing Hormone in the Treatment of Endometriosis

LHRH agonists can be considered in general as a second-line medical treatment for endometriosis-related symptoms, as oral therapy with dienogest is as effective and has fewer side effects.

Agonists of luteinizing hormone-releasing hormone in prostate cancer

Degarelix, a highly clinically effective third-generation L HRH antagonist, is currently available in most countries for therapy of advanced PCa and offers attractive alternatives to LHRH agonists for treatment ofAdvanced PCa.

Gonadotropin-releasing hormone antagonist: A real advantage?

Synthesis and Characterization of Luteinizing Hormone-Releasing Hormone (LHRH)-Functionalized Mini-Dendrimers

Two types of LHRH mini-dendrimers are synthesized using thioether ligation, aiming to enhance the stability and bioavailability of the peptide drug while maintaining its biologically active conformation.

An update on the use of degarelix in the treatment of advanced hormone-dependent prostate cancer

Recent clinical trials demonstrated that treatment with degarelix results in improved disease control when compared with an LHRH agonist in terms of superior PSA progression-free survival, suggesting that degarelIX likely delays progression to castration-resistant disease and has a more significant impact on bone serum alkaline phosphatase and follicle-stimulating hormone.

Overview of elagolix for the treatment of endometriosis

Elagolix demonstrated efficacy in the management of endometriosis-associated pain and had an acceptable safety and tolerability profile, however, further studies are necessary to evaluate its non-inferiority in comparison with other endometRIosis’s treatments.

Antiproliferative Effects of GnRH Agonists: Prospects and Problems for Cancer Therapy

Data on the effects of GnRH agonists on cell proliferation and apoptosis is reviewed, and hypotheses for investigation are put forward to determine whether the GnRH receptor acts as a tumor suppressor in neuroendocrine or epithelial cells.

The role of gonadotropin releasing hormone in normal and pathologic endocrine processes

Research into the role of the fibroblast growth factor receptor-1 and kisspeptin/G-protein-coupled receptor 54 pathways in gonadotropin releasing hormone neuronal development may identify the molecular defects in idiopathic hypogonadotropic hypogONadism and refine the understanding of normal negative and positive feedback by sex steroids.



Luteinizing hormone-releasing hormone analogs: their impact on the control of tumorigenesis☆

The use of luteinizing hormone releasing hormone agonists and antagonists in gynaecological cancers.

Experimental data and several pilot clinical trials suggest that in epithelial ovarian cancer and sex-cord-stromal tumours of the ovary, LHRH agonists might have antitumour activity through the suppression of gonadotrophin secretion (selective medical hypophysectomy).

Hypothalamic Hormones and Cancer

Treatment of many cancers remains a major challenge, but new therapeutic modalities are being developed based on antagonists of GH-RH and bombesin, which inhibit growth factors or their receptors, and somatostatin, which can be targeted to receptors for these peptides in various cancers and their metastases.

Peptidomimetic GnRH receptor antagonists for the treatment of reproductive and proliferative diseases

This review summarises the patent literature during 2001 – 2005 on small-molecule GnRH receptor antagonists.

Use of GnRH antagonists in the treatment of endometriosis.

Inhibition of luteinizing hormone, follicle-stimulating hormone and sex-steroid levels in men and women with a potent antagonist analog of luteinizing hormone-releasing hormone, Cetrorelix (SB-75).

In postmenopausal women, inhibition of the elevated basal serum LH and FSH levels occurred after a single injection of the antagonist analog SB-75 in doses of 75, 150, 300, 600 and 1200 micrograms using im, sc and iv routes of administration.

Inhibitory activity of luteinizing hormone-releasing hormone on tumor growth and progression.

Data indicate that in prostate cancer cells the LHRH receptor is coupled to a Gi-cAMP signal transduction pathway, and in melanoma cells, L HRH might act as an inhibitory factor on both cell proliferation and metastatic behavior.

Efficacy and safety of luteinizing hormone-releasing hormone antagonist cetrorelix in the treatment of symptomatic benign prostatic hyperplasia.

This study demonstrates that in patients with symptomatic BPH, treatment with cetrorelix is safe and produces long term improvement.

Estriol add-back therapy in the long-acting gonadotropin-releasing hormone agonist treatment of uterine leiomyomata.

  • H. NakayamaT. Yano Y. Taketani
  • Medicine, Biology
    Gynecological endocrinology : the official journal of the International Society of Gynecological Endocrinology
  • 1999
Evaluating whether treatment of uterine leiomyomata with GnRHa plus oral estriol add-back therapy could prevent bone loss, without deteriorating the therapeutic effect of GnR Ha found it to be feasible and might be considered for long-term treatment of vaginal cancer.