Figure 1

Figure 1. From: An update on the use of degarelix in the treatment of advanced hormone-dependent prostate cancer.

Mode of action of antagonists of LHRH. (A) LHRH secreted by the hypothalamus binds to its receptor in the pituitary and stimulates the release of LH and FSH. These hormones, in turn, stimulate the release of sex steroids, which can stimulate growth and development of both normal and tumor cells. (B) Some tumors express LHRH receptors and can respond directly to LHRH; cells in these tumors can be sex-steroid-dependent or sex-steroid-independent. (C) LHRH antagonists induce a state of sex steroid deprivation by competitive blockade of pituitary LHRH receptors, whereas LHRH agonists achieve a similar effect by downregulation of the pituitary receptors for LHRH. Consequently, levels of FSH and LH, and subsequently levels of sex steroids, are lowered. The decrease in the levels of sex steroids inhibits the proliferation of both benign and malignant sex-steroid-dependent cells. (D) In tumors that express LHRH receptors, both antagonists and agonists of LHRH may exert direct effects mediated by these LHRH receptors.
Modified from Engel JB and Schally AV with permission.18 Copyright 2013 Nature Publishing Group.
Abbreviations: FSH, follicle-stimulating hormone; LH, luteinizing hormone; LHRH, luteinizing hormone-releasing hormone.

Ferenc G Rick, et al. Onco Targets Ther. 2013;6:391-402.

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