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Review
. 2021 Feb 16:15:639-649.
doi: 10.2147/DDDT.S291369. eCollection 2021.

Progress in Clinical Research on Gonadotropin-Releasing Hormone Receptor Antagonists for the Treatment of Prostate Cancer

Yi-Fu Liu  1 , Sheng-Qiang Fu  1 , Yu-Chang Yan  1 , Bin-Bin Gong  1 , Wen-Jie Xie  1 , Xiao-Rong Yang  1 , Ting Sun  1 , Ming Ma  1
Affiliations
Review

Progress in Clinical Research on Gonadotropin-Releasing Hormone Receptor Antagonists for the Treatment of Prostate Cancer

Yi-Fu Liu et al. Drug Des Devel Ther. .

Abstract

Gonadotropin-releasing hormone (GnRH) receptor agonists are still the most commonly used androgen deprivation treatment (ADT) drugs for prostate cancer in clinical practice. Currently, the GnRH receptor antagonists used for endocrine therapy for prostate cancer primarily include degarelix and relugolix (TAK-385). The former is administered by subcutaneous injection, while the latter is an oral drug. Compared to GnRH agonists, GnRH antagonists reduce serum testosterone levels more rapidly without an initial testosterone surge or subsequent microsurges. This review focuses on the mechanism of action of GnRH antagonists and agonists, the developmental history of GnRH antagonists, and emerging data from clinical studies of the two antagonists used as endocrine therapy for prostate cancer.

Keywords: degarelix; gonadotropin-releasing hormone; prostate cancer; relugolix.

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Conflict of interest statement

All authors declare that they have no conflicts of interest related to this manuscript.

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Figure 1
Figure 1
Flow diagram of evidence collection.
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References

    1. Center MM, Jemal A, Lortet-Tieulent J, et al. International variation in prostate cancer incidence and mortality rates. Eur Urol. 2012;61(6):1079–1092. doi: 10.1016/j.eururo.2012.02.054 - DOI - PubMed
    1. Culp MB, Soerjomataram I, Efstathiou JA, Bray F, Jemal A. Recent global patterns in prostate cancer incidence and mortality rates. Eur Urol. 2020;77(1):38–52. doi: 10.1016/j.eururo.2019.08.005 - DOI - PubMed
    1. Huggins C, Hodges CV. Studies on prostatic cancer. I. The effect of castration, of estrogen and of androgen injection on serum phosphatases in metastatic carcinoma of the prostate. 1941. J Urol. 2002;167(2 Pt 2):948–951. doi: 10.1016/S0022-5347(02)80307-X - DOI - PubMed
    1. Rick FG, Block NL, Schally AV. Agonists of luteinizing hormone-releasing hormone in prostate cancer. Expert Opin Pharmacother. 2013;14(16):2237–2247. doi: 10.1517/14656566.2013.834328 - DOI - PubMed
    1. Schally AV, Arimura A, Baba Y, et al. Isolation and properties of the FSH and LH-releasing hormone. Biochem Biophys Res Commun. 1971;43(2):393–399. doi: 10.1016/0006-291X(71)90766-2 - DOI - PubMed

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