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Recent Trends in Medical Management of Endometriosis.
J Obstet Gynaecol India
December 2024
Nowrosjee Wadia Maternity Hospital, Mumbai, India.
Endometriosis affects about 10 percent women in the reproductive age group globally and approximately 42 million in India. Managing the patient's pain symptoms associated with endometriosis appears to be the cornerstone in endometriosis disease management. The ideal medical treatment in endometriosis would be suppressing estradiol enough to alleviate symptoms of endometriosis but maintain sufficient levels to mitigate hypoestrogenic side effects.
View Article and Find Full Text PDFNovel non-peptide uracil-derived human gonadotropin-releasing hormone receptor antagonists.
Eur J Med Chem
December 2024
Department of Pharmaceutical Sciences, University of Milan, Milan, Italy.
Gonadotropin-releasing hormone (GnRH) is the main regulator of the reproductive system, acting on gonadotropic cells by binding to the GnRH1 receptor (GnRH1R). Traditionally, therapies targeting this receptor have relied on peptide modulators, which required subcutaneous or intramuscular injections. Due to the limitations of the parenteral administrations, there is a growing interest in developing oral small molecule modulators of GnRH1R as more convenient therapeutic alternatives.
View Article and Find Full Text PDFSafety, Pharmacokinetics, and Pharmacodynamics of SHR7280, a Non-peptide GnRH Antagonist in Premenopausal Women with Endometriosis: A Randomized, Double-Blind, Placebo-Controlled Phase 1 Study.
Clin Pharmacokinet
December 2023
Department of Obstetrics and Gynecology, Peking University Third Hospital, 49 Huayuan North Road, Beijing, 100000, China.
Background: Oral gonadotropin-releasing hormone (GnRH) antagonists are promising agents in the treatment of endometriosis-related pain. Here we assessed the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of SHR7280, an oral non-peptide GnRH antagonist in premenopausal women with endometriosis.
Methods: In the Phase 1 part of the randomized, double-blinded, placebo-controlled, dose-ascending, Phase 1/2 trial, premenopausal women with endometriosis were randomized (4:1) to receive SHR7280 or placebo treatment for 21 consecutive days.
Profile of Relugolix in the Management of Advanced Hormone-Sensitive Prostate Cancer: Design, Development, and Place in Therapy.
Drug Des Devel Ther
August 2023
Department of Pathology & Laboratory Medicine, University of Rochester Medical Center, Rochester, NY, USA.
Androgen deprivation therapy, primarily via a gonadotropin-releasing hormone receptor agonist or antagonist together with or without an androgen receptor antagonist, remains the mainstay of medical treatment for advanced prostate cancer. Meanwhile, relugolix has been developed as the first orally active, non-peptide, selective antagonist for the gonadotropin-releasing hormone receptor. Previous randomized studies involving patients with prostate cancer have demonstrated comparable efficacy in androgen suppression between relugolix vs other gonadotropin-releasing hormone antagonists or agonists.
View Article and Find Full Text PDFSuppressive effects of linzagolix, a novel non-peptide antagonist of gonadotropin-releasing hormone receptors, in experimental endometriosis model rats.
Clin Exp Pharmacol Physiol
July 2023
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd., Azumino, Japan.
Endometriosis is an oestrogen-dependent disease in which endometrial-like tissue grows outside the uterus in women of reproductive age. Accordingly, control of oestradiol (E2) levels is an effective treatment for endometriosis. Because gonadotropin-releasing hormone (GnRH) is the main controller of E2 secretion, control of GnRH signalling by GnRH antagonism is an effective strategy for the treatment of sex hormone-dependent diseases such as endometriosis.
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