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High inhibition ratio and transformation index of 2 mg dienogest: further evidence for its use in endometriosis treatment.

Endometriosis is a common, chronic disease with a high burden for women, characterised by the implantation of endometrial cells outside the uterus. Many different treatments have been proposed for this …

Published: Dec. 2, 2025, midnight
Design of a peripherally biased NPSR1 antagonist for neuropeptide S induced inflammation.

Neuropeptide S (NPS) is a potent agonist for the GPCR receptor NPSR1, implicated in various physiological and pathological processes, including inflammation. NPSR1 gene polymorphisms have been linked to asthma, inflammatory …

Published: Aug. 5, 2025, midnight
Safety and pharmacology of AMY109, a long-acting anti-interleukin-8 antibody, for endometriosis: a double-blind, randomized phase 1 trial.

To evaluate the safety and pharmacokinetics/pharmacodynamics of AMY109, an anti-interleukin-8 recycling antibody in a first-in-human phase 1 trial in healthy volunteers (HVs) and patients with endometriosis.

Published: May 2, 2025, midnight
Transfer of the Oral Gonadotropin-Releasing Hormone Receptor Antagonist Relugolix Into Breast Milk of Healthy Lactating Women.

Relugolix is an oral gonadotropin-releasing hormone receptor antagonist that suppresses sex steroid hormones and is approved as monotherapy for prostate cancer and as a fixed-dose combination with estradiol/norethindrone for the …

Published: Feb. 1, 2025, midnight
GnRH Peptide Antagonist: Comparative Analysis of Chemistry and Formulation with Implications for Clinical Safety and Efficacy.

Overexpression of the gonadotropin-releasing hormone receptor (GnRH-R) plays a vital role in the advancement of reproductive malignancies such as ovarian, endometrial, and prostate cancer. Peptidomimetic GnRH antagonists are a substantial …

Published: Dec. 31, 2024, midnight
The oral GnRH antagonists, a new class of drugs in gynecology: from pharmacokinetics to possible clinical applications.

In ovarian steroid-dependent diseases such as uterine fibroids, endometriosis and adenomyosis, oral GnRH antagonists have emerged as new therapeutic alternatives. These oral GnRH antagonists offer key advantages, including oral administration, …

Published: Dec. 12, 2024, midnight
Endometriosis: cannabidiol therapy for symptom relief.

Endometriosis is a common, chronic, incurable condition the hallmark of which is the presence of lesions (tissue resembling endometrium) in sites outside the womb, with symptoms including chronic debilitating pain …

Published: Nov. 14, 2024, midnight
Safety, Pharmacokinetics, and Pharmacodynamics of SHR7280, a Non-peptide GnRH Antagonist in Premenopausal Women with Endometriosis: A Randomized, Double-Blind, Placebo-Controlled Phase 1 Study.

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 …

Published: Oct. 14, 2023, midnight
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