Purpose Of Review: This review is intended to provide perspective on the history of selective progesterone receptor modulators (SPRMs) and progesterone antagonists, their current availability, therapeutic promise and safety concerns.
Recent Findings: Despite keen interest in synthesis of these compounds, only a handful have had clinical test results allowing for commercialization. Mifepristone is well tolerated and effective for single dose first trimester at-home pregnancy termination and is available in much of the world. Ulipristal acetate, at single doses, is well tolerated and effective for emergency contraception, with less availability. Chronic use of these agents has been associated with abnormal liver enzymes, and rarely, with hepatic failure; causality is not understood.
Summary: SPRMs and progesterone antagonists have great therapeutic promise for use in other reproductive disorders, including breast cancer, endometriosis, adenomyosis, estrogen-free contraception and cervical ripening but require additional study. Alternative formulations, whether local (topical breast or intrauterine) or extended-release may reduce the incidence of liver function abnormalities and should be explored.
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http://dx.doi.org/10.1097/MED.0000000000000753 | DOI Listing |
J Chromatogr B Analyt Technol Biomed Life Sci
January 2025
Jilin Ginseng Academy, Changchun University of Chinese Medicine, Changchun 130117 China. Electronic address:
This study aimed to develop molecularly imprinted polymer (MIP) nanoparticles specifically for the selective extraction and enrichment of progesterone (P) from royal jelly (RJ), and quantitatively analyzed them by ultra-performance-liquid chromatography electrospray ionization mass spectrometry (UPLC-ESI-MS). Gaussian software-based theoretical calculations identified methacrylic acid (MAA) as the optimal functional monomer for its strong binding affinity to P. MIP was synthesized by precipitation polymerization, and the preparation process of MIP was optimized by one-way variance design and response surface methodology.
View Article and Find Full Text PDFJ Gerontol A Biol Sci Med Sci
January 2025
Department of Clinical Epidemiology, Leiden University Medical Center, Leiden, The Netherlands.
Chronological age is a major risk factor for numerous diseases. However, chronological age does not capture the complex biological aging process. the difference between the chronological age and biologically driven aging could be more informative in reflecting health status.
View Article and Find Full Text PDFNat Commun
January 2025
Genor Biopharma Co., Ltd, Beijing, China.
Lerociclib (GB491), a highly selective oral CDK4/6 inhibitor, has displayed anti-tumor activity and differentiated safety and tolerability profile in previous ph1/2 clinical trials. The LEONARDA-1, a randomized, double-blind, phase III study, was conducted to evaluate the efficacy and safety of lerociclib in HR+/HER2- locally advanced or metastatic breast cancer patients, who had relapsed or progressed on prior endocrine therapy. A total of 275 patients were randomized at 1:1 ratio to receive lerociclib (137 patients, 150 mg twice daily) or placebo (138 patients) plus fulvestrant.
View Article and Find Full Text PDFPoult Sci
January 2025
College of Animal Science and Technology, Henan Agricultural University, Zhengzhou 450046, China; International Joint Research Laboratory for Poultry Breeding of Henan, Zhengzhou, 450046, China. Electronic address:
The transglutaminase (TGMs) family plays a crucial role in regulating mammalian reproduction, yet its impact on poultry reproductive traits has not been extensively studied. In this study, we identified eight members of the TGMs family in chickens and examined the contributions of genetic variations of coagulation factor XIII A chain (F13A1), transglutaminase 4 (TGM4), and LOC101749664 to selective breeding in commercial layers through genetic variation response pattern analysis. Transcriptome data from various tissues of high- and low-egg-yielding Gushi chickens revealed significant positive correlations between the mRNA expression levels of TGM4 and F13A1 genes and egg production (P < 0.
View Article and Find Full Text PDFExpert Opin Pharmacother
January 2025
Department of Obstetrics and Gynecology, University of Florence, Careggi University Hospital, Florence, Italy.
Introduction: Dysmenorrhea is a painful symptom associated with uterine contractions and menstrual bleeding and is treated by administering analgesic drugs. Since progesterone receptors (PRs) have a major role in regulating uterine tissues (myometrium and endometrium) physiology, oral contraceptives are used off-label for treating primary or secondary dysmenorrhea. The development of selective progesterone receptor modulators (SPRMs), a class of synthetic steroids with agonistic, antagonistic, or mixed effects in targeting PRs in different tissues, stimulated their possible clinical use for treating secondary dysmenorrhea related to uterine diseases (endometriosis, adenomyosis, uterine fibroids).
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