Cardiac Safety of Ozanimod, a Novel Sphingosine‐1‐Phosphate Receptor Modulator: Results of a Thorough QT/QTc Study
Sign Up to like & getrecommendations! Published in 2018 at "Clinical Pharmacology in Drug Development"
DOI: 10.1002/cpdd.383
Abstract: Ozanimod is a novel, selective, oral sphingosine‐1‐phosphate (1 and 5) receptor modulator in development for multiple sclerosis and inflammatory bowel disease. This randomized, double‐blind, placebo‐controlled, positive‐controlled, parallel‐group thorough QT study characterized the effects of ozanimod… read more here.
Keywords: cardiac safety; sphingosine phosphate; phosphate receptor; receptor modulator ... See more keywords
Equine metabolism of the selective androgen receptor modulator YK-11 in urine and plasma following oral administration.
Sign Up to like & getrecommendations! Published in 2022 at "Drug testing and analysis"
DOI: 10.1002/dta.3425
Abstract: YK-11 is a steroidal selective androgen receptor modulator, a compound class prohibited in both equine racing and human sports because of their potentially performance enhancing properties. YK-11 is easily accessible via internet-based supplement vendors making… read more here.
Keywords: metabolism; selective androgen; receptor modulator; androgen receptor ... See more keywords
The progesterone-receptor modulator, ulipristal acetate, drastically lowers breast cell proliferation
Sign Up to like & getrecommendations! Published in 2022 at "Breast Cancer Research and Treatment"
DOI: 10.1007/s10549-021-06503-1
Abstract: The proliferation of breast epithelial cells increases during the luteal phase of the menstrual cycle, when they are exposed to progesterone, suggesting that ulipristal acetate, a selective progestin-receptor modulator (SPRM), may reduce breast cell proliferation… read more here.
Keywords: breast; breast cell; proliferation; treatment ... See more keywords
Selective androgen receptor modulator, S42 has anabolic and anti-catabolic effects on cultured myotubes
Sign Up to like & getrecommendations! Published in 2019 at "Biochemistry and Biophysics Reports"
DOI: 10.1016/j.bbrep.2019.01.006
Abstract: We previously identified a novel selective androgen receptor modulator, S42, that does not stimulate prostate growth but has a beneficial effect on lipid metabolism. S42 also increased muscle weight of the levator ani in orchiectomized… read more here.
Keywords: muscle; selective androgen; c2c12 myotubes; modulator s42 ... See more keywords
Repurposing the estrogen receptor modulator raloxifene to treat SARS-CoV-2 infection
Sign Up to like & getrecommendations! Published in 2021 at "Cell Death and Differentiation"
DOI: 10.1038/s41418-021-00844-6
Abstract: The ongoing coronavirus disease 2019 (COVID-19) pandemic caused by the novel severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) necessitates strategies to identify prophylactic and therapeutic drug candidates to enter rapid clinical development. This is particularly… read more here.
Keywords: sars cov; estrogen receptor; receptor modulator;
Absorption, distribution, metabolism, and excretion of cenerimod, a selective S1P1 receptor modulator in healthy subjects
Sign Up to like & getrecommendations! Published in 2020 at "Xenobiotica"
DOI: 10.1080/00498254.2020.1736688
Abstract: Abstract Cenerimod is a sphingosine-1-phosphate 1 receptor modulator under development for treatment of systemic lupus erythematosus. This single-centre, open-label, single-dose study investigated the mass balance and excretion routes and aimed at identifying and quantifying cenerimod… read more here.
Keywords: excretion; cenerimod; receptor modulator; radioactivity ... See more keywords
The mineralocorticoid receptor as a modulator of innate immunity and atherosclerosis.
Sign Up to like & getrecommendations! Published in 2018 at "Cardiovascular research"
DOI: 10.1093/cvr/cvy092
Abstract: The mineralocorticoid receptor (MR) is a member of the nuclear receptor steroid-binding family. The classical MR ligand aldosterone controls electrolyte and fluid homeostasis after binding in renal epithelial cells. However, more recent evidence suggests that… read more here.
Keywords: modulator innate; mineralocorticoid receptor; receptor; innate immunity ... See more keywords
A plant‐derived glucocorticoid receptor modulator with potency to attenuate the side effects of glucocorticoid therapy
Sign Up to like & getrecommendations! Published in 2022 at "British Journal of Pharmacology"
DOI: 10.1111/bph.15957
Abstract: Continuous efforts have been made to move towards maintaining the beneficial anti‐inflammatory functions of glucocorticoids (GCs) while minimizing side effects. Here, we investigated the selective glucocorticoid receptor (GR) modulator‐like properties of a plant‐derived compound caesaldekarin… read more here.
Keywords: side effects; receptor modulator; glucocorticoid receptor; plant derived ... See more keywords
Safety, Pharmacokinetics and Pharmacodynamics of the Selective Glucocorticoid Receptor Modulator Velsecorat (AZD7594) Following Inhalation in Healthy Volunteers
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DOI: 10.2147/dddt.s334960
Abstract: Introduction Velsecorat (AZD7594) is a non-steroidal, selective, glucocorticoid receptor modulator (SGRM), being developed for the treatment of asthma. This article reports the initial, first-in-human, single and repeat dose-escalating study in healthy male volunteers. Methods The… read more here.
Keywords: velsecorat azd7594; glucocorticoid receptor; receptor modulator; velsecorat ... See more keywords
Relacorilant, a Selective Glucocorticoid Receptor Modulator, Induces Clinical Improvements in Patients With Cushing Syndrome: Results From A Prospective, Open-Label Phase 2 Study
Sign Up to like & getrecommendations! Published in 2021 at "Frontiers in Endocrinology"
DOI: 10.3389/fendo.2021.662865
Abstract: Introduction/Purpose Relacorilant is a selective glucocorticoid receptor modulator (SGRM) with no progesterone receptor activity. We evaluated the efficacy and safety of relacorilant in patients with endogenous Cushing syndrome (CS). Materials and Methods A single-arm, open-label,… read more here.
Keywords: glucocorticoid receptor; relacorilant selective; cushing syndrome; receptor ... See more keywords
Human In Vivo Metabolism and Elimination Behavior of Micro-Dosed Selective Androgen Receptor Modulator RAD140 for Doping Control Purposes
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DOI: 10.3390/metabo12070666
Abstract: RAD140 is a selective androgen receptor modulator which has been abused in sporting competitions. Its use is prohibited by the World Anti-Doping Agency (WADA) for athletes at all times. In addition to its illicit use,… read more here.
Keywords: selective androgen; receptor modulator; rad140 doping; androgen receptor ... See more keywords