Cardiovascular Evaluation of Etrasimod, a Selective Sphingosine 1‐phosphate Receptor Modulator, in Healthy Adults: Results of a Randomized, Thorough QT/QTc Study
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DOI: 10.1002/cpdd.1388
Abstract: Etrasimod is an investigational, once‐daily, oral, selective sphingosine 1‐phosphate receptor 1,4,5 modulator used as an oral treatment option for immune‐mediated inflammatory disorders. This randomized, double‐blind, placebo‐ and positive‐controlled, parallel‐group, healthy adult study investigated etrasimod's effect… read more here.
Keywords: selective sphingosine; sphingosine phosphate; qtc; receptor modulator ... See more keywords
Cardiac Safety of Ozanimod, a Novel Sphingosine‐1‐Phosphate Receptor Modulator: Results of a Thorough QT/QTc Study
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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
Evaluation of the Pharmacokinetics, Disposition, and Metabolism of Miricorilant, a Novel Glucocorticoid Receptor Modulator for the Treatment of Metabolic Dysfunction-Associated Steatohepatitis in Nonclinical and Clinical Studies.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of clinical pharmacology"
DOI: 10.1002/jcph.70113
Abstract: Abstract Miricorilant is a novel selective glucocorticoid receptor (GR) modulator with mixed agonist/antagonist effects at the GR and modest antagonism at the mineralocorticoid receptor that is being developed for the treatment of metabolic dysfunction‐associated steatohepatitis.… read more here.
Keywords: glucocorticoid receptor; receptor; miricorilant; treatment metabolic ... 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
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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
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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