Nonsteroidal anti-inflammatory drugs prostaglandins indications and side effects

Ligand Pharmaceuticals has patents filed for the manufacture and therapeutic use of certain compounds occupying several stated chemical structures, which are intended for use as selective androgen receptor modulators. The patent is filed under the following designations: US8519158 B2, US8865918, US9359285, US20070254875, US20140005186, US20150099720, and WO2005090282A1. The patents will expire on March 12, 2025. These patents effectively protect any future capitalization upon VK5211 in the market by Viking and Ligand through their licensing agreement. [9]

Selective intracellular receptor antagonists are used clinically to ameliorate hormone-dependent disease states. Patients with Cushing's syndrome have high levels of the glucocorticoid, cortisol, and suffer significant consequences from this overexposure. High levels of this hormone are also implicated in exacerbating diabetes and the stress response. Selectively inhibiting this hormone may have clinical benefit in these disease states. To this end, we have identified the first selective, nonsteroidal glucocorticoid receptor (GR) antagonist. This compound is characterized by a tri-aryl methane core chemical structure. This GR-specific antagonist binds with nanomolar affinity to the GR and has no detectable binding affinity for the highly related receptors for mineralocorticoids, androgens, estrogens, and progestins. We demonstrate that this antagonist inhibits glucocorticoid-mediated transcriptional regulation. This compound binds competitively with steroids, likely occupying a similar site within the ligand-binding domain. Once bound, however, the compound fails to induce critical conformational changes in the receptor necessary for agonist activity.

Of the 80,966 men in this study % were considered nonsteroidal anti-inflammatory drug users based on the definitions used and % reported moderate or severe erectile dysfunction. Nonsteroidal anti-inflammatory drug use and erectile dysfunction strongly correlated with age with regular drug use increasing from % in men at ages 45 to 49 years to % in men 60 to 69 years old with erectile dysfunction increasing from 13% to 42%. The unadjusted OR for the association of nonsteroidal anti-inflammatory drugs and erectile dysfunction was (95% CI , ). With adjustment for age, race/ethnicity, smoking status, diabetes mellitus, hypertension, hyperlipidemia, peripheral vascular disease, coronary artery disease and body mass index, a positive association persisted (adjusted OR ). The association persisted when using a stricter definition of nonsteroidal anti-inflammatory drug exposure.

Nonsteroidal anti-inflammatory drugs prostaglandins indications and side effects

nonsteroidal anti-inflammatory drugs prostaglandins indications and side effects

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