Apararenone (

INN Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...

) (developmental code name MT-3995) is a

nonsteroidal A nonsteroidal compound is a drug that is not a steroid nor a steroid derivative. Nonsteroidal anti-inflammatory drugs (NSAIDs) are distinguished from corticosteroids as a class of anti-inflammatory agents. List of nonsteroidal steroid receptor mo ...

antimineralocorticoid An antimineralocorticoid, also known as a mineralocorticoid receptor antagonist (MRA or MCRA) or aldosterone antagonist, is a diuretic drug which antagonizes the action of aldosterone at mineralocorticoid receptors. This group of drugs is ofte ...

which is under development by

Mitsubishi Tanabe Pharma Mitsubishi Tanabe Pharma Corporation is a Japanese pharmaceuticals company from Osaka, a subsidiary of Mitsubishi Chemical Holdings Corporation. was formed in 2001 from the merger of Mitsubishi-Tokyo Pharmaceuticals and Welfide Corporation. O ...

for the treatment of diabetic nephropathies and

non-alcoholic steatohepatitis Non-alcoholic fatty liver disease (NAFLD), also known as metabolic (dysfunction) associated fatty liver disease (MAFLD), is excessive fat build-up in the liver without another clear cause such as alcohol use. There are two types; non-alcoholic ...

. It was also previously being developed for the treatment of hypertension, but development was discontinued for this indication. Apararenone acts as a highly selective antagonist of the

mineralocorticoid receptor The mineralocorticoid receptor (or MR, MLR, MCR), also known as the aldosterone receptor or nuclear receptor subfamily 3, group C, member 2, (NR3C2) is a protein that in humans is encoded by the ''NR3C2'' gene that is located on chromosome 4q31 ...

(K_i < 50 nM), the

receptor Receptor may refer to: * Sensory receptor, in physiology, any structure which, on receiving environmental stimuli, produces an informative nerve impulse *Receptor (biochemistry), in biochemistry, a protein molecule that receives and responds to a ...

for aldosterone. As of 2017, it is in phase II

clinical trial Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, diet ...

References

External links

Apararenone - AdisInsight
Antimineralocorticoids Benzoxazines Experimental drugs Fluoroarenes Sulfonamides {{cardiovascular-drug-stub

See also

References

External links