Pexacerfont (

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 ...

, previously known as BMS-562,086) is a drug developed by

Bristol-Myers Squibb The Bristol Myers Squibb Company (BMS) is an American multinational pharmaceutical company. Headquartered in New York City, BMS is one of the world's largest pharmaceutical companies and consistently ranks on the ''Fortune'' 500 list of the lar ...

which acts as a CRF₁ antagonist. Corticotropin-releasing factor (CRF), also known as

corticotropin-releasing hormone Corticotropin-releasing hormone (CRH) (also known as corticotropin-releasing factor (CRF) or corticoliberin; corticotropin may also be spelled corticotrophin) is a peptide hormone involved in stress (biology), stress responses. It is a releasing ...

, is an endogenous peptide hormone which is released in response to various triggers such as

chronic stress Chronic stress is the physiological or psychological response induced by a long-term internal or external stressor. The stressor, either physically present or recollected, will produce the same effect and trigger a chronic stress response. There is ...

. This then triggers the release of

corticotropin Adrenocorticotropic hormone (ACTH; also adrenocorticotropin, corticotropin) is a Peptide, polypeptide tropic hormone produced by and secreted by the Anterior pituitary, anterior pituitary gland. It is also used as a Adrenocorticotropic hormone ...

(ACTH), another hormone which is involved in the physiological response to stress. Chronic release of CRF and ACTH is believed to be directly or indirectly involved in many of the harmful physiological effects of chronic stress, such as excessive

glucocorticoid Glucocorticoids (or, less commonly, glucocorticosteroids) are a class of corticosteroids, which are a class of steroid hormones. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor that is present in almost every vertebr ...

release,

diabetes mellitus Diabetes, also known as diabetes mellitus, is a group of metabolic disorders characterized by a high blood sugar level ( hyperglycemia) over a prolonged period of time. Symptoms often include frequent urination, increased thirst and increased ap ...

osteoporosis Osteoporosis is a systemic skeletal disorder characterized by low bone mass, micro-architectural deterioration of bone tissue leading to bone fragility, and consequent increase in fracture risk. It is the most common reason for a broken bone ...

stomach ulcers Peptic ulcer disease (PUD) is a break in the inner lining of the stomach, the first part of the small intestine, or sometimes the lower esophagus. An ulcer in the stomach is called a gastric ulcer, while one in the first part of the intestines ...

anxiety Anxiety is an emotion which is characterized by an unpleasant state of inner turmoil and includes feelings of dread over anticipated events. Anxiety is different than fear in that the former is defined as the anticipation of a future threat wh ...

, depression, and development of

high blood pressure Hypertension (HTN or HT), also known as high blood pressure (HBP), is a long-term medical condition in which the blood pressure in the arteries is persistently elevated. High blood pressure usually does not cause symptoms. Long-term high bl ...

and consequent cardiovascular problems. Pexacerfont is a recently developed CRF-1 antagonist which was in clinical trials for the treatment of

anxiety disorder Anxiety disorders are a cluster of mental disorders characterized by significant and uncontrollable feelings of anxiety and fear such that a person's social, occupational, and personal function are significantly impaired. Anxiety may cause physi ...

s, and has also been proposed to be useful for the treatment of depression and

irritable bowel syndrome Irritable bowel syndrome (IBS) is a "disorder of gut-brain interaction" characterized by a group of symptoms that commonly include abdominal pain and or abdominal bloating and changes in the consistency of bowel movements. These symptoms may ...

. A recent multicenter, randomized, double-blind, placebo-controlled trial found that pexacerfont (100 mg/day) did not separate from placebo on the primary outcome measure (the mean change from baseline to end point in the

Hamilton Anxiety Scale The Hamilton Anxiety Rating Scale (HAM-A) is a psychological questionnaire used by clinicians to rate the severity of a patient's anxiety. Anxiety can refer to things such as "a mental state...a drive...a response to a particular situation…a pers ...

score). These results suggest that blockade of CRF₁ receptor may not be a feasible treatment for anxiety disorders in certain human populations.

References

Anxiolytics Corticotropin-releasing hormone antagonists Bristol Myers Squibb Pyridines Phenol ethers {{systemic-hormonal-drug-stub

See also

References