Silosure is a medication for the symptomatic treatment of benign prostatic hyperplasia. It acts as an α1-adrenoceptor antagonist with high uroselectivity (selectivity for the prostate).
Benign prostate hyperplasia (BPH), or an enlarged prostate, is a condition found only in men and is characterized by a non-cancerous enlargement of the prostate gland. Symptoms of BPH include urinary difficulty, urinary frequency and an inability to complete bladder emptying. Silosure is highly uroselective for the alpha (1A) receptors located in the prostate, [urethrea and bladder trigone in the lower urinary tract]. Blocking these receptors relaxes the smooth muscles, resulting in an improvement in urine flow and a reduction in BPH symptoms.
The selective binding of silosure to the alpha (1A) receptors is substantially greater than the binding to the cardiovascular-associated alpha (1B) receptors and thereby maximizes target organ activity while minimizing the potential for blood pressure effects. Silosure is alpha 1A-adrenoceptor selective antagonist which inhibits sympathetic nerve stimulation and relaxation of smooth muscle tone in the lower urinary tract which relieves the pressure from contraction of smooth muscle. The reduction of intraurethral pressure improves voiding and storage issues associated with BPH.
Silosure is 583 times more selective for human alpha-1A receptors than alpha-1B receptors. It is also 56 times more selective for human alpha-1A receptors than alpha-1D. Silosure does not prolong the QT interval.