Drug intelligence / Profile preview

alpha blockers + phosphodiesterase 5 inhibitors

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination therapy consisting of an alpha blocker and a phosphodiesterase 5 inhibitor (PDE5I). Alpha blockers, such as tamsulosin, alfuzosin, doxazosin, and terazosin, act by antagonizing alpha-1 adrenergic receptors in the smooth muscle of the prostate and bladder neck, leading to muscle relaxation and improved urine flow. Phosphodiesterase 5 inhibitors (e.g., sildenafil, tadalafil, vardenafil) inhibit the PDE5 enzyme in smooth muscle cells of the lower urinary tract and corpus cavernosum. This increases cyclic guanosine monophosphate (cGMP) levels resulting in smooth muscle relaxation via nitric oxide pathways. The combination is primarily used for men with benign prostatic hyperplasia (BPH) presenting with lower urinary tract symptoms (LUTS), often coexisting with erectile dysfunction (ED). Clinical studies show that this combination provides greater improvement in LUTS compared to either agent alone[1][2][4][5][6]. The most commonly studied combinations are tamsulosin or alfuzosin plus tadalafil or sildenafil.

02

Targets

ADRA1A (α1A)PDE5 (Phosphodiesterase 5A)

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