Drug intelligence / Profile preview

sildenafil + testosterone

Development stage
Phase 2
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral (sildenafil), Transdermal (testosterone Gel[1]), Intramuscular (testosterone, Alternative, Not Common In Combo Trials)
01

Overview

sildenafil + testosterone is a combination therapy consisting of two active ingredients: sildenafil, a phosphodiesterase type 5 (PDE5) inhibitor, and testosterone, an androgen hormone. Sildenafil acts by inhibiting PDE5, leading to increased cyclic guanosine monophosphate (cGMP) levels and vasodilation in the corpus cavernosum, thereby facilitating penile erection. Testosterone supplementation is used to normalize serum testosterone levels in men with hypogonadism or low-normal testosterone, supporting sexual function and libido. This combination is primarily used in men with erectile dysfunction (ED) and suboptimal response to sildenafil monotherapy, especially those with low or low-normal testosterone. The synergistic action is based on testosterone’s role in modulating nitric oxide synthase expression and PDE5 regulation in penile tissue, potentially restoring sildenafil responsiveness in patients with inadequate testosterone status[1].

02

Targets

PDE5 (Phosphodiesterase 5A)AR (Adrenergic receptors)

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