madman
Super Moderator
Development of a novel topical formulation of glyceryl trinitrate for the treatment of erectile dysfunction
Abstract
Erectile dysfunction (ED), defined as the inability to initiate or maintain an erection sufficient for satisfactory sexual intercourse, is common, particularly in men aged ≥50 years. Existing treatments have significant limitations, and there remains a need for a fast-acting (to facilitate spontaneity during intercourse) and well tolerated local therapy. Topical glyceryl trinitrate (GTN) may meet this need because GTN undergoes rapid metabolism in penile smooth muscle and endothelial cells to produce nitric oxide, which plays a key role in the development of erection. This paper describes the rationale for the development of MED2005, a topical GTN formulation using DermaSys® technology, which is undergoing clinical trials for the treatment of ED. Pharmacokinetic studies have shown that MED2005 provides rapid delivery of GTN following application to the glans penis, and a Phase 2(a) trial in men with ED showed that MED2005 produced significant improvements in erectile function, compared with placebo. MED2005 was well tolerated in this trial, with only 21 cases of headache in 1003 intercourse attempts. It is anticipated that MED2005 will provide an effective therapy for ED, with a fast onset of action, good local tolerability, and fewer contraindications than phosphodiesterase 5 inhibitors, the current cornerstone of ED therapy.
Conclusion
The MED2005 formulation has been developed in an attempt to optimize topical GTN therapy for men with ED. It is likely that this formulation will provide a fast onset of action, with acceptable efficacy and limited local adverse effects, and fewer contraindications than PDE5-Is. MED2005 could therefore be an important advance in the management of ED, offering an opportunity to improve sexual activity and satisfaction for couples affected by this common condition.
Abstract
Erectile dysfunction (ED), defined as the inability to initiate or maintain an erection sufficient for satisfactory sexual intercourse, is common, particularly in men aged ≥50 years. Existing treatments have significant limitations, and there remains a need for a fast-acting (to facilitate spontaneity during intercourse) and well tolerated local therapy. Topical glyceryl trinitrate (GTN) may meet this need because GTN undergoes rapid metabolism in penile smooth muscle and endothelial cells to produce nitric oxide, which plays a key role in the development of erection. This paper describes the rationale for the development of MED2005, a topical GTN formulation using DermaSys® technology, which is undergoing clinical trials for the treatment of ED. Pharmacokinetic studies have shown that MED2005 provides rapid delivery of GTN following application to the glans penis, and a Phase 2(a) trial in men with ED showed that MED2005 produced significant improvements in erectile function, compared with placebo. MED2005 was well tolerated in this trial, with only 21 cases of headache in 1003 intercourse attempts. It is anticipated that MED2005 will provide an effective therapy for ED, with a fast onset of action, good local tolerability, and fewer contraindications than phosphodiesterase 5 inhibitors, the current cornerstone of ED therapy.
Conclusion
The MED2005 formulation has been developed in an attempt to optimize topical GTN therapy for men with ED. It is likely that this formulation will provide a fast onset of action, with acceptable efficacy and limited local adverse effects, and fewer contraindications than PDE5-Is. MED2005 could therefore be an important advance in the management of ED, offering an opportunity to improve sexual activity and satisfaction for couples affected by this common condition.
