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Development of a novel topical formulation of glyceryl trinitrate for the treatment of erectile dysfunction.
International Journal of Impotence Research ( IF 2.8 ) Pub Date : 2020-01-31 , DOI: 10.1038/s41443-019-0227-7 Adrian Davis 1 , Yacov Reisman 2
International Journal of Impotence Research ( IF 2.8 ) Pub Date : 2020-01-31 , DOI: 10.1038/s41443-019-0227-7 Adrian Davis 1 , Yacov Reisman 2
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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.
中文翻译：
开发一种新型局部用甘油三硝酸酯制剂，用于治疗勃起功能障碍。
勃起功能障碍（ED）被定义为无法开始或维持足以使性交满意的勃起，这很常见，尤其是对于年龄≥50岁的男性。现有的治疗方法有很大的局限性，仍然需要速效（促进性交时的自发性）和良好耐受的局部治疗。局部用三硝酸甘油酯（GTN）可以满足这一需求，因为GTN在阴茎平滑肌和内皮细胞中快速代谢以产生一氧化氮，这在勃起的发展中起关键作用。本文描述了开发MED2005的基本原理，MED2005是一种使用DermaSys®技术的局部GTN制剂，目前正在进行临床试验以治疗ED。药代动力学研究表明，MED2005在应用到阴茎龟头后可提供GTN的快速递送，一项针对ED男性患者的2（a）期试验表明，与安慰剂相比，MED2005的勃起功能得到了显着改善。该试验对MED2005的耐受性良好，在1003次性交尝试中仅有21例头痛。预期MED2005将提供一种有效的ED治疗方法，其起效快，局部耐受性好，禁忌症比目前ED治疗的磷酸二酯酶5抑制剂少。
更新日期：2020-01-31
中文翻译：
开发一种新型局部用甘油三硝酸酯制剂，用于治疗勃起功能障碍。
勃起功能障碍（ED）被定义为无法开始或维持足以使性交满意的勃起，这很常见，尤其是对于年龄≥50岁的男性。现有的治疗方法有很大的局限性，仍然需要速效（促进性交时的自发性）和良好耐受的局部治疗。局部用三硝酸甘油酯（GTN）可以满足这一需求，因为GTN在阴茎平滑肌和内皮细胞中快速代谢以产生一氧化氮，这在勃起的发展中起关键作用。本文描述了开发MED2005的基本原理，MED2005是一种使用DermaSys®技术的局部GTN制剂，目前正在进行临床试验以治疗ED。药代动力学研究表明，MED2005在应用到阴茎龟头后可提供GTN的快速递送，一项针对ED男性患者的2（a）期试验表明，与安慰剂相比，MED2005的勃起功能得到了显着改善。该试验对MED2005的耐受性良好，在1003次性交尝试中仅有21例头痛。预期MED2005将提供一种有效的ED治疗方法，其起效快，局部耐受性好，禁忌症比目前ED治疗的磷酸二酯酶5抑制剂少。
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