Applied Biology, Irvine, California.
Department of Dermatology and Venereology, University of Rome "G.Marconi", Rome, Italy.
Dermatol Ther. 2018 Jan;31(1). doi: 10.1111/dth.12575. Epub 2017 Nov 28.
Approximately 40% of women experience excessive hair shedding during styling (e.g., hair brushing). Previously, we demonstrated that topically applied phenylephrine, a potent α adrenergic receptor agonist, can be used to contract the arrector pili muscle of the follicular unit; thus, increasing the force required to pluck hair and reducing shedding during brushing. While demonstrating efficacy, phenylephrine has several drawbacks when applied to the scalp, including the possibility cardiovascular events. We hypothesized that a high concentration of a weak α agonist would allow for: (a) rapid penetration through the stratum corneum eliciting a quick response; (b) a low probability of cardiac adverse events owing to the low receptor binding affinity; and (c) an efficacy of the weak α agonist similar to that of phenylephrine at the local site of application. Accordingly, we developed a novel topical solution, AB-102, containing a high concentration of a weak α agonist. Several studies were conducted to test the safety and efficacy of AB-102. In a dose escalating safety study, utilizing a wearable holter monitor, we observed no cardiac or hemodynamic adverse events. In addition, in a controlled efficacy study, AB-102 reduced the number of hairs shed during brushing by up to 77% (average of 38%).
大约 40%的女性在造型时(例如梳头)会经历过度脱发。此前,我们证明局部应用苯肾上腺素(一种有效的α肾上腺素能受体激动剂)可用于收缩毛囊单位的竖毛肌,从而增加拔毛所需的力,并减少梳理时的脱发。虽然苯肾上腺素具有疗效,但在头皮上应用时有几个缺点,包括心血管事件的可能性。我们假设高浓度的弱α激动剂将允许:(a)快速穿透角质层,引起快速反应;(b)由于受体结合亲和力低,心脏不良事件的可能性低;和(c)弱α激动剂的功效与局部应用的苯肾上腺素相似。因此,我们开发了一种新型局部溶液 AB-102,其中含有高浓度的弱α激动剂。进行了几项研究来测试 AB-102 的安全性和疗效。在一项使用可穿戴式 Holter 监测器的剂量递增安全性研究中,我们没有观察到心脏或血液动力学不良事件。此外,在一项对照疗效研究中,AB-102 使梳理时脱落的头发数量减少了多达 77%(平均减少 38%)。