Difamilast (OPA-15406) 是一种局部的，具有选择性的非甾体磷酸二酯酶 4 (PDE4) 抑制剂，对 B 亚型具有特别有效的抑制作用 (IC50=11.2 nM)。Difamilast 可用于研究轻度至中度特应性皮炎 (AD)。
Difamilast (OPA-15406) is a topical, selective and nonsteroidal phosphodiesterase-4 (PDE4) inhibitor with particularly efficient inhibition of subtype B (IC50=11.2 nM). Difamilast can be used for the research of mild to moderate atopic dermatitis (AD)[1][2][3].
OPA-15406 is highly selective for inhibition of PDE4 subtype B (IC50=11.2 nM), and OPA-15406 also exerts inhibitory effects on PDE2[2].
OPA-1540 improves skin condition in relevant animal models of AD[1].
[1]. Hanifin JM, et, al. OPA-15406, a novel, topical, nonsteroidal, selective phosphodiesterase-4 (PDE4) inhibitor, in the treatment of adult and adolescent patients with mild to moderate atopic dermatitis (AD): A phase-II randomized, double-blind, placebo-controlled study. J Am Acad Dermatol. 2016 Aug;75(2):297-305.
[2]. Ahluwalia J, et, al. Phosphodiesterase 4 Inhibitor Therapies for Atopic Dermatitis: Progress and Outlook. Drugs. 2017 Sep;77(13):1389-1397.
[3]. Soeberdt M, et, al. Small molecule drugs for the treatment of pruritus in patients with atopic dermatitis. Eur J Pharmacol. 2020 Aug 15;881:173242.
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