Biological Activity of AN-2728

AN-2728 is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines.
IC50 value:
Target: PDE4
AN-2728 appears to have good therapeutic potential, although further and larger trials are required to assess the long-term safety and characterize the broad utility of this drug. AN-2728 shows potent activity both in vitro and in vivo. AN-2728 is now in clinical development for the topical treatment of psoriasis and being pursued for the topical treatment of atopic dermatitis.

Clinical Information of AN-2728

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References on AN-2728

[1]. Freund YR, Akama T, Alley MR, et al. Boron-based phosphodiesterase inhibitors show novel binding of boron to PDE4 bimetal center. FEBS Lett. 2012 Sep 21;586(19):3410-4.
[2]. Tomotaka Mabuchi, Timothy W. Chang, Suzanne Quinter, et al. Chemokine receptors in the pathogenesis and therapy of psoriasis. Journal of Dermatological Science. 2012, 65(1) : 4-11
[3]. Y. Valdman-Grinshpoun, D. Ben-Amitai, A. Zvulunov. Barrier-Restoring Therapies in Atopic Dermatitis: Current Approaches and Future Perspectives. Dermatology Research and Practice Volume.2012, Article ID 923134, 6 pages
[4]. Nazarian R, Weinberg JM. AN-2728, a PDE4 inhibitor for the potential topical treatment of psoriasis and atopic dermatitis. Curr Opin Investig Drugs. 2009 Nov;10(11):1236-42.
[5]. Akama T, Baker SJ, Zhang YK, et al. Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2129-32.