LEO 39652 is a dual-soft PDE4 inhibitor with IC50 values of 1.2 nM for PDE4A, 1.2 nM for PDE4B, 3.0 nM for PDE4C, and 3.8 nM for PDE4D. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used in topical studies of atopic dermatitis.
|Solubility (25°C)||DMSO : 25 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Jens Larsen, et al. J Med Chem. Discovery and Early Clinical Development of Isobutyl 1-[8-Methoxy-5-(1-oxo-3 H-isobenzofuran-5-yl)-[1,2,4]triazolo[1,5- a]pyridin-2-yl]cyclopropanecarboxylate (LEO 39652), a Novel "Dual-Soft" PDE4 Inhibitor for Topical Treatment of Atopic Dermatitis
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