Dovramilast (CC-11050) is an orally active phosphodiesterase 4 (PDE4) inhibitor and can reduce the inflammatory response and improves Isoniazid (INH)-mediated bacillary clearance from the lungs. Dovramilast, as an adjunct, is used for the research of tuberculosis (TB)
In Vivo
Dovramilast (oral gavage, 5, 25, or 50 mg/kg, single) significantly improves antibiotic-mediated bacterial killing and reduces lung pathology. Pharmacokinetic Parameters of Dovramilast in B6D2F1 mice. Sampling time(h) Concentration(ng/ml) CC-11050 only CC-11050+ INH 1 1,331.6±136.97 905.35±594.23 2 1,409.47±140.85 1,309.39±214.08 5 948.85±128.7 1,609.18±167.2 8 820.6±265.98 1,271.73±249.18 24 1.27±1.1 4.96±1.85 T max (h) 2.0 5.0 C max (ng/ml) 1,410 1,610 AUC last (ng × h/ml) 10,200 13,900 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: B6D2F1 miceDosage: 5, 25, or 50 mg/kg Administration: oral, 5, 25, or 50 mg/kg, single Result: Reduced PDE4 expression in mtb-infected mouse lungs. Animal Model: B6D2F1 miceDosage: 5, 25, or 50 mg/kg Administration: oral gavage, 5, 25, or 50 mg/kg, single Result: Improved antibiotic-mediated bacterial killing and reduced lung pathology.
Form:Solid
IC50& Target:PDE4
