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Dovramilast

Names

[ CAS No. ]:
340019-69-4

[ Name ]:
Dovramilast

Biological Activity

[Description]:

Dovramilast (CC-11050) is an oral phosphodiesterase 4 (PDE4) inhibitor and can reduce the inflammatory response and improves Isoniazid (INH)-mediated bacillary clearance from the lungs. Dovramilast (CC-11050), as an adjunct, is used for the research of tuberculosis (TB)[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)
Research Areas >> Infection
Research Areas >> Inflammation/Immunology

[Target]

PDE4


[In Vivo]

Dovramilast (oral gavage, 5, 25, or 50 mg/kg, single) significantly improves antibiotic-mediated bacterial killing and reduces lung pathology[2]. Pharmacokinetic Parameters of Dovramilast in B6D2F1 mice[2]. 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 Tmax(h) 2.0 5.0 Cmax(ng/ml) 1,410 1,610 AUClast(ng × h/ml) 10,200 13,900 Animal Model: B6D2F1 mice[2] Dosage: 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 mice[2] Dosage: 5, 25, or 50 mg/kg Administration: oral gavage, 5, 25, or 50 mg/kg, single Result:

[References]

[1]. International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 36, No. 2, 2022.

[2]. Selvakumar Subbian, et al. Pharmacologic Inhibition of Host Phosphodiesterase-4 Improves Isoniazid-Mediated Clearance of Mycobacterium tuberculosis. Front Immunol. 2016 Jun 17;7:238.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H28N2O6S

[ Molecular Weight ]:
472.55


Related Compounds

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