| Identification | Back Directory | [Name]
Cyclopropanecarboxamide, N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2,3-dihydro-3-oxo-1H-isoindol-4-yl]- | [CAS]
340019-69-4 | [Synonyms]
dovramilast
Dovramilast (Synonyms: CC-11050)
Cyclopropanecarboxamide, N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2,3-dihydro-3-oxo-1H-isoindol-4-yl]- | [Molecular Formula]
C24H28N2O6S | [MOL File]
340019-69-4.mol | [Molecular Weight]
472.55 |
| Chemical Properties | Back Directory | [Boiling point ]
778.5±60.0 °C(Predicted) | [density ]
1.365±0.06 g/cm3(Predicted) | [storage temp. ]
4°C, away from moisture and light | [form ]
Solid | [pka]
14.38±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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)[1]. | [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: | Improved antibiotic-mediated bacterial killing and reduced lung pathology. |
| [IC 50]
PDE4 | [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. DOI:10.3389/fimmu.2016.00238 |
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