Drug intelligence / Profile preview

roflumilast N-oxide

Development stage
Unknown
Lead developer
Arcutis Biotherapeutics, Inc.
Modality
Small Molecules
Administration
Oral (applies As Active Metabolite Following Oral Administration Of Roflumilast)[5]
01

Overview

Roflumilast N-oxide is the **major active metabolite** of roflumilast, a selective phosphodiesterase 4 (PDE4) inhibitor. It is primarily responsible for the pharmacological activity observed with the parent drug, roflumilast, and accounts for a substantially greater plasma exposure than the parent compound. As a PDE4 inhibitor, roflumilast N-oxide suppresses the breakdown of cyclic AMP, leading to anti-inflammatory effects in the lungs. This mechanism is especially relevant in the management of chronic obstructive pulmonary disease (COPD), and research also extends to asthma and other inflammatory airway diseases. Roflumilast N-oxide is not marketed as a drug on its own but is critical in the efficacy profile of roflumilast. Its activity relies on the inhibition of PDE4, leading to decreased inflammation through effects on immune and structural cells in lung tissue[1][3][4][5][6].

Other names
292135-78-5roflumilast N-oxide3,5-dichloro-4-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)benzamido)pyridine 1-oxide
02

Targets

PDE4 (Phosphodiesterase 4A1)

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