Roflumilast

Roflumilast

Definition

An orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3',5'-adenosine monophosphate (cAMP) and cAMP-mediated signaling. cAMP prevents phosphorylation of spleen tyrosine kinase (SYK) and abrogates activation of the PI3K/AKT/mTOR signaling pathway, which may result in the induction of apoptosis. PDE4, a member of the PDE superfamily that hydrolyses cAMP and 3',5'-cyclic guanosine monophosphate (cGMP) to their inactive 5' monophosphates, is upregulated in a variety of cancers and may contribute to chemoresistance; it also plays a key role in inflammation, especially in inflammatory airway diseases.

Also known as 3-Cyclopropylmethoxy-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide, B9302-107, BY217, BYK20869, Daliresp, ROFLUMILAST — per NCIT

Also identified as

Indications

Disease Relation Source
Chronic obstructive pulmonary disease (COPD) may treat MEDRT · Public domain (U.S. Government work)

Organ Effects

Organ Side effect / interaction Source
Lungs may treat a disease of this organ DERIVED · CC BY 4.0
Respiratory system may treat a disease of this organ DERIVED · CC BY 4.0

2 entries above are marked DERIVED: Atlas Médico inferred them by combining two sourced claims, and no source asserts these links directly. Treat them as a navigation aid, not as a clinical statement.