Until recently, IPF therapy consisted of a combination of corticosteroids
and immunosuppressive agents (azathioprine and cyclophosphamide)
to target the inflammation that was believed to be the pathogenic
stimulus.Since IPF is now considered to be predominantly a disorder of
fibroproliferation, agents that intervene in fibrogenesis have moved
to the forefront of treatment options. With demonstrated efficacy in a
bleomycin-induced lung fibrosis animal model, pirfenidone has been
developed and launched as an approved therapy for IPF. Its antifibrotic activity is derived from the inhibition of p38 MAP kinase that is
upstream of transforming growth factor-β (TGF-β), a cytokine implicated
in the stimulation of collagen synthesis and the inhibition of its
degradation. Pirfenidone also inhibits the expression of TNF-α, IL-1,
and ICAM-1, so it possesses the dual benefit of an anti-inflammatory and
antifibrotic agent. This relatively simplistic drug is constructed by the copper-catalyzed reaction of 5-methyl-2(1H)-pyridinone with bromo- or chlorobenzene.
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화학적 성질
Off-White Solid
용도
Pirfenidone is in a group of medicines called antifibrotic agents. Pirfenidone has demonstrated activity in multiple fibrotic conditions, including those of the lung, kidney and liver. It affects your body’s immune system and reduces the amount of fibrosis (scarring) in the lungs. Pirfenidone is one of two medicines that are approved in Canada to treat Idiopathic Pulmonary Fibrosis (IPF). Another name for this medicine is Esbriet.
정의
ChEBI: A pyridone that is 2-pyridone substituted at positions 1 and 5 by phenyl and methyl groups respectively. An anti-inflammatory drug used for the treatment of idiopathic pulmonary fibrosis.
일반 설명
Pirfenidone?(5-methyl-1-phenyl-2-[1H]-pyridone) is a synthetic derivative of pyridine.
생물학적 활성
Antifibrotic agent, effective in models of pulmonary and lung fibrosis. Inhibits collagen production and fibroblast proliferation. Regulates cytokine levels following oral administration in vivo . Potent scavenger of free radicals and inhibitor of lipid peroxidation.
