Pirfenidone 99% White Powder CAS 53179-13-8

Pirfenidone 99% white powder (PFD) is a new pyridine compound with a broad-spectrum anti-fibrosis effect, which can prevent and reverse fibrosis and scar formation; It is the first drug to prove its efficacy in idiopathic pulmonary fibrosis (IPF) through repeated, randomized and placebo-controlled phase III clinical trials; The drug also has a good curative effect on fibrosis diseases such as renal interstitial fibrosis and liver fibrosis; It is also widely used in renal diseases (focal segmental glomerulosclerosis), hypertrophic cardiomyopathy, adult I type multiple neurofibroma, juvenile I multiple neurofibroma and plexiform neurofibroma, diabetes mellitus with renal disease, and uterine leiomyoma.

What is the pharmacological action of this product?

Pirfenidone 99% white powder is an effective cytokine inhibitor, which can inhibit the biological activity of fibroblasts and reduce cell proliferation and matrix collagen synthesis by regulating or inhibiting some factors. At the same time, PFD can also inhibit the secretion of inflammatory mediators, reduce lipid peroxidation and give play to its anti-inflammatory and antioxidant effects.1. Inhibit collagen synthesis, fibroblast growth factor (bFGF), transforming growth factor - β (transforming growth factor－ β, TGF－ β), Connective tissue growth factor (CTGF), and tissue inhibitor of metalloproteinase-1 (TIMP-1) are growth factors related to fibrotic diseases, which can promote the proliferation and growth of fibroblasts, increase the synthesis of matrix collagen and prevent the degradation of extracellular matrix (ECM). They are expressed in varying degrees in the process of organ fibrosis. PFD can reduce bFGF and TGF in fibroblasts of lung, kidney, and other organs- β, The expression of CTGF and TIMP-1 was correlated with collagen synthesis and matrix reduction. The production of type I and type III collagen fibers is also closely related to the synthesis of matrix collagen. The role of PFD in reducing TGF - β While expressing, it can also reduce α Production of type I collagen. PFD can also inhibit the expression of type I collagen in the pulmonary fibrosis model. In addition, PFD can also inhibit the expression of type III collagen mRNA and reduce the synthesis of type III collagen. 2. Anti-inflammatory effect PFD can inhibit inflammatory mediators in varying degrees and exert its anti-inflammatory effect. When inflammatory factors are overexpressed in the lung, it will aggravate the inflammatory reaction, thicken the alveolar wall, reduce the alveolar function, and finally produce fibrosis. PFD mainly plays an anti-inflammatory role by inhibiting the expression of inflammatory mediators, reducing vascular permeability, and reducing the aggregation of neutrophils and inflammatory cells, so as to prevent or slow down the fibrosis of organ tissues. 3. Antioxidant effect PFD exerts its antioxidant effect mainly by scavenging free radicals, inhibiting lipid peroxidation, and reducing oxidative stress.

What are the pharmacokinetics and adverse reactions of this product?

The common adverse reactions of Pirfenidone 99% white powder include malignant, photosensitive rash, fatigue, and nausea,; Other adverse reactions include upper gastrointestinal discomfort, upper abdominal fullness, anorexia, diarrhea, skin pruritus, etc.

In the clinical experiment stage, after the use of 400mg · kg-1, the drug was removed from the plasma according to the two-compartment model. The plasma clearance rate was 0.10ml · min-1 · g-1, the apparent distribution volume was 0.6ml · g-1, and the half-life was 8.6min. After use, pirfenidone was rapidly distributed in the body fluid. After 5min, the drug concentration in the tissue reached its peak. The concentration in the liver, kidney, lung and other parts with rich blood flow was higher, and the concentration in adipose tissue was lower; The bioavailability of pirfenidone in rats was 25.7% after use administration of 250 ~ 300 mg · kg-1 · D-1, and the average blood concentration was (1.9 ± 0.1) 24 hours after 14 days of administration μ g·mL-1; 97% of the metabolites were excreted from the kidney, and the excretion in 24 hours accounted for 97% of the total excretion.

About the clinical application of this product

1. Idiopathic pulmonary fibrosis (IPF) is a chronic inflammatory interstitial lung disease with an unknown cause, poor prognosis, and high mortality. (PFD)Pirfenidone 99% white powder is an anti-inflammatory and anti-fibrosis preparation, which can be used in the treatment of IPF. 2. Hepatic fibrosis 3 Renal fibrosis 4 Multiple sclerosis (MS) is an inflammatory and demyelinating disease related to the central nervous system and immunity. The related immune factors are the activation of stellate cells, glial cells, and endothelial cells and the increase of lymphocytes, while PFD has the characteristic of inhibiting cell activation. 5. Myocardial fibrosis cardiovascular diseases such as hypertension, cardiomyopathy, and atrial fibrillation can lead to myocardial fibrosis, which can worsen or develop the disease. Treating cardiomyopathy caused by progressive pseudo hypertrophic muscular dystrophy with PFD can inhibit myocardial fibrosis and improve cardiac function. PFD reduces myocardial remodeling and atrial fibrillation by inhibiting fibrosis. 6. Neoplastic diseases: neurofibroma, uterine leiomyoma, and malignant glioma. 7. Prevention of fibrosis after organ transplantation 8 Rheumatoid arthritis

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