Pirfenidone (1) is a bioactive small molecule, and was first reported as an anti-inflammatory agent in the 1970s.1) Recently, Oku et al. have reported its unique anti-inflammatory properties.2) Additionally in the 1990s, Margolin et al. discovered that pirfenidone had an antifibrotic action.3) Here, they showed that pirfenidone was an inhibitor of collagen production and fibroblast proliferation in the lungs of rats and hamsters. The study of antifibrotic activity in various organs has been developed by using a variety of animal models.4)
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Pirfenidone: A Unique Antifibrotic and Anti-Inflammatory Agent
No.156(January 2013)
References
- 1)The first reports of pirfenidone as an anti-inflammatory agent
- a)S. M. Gadekar, U.S. Patent 3839346, 1974.
- b)S. M. Gadekar, U.S. Patent 3974281, 1976.
- c)S. M. Gadekar, Jpn. Kokai Tokkyo Koho S49-87677, 1974.
- d)S. M. Gadekar, Jpn. Kokai Tokkyo Koho S51-128437, 1976.
- 2)Unique anti-inflammatory properties of pirfenidone
- 3)The first reports of pirfenidone as an antifibrotic agent
- a)H. Suga, S. Teraoka, K. Ota, S. Komemushi, S. Furutani, S. Yamauchi, S. B. Margolin, Exp. Toxic. Pathol. 1995, 47, 287
- b)S. N. Iyer, J. S. Wild, M. J. Schiedt, D. M. Hyde, S. B. Margolin, S. N. Giri, J. Lab. Clin. Med. 1995, 125, 779.
- c)J. P. Kehrera, S. B. Margolin, Toxicol. Lett. 1997, 90, 125.
- a)H. Suga, S. Teraoka, K. Ota, S. Komemushi, S. Furutani, S. Yamauchi, S. B. Margolin, Exp. Toxic. Pathol. 1995, 47, 287
- 4)The antifibrotic activity of pirfenidone in various organs
- a)S. N. Iyer, G. Gurujeyalakshmi, S. N. Giri, J. Pharmacol. Exp. Ther. 1999, 291, 367.
- b)G. Miric, C. Dallemagne, Z. Endre, S. Margolin, S. M. Taylor, L. Brown, Br. J. Pharmacol. 2001, 133, 687.
- c)H. Oku, T. Shimizu, T. Kawabata, M. Nagira, I. Hikita, A. Ueyama, S. Matsushima, M. Torii, A. Arimura, Eur. J. Pharmacol. 2008, 590, 400.
- d)C. J. Schaefer, D. W. Ruhrmund, L. Pan, S. D. Seiwert, K. Kossen, Eur. Respir. Rev. 2011, 20, 85.
- e)K. Hisatomi, H. Mukae, N. Sakamoto, Y. Ishimatsu, T. Kakugawa, S. Hara, H. Fujita, S. Nakamichi, H. Oku, Y. Urata, H. Kubota, K. Nagata, S. Kohno, BMC Pulm. Med. 2012, 12, 24.
- 5)Reviews
- a) Forced vital capacity in idiopathic pulmonary fibrosis--FDA review of pirfenidone and nintedanib
- B. A. Karimi-Shah, B. A. Chowdhury, N. Engl. J. Med. 2015, 372, 1189.
- b) Pirfenidone: A Review of Its Use in Idiopathic Pulmonary Fibrosis
- E. S. Kim, G. M. Keating, Drugs 2015, 75, 219.
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