Jpn. J. Pharmacol. 78 (4), 505-509 (1998)


Local Anti-inflammatory Activity and Systemic Side Effects of NM-135, a New Prodrug Glucocorticoid, in an Experimental Inflammatory Rat Model

Takayuki Ishii (1,#), Nobuyuki Kibushi (1), Takashi Nakajima (1), Tae Kakuta (1), Noriko Tanaka (1), Chiaki Sato (1), Kei Sugai (1), Isao Kijima-Suda (1), Hirofumi Kai (2) and Takeshi Miyata (2)


(1) Tokyo Pharmaceutical Research Laboratories, Nissin Food Products Co., Ltd.,1780 Kitano, Tokorozawa, Saitama 359-1152, Japan
(2) Department of Pharmacological Sciences, Faculty of Pharmaceutical Sciences, Kumamoto University, 5-1 Oe-honmachi, Kumamoto 862-0973, Japan
(#) Present address for correspondence: 1-24-3-402 Ishihara-cho, Kawagoe, Saitama 350-0824, Japan


Abstract: The local anti-inflammatory activity and systemic side effects of NM-135 (6alpha,9-difluoro-11beta-hydroxy-16alpha-methyl-21[[2,3,4,6-
tetrakis-0-(4-methylbenzoyl)-beta-D-glucopyranosyl]oxy]-
pregna-1,4-diene-3,20-dione) in croton oil-induced granuloma pouches and ear edema in rats were studied. The local anti-inflammatory activity of NM-135 was stronger than that of betamethasone 17-valerate (BV). As to systemic side effects, BV and diflucortolon valerate (DFV) caused thymolysis at the doses required for the anti-inflammatory activity. In contrast, no clear systemic side effect was observed in rats administered NM-135 at the dose producing the anti-inflammatory activity. These results suggest that NM-135 is a drug exhibiting a high degree of dissociation between the local anti-inflammatory activity and systemic side effects.

Keywords: Glucocorticoid, Systemic side effect, Prodrug


Copyrightę The Japanese Pharmacological Society 1998

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