生物活性

• 描述Iguratimod (T-614) is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC50 of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod (0.1, 1, 10 μg/mL) inhibits bradykinin-stimulated PGE2 (prostaglandin E2) release from fibroblasts. Iguratimod suppresses the COX activity from bradykinin stimulated fibroblasts in a concentration-dependent manner, with an IC50 of 48 μg/mL. Iguratimod (10 and 30 μg/mL) also dose-dependently inhibits COX-2 mRNA levels^[3]. Mechanical paw withdrawal thresholds and the expression levels of pERK (phosphorylated extracellular signal-related kinase) and c-Fos declined in a dose-dependent manner in rats treated with iguratimod, and bone destruction severity was also reduced^[4]. In addition, Iguratimod potently inhibits macrophage migration inhibitory factor (MIF) with an IC50 of 6.81 μM. Iguratimod is synergetic with glucocorticoids in vitro. Iguratimod (20 mg/kg i.p.) shows significantly increased survival in BALB/c mice that are vulnerable to endotoxemia, and attenuates TNFα release measured in serum isolated 90 min post-LPS administration in wild-type C57BL/6 mice^[5].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT03368274	IgG4-related Disease	Phase 4	Recruiting	June 1, 2018	China, Beijing ... more >> Peking Union Medical College Hospital Recruiting Beijing, Beijing, China, 100032 Contact: Panpan Zhang    +8618800159311    panpanzhang2016@163.com    Contact: Wen Zhang       zhangwen91@sina.com Collapse <<
  NCT03660059	Rheumatoid Arthritis (RA)	Phase 3	Recruiting	August 2022	China ... more >> Site CN00058 Recruiting Inner Mongolia, China Site CN00047 Recruiting Shantou, China Site CN00059 Recruiting Wuhan, China Site CN00049 Recruiting Zhuzhou, China Korea, Republic of Site KR00037 Recruiting Gwangju, Korea, Republic of Site KR00036 Recruiting Incheon, Korea, Republic of Site KR00033 Recruiting Seoul, Korea, Republic of Site KR00034 Recruiting Seoul, Korea, Republic of Site KR00035 Recruiting Seoul, Korea, Republic of Taiwan Site TW00025 Recruiting Taipei, Taiwan Site TW00026 Recruiting Taipei, Taiwan Collapse <<
  NCT01548001	Rheumatoid Arthritis	Phase 4	Unknown	January 2017	China ... more >> Renji Hospital Affiliated to Shanghai Jiaotong University School of Medicine Shanghai, China Collapse <<

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• 参考文献

• [1] Zhou T, Ding L, et al. Determination of iguratimod in rat plasma by high performance liquid chromatography: method and application. Biomed Chromatogr. 2008 Mar;22(3):260-4.

  [2] Tanaka K, Urata N, et al. Effect of iguratimod and other anti-rheumatic drugs on adenocarcinoma colon 26-induced cachexia in mice. Inflamm Res. 2007 Jan;56(1):17-23.

  [3] Tanaka K, Kawasaki H, Kurata K, Aikawa Y, Tsukamoto Y, Inaba T. T-614, a novel antirheumatic drug, inhibits both the activity and induction of cyclooxygenase-2 (COX-2) in cultured fibroblasts. Jpn J Pharmacol. 1995;67(4):305-314

  [4] Sun Y, Wu YX, Zhang P, Peng G, Yu SY. Anti-rheumatic drug iguratimod protects against cancer-induced bone pain and bone destruction in a rat model. Oncol Lett. 2017;13(6):4849-4856

  [5] Bloom J, Metz C, Nalawade S, et al. Identification of Iguratimod as an Inhibitor of Macrophage Migration Inhibitory Factor (MIF) with Steroid-sparing Potential. J Biol Chem. 2016;291(51):26502-26514

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