1: Noguchi T, Onodera A, Tomisawa K, Yamashita M, Takeshita K, Yokomori S. Synthesis and antirheumatic activity of the metabolites of esonarimod. Bioorg Med Chem. 2002 Aug;10(8):2713-21. PubMed PMID: 12057660.
2: Ohmi N, Yoshida H, Endo H, Hasegawa M, Akimoto M, Higuchi S. S-oxidation of S-methyl-esonarimod by flavin-containing monooxygenases in human liver microsomes. Xenobiotica. 2003 Dec;33(12):1221-31. PubMed PMID: 14742144.
3: Yamaguchi J, Ohmichi M, Hasegawa M, Yoshida H, Ogawa N, Higuchi S. Identification of rat urinary and biliary metabolites of esonarimod, a novel antirheumatic drug, using liquid chromatography/electrospray ionization tandem mass spectrometry with postcolumn addition of 2-(2-methoxyethoxy)ethanol, a signal-enhancing modifier. Drug Metab Dispos. 2001 Jun;29(6):806-12. PubMed PMID: 11353748.
4: Hasegawa M, Omi N, Endo H, Yoshida H, Higuchi S. Formation of a disulfide protein conjugate of the SH-group-containing metabolite (M-I) of esonarimod (KE-298) and its elimination in rats. J Pharm Pharmacol. 2002 Apr;54(4):493-8. PubMed PMID: 11999126.
5: Noguchi T, Onodera A, Tomisawa K, Yokomori S. A practical procedure for the synthesis of esonarimod, (R,S)-2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid, an antirheumatic agent (part 1). Chem Pharm Bull (Tokyo). 2002 Oct;50(10):1407-12. PubMed PMID: 12372877.
6: Noguchi T, Hasegawa M, Tomisawa K, Mitsukuchi M. Synthesis and structure-activity relationships of 5-phenylthiophenecarboxylic acid derivatives as antirheumatic agents. Bioorg Med Chem. 2003 Nov 3;11(22):4729-42. PubMed PMID: 14556788.
7: Zhang J, Cerny MA, Lawson M, Mosadeghi R, Cashman JR. Functional activity of the mouse flavin-containing monooxygenase forms 1, 3, and 5. J Biochem Mol Toxicol. 2007;21(4):206-15. PubMed PMID: 17721934.
8: Nagai H, Takaoka Y, Mori H, Kawada K. Effect of KE-298 on experimental arthritis in mice. Pharmacology. 1996 Sep;53(3):190-6. PubMed PMID: 8931104.
9: Hashimoto M, Kobayashi K, Yamagata N, Katsura T, Sugihara S, Iwabuchi H, Kasama T, Kasahara K, Takahashi T, Takeshita K, et al. Suppression of pulmonary granulomatous inflammation by immunomodulating agents. Agents Actions. 1992 Sep;37(1-2):99-106. PubMed PMID: 1456185.
10: Yoshida H, Kohno Y, Endo H, Ohmi N, Fukushima K, Suwa T, Hayashi M. Stereoselective disposition and chiral inversion of KE-298, a new antirheumatic drug, in rats. Chirality. 1997;9(1):22-8. PubMed PMID: 9094199.
11: Yasuda Y, Inoue T, Takeshita K. Pharmacological profile of KE-758, the main metabolite of the antirheumatic agent KE-298. Drugs Exp Clin Res. 1996;22(1):1-8. PubMed PMID: 8839631.
12: Endo H, Yoshida H, Hasegawa M, Ohmi N, Horiuchi N, Hamada Y, Higuchi S. Stereoselectivity and species difference in plasma protein binding of KE-298 and its metabolites. Biol Pharm Bull. 2001 Jul;24(7):800-5. PubMed PMID: 11456121.
13: Honda S, Migita K, Hirai Y, Origuchi T, Yamasaki S, Kamachi M, Shibatomi K, Fukuda T, Kita M, Hida A, Ida H, Aoyagi T, Kawakami A, Kawabe Y, Oizumi K, Eguchi K. Expression of membrane-type 1 matrix metalloproteinase in rheumatoid synovial cells. Clin Exp Immunol. 2001 Oct;126(1):131-6. PubMed PMID: 11678909; PubMed Central PMCID: PMC1906171.
14: Sakane T, Suzuki N, Hirose Y, Miura K, Wakisaka S, Nagafuchi H, Ichino M, Tomita T, Hashimoto H, Ochi T, Mihara S. Mechanisms of KE298, 2-acetylthiomethyl-3-(4-methylbenzoyl) propionic acid, to suppress abnormal synovial cell functions in patients with rheumatoid arthritis. J Rheumatol. 1997 Nov;24(11):2213-20. PubMed PMID: 9375886.
15: Sugimoto M, Inoue T, Takeshita K, Nakamura H, Yodoi J. Effects of a new anti-rheumatic drug KE-298 and its active metabolite: KE-758 on secretion of thioredoxin and on the level of intracellular glutathione in human monocytes and T cells. Mol Immunol. 2002 Feb;38(10):793-9. PubMed PMID: 11841839.
16: Inoue T, Yamashita M, Higaki M. The new antirheumatic drug KE-298 suppresses monocyte chemoattractant protein (MCP)-1 and RANTES production in rats with adjuvant-induced arthritis and in IL-1beta-stimulated synoviocytes of patients with rheumatoid arthritis. Rheumatol Int. 2001 May;20(4):149-53. PubMed PMID: 11411959.
17: Takahashi S, Inoue T, Higaki M, Mizushima Y. Suppressive effects of the new antirheumatic drug KE-298 on TNF alpha-induced production of matrix metalloproteinases but not of tissue inhibitor-1 of metalloproteinases in human rheumatoid synoviocytes. Drugs Exp Clin Res. 1998;24(2):67-71. PubMed PMID: 9675546.
18: Inoue T, Hamada Y, Takeshita K, Fukushima K, Higaki M. KE-298 and its active metabolite KE-758 suppress nitric oxide production by murine macrophage cells and peritoneal cells from rats with adjuvant induced arthritis. J Rheumatol. 2001 Jun;28(6):1229-37. PubMed PMID: 11409114.
19: Sugimoto M, Inoue T, Yamashita M, Takeshita K, Nakaike S. KE-758, an active metabolite of the new anti-rheumatic drug KE-298, suppresses production of tumor necrosis factor-alpha and interleukin-1 beta in THP-1, a human monocyte cell line. Drugs Exp Clin Res. 2002;28(5):197-205. PubMed PMID: 12635495.
20: Inoue T, Takeshita K, Fukushima K. Effects of KE-758; an active metabolite of the new anti-rheumatic drug KE-298, D-penicillamine, bucillamine and auranofin on the proliferation of murine lymphocytes, and the production of nitric oxide by murine macrophages. Int Immunopharmacol. 2001 May;1(5):833-42. PubMed PMID: 11379039.
