Description and references

Macrolide calcineurin inhibitor. Isoln from Streptomyces tsukubaensis no. 9993: M. Okuhara et al., EP 184162 (1986 to Fujisawa); and characterization: T. Kino et al., J. Antibiot. 40, 1249 (1987). Structure determn: H. Tanaka et al., J. Am. Chem. Soc. 109, 5031 (1987). Total synthesis of ()-form: T. K. Jones et al., J. Am. Chem. Soc. 111, 1157 (1989). In vitro immunosuppressant activity in comparison with cyclosporin, q.v.: T. Kino et al., J. Antibiot. 40, 1256 (1987). Toxicology: K. Ohara et al., Transplant. Proc. 22, 83 (1990). Symposium on pharmacology and clinical trials: ibid. 23, 2709-3376 (1991). Review of mechanism of action: G. Wiederrecht et al., Ann. N.Y. Acad. Sci. 696, 9-19 (1993); of clinical trials in comparison with cyclosporin in renal transplantation: G. A. Knoll, R. C. Bell, Br. Med. J. 318, 1104-1107 (1999). Review of use in dermatoses: A. K. Gupta et al., J. Eur. Acad. Dermatol. Venereol. 16, 100-114 (2002); treatment of inflammatory bowel disease: D. K. L. Chow, R. W. L. Leong, Expert Opin. Drug Saf. 6, 479-485 (2007).

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