Section Review; Pulmonary-Allergy, Dermatological, Gastrointestinal & Arthritis: Recent developments with immunosuppressant macrolides: Tacrolimus and sirolimus

References

• KINO T, HATANAKA Fl, HASHIMOTO M et al.: FK506, a novel inununosuppressant isolated from a streptomy-ces. I. Fermentation, isolation and physico-chemical and biological characteristics. J. Antibiot. (1987) 40:1249–1255.
   Google Scholar
• KING T, HATANAKA H, MIYATA S at al.- FK506, a novel immunosuppressant isolated from a streptomyces. U. Inununosuppressive effect of FK506 in vitro. J. Antibiot. (1987) 40:1256–1265.
   Google Scholar
• SAWADA S, SUZUKI G, KAWASE Y, TAKAKU F: Novel immunosuppressive agent, FK506. In vitro effects on the cloned T-cell activation. J. Immunol. (1987) 139:1797–1803.
   Google Scholar
• GOTO T, KINO T, HATANAKA H et al.: Discovery of FK506, a novel immunosuppressant isolated from Streptomyces tsukubaensis. Transplant. Proc. (1987) 19\(Suppl. 6):4–8.
   Google Scholar
• OCHIAI T, NAKAJIMA K, NAGATA M et al.: Effect of a new immunosuppressive agent, FK506 on heterotopic car-diac allotransplantation in the rat. Transplant. Proc. (1987) 19:1284–1286.
   PubMed Web of Science ®Google Scholar
• OCHIAI T, NAKAJIMA K, NAGATA M, HORI S, ASANO T, ISONO K: Studies of the induction and maintenance of long-term graft acceptance by treatment with FK506 in heterotopic cardiac allotransplantation in rats. Trans-plantation (1987) 44:734–738.
   Google Scholar
• CALNE R, COLLIER DSTJ, THIRU S: Observations about FK506 in primates. Transplant. Proc. (1987) 19\(Suppl. 6):63,
   Google Scholar
• COLLIER DSTJ, THIRL55, CALNE R: Kidney transplantation in the dog receiving FK506. Transplant. Proc. (1987) 19\(Suppl. 6):62.
   Google Scholar
• TODO S, PODESTA L, STARZL TE A al.: Orthotopic liver transplantation in dogs receiving FK506. Transplant. Proc. (1987) 19\(Suppl. 6):64–67.
   Google Scholar
• MURASE N, TODO S, LEE PH et al.: Heterotopic heart transplantation in the rat receiving FK506 alone or with cyclosporine. Transplant. Proc. (1987) 19\(Suppl. 6):71–75.
   Google Scholar
• TANAKA H, KURODA A, MARUSAWA II at al.: Structure of FK506: a novel immunosuppressant isolated from streptomyces. J. Am. Chem. Soc. (1987) 109:5031–5033.
   Google Scholar
• IIONBO T, KOBAYASI II M, I IANE K, I IATA T, UEDA y: The oral dosage form of FK506. Transplant. Proc. (1987) 19\(Suppl. 0:17–22.
   Google Scholar
• KOBAYASHI M, TAMURA K, KATAYAMA N at al.: FK506 assay past and present - characteristics of FK506 ELISA. Transplant. Proc. (1991) 232725–2729.
   Google Scholar
• VEZINA C, KUDELSKI A, SEHGAL SN. Rapamycin (AY-22,989), a new antifungal antibiotic. I. Taxonomy of the producing streptomycete and isolation of the active principle. J. Antibt. (1975) 28,721–726.
   Google Scholar
• SEHGAL SN, BAKER Ti, VEZINA C: Rapamycin (AY-22,989), a new antifungal antibiotic. II. Fermentation, isolation and characterization. J. Antihiot. (1975) 28:727–732.
   Google Scholar
• MORRIS RE: Rapamycins: antifungal, antitumor, an- tiproliferative and immunosuppressive naacrolides.Transplant. Rev. (1992) 6:39-87. A thorough review of initial studies with rapamycin.
   Google Scholar
• DOUROS J, SUFFNESS M: New antitumor substances of natural origin. Cancer Treatment (1981) 8:63–87.
   Google Scholar
• ENG CP, SEHGAL SN, VEZINA C: Activity of rapamycin against transplanted tumors. J. Antibiot. (Tokyo) (1984) 37:1231–1237.
   PubMed Web of Science ®Google Scholar
• SEHGAL SN: Lnununosuppressive profile of rapamycin.Ann. NY Acad. Sci. (1993) 696:1–8.
   PubMed Web of Science ®Google Scholar
• CALNE RY, COLLIER DS, LIM S, POLLARD SG, SAMAAN A.WHITE DJ, THIRLI S: Rapamycin for imnauttosuppres-sion in organ allograft.ing. Lancet (1989) 2:227.
   Google Scholar
• WIEDERRECHT G, LAM E, HUNG S at al.: The mechanismof action of FK506 and cyclosporin A. Ann. NY Acad. Sci. (1993) 696:9–19.
   Google Scholar
• SIEKIERKA JJ, HUNG SH, POE M et al A cytosolic binding protein for the imnaunosuppressant FK506 has pep-tidylprolyl isomerase activity but is distinct from cyclo-philin. Nature (1989) 341:755–757
   PubMed Web of Science ®Google Scholar
• HARDING MW, GALAT A, UEHLING DE, SCHREIBER SL: Areceptor for the immunosuppressant FK506 is a cis-trans peptidyl-prolyl isomerase. Nature (1989) 341:758–760.
   PubMed Web of Science ®Google Scholar
• BIERER BE, MATHLA PS, STANDAERT RF at al.: Two distinct signal transmission pathways in T-Iympho-cytes are inhibited by complexes formed between an irannmophilin and either FK506 or rapamycin. Proc Natl. Acad. Sci. USA (1990) 87:9231–9235.
   Google Scholar
• FRIEDMAN J, WEISSMAN I: Two cytoplasmic candidatesfor immunophilin action are revealed by affinity for a new cyclophilin: one in the presence and one in the absence of CsA. Cell (1991) 66:799–806.
   PubMed Web of Science ®Google Scholar
• FLANAGAN WM, CORTHESY B, BEAM RJ at al.: Nuclear association of a T-cell transcription factor blocked by FK506 and cyclosporin A. Nature (1991) 352:803–807.
   Google Scholar
• SEHGAL SN: Rapamune (sirolimus, rapamycin): an over- view and mechanism of action. Ther. Drug Monit. (1995) 17:660-665. A comprehensive review of the current knowledge of sirolirnus's mechanism of action.
   Google Scholar
• CHEN Y, CHEN H, RHOAD A at al.: A putative sirolimus (rapamycin) effector protein. Biochem. Biophys. Res. Commun. (1994) 2031–7.
   Google Scholar
• BROWN EJ, ALBERS MW, SHIN TB et al Purification and molecular cloning of FRAP, a direct target of GI arrest complex FKBP12-rapamycin. Nature (1994) 369:756–761
   PubMed Web of Science ®Google Scholar
• SABATINI DM, ERDIUMENT B, LU1 M at al.. RAFF1: a mammalian protein that binds to FICBP12 in a rapamy-cindependent fashion and is homologous to yeast TORs. Cell (1994) 78.35–43.
   Google Scholar
• SABERS CJ, MARTIN MM, BRUNN GJ el al.: Isolation of a protein target of FICEIP12-rapamycin complex in mam-malian cells. J. Biol. Chem. (1995) 270:815.
   Google Scholar
• ARAI K, HOTOKEBUCIII T MIYAHARA II et al. Limb allografts in rats inununosuppressed with FK506: I. Reversal of rejection and indefinite survival_ Transplan-tation(1989) 48782–786.
   Google Scholar
• ERICZON BG, KUBOTA K, GROTH CG et al.: Pancreati-coduodenal allotransplantation with FK506 in the cynomolgus monkey. Transplant. Proc. (1990) 22:72–73.
   PubMedGoogle Scholar
• HOFFMAN AL, MAKOWKA L, CAI X et al.: The effect of FK506 on small intestine allotrans plantation in the rat. Transplant. Proc. (1990) 22\(Suppl. 1):76–77.
   Google Scholar
• INAMURA N, NAKAHARA K, KINO T et al.: Prolongation of skin allograft survival in rats by a novel immunosup-pressive agent, FK506. Transplantation (1988) 45:206–209.
   PubMed Web of Science ®Google Scholar
• MURASE N, TODO S, LEE P et al.: Heterotopic heart transplantation in the rat receiving F1(506 alone or with ciclosporine. Transplant. Proc. (1987) 19\(Suppl. 6)71–75
   Google Scholar
• MONDEN M, GOTOH M, KANAI T et al.: A potent immu-nosuppressive effect of FK506 in orthotopic liver trans-plantation in primates. Transplant. Proc. (1990) 22\(Suppl. 1):66–71.
   Google Scholar
• MORIMOTO T, YAMADA T, KOBAYASHI M et al.: Pancrea-ticoduodenal allotransplantation with F1(506 in the dog. Transplant. Proc. (1990) 22:717–719.
   PubMedGoogle Scholar
• SATO K, YAIMAGISHI Y, NAKAYAMA K et al.: Pancreati-coduodenal allotransplantation with cyclosporine and FK506. Transplant. Proc. (1989) 21:1074–1075.
   PubMed Web of Science ®Google Scholar
• TODO S, DEMETRIS AJ, UEDA Y et al.: Canine kidney transplantation with F1(506 alone or in combination with cyclosporine and steroids. Transplant. Proc. (1987) 19\(Suppl. 6):57–61.
   Google Scholar
• TODO S, UEDA Y, DEMETRIS AJ et al.: Immunosuppres-sion of canine, monkey and baboon allografts by F1/506 with special reference to synergism with other drugs, and to tolerance induction. Surgery (1988) 104:239–249.
   PubMed Web of Science ®Google Scholar
• TSUCHIMOTO S, KUSUMOTO K, NAKJIMA Y et al.: Ortho-topic liver transplantation in rats receiving F1(506. Transplant. Proc. (1989) 21:1064–1065.
   PubMed Web of Science ®Google Scholar
• YOKOTA K, TAKISHIMA T, SATO K et al.: Comparative studies of F1(506 and cyclosporine in canine orthotopic hepatic allografts survival Transplant. Proc. (1989) 21:1066–1068.
   Google Scholar
• THE EUROPEAN MULTICENTER FK506 LIVER STUDY GROUP: Randomized trial comparing tacrolimus (F1(506) and cyclosporin in prevention of liver allograft rejection. Lancet (1994) 344:423-428. A good overview of the clinical experience of tacrolimus in trans-plantation.
   Google Scholar
• THE US MULTICENTER FK506 LIVER STUDY GROUP: A comparison of tacrolimus (F1(506) and cyclosporine for immunosuppression in liver transplantation. Neuf Engl. J. Med. (1994) 331:1110-1115, A good overview of the clinical experience of tacrolimus in trans-plantation.
   Google Scholar
• MCDIARMID SV, BUSUTTIL RW, ASCHER NL et al.: F1(506 (tacrolimus) compared with cyclosporine for primary immunosuppression after pediatric liver transplanta-tion. Transplantation (1995) 59:530–536.
   PubMed Web of Science ®Google Scholar
• FUNG JJ, TODO S, JAIN A et al.: Conversion from cy-closporine to FK506 in liver allograft recipients with cyclosporine-related complications. Transplant. Proc. (1990) 22\(Suppl. 1):6–12.
   Google Scholar
• FUNG JJ, TODO S. TZAKIS A et al.: Conversion of liver allograft recipients from cydosporine to F1(506 based irnunosuppression: benefits and pitfalls. Transplant. Proc. (1991) 23:14–21.
   Google Scholar
• DEMETRIS AJ, FUNG JJ, TODO S et al.: Conversion of liver allograft recipients from cydosporine to FK506 iinmu-nosuppressive therapy - a clinkopathological study of 96 patients. Transplantation (1992) 53:1056–1062.
   PubMedGoogle Scholar
• REDING R, DE VILLE DE GOYET J, SOKAL E et al.: Com-passionate use of F1(506 in pediatric liver transplanta-tion: a pilot study. Transplant. Proc. (1991) 23:3002–3004.
   Google Scholar
• REDING R. WALLEMACQ PE, LAMY M et al.: Conversion from cyclosporine to FIC506 for salvage of immunocom-promised pediatric liver allografts. Transplantation (1994) 57:93–100.
   Google Scholar
• ARMITAGE .1M, KORMOS RL, FLING J, STARZL TE: The clinical trial of F1(506 as primary and rescue inununo-suppression in adult cardiac transplantation. Trans-plant. Proc. (1991) 23:3054–3057.
   PubMed Web of Science ®Google Scholar
• STARZL TE, FUNG J, JORDAN M et al.: Kidney transplan-tation under FK506. JAMA (1990) 264:63–67.
   PubMed Web of Science ®Google Scholar
• SHAPIRO R, JORDAN M, SCANTLEBURY V et al.: F1(506 in clinical kidney transplantation. Transplant. Proc. (1991) 23:3065–3067.
   PubMed Web of Science ®Google Scholar
• JAPANESE FK506 STUDY GROUP: Japanese study on kid-ney transplantation: results of an early Phase II study. Transplant. Proc. (1992) 23:3071–3074.
   Web of Science ®Google Scholar
• OCHIAI T, ISHIBASHI M, FUKAO K et al.: Japanese multi-center studies of FK506 in renal transplantation. Trans-plant. Proc. (1995) 27:50–53.
   PubMed Web of Science ®Google Scholar
• TODO S, TZAKIS A, REYES J et al.: Clinical small bowel or small bowel plus liver transplantation under F1(506. Transplant. Proc. (1991) 23:3093–3095,
   PubMed Web of Science ®Google Scholar
• BACH JF: The new era of immunosuppressive therapyin autoimmune diseases. Transplant. Proc. (1991) 23:3319–3321.
   PubMed Web of Science ®Google Scholar
• STEPKOWSKI SM, CHEN H, DALOZE P, KAHAN BD: Ra-pamycin, a potent immunosuppressive drug for vascu-larized heart, kidney, and small bowel transplantation in the rat. Transplantation (1991) 51:22–26,
   PubMed Web of Science ®Google Scholar
• CHEN ii, WU J, XU D et al,: Raparnycin reverses acute heart, kidney, and pancreas allograft rejection and prevents accelerated heart allograft rejection in the rat. Transplant. Proc. (1993) 25:719–720.
   PubMed Web of Science ®Google Scholar
• FRYER J, YATSCOFF RW, PASCOE EA, THLIVERIS J: Rela-tionship of blood concentrations of rapamycin and cyclosporine to suppression of allograft rejection in a rabbit heterotopic heart transplant model Transplanta-tion (1993) 55:340–345.
   Google Scholar
• ALMOND PS, MOSS A, INAKIREH RF et al.: Rapamycin, immunosuppressive and tolerogenic effects in a por-cine renal allograft model Transplantation (1993)56:275–279.
   Google Scholar
• YAKIMETS WJ, LAKEY JR, YATSCOFF RW et al.: Prolonga-tion of canine pancreatic islet allograft survival with combined rapamycin and cyclosporine therapy at low doses. Rapamycin efficacy is blood level related. Trans-plantation (1993) 56:1293–1298.
   Google Scholar
• OLEN II, VU D, WU J, DALOZE P: Prolongation of hamster to rat xenograft survival by rapamycin. Transplant. Proc. (1992) 24:715–718.
   PubMed Web of Science ®Google Scholar
• ROBERGE FG, DASIIENG X, CI IAN CC et al.: Treatment of autoittunune uveoretinitis in the rat with rapamycin, an inhibitor of lymphocyte growth factor signal transduction. Con- Eve Res. (1993) 12:197–203. 78. -79
   Google Scholar
• KAI IAN BD, MURGIA MG, SLATON J, NAPOLI K: Potential applications of therapeutic drug monitoring of si-rolimus immunosuppression in clinical renal trans-plantation. Ther Drug. Mon it. (1995) 17:672-675. First clinical data on sirolimus in kidney transplantation.
   Google Scholar
• ABoujoun MS, LEVY MF, KLINTMALM GB AND THE US MULTICENTER STUDY GROUP: Hyperlipidemia after liver transplantation: long-term results of the FK506/cyclosporine A US multicenter trial. Transplant. Proc. (1995) 27:1121–1123.
   PubMed Web of Science ®Google Scholar
• KAHAN BD, CHANG JY, SEHGAL SN: Preclinical evalu- ation of a new potent immunosuppressive agent, ra-parnycin. Transplantation (1991) 52:185–190.
   PubMed Web of Science ®Google Scholar
• WHITING PH, WOO J, ADAM BJ et al.: Toxicity of rapamy-cin - a comparative and combination study with cy-closporine at immunotherapeutic dosage in the rat. Transplantation (1991) 52:203–206.
   PubMed Web of Science ®Google Scholar
• VENKATARAMANAN R, JAIN A, CADOFF E et al.: Phartna-cokinetics of FK506: preclinical and clinical studies. Transplant. Proc. (1990) 22\(Suppl. 1):52–56.
   Google Scholar
• VENKATARAMANAN R, JAIN A, WARTY VS et al.: Pharma- cokinetics of FK506 in transplant patients. Transplant. Proc. (1991) 23:2736-2740. First clinical pharmacokinetic study of tacrolimus.
   Google Scholar
• VENKATARAMANAN R, JAIN A, WARTY VS et al Pharma- cokinetics of FK506 following oral administration: a comparison of FK506 and cyclosporine. Transplant Prix (1991) 23:931-933. TAKADA K, OH-HASI II M, YOSHIKAWA II, MURANISHI S Determination of a novel potent inununosuppressant (FK506) in rat serum and lymph by high-performance liquid chromatography with chemilutninescence de-tection. (Jhromatogr. (1990) 530.212–218.
   Google Scholar
• SEWING KF, CHRISTIANS 1:: FK506. Lancet (1991) 337:499. ZLEVI A, EMS G. KAUFMAN C eta! Correlation between bioassayed plasma levels of FK506 and lymphocyte growth from liver transplant biopsies with histological evidence of rejection. Transplant Proc (1991) 23:1406–1408
   Google Scholar
• FRIOI3 MC, IIASS01.7N A, LATINNE D, LIIOEST G, 011E JB. WALLEMACQ PE: A combined HPLC-ELISA evaluation of FK506 in transplant patients. Transplant. Proc. (1991) 23:2750–2752.
   Google Scholar
• VENKATARAMANAN R, WARTY VS, ZEMAITIS MA et al.: Biopharmaceutical aspects of FK506. Transplant. Proc (1987) 19(Suppl 61:30–35.
   PubMedGoogle Scholar
• WARTY V. VENKATARAMANAN R, ZENDEHROUI I P et al.: Distribution of FK506 in plasma lipoproteins in trans-plant patients. Transplant. Proc. (1991) 23:954–955.
   Google Scholar
• IAIN AB, VENKATARAMANAN R, CADOFF E et al.: Effect of hepatic dysfunction and T tube damping on FK506 pharmacokinetics and trough concentrations. Trans-plant Proc. (1990) 22\(Suppl. 1):57–59
   Google Scholar
• SATTLER M. GUENGERICH FP, YUN C, CHRISTIANS U, SEWING KF: Crochrome P-450 3A enzymes are respon-sible for biotransforrnation of FK506 and raparnycin in man and rat. Drug .11etah. Dispos. 119921 20:753–761.
   Google Scholar
• CHRISTIANS U, KRUSE C, KOWNATZKI R et al.: Measure-ment of FK506 by HPLC and isolation and charac-terization of its metabolites. Transplant. Proc. (1991) 23:940–941.
   PubMedGoogle Scholar
• CHRISTIANS U, BRAUN F, KOSIAN N et al.: High perform-ance liquid chromatography/mass spectrometry of FK506 and its metabolites in blood, bile, and urine of liver grafted patients. Transplant. Proc. (1991) 23:2741–2744.
   PubMed Web of Science ®Google Scholar
• LHOEST G, WALLEMACQ P, VERBEECK R: Isolation and mass spectrometric identification of five metabolites of FK506, a novel macron& immunosuppressive agent, from human plasma. Pharni. Acta Hely. (1991) 66:302–306.
   PubMedGoogle Scholar
• JAIN AB, TODO 5, FUNG JJ et al.: Correlation of rejection episodes with FK506 dosage, FK506 level, and steroids following primary orthotopic liver transplant. Trans-plant. Proc. (1991) 23:3023–3025.
   Google Scholar
• BACICMAN L, LEVY MF, KLINTMALM G AND THE FK506 MULTICENTER STUDY GROUP: Whole-blood and plasma levels of FK506 after liver transplantation: results from the US multicenter triaL Transplant. Proc. (1995) 27:1124.
   Google Scholar
• WALLEMACQ PE, REDING R: FK506 (tacrolimus), a novel imniunosuppressant in organ transplantation: cLinical, biomedical and analytical aspects. Clin. Chem. (1993) 39:2219–2228.
   PubMed Web of Science ®Google Scholar
• WALLEMACQ PE, FIRDAOUS I, HASSOUN A: Improvementand assessment of enzyme-linked immunosorbent as-say to detect low FK506 concentrations in plasma or whole blood within 6 hours. Clin. Chem. (1993) 39:1045–1049.
   PubMed Web of Science ®Google Scholar
• FIRDAOUS I, HASSOUN A, OTTE JB et al.: HPLC-MEIA specific for tacrolimus in whole blood of hepatic and renal transplant patients. Clin Chem. (1995) 41:1292–1296.
   PubMed Web of Science ®Google Scholar
• BAKER H, SIDOROWICZ A, SEHGAL SN et al Rapamycin(AY-22,989), a new antifungal antibiotic. III. In vitro and in vivo evaluation. Antibiot (Tokyo) (1978) 31.539–546.
   PubMed Web of Science ®Google Scholar
• NAPOLI K, KAHAN BD: High-performance liquid chro-matography of rapamycin. Clin. Chem. (1991) 37:294–295.
   PubMed Web of Science ®Google Scholar
• YATSCOFF RW, FARACI C, BOLINGBROKE P: Measure-ment of raparnycin in whole blood using reversed-phase high-performance liquid chromatography. Ther. Drug Monit. (1992) 14:138–141.
   PubMed Web of Science ®Google Scholar
• NAPOLI K, KAHAN BD: Sample clean-up and high-per-formance liquid chromatography techniques for meas-urement of whole blood rapamycin concentrations. J. Chromatogr. B (1994) 654:111–120.
   PubMed Web of Science ®Google Scholar
• YATSCOFF RW, WANG P, CHAN K et al.: Rapamycim distribution, pharmacokinetics, and therapeutic range investigations. Ther. Drug Montt. (1995) 17:666-671. First clinical pharmacokinetic study of sirolimus.
   Google Scholar
• YATSCOFF RW, LEGATT DF, KNETEMAN NM: Therapeutic monitoring of rapamycin: a new immunosuppressive drug. Ther. Drug Monit (1993) 15:478–482.
   PubMed Web of Science ®Google Scholar