MorrisRE. New small molecule immunosuppressants for transplantation: Review of essential concepts. J Heart Lung Transplant1993; 12: 275–86.
2.
European FK506 Multicentre Liver Study Group. Randomised trial comparing tacrolimus (FK506) and cyclosporin in prevention of liver allograft rejection. Lancet1994; 344: 423–8.
3.
US Multicentre FK506 Liver Study Group. A comparison of tacrolimus (FK506) and cyclosporin for immunosuppression in liver transplantation. N Engl J Med1994; 331: 1110–5.
4.
DenesyukAIKorpelaTLundellJSaraRZav'yalovVP. Comparison of conformations of cyclosporin A and macrolide FK506 fragments: Localization of putative binding sites with phosphatase calcineurin. Biochem Biophys Res Commun1993; 194: 280–6.
5.
BraunWKallenJMikolVWalkinshawMDWuthrichK.Three-dimensional structure and actions of immunosuppressants and their immunophilins. FASEB J1995; 9: 63–72.
6.
HendersonDJNayaIBundickRVSmithGMSchmidtJA. Comparison of the effects of FK-506, cyclosporin A and rapamycin on IL-2 productions. Immunology1991; 73: 316–21.
7.
JohanssonAMollerE.Evidence that the immunosuppressive effects of FK506 and cyclosporin are identical. Transplantation1990; 50: 1001–7.
8.
LiuJFarmerJDLaneWSFriedmanJWeissmanISchreiberSL. Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell1991; 66: 807–15.
9.
McCaffreyPGPerrinoBASoderlingTRRaoA.NFATp, a T lymphocyte DNA-binding protein that is a target for calcineurin and immunosuppressive drugs. J Biol Chem1993; 268: 3747–52.
10.
ShawKT-YHoAMRaghavanAKimJJainJParkJImmunosuppressive drugs prevent a rapid dephosphorylation of transcription factor NFATI in stimulated immune cells. Proc Natl Acad Sci USA1995; 92: 11205–9.
11.
ShawJ-PUtzPJDurandDBTooleJJEmmelEACrabtreeGR. Identification of a putative regulator of early T-cell activation genes. Science1988; 241: 202–5.
12.
FrumanDABurakoffSJBiererB.Immunophilins in protein folding and immunosuppression. FASEB J1994; 8: 391–400.
13.
TakadaKKatayamaNKiriyamaAUsudaH.Distribution characteristics of immunosuppressants FK506 and cyclosporin in the blood component. Biopharm Drug Disp1993; 14: 659–72.
14.
DemetrisAJFungJJTodoSMcCauleyJJainATakayaSConversion of liver allograft recipients from cyclosporin to FK506 immunosuppressive therapy—a clinicopathologic study of 96 patients. Transplantation1992; 53: 1056–62.
15.
JordanMLShapiroRVivasCAScantleburyVPRhandhawaPCarrieriGFK506 “rescue” for resistant rejection of renal allografts under primary cyclosporin immunosuppression. Transplantation1994; 57: 860–5.
16.
CoxKLLawrence-MiyasakiLSGarcia-KennedyRLennetteETMartinezOMKramsSMAn increased incidence of Epstein-Barr virus infection and lymphoproliferative disorder in young children on tacrolimus after liver transplantation. Transplantation1995; 59: 524–9.
17.
CollinsRH. Tacrolimus (FK506) versus cyclosporin in prevention of liver allograft rejection. [Letter]. Lancet1994; 344: 949.
18.
DumontFJStaruchMJKoprakSLSiekerkaJJLinCSHarrisonRThe immunosuppressive and toxic effects of FK-506 are mechanistically related: Pharmacology of a novel antagonist of FK-506 and rapamycin. J Exp Med1992, 176: 751–60.
19.
SpectorRParkGDJohnsonGFVesellES. Commentary: Therapeutic drug monitoring. Clin Pharmacol Ther1988; 43: 345–53.
20.
McInnesL.The value of therapeutic drug monitoring to the practising physician—an hypothesis in need of testing. Br J Clin Pharmacol1989; 27: 281–4.
21.
AronsonJKHardmanM.ABC of monitoring drug therapy: Measuring plasma drug concentrations. BMJ1992; 305: 1078–80.
22.
IharaHShinkumaDIchikawaYNojimaMNaganoSIkomaF.Intra- and interindividual variation in the pharmacokinetics of tacrolimus (FK506) in kidney transplant recipients—importance of trough level as a practical indicator. Int J Urol1995; 2: 151–5.
23.
JainABAbu-ElmagdKAbdallahHWartyVFungJTodoSPharmacokinetics of FK506 in liver transplant recipients after continuous intravenous infusion. J Clin Pharmacol1993; 33: 606–11.
24.
JuskoWJPiekoszewiskiWKlintmalmGBShaeferMSHerbertMFPiergiesAAPharmacokinetics of tacrolimus in liver transplant recipients. Clin Pharmacol Ther1995; 57: 281–90.
25.
SewingK-Fr.Pharmacokinetics, dosing principles, and blood level monitoring of FK506. Transplant Proc1994; 26: 3267–9.
26.
JainABVenkataramananRCadoffEFungJJTodoSKrajackAEffect of hepatic dysfunction and T tube clamping on FK506 pharmacokinetics and trough concentrations. Transplant Proc1990; 22: 57–9.
27.
FurukawaHImventarzaOVenkataramananRSusukiMZhuYWartyVSThe effect of bile duct ligation and bile diversion on FK506 pharmacokinetics in dogs. Transplantation1992; 53: 722–5.
28.
WartyVDivenWCadoffETodoSStarzlTSanghviA.FK506: A novel immunosuppressive agent. Characteristics of binding and uptake by human lymphocytes. Transplantation1988; 46: 453–5.
29.
JuskoWJ. Analysis of tacrolimus (FK506) in relation to therapeutic drug monitoring. Ther Drug Monit1995; 17: 596–601.
30.
WallemacqPEFirdaousIHassounA.Improvement and assessment of enzyme-linked immunosorbent assay to detect low FK506 concentrations in plasma or whole blood within 6 hours. Clin Chem1993; 39: 1045–9.
31.
MachidaMTakaharaSIshibashiMHayashiMSekiharaTYamanakaH.Effect of temperature and hematocrit on plasma concentration of FK506. Transplant Proc1991; 23: 2753–4.
32.
ChristiansURadekeHHKownatzkiRSchiebelHMSchottmanRSewingK-Fr.Isolation of an immunosuppressive metabolite of FK506 generated by human microsome preparations. Clin Biochem1991; 24: 271–5.
33.
ChristiansUBraunFSchmidtMKosianNSheibelHMErnstLSpecific and sensitive measurement of FK506 and its metabolites in blood and urine of liver graft recipients. Clin Chem1992; 38: 2025–32.
34.
McDiarmidSVColonnaJOShakedAVargasJAmentMEBusuttilRW. Differences in oral FK506 dose requirements between adult and pediatric liver transplant recipients. Transplantation1993; 55: 1328–32.
35.
UndreNMollerAStadlerP.Clinical Pharmacokinetics of Tacrolimus. München: W. Zuckschwerdt Verlag, 1995: 32–3.
36.
SattlerMGuengerichFPYunC-HChristiansUSewingK-F.Cytochrome P-450 3A enzymes are responsible for biotransformation of FK506 and rapamycin in man and rat. Drug Metab Dispos Biol Fate Chem1992; 20: 753–61.
37.
ShigaraTMatsudaHNagaseKIwasakiKYamazakiHMetabolism of FK.506, a potent immunosuppressive agent, by cytochrome P450 3A enzymes in rat, dog and human liver microsomes. Biochem Pharmacol1994; 47: 727–35.
38.
MielesLVenkataramananRYokoyamaIWartyVJStarzlTE. Interaction between FK.506 and clotrimazole in a liver transplant recipient. Transplantaion1991; 52: 1086–7.
39.
ShapiroRVenkataramananRWartyVScantleburyVRybkaWMcCauleyJFK.506 interaction with danazol. Lancet1993; 341: 1344–5.
40.
WolterKWagnerKPhilipTFritschkaE.Interaction between FK506 and clarithromycin in renal transplant patient. Eur J Clin Pharmacol1994; 47: 207–8.
41.
ScheinerPAMorEChodoffLSheldonG.Acute renal failure associated with the use of ibuprofen in two liver transplant recipients on FK506. Transplantation1994; 57: 1132.
42.
SchaefferMSCollierDSorrellMF. Interaction between FK506 and erythomycin. Ann Pharmacother1994; 28: 280–1.
43.
ManezRMartinMVenkataramananRSilvermanDJainAWartyVFluconazole therapy in transplant recipients receiving FK506. Transplantation1994; 57: 1521–35.
44.
FurlanVPerelloLJacqueminEDebrayDTaburetAM, Interactions between FK506 and rifampicin or erythromycin in paediatric liver transplant recipients. Transplantation1995; 59: 1216–7.
45.
LakeKDCanafaxDM. Important interactions of drugs with immunosuppressive agents used in transplant recipients. J Antimicrob Chemother1995; 36 (suppl B): 11–22.
46.
IwasakiKMatsudaHNagaseKShiragaTTokumaYUchidaK.Effects of twenty-three drugs on the metabolism of FK506 by human liver microsomes. Res Commun Chem Pathol Pharmacol1993; 82: 209–16.
47.
VathsalaAGotoS.Yoshimura N, Stepkowski S, Chou T-C, Kahlan D. The immunosuppressive antagonism of low doses of FK506 and cyclosporin. Transplantation1991; 52: 121–8.
48.
TamuraKKobayashiMHashimotoKKojimaKNagaseKIwasakiKA highly sensitive method to assay FK-506 in plasma. Transplant Proc1987; 19 (suppl 6): 23–9.
49.
CadoffEMVenkataramananRKrajackAJainASFungJJTodoSAssay of FK506 in plasma. Transplant Proc1990; 22 (Suppl 1): 50–1.
50.
WartyVZuckermanSVenkataramananRLeverJFungJStarzlT.FK506 measurement: Comparison of different analytical measurements. Ther Drug Monit1993: 15: 204–8.
51.
JuskoWJD'AmbrosioR.Monitoring FK506 concentrations in plasma and whole blood. Transplant Proc1991; 23: 2732–5.
52.
D'AmbrosioRGirzaitisNJuskoWJ. Validation and quality assurance program for monitoring tacrolimus (FK506) concentrations in plasma and whole blood. Ther Drug Monit1993: 15: 414–26.
53.
GrenierFCLuczkiwJBergmannMLunettaSMorrisonMBlonskiDA whole blood FK.506 assay for the IMxch analyzer. Transplant Proc1991; 23: 2748–9.
54.
D'AmbrosioRGirzaitisNJuskoWJ. Multi-centre comparison of tacrolimus (FK506) whole blood concentrations as measured by the Abbott IMx analyzer and enzyme immunoassay with methylene chloride extraction. Ther Drug Monit1994; 16: 287–92.
55.
HoltDWJohnstonARobertsNTredgerJMTrullAK. Methodological and clinical aspects of cyclosporin monitoring: Report of the Association of Clinical Biochemists' task force. Ann Clin Biochem1994; 31: 420–46.
56.
WallemacqPERedingR.FK506 (tacrolimus), a novel immunosuppressant in organ transplantation: Clinical, biomedical and analytical aspects. Clin Chem1993; 39: 2219–28.
57.
WinklerMChristiansUBaumannJGonschiorAKWonigkeitKPichlmayrR.Evaluation of the Pro-Trac tacrolimus monoclonal whole-blood enzyme-linked immunosorbent assay for monitoring of tacrolimus levels in patients after kidney, heart and liver transplantation. Ther Drug Monit1996; 18: 640–6.
58.
MacFarlaneGSchellerDErsfeldDJensenTJevansAWongP-YA simplified whole blood ELISA [ProTrac-II] for tacrolimus (FK506) using a proteolytic extraction in place of organic solvents. Ther Drug Monit1996; 18: 698–705.
59.
GrenierFKoshyTLuczkiwJSulMVannestR.The new IMx tacrolimus II assay. In: IMx Tacrolimus II: Clinical Utility and Monitoring. Wiesbaden, Germany: Abbott Diagnostics Educational Services, Abbott Diagnostics, 1997: 6–7.
60.
TredgerMGilkesCDGondeCE. Therapeutic monitoring of tacrolimus (FK560) with the first and second generation MEIA assays: Performance and results in four patient populations. Ther Drug Monit (in press).
61.
VenkataramananRWartyVSZemaitisMASanghviATBurckartGJSeltmanHBipoharmaceutical aspects of FK-560. Transplant Proc1987; 19 (suppl 6): 30–5.
62.
FriobMCHassounALattineDLnoestGOtteJBWallemacqPE. A combined HPLC-ELISA evaluation of FK506 in transplant patients. Transplant Proc1991; 23: 2750–2.
63.
WartyVZuckermanSVenkataramananRLeverJChaoJMcKavereyTTacrolimus analysis: A comparison of different methods and matrices. Ther Drug Monit1995; 17: 159–67.
64.
TakadaKOh-HaskiMYoshikawaHMuranishiS.Determination of a novel potent immunosuppressant (FK-506) in rat serum and lymph by high-performance liquid chromatography with chemiluminescence detection. J Chromatogr1990: 530: 212–8.
65.
TaylorPJJonesABaldersonGALynchSV. Norris RLG, Pond SM. Sensitive, specific quantitative analysis of tacrolimus (FK506) in blood by liquid chromatography-electrospray tandem mass spectrometry. Clin Chem1996; 42: 279–85.
66.
IngelsSCKoenigJScottMG. Stability of FK506 (tacrolimus) in whole-blood specimens. Clin Chem1995; 41: 1320–1.
67.
ErdenEWartyVMagnoneMShapiroRDemetrisJRandhawaP.Plasma FK506 levels in patients with histologically documented renal allograft rejection. Transplantation1994; 58: 397–8.
68.
Japanese FK506 Study Group. Morphological characteristics of renal allografts under FK506 therapy: Is graft biopsy available to reveal the morphological findings corresponding with FK506 nephropathy?Transplant Proc1993; 25: 624.
69.
BackmanLNicarMLevyMDistantDEisensteinCRenardTFK506 trough levels in whole blood and plasma in liver transplant recipients: Correlation with clinical events and side effects. Transplantation1994; 57: 519–25.
70.
SigalNHDumontFJ. Cyclosporin A. FK-506, and rapamycin: Pharmacological probes of lymphocyte signal transduction. Annu Rev Immunol1991; 10: 519–60.
71.
BeysensAJWijnenRMHBeumanGHvan de HeydenJ.KootstraGvan AsH. FK506: Monitoring in plasma or in whole blood?Transplant Proc1991; 23: 2745.
72.
UedaMUemotoSInomataYOkajimaHHashidaTTanakaKA proposal of FK506 optimal dosing in living related liver transplantations. Transplantation1995; 60: 258–64.
73.
EsquivelCOSoSKMcDiarmidSVAndrewsWSColombaniPM. Suggested guidelines for the use of tacrolimus in pediatric liver transplant patients. Transplantation1996; 61: 847–8.
LiebermanRNelsonA.Dose-response and concentration-response relationships: Clinical and regulatory perspectives. Ther Drug Monit1993; 15: 498–502.
76.
KershnerRPFitzsimmonsWE. Relationship of FK506 whole blood concentrations and efficacy and toxicity after liver and kidney transplantation. Transplantation1996; 62: 920–6.
77.
GonschiorA-KChristiansUWinklerMLinckABaumannJSewingK-F, Tacrolimus (FK506) metabolite patterns in blood from liver and kidney transplant patients. Clin Chem1996; 42: 1426–32.
78.
GonschiorA-KChristiansUBraunFWinklerMLinckABaumannJMeasurement of blood concentrations of FK560 (tacrolimus) and its metabolites in seven liver graft recipients after the first dose by HPLC-MS and microparticle enzyme immunoassay (MEIA). Br J Clin Pharmacol1994; 38: 567–71.
79.
IwasakiKShigaraTNagaseKTozukaZNodaKSakumaSIsolation, identification, and biological activities of oxidative metabolites of FK506, a potent immunosuppressive macrolide lactone. Drug Metab Dispos Biol Fate Chem1993; 21: 971–7.
80.
IwasakiKShigaraTMatsudaHNagaseKTokumaYHataTFurther metabolism of FK506 (tacrolimus). Identification and biological activities of the metabolites at multiple sites of FK506. Drug Metab Dispos Biol Fate Chem1995; 23: 28–34.
81.
WinklerMChristiansUStollKPichlmayrR.Comparison of different assays for the quantification of FK506 levels in blood or plasma. Ther Drug Monit1994; 16: 281–6.
WinklerM.Practical aspects of tacrolimus immunosuppression in patients after solid organ transplantation. In: Tacrolimus—Clinical Utility and Monitoring. Witsbaden, Germany: Abbott Diagnostic Educational Services, Abbott Diagnostics, 1995: 18–20.
84.
Abu-ElmagdKFungJFAlessianiMJainAVenkataramananRWartyVSThe effect of graft function on FK506 plasma levels, dosages, and renal function, with particular reference to the liver. Transplantation1991; 52: 71–7.
85.
ShirakataYKobayashiMOhtsukaKSuganoMTerajimaHIkaiIInhibitory effect of plasma FKBP12 on immunosuppressive activity of FK506. Transplantation1995; 60: 1582–7.
86.
ErdenEWartyVMagnoneMShapiroRDemetrisJRandhawaP.Plasma FK506 levels in patients with histologically documented renal allograft rejection. Transplantation1994; 58: 397–8.
87.
SandbornWJLawsonGMCodyTJPoraykoMKHayJEGoresGJEarly cellular rejection after orthotopic liver transplantation correlates with low concentrations of FK506 in hepatic tissue. Hepatology1995; 21: 70–6.
88.
SchreiberSL. Chemistry and biology of the immunophilins and their immunosuppressive ligands. Science1991; 151: 283–7.
89.
WartyVVenkataramananRZendehrouhPMcKaveneyTChaoJTodoSDistribution of FK506 in plasma lipoproteins in transplant patients. Transplant Proc1991; 23: 954–5.
90.
BakhtiarRStearnsRA. Studies on non-covalent associations of immunosuppressive drugs with serum albumin using pneumatically assisted electrospray ionization mass spectrometry. Rapid Commun Mass Spectrom1995; 9: 240–4.
91.
UndreNMollerA. FK 506 European Study Group. Pharmacokinetic interpretation of FK506 levels in blood and plasma during a European randomised study in primary liver transplant patients. Transpl Int1994; 7: 15.
92.
LewisGPJuskoWJBurkeCGravesL.Prednisolone side-effects and serum-protein levels. Levels1971; ii: 778–80.
93.
Boston Collaborative Drug Surveillance Program (BCDSP). Diphenylhydantoin side-effects and serum albumin levels. Clin Pharmacol Ther1973; 14: 529.
94.
GreenblattDJKoch-WeserJ.Clinical toxicity of chloridazepoxide and diazepam in relation to serum albumin concentration: A report from BCDSP. Eur J Clin Pharmacol1974; 7: 259.
95.
BlaschkeTFMeffinPJMelmonKLRowlandM.Influence of acute viral hepatitis on phenytoin kinetics and protein binding. Clin Pharmacol Ther1975; 17: 685.
96.
PiafskyKMSitarDSRangnoREOgilvieRI. Theophylline disposition in patients with hepatic cirrhosis. N Engl J Med1977; 296: 1495.
97.
JainABVenkataramananRCadoffEFungJTodoSKrajakAEffect of hepatic dysfunction and T-tube clamping on FK506 pharmacokinetics. Transplant Proc1990; 22: 57.
98.
MuellerARPlatzK-PBechsteinWOSchattenfrohNStoltenbur-DidingerGBlumhardtFNeurotoxicity after orthotopic liver transplantation. Transplantation1994; 58: 155.
99.
DawsonTMSteinerJPLyonsWEFotuhiMBlueMSnyderSH. The immunophilins, FK506 binding protein and cyclophilin, are discretely localized in the brain: Relationship with calcineurin. Neuroscience1994; 62: 569–80.
100.
ZeeviAEirasGKaufmanCAlessianiMDemetrisAJAbu-ElmagdKCorrelation between bioassayed plasma levels of FK506 and lymphocyte growth from liver transplant biopsies with histological evidence of rejection. Transplant Proc1991; 23: 1406–8.
101.
BurresNSPremachandranUHoseltonSCwikDHochlowskiJEYeQSimple aromatics identified with a NFAT-lacZ transcription assay for the detection of immunosuppressants. J Antibiot1995; 48: 380–6.
102.
DonnellyJGSoldinSJ. Radioreceptor assays for the measurement of cyclosporin activity: A preliminary report. Ther Drug Monit1989; 11: 696–700.
103.
LorberMIPaulKHardingREHandschumacherREMarksWH. Cyclophilin binding: A receptor-mediated approach to monitoring cyclosporin immunosuppressive activity following organ transplantation. Transplant Proc1990; 22: 1240–4.
104.
MurthyJNChenYWartyVSVenkataramananRDonnellyJGZeeviARadioreceptor assay for quantifying FK-506 immunosuppressant in whole blood. Clin Chem1992; 38: 1307–10.
105.
RussellRLDonnellyJGPalaszynskiEWChanMMSoldinSJ. A preliminary study to evaluate an in vitro assay for determining patient whole blood immunosuppressive cyclosporin A and metabolite activity: Comparison with cytosolic binding assays using cyclophilin or a 50-kilodalton binding protein, and the Abbott TDx cyclosporin A parent, and metabolites assays. Ther Drug Monit1991; 13: 32–6.
106.
AsamiMKunoTMukaiHTanakaC.Detection of the FK506-FKBP-calcineurin complex by simple binding assay. Biochem Biophys Res Commun1993; 192: 1388–94.
107.
TamuraKFujimuraTIwasakiKSakumaSNakamuraKShimomuraKInteraction of tacrolimus (FK506) and its metabolites with FKBP and calcineurin. Biochem Biophys Res Commun1994; 202: 437–43.
108.
SoldinSJMurthyJNDonnellyJGChenYGoodyearN.Immunophilin receptors for immunosuppressive drugs. Ther Drug Monit1993; 15: 468–71.
109.
SuQWeberLLe HirMZenkeGRyffelB.Nephrotoxicity of cyclosporin A and FK506: Inhibition of calcineurin phosphatase. Renal Physiol Biochem1995; 18: 128–39.
110.
BiererBE. Cyclosporin A, FK506, and rapamycin: Binding to immunophilins and biological action. Chem Immunol1994; 59: 128–55.
111.
BaughmanGWiederrechtGJCampbellNFMartinMMBourgeoisS.FKBP51, a novel T-cell-specific immunophilin capable of calcineurin inhibition. Mol Cell Biol1995; 15: 4395–402.