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. Author manuscript; available in PMC: 2016 Mar 1.
Published in final edited form as: Bioanalysis. 2015 May;7(8):1037–1058. doi: 10.4155/bio.15.35

Table 4.

Published LC–MS/MS assays for quantification of immunosuppressive drugs in lymphocytes.

Drug Subjects Extraction Chromatographic conditions Precursor ion (m/z) > product ion (m/z) Ref.
CsA HV (n = NR); LTRs, LgTRs, and RTRs (n = 64) At 4°C to prevent efflux of CsA Gradient: H2O (A), MeOH (B) LC-MS [110]
Lymphocyte isolated from 8 ml blood with BD Vacutainer® CPT™ Cell Preparation Tubes Online SPE: XTerra™ MS C8 [M + Na] + [111]
Cells lysed with MeOH/dry reconstituted with MeOH Column: XTerra™ MS C18 (Waters) CsA: 1224.7/NR [120]
IV: 40μl Run time: 31 min IS: 27 demethoxy-sirolimus
R: 98% LLOQ: 5ng/ml;0.5fg/PBMC

CsA Early RTRs (n = 20); HTRs (n = 10) Verapamil added prevent efflux of CsA Gradient: ACN/20 mM ammonium formate buffer pH 3.6 (20:80) (A), ACN/(NH4 + COO-) pH 3.6 (80:20) (B) [M + H] + [118]
T-lymphocyte isolated from 7 ml blood with Prepacyte®. SPE: Water Oasis®, HLB 1 cc, 30 mg CsA: 1203.7 > 1101.7/1185.7 [121]
Cells were lysed and protein precipitated with MeOH: ACN: water (1:1:3) followed by SPE Column: C8, (Thermo Electron Corp) IS: CsC
IV: 100 μl Run time: 38 min
R: CsA and metabolites 73.5–98.6 LLOQ: 0.25 ng/ml

CsA and metabolites Early (n = 57) and chronic RTRs (n = 54) Verapamil added to prevent efflux of CsA Gradient: 5% ACN (A), 95% ACN (B); both contain 2 mM/l ammonium acetate/0.1 FA [M + H] + [122]
Lymphocyte isolated from 1.5 ml blood with Histopaque 1077 solution Column: Acquity UPLC RP BEH, C18 CsA: 1202.8 > 156.2.
Precipitation solution ACN: MeOH (40:60, v/v); (v:v:v) Run time: 5 min IS: CsD
IV: NR, LLOQ: 5 ng/ml
R: CsA and metabolites 71.9–78.4%.

CsA HTRs (n = 17) 10 ml whole blood incubated with E-Rosette solution, followed by density separation using Histiopaque solution. Isocratic: ACN: 2 mM ammonium acetate: FA (70:30:0.1) [M + NH] + [125]
IV: 1 μl Column: Supelco LC-CN CsA: 1,220.8 > 1202.7
R: NR Run time: NA IS: CsD
LLOQ: 1 pg

EVE HTRs (n = 36) At 4°C to prevent efflux of EVE Gradient: H2O (A), MeOH (B); both contain 2 mM ammonium acetate/0.1% FA [M + NH4] + [132]
Lymphocyte isolated from 8 ml blood with BD Vacutainer® CPT™ Cell Preparation Tubes. Cells were lysed with MeOH dry & reconstituted with MeOH. Extract one part with 4:5:3 parts of zinc sulfate 0.1 M: 5: H20: CAN Column: MassTrak TDM C18 (Waters). EVE: m/z 975.5 > 908.5
IV: 20 μl Run time: 1.5 min IS: ASC
R: 79.4–87.1%. LLOQ: 1.25 ng/ml

TAC RTRs (n = 65) At 4°C to prevent efflux of TAC Isocratic: 90% ACN contains 2 mM ammonium acetate/0.1% FA [M + NH4] + [123,124]
Lymphocyte isolated from 7 ml blood with Ficoll-Paque Plus solution. Reconstituted with PBS and extracted with 1-chlorobutan. Organic phase dried and reconstituted with MeOH containing 2 mmol/l ammonium acetate/0.1 % FA Column: Xterra C18 (Waters) TAC: m/z 821.6 > 768.5
IV: 25 μl Run time: NR IS: ASC
R: 74.8–86.7% LLOQ: 0.01 ng/ml/0.006 ng/106 PBMCs

TAC HTRs (n = 24) At 4°C to prevent efflux of TAC Gradient: H2O (A); MeOH (B) both contain 2 mM ammonium acetate/0.1% FA NR [119]
Lymphocyte isolated from 7 ml blood with BD Vacutainer® CPT™ Cell Preparation Tubes. Cells lysed with MeOH dried/reconstituted with MeOH and extracted with zinc sulfate 0.1 M: 1: 2.5 (v:v) Column: MassTrak TDM C18 (Waters)
IV: 20 μl Run time: NR
R: 97.2–103.4%. LLOQ: 12.5 pg/million PBMCs

Ammonium adduct: [M+NH4]+; ASC: Ascomycin; CsA: Cyclosporine A; CsA: CsC: Cyclosporine C; CsD: Cyclosporine; EVE: Everolimus; FA: Formic acid; HTR: Heart transplant recipient: Ion adduct [M + H7rsqb;+; IV: Injection volume: LTR: Liver transplant recipient: LgTR: Lung transplant recipient: MeOH: Methanol: NR: Not reported: PBS: Phosphate buffer solution: R: Recovery: RTR: Renal transplant recipient; TAC: Tacrolimus.