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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 5.

Published LC–MS/MS assays for quantification of immunosuppressive drugs in biopsies from transplanted organs.

Drug Subjects Extraction/Injection volume/Recovery Correlation blood vs tissue Chromatographic conditions Precursor ion (m/z) > production (m/z Ref.
CsA RTRs (n = 21) Tissues solubilized in digestion buffer (Proteinase K solution in a tissue lysis (ATL)buffer) at 56°C/2 h Precipitate with 0.4 M zinc sulfate: MeOH, 20:80 (v:v) r = 0.168, Gradient: (A): 50% MeOH, MeOH (B), both contain 2 mM ammonium acetate/0.1% FA [M + NH4]+ [143]
IV: 25 μl p = 0.53 Online cleaning: POROS R1/20 CsA: 1220.0 > 1203.0
R: NR Column: Luna Phenyl-Hexyl (Phenomenex) IS: labeled CsA
Run time: 5.5 min
LLOQ: 1 ng/ml

CsA Biopsies (n = 19) from 7 HTRs Tissues homogenized with water and mixed with two parts of ACN:MeOH: H2O (1:1:3, v:v:v). Precipitation with ACN. The organic phase was dried and reconstituted with MPs A:B, 65:35 (v:v) NR Gradient: 20% ACN (A), 80% ACN (B), both contain 20 mM ammonium format [M + H]+ [118]
IV: 20 μl Column: (Acquity) UPLC C18 (Waters) CsA: 1203.7 > 1101.7/1185.7
R: NR Run time: 36 min IS: CsC
LLOQ: 0.25 ng/ml

MPA Biopsies (n = 4) from 4 RTRs Tissues grounded to a fine powder and reconstituted with PBS (pH 7.4). Add 60 μl of HCl (0.4 M) and 1 ml of tertiary-butyl methyl ether. Evaporate/reconstitute with 1:1 (v:v) MeOH: H2O. NR Gradient: H20 (A), and MeOH (B), both containing 2 mM ammonium acetate/0.1% formic acid [M + H]+. [145]
IV: NR Column: Luna Phenyl-Hexyl (Phenomenex) MPA: 321.1 > 207.3
R: 97% Run time: 2.2 min IS: N-phthaloyl-l-phenylalanine
LLOQ: 0.6 ng/ml

TAC Biopsies (NR) from 90 and 146 LTRs Tissues homogenized PBS (0.1 mol/l, pH = 6.5 Extracted with MeOH/ethyl acetate, dried and reconstituted with MeOH. Banff score Isocratic: 70% MeOH (B) containing 2 mM ammonium acetate/0.1% FA [M + NH4] + [123,142]
IV: 20 μl (r2 =0.984, p = 0.002) Column: C18 cartridge, (Phenomenex) TAC: 822 > 768
R: 75.3-83.1% Run time: 1.5 min IS: ASC
LLOQ: 5 pg/mg

TAC Biopsies (n = 6) from 2 RTRs Tissues solubilized in digestion buffer. Mix with 7 μl of IS + 300 μl water+1 ml of tert-butyl methyl ether in glass tube. Organic phase evaporated and reconstituted in 50:50 MeOH: H2O NR Gradient: H2O (A) and MeOH (B) both contain 2 mM ammonium acetate/0.1% FA [M + NH4] + [144]
IV: 25 μl Column: Luna Phenyl-Hexyl (Phenomenex) TAC: 821.5 > 768.6
R: 70% Run time: 2 min IS: ASC
LLOQ: 0.04 ng/ml

Ammonium adduct: [M+NH4]+; ACN: Acetonitrile; ASC: Ascomycin; CsA: Cyclosporine A; CsA: Cyclosporine C; EVE: Everolimus; FA: Formic acid; HTRs: Heart transplant recipients: IV: Injection volume: Ion adduct [M + H]+: LTRs: Liver transplant recipients: LLOQ: Lower limit of quantification: MeOH: Methanol: MPA: Mycophenolic acid: NR: Not reported: PBS: Phosphate buffer solution: R: Recovery: RTRs: Renal transplant recipients: SPE: Solid-phase extraction: TAC: Tacrolimus.