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24 ADME-Tox & PK 2011 catalog❚ In vitro ADME [drug absorption/drug transport] - A-B / B-A permeabilityA-B permeability (MDCKII, pH 7.4/7.4)Ref. 1805Q 2 weeksSourceMDCKII cell lineTest concentration 10 µMIncubation 0 and 60 min/37°CDetection method HPLC-MS/MSReference colchicine, labetalol, propranolol, ranitidineIrvine, J.D. et al.(1999) J. Pharm. Sci., 88: 28-33. A-B permeability (MDR1-MDCKII, pH 7.4/7.4)Ref. 1809Ref. 2081 (+ verapamil)Q 2 weeksSourceTest concentration 10 µMMDR1-MDCKII cell lineIncubation 0 and 60 min/37°CDetection method HPLC-MS/MSReferencecolchicine, labetalol, propranolol, ranitidineHorio, M. et al.(1989) J. Biol. Chem., 264: 14880-14884. B-A permeability (Caco-2, pH 6.5/7.4)Ref. 3320Q 2 weeksIncluded in: BioPrint ® profileSourceTest concentration 10 µMCaco-2 cell lineIncubation 0 and 40 min/37°CDetection method HPLC-MS/MSReferencepropranolol, labetalol, colchicine, ranitidineHidalgo, I.J. et al.(1989) Gastroenterology, 96: 736-749. B-A permeability (Caco-2, pH 7.4/7.4) - verapamil + verapamilRef. 3321Ref. 3326 (+ verapamil)Q 2 weeksSourceCaco-2 cell lineTest concentration 10 µMIncubation 0 and 40 min/37°CDetection method HPLC-MS/MSReference propranolol, labetalol, colchicine, ranitidineHidalgo, I.J. et al.(1989) Gastroenterology, 96: 736-749. B-A permeability (MDCKII, pH 7.4/7.4)Ref. 1806Q 2 weeksSourceMDCKII cell lineTest concentration 10 µMIncubation 0 and 40 min/37°CDetection method HPLC-MS/MSReference colchicine, labetalol, propranolol, ranitidineIrvine, J.D. et al.(1999) J. Pharm. Sci., 88: 28-33. B-A permeability (MDR1-MDCKII, pH 7.4/7.4)SourceMDR1-MDCKII cell lineTest concentration 10 µMIncubation 0 and 40 min/37°CDetection method HPLC-MS/MSRef. 1810Ref. 2082 (+ verapamil) Reference colchicine, labetalol, propranolol, ranitidineQ 2 weeksHorio, M. et al.(1989) J. Biol. Chem., 264: 14880-14884. ■■
25❚ p-glycoprotein interactionsP-gp substrate assessment - Option I (Caco-2, 96-well)Ref. G206Q 2 weeksSourceCaco-2 cell lineTest concentration 10 µMDetection method HPLC-MS/MS❚ A-B permeability (Caco-2, pH 7.4/7.4) ± 100 µM verapamil❚ B-A permeability (Caco-2, pH 7.4/7.4) ± 100 µM verapamilHidalgo, I.J et al.(1989) Gastroenterology, 96: 736-749.P-gp substrate assessment - Option II (MDR1-MDCKII, 96-well)Ref. G207Q 2 weeksSourceMDR1-MDCKII and MDCKII cell linesTest concentration 10 µMDetection method HPLC-MS/MS❚ A-B / B-A permeability (MDR1-MDCKII, pH 7.4/7.4) ± 100 µM verapamil❚ A-B / B-A permeability (MDCKII, pH 7.4/7.4)Horio, M. et al.(1989) J. Biol. Chem., 264: 14880-14884.P-gp substrate evaluation (Caco-2, 24-well)fda draft guidanceRef. P21-m1Q 4 weeksSourceCaco-2 cell lineTest concentration 1 to 100 µMIncubation up to 3 hours/37°CDetection method HPLC-MS/MSReference colchicine, propranolol, ranitidine❚ Step I - Preliminary verification- A-B / B-A permeability (Caco-2, pH 7.4/7.4, multiple tps,24 w, calibration curve)- A-B permeability (blank filters, pH 7.4/7.4, 2 tps, 24 w, calibration curve)❚ Step II - Full evaluation- A-B / B-A permeability (Caco-2, pH 7.4/7.4, 2 tps, 24 w, calibration curve)- A-B / B-A permeability (Caco-2, pH 7.4/7.4, 2 tps, 24 w, + ketoconazole, calibration curve)- A-B / B-A permeability (Caco-2, pH 7.4/7.4, 2 tps, 24 w, + verapamil, calibration curve) FDA Guidance for Industry (2006) Drug Interaction Studies - Study Design, Data Analysis, and Implications for Dosing and Labeling■ A-B■ B-A<strong>Cerep</strong>servicesassayselectionguidein vitroADME[Drugabsorption/drugtransport]in vitrotoxicity P-gp inhibition (Caco-2, [ 3 H]-digoxin substrate)Ref. 3349Q 2 weeksIncluded in: BioPrint ® profileSourceTest concentration 10 µMCaco-2 cell lineIncubation 3 hours/37°CDetection method scintillation countingReferenceverapamil (IC 50 : 4.6 µM)Cavet, M.E. et al. (1996) Br.J. Pharmacol., 118:1389-1396. in vivo PK/bioanalyticalstandardprofilesP-gp inhibition (MDR1-MDCKII, calcein AM substrate)100Ref. 1324Q 2 weeksIncluded in: ADME-Tox Option II (Leadselection/Prioritization) profileSourceMDR1-MDCKII cell lineTest concentration 10 µMIncubation 30 min/37°CDetection method fluorimetryReferenceverapamil (IC 50 : 5.2 µM)Polli J. W. et al. (2001) J. Pharmacol. Experimt. Therap., 299 : 620-628P-gp activity (% of control)500-8 -7 -6 -5 -4log [drug] (M) verapamilapplicationnotesorderinginformationFor further details and updated information on assays:❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568 Assay developed in 2010 New assay conditions Human Human & other species Q Standard turnaround timeassay list& index
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