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karl2100: ½ð±Ò+1, лл£¡ 2012-11-21 00:25:17
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¹¾ß˲»¶¯: ½ð±Ò+1, ¡ïÓаïÖú 2012-11-28 20:40:23
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PSA: ½ð±Ò+1, ²»´í£¬·Ç³£¸Ðл£¡ 2012-11-28 10:32:08
¹¾ß˲»¶¯: ½ð±Ò+3, ¡ï¡ï¡ïºÜÓаïÖú 2012-11-28 20:40:45
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http://www.fda.gov/drugs/develop ... eling/ucm093664.htm

P-gp Transporters

Table 8. Acceptable In Vitro P-gp Substrates * (5/1/2006)

    Ratio**
Drug Conc. Used
(µM) Caco-2 MDR1-
MDCK*** MDR1-
LLCPK***
Digoxin 0.01-10 4-14 4 4
Loperamide 1-10 2-5   3.4

Table 9. In Vitro P-gp Inhibitors * (5/1/2006)



Inhibitor  
IC50 (µM) Ki (µM)
Caco-2*
  Caco-2*
  MDCK-
MDR1*



LLC-PK1
MDR1**




Cyclosporine A a 1.3 0.5 2.2 1.3
Ketoconazole a 1.2     5.3
LY335979 0.024      
Nelfinavir a 1.4      
Quinidine b 2.2 3.2 8.6   
Ritonavir a 3.8      
Saquinavir a 6.5      
Tacrolimus 0.74      
Valspodar (PSC833) 0.11      
Verapamil 2.1 8 15 23
Elacridar
(GF120918)
(GG 918)   0.4 0.4   
Reserpine   1.4 11.5   

Quinidine 0.05 3   5
Vinblastine a 0.004-10 2-18 > 9 b 3
Talinolol 30 26
3Â¥2012-11-27 05:11:54
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3Â¥: Originally posted by bigpalewolf at 2012-11-27 05:11:54
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http://www.fda.gov/drugs/developmentapprovalprocess/developmentresources/druginteractionslabeling/ucm093664.htm

P-gp Transporters

Table 8. Acceptable In Vitro P-gp Substrates * (5/1/2 ...

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