Table 1.

Trough drug levels of PKC412 and of its active metabolite GCP62221 during therapy with PKC412 in patient UPN1


Day of treatment

PKC412 trough level, ng/mL

PKC412 trough level, nM*

CGP62221 trough level, ng/mL

CGP62221 trough level, nM*

Sum of trough levels of PKC412 and CGP62221*
0   0   0   0   0   0  
1   8950   157.0   313   5.6   162.6  
7   8660   151.9   4950   89.0   240.9  
28   1070   18.8   1360   24.5   43.3  
56   804   14.1   1190   21.4   35.5  
84   1230   21.6   1240   22.3   43.9  
119   815   14.3   1130   20.3   34.6  
148   1129   19.8   1171   21.1   40.9  
176   1547   27.1   1090   19.6   46.7  
288
 
707
 
12.4
 
1790
 
32.2
 
44.6
 

Day of treatment

PKC412 trough level, ng/mL

PKC412 trough level, nM*

CGP62221 trough level, ng/mL

CGP62221 trough level, nM*

Sum of trough levels of PKC412 and CGP62221*
0   0   0   0   0   0  
1   8950   157.0   313   5.6   162.6  
7   8660   151.9   4950   89.0   240.9  
28   1070   18.8   1360   24.5   43.3  
56   804   14.1   1190   21.4   35.5  
84   1230   21.6   1240   22.3   43.9  
119   815   14.3   1130   20.3   34.6  
148   1129   19.8   1171   21.1   40.9  
176   1547   27.1   1090   19.6   46.7  
288
 
707
 
12.4
 
1790
 
32.2
 
44.6
 
*

Corrected for 99% protein binding12 

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