Table 2.

Range of In Situ TSI50 Values for Novel Antifolates in Clinical Leukemia Samples and Plasma Levels Obtained in Phase I/II Clinical Trials

TSIcont (μmol/L) TSIshort (μmol/L) Plasma Levels Trial Reference
MTX 0.01-0.78  <0.16 − >40.0  25 μmol/L  Children Evans et al49 
TMQ  <0.0016-0.16 <0.08-14.3  7 μmol/L  Children  Hum et al45 
GW1843  <0.00025-0.047  <0.0010 >0.63  3 μmol/L  Adults  Burris et al50 
MTA  <0.039 − >10.0  <0.039 − >10.0 300 μmol/L  Adults  Rinaldi51 
Raltitrexed 0.0014-0.092  0.0043 − >0.32  3 μmol/L  Children Widemann et al46 
ZD9331  0.0016-0.19 0.9 − >25.0  No data published 
TSIcont (μmol/L) TSIshort (μmol/L) Plasma Levels Trial Reference
MTX 0.01-0.78  <0.16 − >40.0  25 μmol/L  Children Evans et al49 
TMQ  <0.0016-0.16 <0.08-14.3  7 μmol/L  Children  Hum et al45 
GW1843  <0.00025-0.047  <0.0010 >0.63  3 μmol/L  Adults  Burris et al50 
MTA  <0.039 − >10.0  <0.039 − >10.0 300 μmol/L  Adults  Rinaldi51 
Raltitrexed 0.0014-0.092  0.0043 − >0.32  3 μmol/L  Children Widemann et al46 
ZD9331  0.0016-0.19 0.9 − >25.0  No data published 

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