Table 1 |
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|
Characteristics of drugs and mean IC-50 values (± standard deviation) |
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|
Mean IC-50 for TNF-α inhibition |
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|
|
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|
Drug |
Target |
Reduced folate carrier affinity (cell uptake) |
Folylpolyglutamate synthetase affinity (cell retention) |
Rheumatoid arthritis patients (n = 11) |
Controls (n = 6) |
|
|
|||||
|
MTX |
DHFR |
++ |
+ |
78 (77) nM |
57 (27) nM |
|
PT523 |
DHFR |
+++ |
- |
5.8 (3.2) nM |
6.4 (8.3) nM |
|
ZD1694 |
TS |
+++ |
+++ |
16 (26) nM |
4.8 (3.0) nM |
|
SSZ |
NF-κB |
- |
- |
278 (216) μM |
191 (29) μM |
|
|
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|
van der Heijden et al. Arthritis Research & Therapy 2005 7(Suppl 1):P84 doi:10.1186/ar1605 |
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