Table 1

Characteristics of drugs and mean IC-50 values (± standard deviation)

Mean IC-50 for TNF-α inhibition


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


van der Heijden et al. Arthritis Research & Therapy 2005 7(Suppl 1):P84   doi:10.1186/ar1605