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Plasma levels and binding potential of
flutamide and
bicalutamide during first week
Day
Total levels (ng/mL)
Free levels (ng/mL)
Ratios
Bicalutamide
Flutamidea
Bicalutamide
Flutamidea
Free
Binding potentialb
1
901
940
36.0
66
0.55
2.18
2
1613
1500
64.5
105
0.61
2.46
3
2345
1500
93.8
105
0.89
3.57
4
2969
1500
118.8
105
1.13
4.53
7
4259
1500
170.4
105
1.62
6.49
Notes: During first week of treatment. Dosages not provided. Footnotes: a = As
2-hydroxyflutamide (the
active form of flutamide). b = Assumes, on the basis of
ligand binding assays , that bicalutamide possesses 4-fold greater
affinity for the
androgen receptor than 2-hydroxyflutamide. Sources:
[1]
References
^ Blackledge GR (1996). "Clinical progress with a new antiandrogen, Casodex (bicalutamide)". Eur. Urol . 29 Suppl 2: 96–104.
doi :
10.1159/000473847 .
PMID
8717470 .