The Discovery of UK-390957: the Challenge of Targeting a Short Half-life, Rapid T SSRI - Accounts in Drug Discovery Case Studies in Medicinal Chemistry - page 161

Figure 7.9
Figure 7.10 Free drug levels of UK-390957 following oral dosing in man.
this polymorphic enzyme. While this prediction did not quite meet the target
that we had set, the overall profile of sulfonamide 63 (UK-390957) was com-
pelling enough for it to be selected for clinical development.
7.4.6 Clinical Data for UK-390957
UK-390957 successfully progressed to FIH studies and gave exposure in man
(Figure 7.10) that was linear with increasing dose from 1 to 20mg. A dose of
5mg UK-390957 exceeded the SRI IC 20 for approximately 10 h. The PK
parameters in man are very close to those predicted, with UK-390957 having