TABLE 1

Physicochemical properties of GSK drugs used in clinical DDI studies

DrugMol. Wt.ClogPpKaPredominant Ionized Form at pH 7.4Nominal BCS Class
GSK-14645.810.4Base4
GSK-24214.07.6Base4
GSK-36675.19.7Base4
GSK-43531.88.6Base1
GSK-53573.06.3Acid1
GSK-64562.54.08Neutral2
GSK-74783.20.12Neutral2
GSK-82563.67.7Base1
GSK-94915.77.9Base3
GSK-10a6175.67.13Neutral1
GSK-114724.18.4Base4
GSK-123825.86.7Acid2
GSK-134424.74.0Acid4
GSK-143273.23.5AcidNDb
GSK-154544.83.2Acid2
GSK-164483.14.5/9.5Zwitterion4
GSK-175786.84.3/8.2Zwitterion2
GSK-183731.97.04Neutral1
GSK-193710.74.5Acid1
GSK-20a2402.37.2Neutral1
GSK-214383.16.4Neutral2
GSK-224800.16.8Neutral3
GSK-236692.07.9Base4
GSK-244633.05.9/7.6Zwitterion2
GSK-253332.68.7Base2
GSK-266452.57.7Base4
  • ND, not determined.

  • a Structures for GSK-10 (casopitant) and GSK-20 (bupropion) are given in Fig. 4.

  • b Insufficient information available to assign a nominal BCS class.