Peak ID

Mean Cmax (ng/mL)

Mean Cmax (µM)

% SB636406

Parent

118a

0.2

-

SB636406

N-dealkylation

6372

22.1

-

M3

N,N-debutylation

472

1.1

7.4%

M18

Oxidation

1062

2.1

17%

M19

Oxidation

<354

<0.7

<5.6%

M27 N, N-debutylation, O-demethylation, O-glucuronidation

<118

<0.2

<1.9%

M28

N-dealkylation,
O-demethylation,
O-sulfation

<118

<0.3

<1.9%

M59

N,N-debutylation, hydroxylation and
O-glucuronidation

236

0.4

3.7%

M65

Dehydrogenation and hydroxylation

<354

<0.7

<5.6%

M75

N,N-debutylation, oxidation to acid,
di-hydroxylation and
O-glucuronidation

236

0.4

3.7%

M76

O-demethylated M59

<118

<0.2

<1.9%

M77

N,N-debutylation, hydroxylation, oxidation
to acid and glucuronidation

118

0.2

1.9%

M78

O-demethylated M77

236

0.4

3.7%

M79

Oxidation

<118

<0.2

<1.9%

M80

Amide hydrolysis,
O-demethylation

118

0.4

1.9%

M81

N-dealkylation and hydroxylation

<118

<0.4

<1.9%


aClinical Cmax
Table 3: Mean Maximum Concentration Estimates of Metabolites Identified in Pooled Human Plasma Extracts at Steady State and Their Percentages Relative to Metabolite SB636406.