Compound Name | Major In Vivo Human Metabolites | Excreta | Circulating Radioactivitya | Biotransformation Phase | 1°/2° metabolite | Metabolites Detected in Matrix | ||
---|---|---|---|---|---|---|---|---|
Suspended Hepatocytesb | MPCCc Hepatocytesd | Hepatocyte Relay | ||||||
% | % | |||||||
Capromorelin | Nitrocapromoreline (A) | 11 | 14 | 1 | 2° | Yes | ||
O-desbenzyl hydroxycapromorelin (B) | 12 | 1 | 2° | Yes | Yes | |||
N-desmethyl-O-desbenzyl nitrocapromoreline (C) | 12 | 1 | 2° | Yes | ||||
N-desmethyl-O-desbenzyl hydroxycapromorelin (D) | 15 | 1 | 2° | Yes | Yes | |||
CP-122721 | Desmethyl O-glucuronide | 27 | 14 | 2 | 2° | Yes | Yes | Yes |
N-dealkylated, reduced O-glucuronide | 11 | 2 | 2° | |||||
Desmethylhydroxy O-glucuronide | 25 | 2 | 2° | Yes | ||||
5-trifluoromethoxysalicylic acid | 56 | 1 | 2° | Yesf | ||||
Ziprasidone | Sulfoxide | 18 | 69 | 1 | 1° | Yes | Yes | Yes |
S-methyldihydroziprasidone | 18 | 69 | 1 | 2° | Yes | Yes | Yes | |
N-dealkylated sulfoxide | 11 | 21 | 1 | 2° | Yes | |||
N-dealkylated sulfone | 11 | 21 | 1 | 2° | ||||
Celecoxib | Carboxylic acid | 73 | 20 | 1 | 2° | Yes | Yes | Yes |
Carboxylic acid glucuronide | 15 | 2 | 2° | Yes | Yes | Yes | ||
Linezolid | O-dealkylation/ring opening, carboxylic acid | 45 | 1 | 2° | Yes | Yes | ||
N-dealkylation/ring opening, carboxylic acid | 10 | 1 | 2° | Yes | Yes |
↵a Percentage of total drug-related material radioactivity in circulation.
↵b Dalvie et al., 2009.
↵c Micropatterned coculture hepatocytes (7-day incubation).
↵d Wang et al., 2010.
↵e Metabolites originally reported as carboxylic acids but later determined to be nitroalkanes (Pfizer internal communication).
↵f MS negative mode detection only.