Phase II glucuronide conjugates

Masitinib (MST) is an orally administered drug that targets mast cells and macrophages, important cells for immunity, by inhibiting a limited number of tyrosine kinases. It is currently registered in Europe and USA for the treatment of mast cell tumors in dogs.

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However, cellular uptake of aglycones has been suggested to occur in their native form by passive diffusion. Absorbed polyphenols can directly undergo phase II metabolism as phenolic structures are generally unfavorable substrates to the cytochrome P450s (phase I metabolism). At nutritional doses, almost all polyphenols are conjugated to form O- glucuronides, sulfate esters and O-methyl ethers, by glucuronidation, sulfation and methylation, in the gut mucosa and later in the liver or kidney.

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