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N-glucuronidation: the human element

Metabolite Tales Blog

The pyrazole in a drug compound developed by LEO as an oral IL-17A protein-protein interaction modulator for the treatment of psoriasis and other inflammatory disorders is susceptible to N -glucuronidation. A route to be avoided or a desired route of metabolism? Tukey, Ryoichi Fujiwara. PMID: 9733662. [8] Antimicrob Agents Chemother.

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Metabolism of 2022 FDA approved small molecule drugs PART 2

Metabolite Tales Blog

3 Metabolism differences at steady state Adagrasib, Mirati’s irreversible KRASG12C inhibitor for treatment of non-small cell lung cancer is mainly metabolised by CYP3A4. Interestingly however, since adagrasib (MRTX849) inhibits CYP3A4 following multiple dosing, its metabolism is subsequently taken over by other CYPs.