What are the pharmacokinetic properties of TAK-285 and its metabolite M-I?

Label:chem

Topic
The pharmacokinetic (PK) properties of TAK-285 and its metabolite M-I were evaluated in a phase I first-in-human study. Understanding these properties is crucial for determining the drug's efficacy and safety profile.
Answer
TAK-285 and M-I were rapidly absorbed after oral administration, with plasma concentrations reaching maximum (Cmax) within 2.5 hours. The estimated terminal-phase half-life (t1/2) was 6–9 hours for TAK-285 and 7–10 hours for M-I. A dose-proportional increase in exposure was observed for TAK-285 at steady state over the dose range tested (50–300 mg b.i.d.), but not for M-I at 300 mg b.i.d. The accumulation ratios for Cmax and AUC were below 4.6 for both TAK-285 and M-I, indicating moderate accumulation. Urinary excretion of TAK-285 and M-I was negligible, suggesting that renal excretion does not significantly contribute to their clearance.
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