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Chemical Characteristic

Product NameAprepitant
CAS No.170729-80-3
Molecular Weight 534.43
FormulaC23H21F7N4O3
Chemical Structure

Biological activities

Aprepitant is an orally available and selective neurokinin-1 receptor antagonist. In vitro, Aprepitant also was a moderate inhibitor of CYP3A4, and can inhibit CYP3A4 enzyme activity [1]. The clinical use of aprepitant in patients receiving multiple doses of CR oxycodone for cancer pain significantly altered plasma concentration levels, but would not appear to need modification of the CR oxycodone dose [2].

References

[1] Sanchez RI, Wang RW, Newton DJ, et al. Cytochrome P450 3A4 is the major enzyme involved in the metabolism of the substance Preceptor antagonist aprepitant. Drug Metab Dispos. 2004, 32: 1287閳?292.
[2] Fujiwara Y, Toyoda M, Chayahara N, et al. Effects of aprepitant on the pharmacokinetics of controlled-release oral oxycodone in cancer patients. PLoS One. 2014,9(8):e104215.

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