Pharmacodynamics Both<unk>  and its active metabolite M19 block the NK1 receptor with high affinity and selectivity: to block the closely related receptor NK2 or any other of 115 tested receptors and enzymes, more than 1000-fold therapeutic concentrations are necessary. Pharmacokinetics The major active metabolite, M19 (C4-pyrrolidine-hydroxylated<unk> . The stereochemistry of the hydroxyl group is unknown.<unk>  is practically completely absorbed from the gut, independently of food intake. It undergoes no measurable first-pass effect in the liver. Highest blood plasma concentrations are reached after about four hours. When in the bloodstream, 99.8% of the substance are bound to plasma proteins. It is metabolized by the liver enzyme CYP3A4, resulting in the major active metabolite M19 (C4-pyrrolidine-hydroxylated<unk>  and a number of inactive metabolites.<unk>  is mainly excreted via the feces (52–89%) in unchanged form, and to a lesser extent via the urine (9–20%) in form of its inactive metabolites. Elimination half-life is about seven days (169 to 183 hours) over a wide dosing range.
Rolapitant
Ezlopitant
Terguride
Telmisartan
Isosorbide dinitrate
Mitapivat
Cobicistat
Eluxadoline