TABLE 2.

Pharmacokinetic proprieties of cariprazine.

Pharmacokinetic	Drug information
Absorption	Following multiple-dose administration, peak plasma concentrations for cariprazine and the major active metabolites occur at approximately 3–8 h post dose
Distribution	Based on a population pharmacokinetic analysis, the apparent volume of distribution (V/F) was 916 L for cariprazine, 475 L for DCAR, and 1,568 L for DDCAR, indicating an extensive distribution of cariprazine and its major active metabolites. Cariprazine and its major active metabolites are highly bound (96–97% for CAR, 94–97% for DCAR, and 92–97% for DDCAR) to plasma proteins.
Metabolism	Cariprazine is metabolized by CYP3A4 and, to a lesser extent, by CYP2D6, to DCAR and HCAR. DCAR is further metabolized by CYP3A4 and to a lesser extent by CYP2D6 to DDCAR and HDCAR. DDCAR is further metabolized to HDDCAR by CYP3A4.
Elimination	Mainly through hepatic metabolism. Following administration of 12.5 mg/day cariprazine to patients with schizophrenia, 20.8% of the dose was excreted in urine as cariprazine and its metabolites. Unchanged cariprazine is excreted by 1.2% of the dose in urine and 3.7% of the dose in feces.

HCAR, hydroxy cariprazine; HDDCAR, hydroxy didesmethyl cariprazine.