Clinical pharmacology study of cariprazine (MP-214) in patients with schizophrenia (12-week treatment).

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Nakamura T, Kubota T, Iwakaji A, Imada M, Kapas M, Morio Y

Clinical pharmacology study of cariprazine (MP-214) in patients with schizophrenia (12-week treatment).

Drug Des Devel Ther. 2016 Jan 14;10:327-38. doi: 10.2147/DDDT.S95100. eCollection 2016.

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26834462 [ View in PubMed
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Abstract

PURPOSE: Cariprazine is a potent dopamine D3-preferring D3/D2 receptor partial agonist in development for the treatment of schizophrenia, bipolar mania, and depression. Pharmacokinetics of cariprazine and the two clinically relevant metabolites (desmethyl- and didesmethyl-cariprazine) was evaluated in a clinical pharmacology study. METHODS: This was a multicenter, randomized, open-label, parallel-group, fixed-dose (3, 6, or 9 mg/day) study of 28-week duration (90% within 1 week after the last dose, didesmethyl-cariprazine decreased ~50% at 1 week, and total active moieties decreased ~90% within 4 weeks. Terminal half-lives of cariprazine, desmethyl-cariprazine, and didesmethyl-cariprazine ranged from 31.6 to 68.4, 29.7 to 37.5, and 314 to 446 hours, respectively. Effective half-life (calculated from time to steady state) of total active moieties was ~1 week. Incidence of treatment-emergent adverse events was 97.4%; 15.8% of patients discontinued due to adverse events. No abnormal laboratory values or major differences from baseline in extrapyramidal symptoms were observed. CONCLUSION: Cariprazine and its active metabolites reached steady state within 4 weeks, and exposure was dose proportional over the range of 3-9 mg/day. Once-daily cariprazine was generally well tolerated in adult patients with schizophrenia.

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