Cariprazine as a therapeutic option for schizophrenia: a drug evaluation

ABSTRACT

Introduction: Schizophrenia is a very disabling condition that may result in a significant impairment of individual, professional, and social adjustments. Antipsychotics (APs), the first-line treatment for schizophrenia, in many cases modify the course of the disease, by reducing the institutionalization risk, at the price of severe and invalidating side effects. Cariprazine is one of the latest second-generation APs (SGAs) acting as a partial agonist of type 2 and 3 dopamine receptors, which was recently approved for the treatment of adult schizophrenia.

Areas covered: The authors provide a critical review and commentary on the currently available data on the effectiveness and tolerability of cariprazine in schizophrenic patients, with a particular focus on its specific target symptoms.

Expert opinion: Cariprazine appears significantly effective on both acute and maintenance treatment of schizophrenia, and in improving positive, negative, and cognitive symptoms, slightly more than other SGAs. It shows a good safety and tolerability profile, with akathisia being its most common side effect. Although further independent studies are needed to clarify its precise advantages over other SGAs, cariprazine seems a promising compound not only in schizophrenia, but also in a broad range of psychiatric conditions, including perhaps bipolar and addictive disorders.

KEYWORDS:

• Schizophrenia
• psychosis
• negative symptoms
• antipsychotics
• second-generation antipsychotics
• cariprazine
• partial agonism
• dopamine receptors

Box 1. Drug Summary Box:

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Article highlights

• Cariprazine is a second-generation antipsychotic (SGA) currently approved for the treatment of schizophrenia, being also effective in the management of acute mania and bipolar depression.

• Cariprazine behaves as a D3 and D2 receptor partial agonist, or antagonist depending on the endogenous dopamine level, with a higher selectivity for D3.

• Available data show that cariprazine exerts its effectiveness not only on positive, but also on negative and cognitive symptoms of schizophrenia.

• As compared with older SGAs, cariprazine seems to be well-tolerated with a significantly lower incidence of weight gain, onset of metabolic syndrome and extra-pyramidal symptoms, with the notable exception of akathisia.

• Most (if not all) available clinical trials were sponsored and funded by the manufacturer, therefore, more independent controlled and long-term studies, carried out in larger samples of “real life patients” and in “special populations”, appear necessary to better clarify and, perhaps broaden the clinical potentials and the specificities of cariprazine.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer Disclosures

One reviewer declares employment with Gedeon Richter Plc, the company that discovered and manufactures cariprazine. Peer reviewers on this manuscript have no other relevant financial relationships or otherwise to disclose.