Investigational dopamine antagonists for the treatment of schizophrenia

Sheng Min Wang, Changsu Han, Soo Jung Lee, Tae Youn Jun, Ashwin A. Patkar, Prakash S. Masand, Chi Un Pae

    Research output: Contribution to journalReview articlepeer-review

    12 Citations (Scopus)


    Introduction: Schizophrenia is a debilitating illness with a chronic impact on social function and daily living. Although various antipsychotics are available, there are still many challenges and unmet needs. Thus, many compounds with diverse mechanisms have been investigated, but all approved antipsychotics still require interactions with dopamine D2 receptors. Areas covered: We searched for investigational drugs using the key words ‘dopamine’ and ‘schizophrenia’ in American and European clinical trial registers (; Published articles were searched in PubMed, Embase, Medline, PsycINFO, Cumulative Index to Nursing and Allied Health Literature (CINAHL), the Web of Science and the Cochrane Central Register of Controlled Trials Library. Expert opinion: The prospect of developing a dopamine antagonist is hopeful. Brexpiprazole and cariprazine, which were agents listed as ‘investigational dopamine antagonists,’ just received FDA approval. Novel agents such as BL 1020, ITI-007, and JNJ-37822681 have solid published data available, and agents such as L-THP, Lu AF35700, S33138, and SB-773812 are under vigorous investigation. However, the expected benefits of the newly developed antagonists may not be great because they offer little enhanced efficacy for negative symptoms, cognition and functional outcomes.

    Original languageEnglish
    Pages (from-to)687-698
    Number of pages12
    JournalExpert Opinion on Investigational Drugs
    Issue number6
    Publication statusPublished - 2017 Jun 3


    • Investigational antipsychotics
    • Phase II
    • Schizophrenia
    • agonist
    • antagonist
    • dopamine

    ASJC Scopus subject areas

    • Pharmacology
    • Pharmacology (medical)


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