Lumateperone tosylate, A Selective and Concurrent Modulator of Serotonin, Dopamine, and Glutamate, in the Treatment of Schizophrenia

Abstract

This is a comprehensive review of the literature regarding the use of Lumateperone tosylate for schizophrenia. This review presents the background, evidence, and indications for the use of lumateperone tosylate in the treatment of schizophrenia. Recent FindingsSchizophrenia is a chronic mental health disorder that affects approximately 3.3 million people in the United States. Its symptoms, which must be present more than six months, are comprised of disorganized behavior and speech, a diminished capacity to comprehend reality, hearing voices unheard by others, seeing things unseen by others, delusions, decreased social commitment, and decreased motivation. The majority of these symptoms can be managed with antipsychotic medication. Lumateperone is a selective and concurrent modulator of serotonin, dopamine, and glutamate, which all mediate or modulate serious mental illness.

Anesthetic Concerns in Psychiatric Disease

“…This is a new second-generation antipsychotic FDA approved for the treatment of schizophrenia in 2019 and Bipolar depression in 2022 [137]. It works as a presynaptic partial agonist and post-synaptic antagonist at D2 receptors and has high affinity for serotonin receptors [138].…”

Differentiating the third generation of antipsychotics: a focus on lumateperone’s similarities and differences

“…Table 1 lists all current approved indications for these four agents. Lumateperone is approved for the treatment of schizophrenia in adults, and for depressive episodes associated with bipolar I or II disorder in adults as monotherapy or as adjunctive treatment to lithium or valproate (Maini et al , 2021; Titulaer et al , 2022).…”

“…Partial agonism at D 2 R, along with partial agonism at 5-HT 1A R, have been reported to be effective in treating anxiety, depressive symptoms, cognitive symptoms, and negative symptoms (Veznedaroglu et al , 2018). Lumateperone is the only medication of the four that acts as a full postsynaptic antagonist at the D 2 R (Blair, 2020; Maini et al , 2021). Even though lumateperone has the weakest affinity for D 2 R, it demonstrates comparable antipsychotic activity at relatively low D 2 R occupancy to other atypical antipsychotics (e.g.…”

“…Lumateperone currently is only available in capsule form; however, a LAI formulation for schizophrenia is being researched (Blair, 2020; Maini et al , 2021; Therapies, 2021). The capsule is available in 10.5 mg, 21 mg, and 42 mg (equivalent to lumateperone tosylate 60 mg).…”

“…No titration dose is required. Lumateperone is highly metabolized by the liver, yielding 20 metabolites through multiple enzymes, including CYP3A4, CYP2C8, CYP1A2, UGT1A1, UGT1A4, UGT2B15, aldo-keto reductase (AKR)1C1, AKRB10, and AKR1C4 (Blair, 2020; Maini et al , 2021). Concomitant administration of lumateperone with CYP3A4 inducers should be avoided, as it can decrease the exposure of lumateperone (Maini et al , 2021).…”