Peringatan Keamanan

Neonates exposed to antipsychotic drugs during the third trimester are at risk for extrapyramidal and/or withdrawal symptoms following delivery. Available data from case reports on lumateperone use in pregnant women are insufficient to establish any drug associated risks for birth defects, miscarriage, or adverse maternal or fetal outcomes. There are risks to the mother associated with untreated schizophrenia and with exposure to antipsychotics, including lumateperone, during pregnancy. In animal reproduction studies, no malformations were observed with oral administration of lumateperone to pregnant rats and rabbits during organogenesis at doses up to 2.4 and 9.7 times, respectively, the maximum recommended human dose (MRHD) of 42 mg/day on a mg/m2 basis. When pregnant rats were administered lumateperone during the period of organogenesis through lactation, the number of perinatal deaths of pups was increased at 4.9 times the MRHD, with no adverse effects on pups at 2.4 times the MRHD.L47171

Based on findings from animal studies, lumateperone may impair male and female fertility.L47171

No specific antidotes for CAPLYTA are known. In managing overdose, provide supportive care, including close medical supervision and monitoring and consider the possibility of multiple drug involvement. In case of overdose, consult a Certified Poison Control Center (1-800-222-1222 or www.poison.org).L47171

Lifetime carcinogenicity studies were conducted in rats and mice, and results showed no carcinogenic potential in either species. No evidence of mutagenic potential was found in the in vitro bacterial reverse mutation assay (Ames test) and the mouse lymphoma test without metabolic activation. Lumateperone was positive in the Ames test only in the presence of metabolic activation and only in the TA1537 strain and was positive in the mouse lymphoma test only in the presence of metabolic activation and only at high concentrations that inhibited cell growth; together these results were thought to be related to solubility limits and/or nonspecific effects on cellular function. Lumateperone was negative for clastogenic activity in the in vivo micronucleus assay in rats and was not genotoxic in the in vivo Comet assay in rats.L47171

Lumateperone

DB06077

small molecule approved investigational

Deskripsi

Schizophrenia is a complex mental illness and impacts approximately 1% of the population.L10902 Although there are several antipsychotics including aripiprazole, paliperidone and clozapine available for clinical use, they are generally accompanied by significant metabolic and/or neurological adverse effects.A189093

Lumateperone is a newly approved 2nd generation antipsychotic currently indicated for the treatment of schizophrenia.A189093 It has a unique receptor binding profile and differs from other antipsychotics in that it modulates glutamate, serotonin and dopamine, which are all neurotransmitters that contribute to the pathophysiology of schizophrenia.A189093,A189174

The data so far indicates that lumateperone can alleviate both positive and negative symptoms of schizophrenia.A189093 Further, not only is the new antipsychotic selective for dopamine (D2) receptors in the mesolimbic and mesocortical brain regions, but it also has minimal off-target activity.A189093 Both characteristics lend to a more favourable adverse effect profile and ultimately safer drug.A189093,L10908

Struktur Molekul 2D

Berat 393.506
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Lumateperone's half life is reported to be between 13 to 18 hours.[A189093,L10860] The reported half lives of the metabolites ICI200161 and ICI200131, are 20 and 21 hours respectively.[A189093]
Volume Distribusi The volume of distribution of lumateperone is approximately 4.1 L/Kg after intravenous administration.[L10860]
Klirens (Clearance) Lumateperone's clearance is estimated to be 27.9 L/hour.[L10860]

Absorpsi

Lumateperone is able to permeate multidrug resistance protein 1 (MDR1) and is very lipophilic at a pH of 7.4, which are characteristics that allow the antipsychotic to be absorbed in the small intestine and the blood brain barrier.A189093 Tmax occurs 3-4 hours after oral administration.A189093

Metabolisme

Lumateperone is extensively metabolized. The carbonyl side chain is reduced by ketone reductase to produce the primary active metabolite.A189093,A188991 Cytochrome P450 3A4 enzymes metabolize lumateperone to 2 metabolites: the active N-desmethylated carbonyl metabolite (IC200161) or the N-desmethylated alcohol metabolite (IC200565).A189093,A188991

Rute Eliminasi

Due to it's molecular weight, virtually all unchanged lumateperone is excreted in the feces.L10860,A189093 Lumateperone's metabolites are very water soluble which is a property that allows for complete elimination.A189093 Approximately 58% of a lumateperone dose can be recovered in the urine, while 29% can be recovered in the feces.L10860

Interaksi Makanan

3 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of lumateperone, which may increase its serum concentration.
  • 2. Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of lumateperone, causing a reduction in its serum concentration.
  • 3. Take with food. Administration with food reduces the Cmax by 33% and prolongs the Tmax by one hour.

Interaksi Obat

959 Data
Buprenorphine Lumateperone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Lumateperone.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Lumateperone.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Lumateperone.
Hydrocodone Lumateperone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Lumateperone.
Magnesium sulfate The therapeutic efficacy of Lumateperone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Lumateperone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Lumateperone may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Lumateperone.
Mirtazapine Lumateperone may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Lumateperone.
Orphenadrine Lumateperone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Lumateperone may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Rotigotine Lumateperone may increase the sedative activities of Rotigotine.
Sodium oxybate Lumateperone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Lumateperone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Lumateperone.
Thalidomide Lumateperone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Lumateperone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Amisulpride Lumateperone may increase the antipsychotic activities of Amisulpride.
Methylphenidate The risk or severity of adverse effects can be increased when Lumateperone is combined with Methylphenidate.
Dexmethylphenidate The risk or severity of adverse effects can be increased when Lumateperone is combined with Dexmethylphenidate.
Metoclopramide The risk or severity of adverse effects can be increased when Metoclopramide is combined with Lumateperone.
Quinagolide The therapeutic efficacy of Quinagolide can be decreased when used in combination with Lumateperone.
Sulpiride Lumateperone may increase the antipsychotic activities of Sulpiride.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Lumateperone.
Lithium citrate Lithium citrate may increase the neurotoxic activities of Lumateperone.
Lithium hydroxide Lithium hydroxide may increase the neurotoxic activities of Lumateperone.
Mequitazine Lumateperone may increase the arrhythmogenic activities of Mequitazine.
Desogestrel The metabolism of Lumateperone can be increased when combined with Desogestrel.
Zidovudine The metabolism of Lumateperone can be increased when combined with Zidovudine.
Ethinylestradiol The metabolism of Lumateperone can be increased when combined with Ethinylestradiol.
Testosterone propionate The metabolism of Lumateperone can be increased when combined with Testosterone propionate.
Tedizolid phosphate The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Lumateperone.
Ethanol Lumateperone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Lumateperone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Lumateperone.
Citalopram The risk or severity of adverse effects can be increased when Lumateperone is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Lumateperone is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Lumateperone is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Lumateperone is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Lumateperone is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Lumateperone is combined with Sibutramine.
Escitalopram The risk or severity of adverse effects can be increased when Lumateperone is combined with Escitalopram.
Dapoxetine The risk or severity of adverse effects can be increased when Lumateperone is combined with Dapoxetine.
Levomilnacipran The risk or severity of adverse effects can be increased when Levomilnacipran is combined with Lumateperone.
Ritanserin The risk or severity of adverse effects can be increased when Lumateperone is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Lumateperone is combined with Alaproclate.
Carbidopa The therapeutic efficacy of Carbidopa can be decreased when used in combination with Lumateperone.
Cabergoline The therapeutic efficacy of Cabergoline can be decreased when used in combination with Lumateperone.
Tolcapone The therapeutic efficacy of Tolcapone can be decreased when used in combination with Lumateperone.
Metixene The therapeutic efficacy of Metixene can be decreased when used in combination with Lumateperone.
Trihexyphenidyl The therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Lumateperone.
Procyclidine The therapeutic efficacy of Procyclidine can be decreased when used in combination with Lumateperone.
Profenamine The therapeutic efficacy of Profenamine can be decreased when used in combination with Lumateperone.
Entacapone The therapeutic efficacy of Entacapone can be decreased when used in combination with Lumateperone.
Lisuride The therapeutic efficacy of Lisuride can be decreased when used in combination with Lumateperone.
Apomorphine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Lumateperone.
Biperiden The therapeutic efficacy of Biperiden can be decreased when used in combination with Lumateperone.
Progabide The therapeutic efficacy of Progabide can be decreased when used in combination with Lumateperone.
Amantadine The therapeutic efficacy of Amantadine can be decreased when used in combination with Lumateperone.
Selegiline The therapeutic efficacy of Selegiline can be decreased when used in combination with Lumateperone.
Memantine The therapeutic efficacy of Memantine can be decreased when used in combination with Lumateperone.
Pergolide The therapeutic efficacy of Pergolide can be decreased when used in combination with Lumateperone.
Bromocriptine The therapeutic efficacy of Bromocriptine can be decreased when used in combination with Lumateperone.
Levodopa The therapeutic efficacy of Levodopa can be decreased when used in combination with Lumateperone.
Rasagiline The therapeutic efficacy of Rasagiline can be decreased when used in combination with Lumateperone.
3,5-Dinitrocatechol The therapeutic efficacy of 3,5-Dinitrocatechol can be decreased when used in combination with Lumateperone.
Etilevodopa The therapeutic efficacy of Etilevodopa can be decreased when used in combination with Lumateperone.
Safinamide The therapeutic efficacy of Safinamide can be decreased when used in combination with Lumateperone.
Ifenprodil The therapeutic efficacy of Ifenprodil can be decreased when used in combination with Lumateperone.
Dexetimide The therapeutic efficacy of Dexetimide can be decreased when used in combination with Lumateperone.
Opicapone The therapeutic efficacy of Opicapone can be decreased when used in combination with Lumateperone.
Piribedil The therapeutic efficacy of Piribedil can be decreased when used in combination with Lumateperone.
Benserazide The therapeutic efficacy of Benserazide can be decreased when used in combination with Lumateperone.
Tropatepine The therapeutic efficacy of Tropatepine can be decreased when used in combination with Lumateperone.
Melevodopa The therapeutic efficacy of Melevodopa can be decreased when used in combination with Lumateperone.
Dihydroergocryptine The therapeutic efficacy of Dihydroergocryptine can be decreased when used in combination with Lumateperone.
Phenglutarimide The therapeutic efficacy of Phenglutarimide can be decreased when used in combination with Lumateperone.
Mazaticol The therapeutic efficacy of Mazaticol can be decreased when used in combination with Lumateperone.
Etybenzatropine The therapeutic efficacy of Etybenzatropine can be decreased when used in combination with Lumateperone.
Budipine The therapeutic efficacy of Budipine can be decreased when used in combination with Lumateperone.
Bornaprine The therapeutic efficacy of Bornaprine can be decreased when used in combination with Lumateperone.
Etanautine The therapeutic efficacy of Etanautine can be decreased when used in combination with Lumateperone.
Dexpramipexole The therapeutic efficacy of Dexpramipexole can be decreased when used in combination with Lumateperone.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Lumateperone.
Imipramine The risk or severity of adverse effects can be increased when Imipramine is combined with Lumateperone.
Nortriptyline The risk or severity of adverse effects can be increased when Nortriptyline is combined with Lumateperone.
Amoxapine The risk or severity of adverse effects can be increased when Amoxapine is combined with Lumateperone.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Lumateperone.
Maprotiline The risk or severity of adverse effects can be increased when Maprotiline is combined with Lumateperone.
Doxepin The risk or severity of adverse effects can be increased when Doxepin is combined with Lumateperone.
Desipramine The risk or severity of adverse effects can be increased when Desipramine is combined with Lumateperone.
Pizotifen The risk or severity of CNS depression can be increased when Lumateperone is combined with Pizotifen.
Dosulepin The risk or severity of adverse effects can be increased when Dosulepin is combined with Lumateperone.
Zopiclone The risk or severity of adverse effects can be increased when Lumateperone is combined with Zopiclone.
Eletriptan The risk or severity of adverse effects can be increased when Eletriptan is combined with Lumateperone.
Zolmitriptan The risk or severity of adverse effects can be increased when Zolmitriptan is combined with Lumateperone.
Dihydroergotamine The risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Lumateperone.

Target Protein

Sodium-dependent serotonin transporter SLC6A4
5-hydroxytryptamine receptor 2A HTR2A
D(2) dopamine receptor DRD2
D(1A) dopamine receptor DRD1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 31790322
    Vyas P, Hwang BJ, Brasic JR: An evaluation of lumateperone tosylate for the treatment of schizophrenia. Expert Opin Pharmacother. 2019 Nov 30:1-7. doi: 10.1080/14656566.2019.1695778.
  • PMID: 24904434
    Brisch R, Saniotis A, Wolf R, Bielau H, Bernstein HG, Steiner J, Bogerts B, Braun K, Jankowski Z, Kumaratilake J, Henneberg M, Gos T: The role of dopamine in schizophrenia from a neurobiological and evolutionary perspective: old fashioned, but still in vogue. Front Psychiatry. 2014 May 19;5:47. doi: 10.3389/fpsyt.2014.00047. eCollection 2014.
  • PMID: 30449883
    Vanover KE, Davis RE, Zhou Y, Ye W, Brasic JR, Gapasin L, Saillard J, Weingart M, Litman RE, Mates S, Wong DF: Dopamine D2 receptor occupancy of lumateperone (ITI-007): a Positron Emission Tomography Study in patients with schizophrenia. Neuropsychopharmacology. 2019 Feb;44(3):598-605. doi: 10.1038/s41386-018-0251-1. Epub 2018 Oct 26.
  • PMID: 30596390
    Kumar B, Kuhad A, Kuhad A: Lumateperone: a new treatment approach for neuropsychiatric disorders. Drugs Today (Barc). 2018 Dec;54(12):713-719. doi: 10.1358/dot.2018.54.12.2899443.
  • PMID: 29559781
    Ceskova E, Silhan P: Novel treatment options in depression and psychosis. Neuropsychiatr Dis Treat. 2018 Mar 13;14:741-747. doi: 10.2147/NDT.S157475. eCollection 2018.

Contoh Produk & Brand

Produk: 4 • International brands: 0
Produk
  • Caplyta
    Capsule • 21 mg/1 • Oral • US • Approved
  • Caplyta
    Capsule • 10.5 mg/1 • Oral • US • Approved
  • Caplyta
    Capsule • 42 mg/1 • Oral • US • Approved
  • Caplyta
    Capsule • 42 mg/1 • Oral • US • Approved

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