Lumateperone
Identification
- Summary
Lumateperone is a novel 2nd generation antipsychotic used to manage both positive and negative symptoms in patients with schizophrenia.
- Brand Names
- Caplyta
- Generic Name
- Lumateperone
- DrugBank Accession Number
- DB06077
- Background
Schizophrenia is a complex mental illness and impacts approximately 1% of the population.7 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.1
Lumateperone is a newly approved 2nd generation antipsychotic currently indicated for the treatment of schizophrenia.1 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.1,5
The data so far indicates that lumateperone can alleviate both positive and negative symptoms of schizophrenia.1 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.1 Both characteristics lend to a more favourable adverse effect profile and ultimately safer drug.1,8
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 393.506
Monoisotopic: 393.221640697 - Chemical Formula
- C24H28FN3O
- Synonyms
- Lumateperone
- External IDs
- ITI 007
- ITI-007
- ITI-722
- ITI007
Pharmacology
- Indication
Lumateperone is approved for the treatment of schizophrenia in adults.6 It is also approved for the treatment of depressive episodes associated with bipolar disorder (i.e. bipolar depression) in adults, as monotherapy and/or adjunctive therapy with lithium or valproate.6
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to manage Depressive episodes •••••••••••• ••••• ••••••• Used in combination to manage Depressive episodes Regimen in combination with: Valproic acid (DB00313) •••••••••••• ••••• ••••••• Used in combination to manage Depressive episodes •••••••••••• ••••• ••••••• Used in combination to manage Depressive episodes Regimen in combination with: Valproic acid (DB00313) •••••••••••• ••••• ••••••• Management of Depressive episodes •••••••••••• ••••• ••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Lumateperone, also known as ITI-007, is an atypical antipsychotic that has proven to be effective in the treatment of schizophrenia.1 Lumateperone's receptor binding profile is unique, allowing it to target schizophrenia related symptoms while minimizing adverse effects.1,5 In contrast to other second generation antipsychotics such as lurasidone and brexpiprazole, lumateperone behaves as a partial agonist and as an antagonist at pre and postynaptic dopamine (D2) receptors respectively.1
Patients with moderate or severe hepatic impairment (Child-Pugh class B or C) tend to have higher plasma concentrations of lumateperone than those with normal hepatic function. For this reason, patients with moderate or severe hepatic impairment should receive half the recommended daily dosage.6
- Mechanism of action
There is much to learn about the pathophysiology of schizophrenia; however, dopamine abnormalities, specifically in the prefrontal and mesolimbic brain regions, are consistent in people with schizophrenia.2 In addition to dopamine, other neurotransmitters such as serotonin, glutamate, GABA and acetylcholine are thought to play a role.2
Lumateperone is unique among second generation antipsychotics based on its target profile and dopamine D2 receptor occupancy.1,3 Unlike other antipsychotics, lumateperone has partial agonist activity at presynaptic dopamine (D2) receptors, resulting in reduced presynaptic release of dopamine, and antagonistic activity at postsynaptic dopamine (D2) receptors.3 These characteristics allow lumateperone to efficiently reduce dopamine signaling.3
Lumateperone also targets dopamine (D1) receptors, and a useful secondary result of D1 activation is increased glutamatergic N-methyl-D-aspartate (NMDA) GluN2B receptor phosphorylation.1,3,4 This is significant since NMDA mediated glutamate signaling appears to be impaired in patients who have schizophrenia.1
Finally, lumateperone is capable of modulating serotonin by inhibiting serotonin transporters (SERT), and by behaving as a 5-HT2A receptor antagonist.3
Target Actions Organism ASodium-dependent serotonin transporter inhibitorHumans AGlutamate receptor ionotropic, NMDA 2B Not Available Humans A5-hydroxytryptamine receptor 2A antagonistHumans ADopamine D2 receptor partial agonistHumans UDopamine D1 receptor Not Available Humans - Absorption
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.1 Tmax occurs 3-4 hours after oral administration.1
- Volume of distribution
The volume of distribution of lumateperone is approximately 4.1 L/Kg after intravenous administration.6
- Protein binding
Lumateperone is approximately 97.4% plasma protein bound.1,6
- Metabolism
Lumateperone is extensively metabolized. The carbonyl side chain is reduced by ketone reductase to produce the primary active metabolite.1,3 Cytochrome P450 3A4 enzymes metabolize lumateperone to 2 metabolites: the active N-desmethylated carbonyl metabolite (IC200161) or the N-desmethylated alcohol metabolite (IC200565).1,3
Hover over products below to view reaction partners
- Route of elimination
Due to it's molecular weight, virtually all unchanged lumateperone is excreted in the feces.6,1 Lumateperone's metabolites are very water soluble which is a property that allows for complete elimination.1 Approximately 58% of a lumateperone dose can be recovered in the urine, while 29% can be recovered in the feces.6
- Half-life
Lumateperone's half life is reported to be between 13 to 18 hours.1,6 The reported half lives of the metabolites ICI200161 and ICI200131, are 20 and 21 hours respectively.1
- Clearance
Lumateperone's clearance is estimated to be 27.9 L/hour.6
- Adverse Effects
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- Toxicity
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.9
Based on findings from animal studies, lumateperone may impair male and female fertility.9
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).9
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.9
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Lumateperone is combined with 1,2-Benzodiazepine. Abametapir The serum concentration of Lumateperone can be increased when it is combined with Abametapir. Acetaminophen The serum concentration of Lumateperone can be decreased when it is combined with Acetaminophen. Acetazolamide The risk or severity of CNS depression can be increased when Acetazolamide is combined with Lumateperone. Acetophenazine The risk or severity of adverse effects can be increased when Lumateperone is combined with Acetophenazine. - Food Interactions
- Avoid grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of lumateperone, which may increase its serum concentration.
- Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of lumateperone, causing a reduction in its serum concentration.
- Take with food. Administration with food reduces the Cmax by 33% and prolongs the Tmax by one hour.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Lumateperone tosylate JIE88N006O 1187020-80-9 LHAPOGAFBLSJJQ-GUTACTQSSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Caplyta Capsule 21 mg/1 Oral Intra-Cellular Therapies, Inc 2022-08-09 Not applicable US Caplyta Capsule 42 mg/1 Oral REMEDYREPACK INC. 2022-08-24 Not applicable US Caplyta Capsule 42 mg/1 Oral Intra-Cellular Therapies, Inc 2020-02-01 Not applicable US Caplyta Capsule 10.5 mg/1 Oral Intra-Cellular Therapies, Inc 2022-08-09 Not applicable US
Categories
- ATC Codes
- N05AD10 — Lumateperone
- Drug Categories
- Antidepressive Agents
- Antipsychotic Agents
- Antipsychotic Agents (Second Generation [Atypical])
- Butyrophenone Derivatives
- Central Nervous System Depressants
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP2C8 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Dopamine Agonists
- Dopamine Antagonists
- Dopamine D2 Receptor Agonists
- Heterocyclic Compounds, Fused-Ring
- Nervous System
- Neurotoxic agents
- Psycholeptics
- Serotonin 5-HT2 Receptor Antagonists
- Serotonin 5-HT2A Receptor Antagonists
- Serotonin Agents
- Serotonin Modulators
- Serotonin Receptor Antagonists
- UGT1A1 Substrates
- UGT1A4 substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as alkyl-phenylketones. These are aromatic compounds containing a ketone substituted by one alkyl group, and a phenyl group.
- Kingdom
- Organic compounds
- Super Class
- Organic oxygen compounds
- Class
- Organooxygen compounds
- Sub Class
- Carbonyl compounds
- Direct Parent
- Alkyl-phenylketones
- Alternative Parents
- Phenylbutylamines / Butyrophenones / Indoles and derivatives / Aryl alkyl ketones / Benzoyl derivatives / Dialkylarylamines / Aralkylamines / Fluorobenzenes / Piperidines / Aryl fluorides show 7 more
- Substituents
- Alkyl-phenylketone / Amine / Aralkylamine / Aromatic heteropolycyclic compound / Aryl alkyl ketone / Aryl fluoride / Aryl halide / Azacycle / Benzenoid / Benzoyl show 20 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 70BSQ12069
- CAS number
- 313368-91-1
- InChI Key
- HOIIHACBCFLJET-SFTDATJTSA-N
- InChI
- InChI=1S/C24H28FN3O/c1-26-14-15-28-21-11-13-27(16-20(21)19-4-2-5-22(26)24(19)28)12-3-6-23(29)17-7-9-18(25)10-8-17/h2,4-5,7-10,20-21H,3,6,11-16H2,1H3/t20-,21-/m0/s1
- IUPAC Name
- 1-(4-fluorophenyl)-4-[(10R,15S)-4-methyl-1,4,12-triazatetracyclo[7.6.1.0^{5,16}.0^{10,15}]hexadeca-5(16),6,8-trien-12-yl]butan-1-one
- SMILES
- [H][C@]12CCN(CCCC(=O)C3=CC=C(F)C=C3)C[C@@]1([H])C1=CC=CC3=C1N2CCN3C
References
- General References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- FDA Approved Drug Products: Caplyta (lumateperone) capsules for oral use [Link]
- 24. The Clinical Development of Lumateperone (ITI-007) for the Treatment of Schizophrenia [Link]
- S44. Lumateperone (ITI-007) for the Treatment of Schizophrenia: Placebo-Controlled Clinical Trials and an Open-Label Safety Switching Study [Link]
- FDA Approved Drug Products: Caplyta (lumateperone) capsules for oral use (June 2023) [Link]
- External Links
- PubChem Compound
- 21302490
- PubChem Substance
- 310264860
- ChemSpider
- 19328801
- 2275602
- ChEMBL
- CHEMBL3306803
- ZINC
- ZINC000116262036
- PDBe Ligand
- 92S
- Wikipedia
- Lumateperone
- PDB Entries
- 7wc8
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Not Yet Recruiting Treatment Schizoaffective Disorders / Schizophrenia 1 4 Recruiting Other Psychosis 1 3 Completed Treatment Depression, Bipolar 3 3 Completed Treatment Depression, Bipolar / Major Depressive Disorder (MDD) 1 3 Completed Treatment Schizophrenia 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Oral 10.5 mg/1 Capsule Oral 21 mg/1 Capsule Oral 42 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US10464938 No 2019-11-05 2028-03-12 US US8648077 No 2014-02-11 2029-12-01 US US9616061 No 2017-04-11 2029-05-27 US US7183282 No 2007-02-27 2020-06-15 US US9586960 No 2017-03-07 2029-03-12 US US8598119 No 2013-12-03 2029-12-28 US USRE39680 No 2007-06-05 2020-06-15 US US9199995 No 2015-12-01 2029-03-12 US US9956227 No 2018-05-01 2034-12-03 US US10695345 No 2020-06-30 2039-08-30 US US10960009 No 2021-03-30 2034-12-03 US USRE48839 No 2021-12-07 2029-12-28 US USRE48825 No 2021-11-23 2029-03-12 US US10117867 No 2018-11-06 2029-05-27 US US11026951 No 2021-06-08 2034-12-03 US US11052084 No 2021-07-06 2039-08-30 US US11690842 No 2019-08-30 2039-08-30 US US11753419 No 2020-12-10 2040-12-10 US US11806348 No 2019-08-30 2039-08-30 US US9168258 No 2009-05-27 2029-05-27 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 2.328 http://www.chemspider.com/Chemical-Structure.19328801.html - Predicted Properties
Property Value Source Water Solubility 0.0805 mg/mL ALOGPS logP 3.87 ALOGPS logP 3.59 Chemaxon logS -3.7 ALOGPS pKa (Strongest Acidic) 16.61 Chemaxon pKa (Strongest Basic) 8.47 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 26.79 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 116.42 m3·mol-1 Chemaxon Polarizability 44.27 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0006-0009000000-130df7fcb46781ce351b Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-00dl-0009000000-cbfee8439271c711fd3c Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0006-0109000000-aa3818c44f556d727632 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0006-0009000000-e3a3093640dba70d049a Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-00sl-1479000000-9d2d1a225edbb7aa69d7 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0200-1159000000-1bb07e18925223ead05a Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 201.90852 predictedDeepCCS 1.0 (2019) [M+H]+ 204.35316 predictedDeepCCS 1.0 (2019) [M+Na]+ 212.36826 predictedDeepCCS 1.0 (2019)
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Serotonin:sodium symporter activity
- Specific Function
- Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into t...
- Gene Name
- SLC6A4
- Uniprot ID
- P31645
- Uniprot Name
- Sodium-dependent serotonin transporter
- Molecular Weight
- 70324.165 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- General Function
- Zinc ion binding
- Specific Function
- NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. In concert with DAPK1 at extrasynaptic site...
- Gene Name
- GRIN2B
- Uniprot ID
- Q13224
- Uniprot Name
- Glutamate receptor ionotropic, NMDA 2B
- Molecular Weight
- 166365.885 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Virus receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
- Gene Name
- HTR2A
- Uniprot ID
- P28223
- Uniprot Name
- 5-hydroxytryptamine receptor 2A
- Molecular Weight
- 52602.58 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Partial agonist
- General Function
- Potassium channel regulator activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
- Gene Name
- DRD2
- Uniprot ID
- P14416
- Uniprot Name
- D(2) dopamine receptor
- Molecular Weight
- 50618.91 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- G-protein coupled amine receptor activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
- Gene Name
- DRD1
- Uniprot ID
- P21728
- Uniprot Name
- D(1A) dopamine receptor
- Molecular Weight
- 49292.765 Da
References
- 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. [Article]
Enzymes
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Catalyzes the NADPH-dependent reduction of 1,5-anhydro-D-fructose (AF) to 1,5-anhydro-D-glucitol (By similarity). Has low NADPH-dependent reductase activity towards 9,10-phenanthrenequinone (in vitro) (PubMed:12604216, PubMed:15118078).
- Specific Function
- 1,5-anhydro-d-fructose reductase activity
Components:
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- FDA Approved Drug Products: Caplyta (lumateperone) capsules for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- FDA Approved Drug Products: Caplyta (lumateperone) capsules for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
- Gene Name
- UGT1A1
- Uniprot ID
- P22309
- Uniprot Name
- UDP-glucuronosyltransferase 1-1
- Molecular Weight
- 59590.91 Da
References
- FDA Approved Drug Products: Caplyta (lumateperone) capsules for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Protein homodimerization activity
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
- Gene Name
- UGT1A4
- Uniprot ID
- P22310
- Uniprot Name
- UDP-glucuronosyltransferase 1-4
- Molecular Weight
- 60024.535 Da
References
- FDA Approved Drug Products: Caplyta (lumateperone) capsules for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Glucuronosyltransferase activity
- Specific Function
- UDPGTs are of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isozyme displays activity toward several classes of xeno...
- Gene Name
- UGT2B15
- Uniprot ID
- P54855
- Uniprot Name
- UDP-glucuronosyltransferase 2B15
- Molecular Weight
- 61035.815 Da
References
- FDA Approved Drug Products: Caplyta (lumateperone) capsules for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Trans-1,2-dihydrobenzene-1,2-diol dehydrogenase activity
- Specific Function
- Converts progesterone to its inactive form, 20-alpha-dihydroxyprogesterone (20-alpha-OHP). In the liver and intestine, may have a role in the transport of bile. May have a role in monitoring the in...
- Gene Name
- AKR1C1
- Uniprot ID
- Q04828
- Uniprot Name
- Aldo-keto reductase family 1 member C1
- Molecular Weight
- 36788.02 Da
References
- FDA Approved Drug Products: Caplyta (lumateperone) capsules for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Retinal dehydrogenase activity
- Specific Function
- Acts as all-trans-retinaldehyde reductase. Can efficiently reduce aliphatic and aromatic aldehydes, and is less active on hexoses (in vitro). May be responsible for detoxification of reactive aldeh...
- Gene Name
- AKR1B10
- Uniprot ID
- O60218
- Uniprot Name
- Aldo-keto reductase family 1 member B10
- Molecular Weight
- 36019.295 Da
References
- FDA Approved Drug Products: Caplyta (lumateperone) capsules for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Retinal dehydrogenase activity
- Specific Function
- Catalyzes the transformation of the potent androgen dihydrotestosterone (DHT) into the less active form, 5-alpha-androstan-3-alpha,17-beta-diol (3-alpha-diol). Also has some 20-alpha-hydroxysteroid...
- Gene Name
- AKR1C4
- Uniprot ID
- P17516
- Uniprot Name
- Aldo-keto reductase family 1 member C4
- Molecular Weight
- 37066.52 Da
References
- FDA Approved Drug Products: Caplyta (lumateperone) capsules for oral use [Link]
Drug created at November 18, 2007 18:29 / Updated at July 01, 2023 10:08