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

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used in combination to manageDepressive episodes••••••••••••••••••••••••
Used in combination to manageDepressive episodesRegimen in combination with: Valproic acid (DB00313)••••••••••••••••••••••••
Used in combination to manageDepressive episodes••••••••••••••••••••••••
Used in combination to manageDepressive episodesRegimen in combination with: Valproic acid (DB00313)••••••••••••••••••••••••
Management ofDepressive episodes••••••••••••••••••••••••
Contraindications & Blackbox Warnings
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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

TargetActionsOrganism
ASodium-dependent serotonin transporter
inhibitor
Humans
AGlutamate receptor ionotropic, NMDA 2BNot AvailableHumans
A5-hydroxytryptamine receptor 2A
antagonist
Humans
ADopamine D2 receptor
partial agonist
Humans
UDopamine D1 receptorNot AvailableHumans
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
Not Available

Interactions

Drug Interactions
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.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of CNS depression can be increased when Lumateperone is combined with 1,2-Benzodiazepine.
AbametapirThe serum concentration of Lumateperone can be increased when it is combined with Abametapir.
AcetaminophenThe serum concentration of Lumateperone can be decreased when it is combined with Acetaminophen.
AcetazolamideThe risk or severity of CNS depression can be increased when Acetazolamide is combined with Lumateperone.
AcetophenazineThe 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

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Product Ingredients
IngredientUNIICASInChI Key
Lumateperone tosylateJIE88N006O1187020-80-9LHAPOGAFBLSJJQ-GUTACTQSSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CaplytaCapsule42 mg/1OralREMEDYREPACK INC.2022-08-24Not applicableUS flag
CaplytaCapsule42 mg/1OralIntra-Cellular Therapies, Inc2020-02-01Not applicableUS flag
CaplytaCapsule10.5 mg/1OralIntra-Cellular Therapies, Inc2022-08-09Not applicableUS flag
CaplytaCapsule21 mg/1OralIntra-Cellular Therapies, Inc2022-08-09Not applicableUS flag

Categories

ATC Codes
N05AD10 — Lumateperone
Drug Categories
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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. FDA Approved Drug Products: Caplyta (lumateperone) capsules for oral use [Link]
  7. 24. The Clinical Development of Lumateperone (ITI-007) for the Treatment of Schizophrenia [Link]
  8. S44. Lumateperone (ITI-007) for the Treatment of Schizophrenia: Placebo-Controlled Clinical Trials and an Open-Label Safety Switching Study [Link]
  9. FDA Approved Drug Products: Caplyta (lumateperone) capsules for oral use (June 2023) [Link]
PubChem Compound
21302490
PubChem Substance
310264860
ChemSpider
19328801
RxNav
2275602
ChEMBL
CHEMBL3306803
ZINC
ZINC000116262036
PDBe Ligand
92S
Wikipedia
Lumateperone
PDB Entries
7wc8

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Not Yet RecruitingTreatmentSchizoaffective Disorders / Schizophrenia1
4RecruitingOtherPsychosis1
3Active Not RecruitingTreatmentSchizophrenia1
3CompletedTreatmentDepression, Bipolar3
3CompletedTreatmentDepression, Bipolar / Major Depressive Disorder (MDD)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
CapsuleOral10.5 mg/1
CapsuleOral21 mg/1
CapsuleOral42 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US10464938No2019-11-052028-03-12US flag
US8648077No2014-02-112029-12-01US flag
US9616061No2017-04-112029-05-27US flag
US7183282No2007-02-272020-06-15US flag
US9586960No2017-03-072029-03-12US flag
US8598119No2013-12-032029-12-28US flag
USRE39680No2007-06-052020-06-15US flag
US9199995No2015-12-012029-03-12US flag
US9956227No2018-05-012034-12-03US flag
US10695345No2020-06-302039-08-30US flag
US10960009No2021-03-302034-12-03US flag
USRE48839No2021-12-072029-12-28US flag
USRE48825No2021-11-232029-03-12US flag
US10117867No2018-11-062029-05-27US flag
US11026951No2021-06-082034-12-03US flag
US11052084No2021-07-062039-08-30US flag
US11690842No2019-08-302039-08-30US flag
US11753419No2020-12-102040-12-10US flag
US11806348No2019-08-302039-08-30US flag
US9168258No2009-05-272029-05-27US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP2.328http://www.chemspider.com/Chemical-Structure.19328801.html
Predicted Properties
PropertyValueSource
Water Solubility0.0805 mg/mLALOGPS
logP3.87ALOGPS
logP3.59Chemaxon
logS-3.7ALOGPS
pKa (Strongest Acidic)16.61Chemaxon
pKa (Strongest Basic)8.47Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count0Chemaxon
Polar Surface Area26.79 Å2Chemaxon
Rotatable Bond Count5Chemaxon
Refractivity116.42 m3·mol-1Chemaxon
Polarizability44.27 Å3Chemaxon
Number of Rings5Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleYesChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0006-0009000000-130df7fcb46781ce351b
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-00dl-0009000000-cbfee8439271c711fd3c
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0006-0109000000-aa3818c44f556d727632
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0006-0009000000-e3a3093640dba70d049a
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-00sl-1479000000-9d2d1a225edbb7aa69d7
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0200-1159000000-1bb07e18925223ead05a
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-201.90852
predicted
DeepCCS 1.0 (2019)
[M+H]+204.35316
predicted
DeepCCS 1.0 (2019)
[M+Na]+212.36826
predicted
DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.
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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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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