lumateperone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
tranquillizers, neuroleptics, 4'-fluoro-4-piperidinobutyrophenone derivatives 5358 313368-91-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lumateperone
  • lumateperone tosylate
  • caplyta
  • ITI-007
The mechanism of action of lumateperone in the treatment of schizophrenia is unknown. However, the efficacy of lumateperone could be mediated through a combination of antagonist activity at central serotonin 5-HT2A receptors and postsynaptic antagonist activity at central dopamine D2 receptors.
  • Molecular weight: 393.51
  • Formula: C24H28FN3O
  • CLOGP: 4.09
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 26.79
  • ALOGS: -3.69
  • ROTB: 5
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
S (Water solubility) 0.30 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Dec. 20, 2019 FDA INTRA-CELLULAR

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Dizziness 142.97 46.73 102 1452 429823 63057645
Tardive dyskinesia 104.81 46.73 27 1527 8475 63478993
Mania 94.79 46.73 27 1527 12340 63475128
Sedation 88.95 46.73 34 1520 38775 63448693
Performance status decreased 77.56 46.73 18 1536 3660 63483808
Skin burning sensation 59.52 46.73 19 1535 12715 63474753
Burning sensation 58.84 46.73 28 1526 54379 63433089

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Tardive dyskinesia 99.65 43.45 25 1285 10546 79732532
Dizziness 99.60 43.45 76 1234 526365 79216713
Mania 77.31 43.45 23 1287 18237 79724841
Burning sensation 57.60 43.45 25 1285 58607 79684471
Performance status decreased 55.30 43.45 14 1296 6099 79736979
Sedation 47.29 43.45 21 1289 51874 79691204
Psychotic disorder 45.08 43.45 19 1291 41383 79701695
Skin burning sensation 44.56 43.45 14 1296 13258 79729820

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AD10 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Butyrophenone derivatives
FDA EPC N0000175430 Atypical Antipsychotic

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Schizophrenia indication 58214004 DOID:5419




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.98 Basic
pKa2 4.65 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 10.5MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 9199995 March 12, 2029 MODULATION OF 5-HYDROXYTRYPTAMINE 2 RECEPTOR ACTIVITY IN SCHIZOPHRENIA
EQ 21MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 9199995 March 12, 2029 MODULATION OF 5-HYDROXYTRYPTAMINE 2 RECEPTOR ACTIVITY IN SCHIZOPHRENIA
EQ 42MG BASE CAPLYTA INTRA-CELLULAR N209500 Dec. 20, 2019 RX CAPSULE ORAL 9199995 March 12, 2029 MODULATION OF 5-HYDROXYTRYPTAMINE 2 RECEPTOR ACTIVITY IN SCHIZOPHRENIA
EQ 10.5MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 10117867 May 27, 2029 TREATMENT OF BIPOLAR DEPRESSION
EQ 21MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 10117867 May 27, 2029 TREATMENT OF BIPOLAR DEPRESSION
EQ 42MG BASE CAPLYTA INTRA-CELLULAR N209500 Dec. 20, 2019 RX CAPSULE ORAL 10117867 May 27, 2029 TREATMENT OF BIPOLAR DEPRESSION
EQ 10.5MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL RE48839 Dec. 28, 2029 TREATMENT OF BIPOLAR DEPRESSION
EQ 10.5MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL RE48839 Dec. 28, 2029 TREATMENT OF SCHIZOPHRENIA
EQ 21MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL RE48839 Dec. 28, 2029 TREATMENT OF BIPOLAR DEPRESSION
EQ 21MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL RE48839 Dec. 28, 2029 TREATMENT OF SCHIZOPHRENIA
EQ 42MG BASE CAPLYTA INTRA-CELLULAR N209500 Dec. 20, 2019 RX CAPSULE ORAL 8598119 Dec. 28, 2029 TREATMENT OF SCHIZOPHRENIA
EQ 42MG BASE CAPLYTA INTRA-CELLULAR N209500 Dec. 20, 2019 RX CAPSULE ORAL RE48839 Dec. 28, 2029 TREATMENT OF BIPOLAR DEPRESSION
EQ 42MG BASE CAPLYTA INTRA-CELLULAR N209500 Dec. 20, 2019 RX CAPSULE ORAL RE48839 Dec. 28, 2029 TREATMENT OF SCHIZOPHRENIA
EQ 10.5MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 11026951 Dec. 3, 2034 TREATMENT OF BIPOLAR DISORDER I, BIPOLAR DISORDER II, OR BIPOLAR DEPRESSION
EQ 10.5MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 9956227 Dec. 3, 2034 TREATMENT OF SCHIZOPHRENIA WITH IMPROVEMENT IN RESIDUAL SYMPTOMS OF SCHIZOPHRENIA
EQ 21MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 11026951 Dec. 3, 2034 TREATMENT OF BIPOLAR DISORDER I, BIPOLAR DISORDER II, OR BIPOLAR DEPRESSION
EQ 21MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 9956227 Dec. 3, 2034 TREATMENT OF SCHIZOPHRENIA WITH IMPROVEMENT IN RESIDUAL SYMPTOMS OF SCHIZOPHRENIA
EQ 42MG BASE CAPLYTA INTRA-CELLULAR N209500 Dec. 20, 2019 RX CAPSULE ORAL 10960009 Dec. 3, 2034 TREATMENT OF SCHIZOPHRENIA
EQ 42MG BASE CAPLYTA INTRA-CELLULAR N209500 Dec. 20, 2019 RX CAPSULE ORAL 11026951 Dec. 3, 2034 TREATMENT OF BIPOLAR I DISORDER, BIPOLAR II DISORDER, OR BIPOLAR DEPRESSION
EQ 42MG BASE CAPLYTA INTRA-CELLULAR N209500 Dec. 20, 2019 RX CAPSULE ORAL 9956227 Dec. 3, 2034 TREATMENT OF SCHIZOPHRENIA WITH IMPROVEMENT IN RESIDUAL SYMPTOMS OF SCHIZOPHRENIA
EQ 10.5MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 10695345 Aug. 30, 2039 TREATMENT OF SCHIZOPHRENIA
EQ 10.5MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 11052084 Aug. 30, 2039 TREATMENT OF BIPOLAR DEPRESSION MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS
EQ 10.5MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 11052084 Aug. 30, 2039 TREATMENT OF SCHIZOPHRENIA MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS
EQ 10.5MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 11690842 Aug. 30, 2039 TREATMENT OF BIPOLAR DEPRESSION MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS
EQ 10.5MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 11690842 Aug. 30, 2039 TREATMENT OF SCHIZOPHRENIA MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS
EQ 21MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 10695345 Aug. 30, 2039 TREATMENT OF SCHIZOPHRENIA
EQ 21MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 11052084 Aug. 30, 2039 TREATMENT OF BIPOLAR DEPRESSION MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS
EQ 21MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 11052084 Aug. 30, 2039 TREATMENT OF SCHIZOPHRENIA MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS
EQ 21MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 11690842 Aug. 30, 2039 TREATMENT OF BIPOLAR DEPRESSION MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS
EQ 21MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL 11690842 Aug. 30, 2039 TREATMENT OF SCHIZOPHRENIA MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS
EQ 42MG BASE CAPLYTA INTRA-CELLULAR N209500 Dec. 20, 2019 RX CAPSULE ORAL 10695345 Aug. 30, 2039 TREATMENT OF SCHIZOPHRENIA
EQ 42MG BASE CAPLYTA INTRA-CELLULAR N209500 Dec. 20, 2019 RX CAPSULE ORAL 11690842 Aug. 30, 2039 TREATMENT OF BIPOLAR DEPRESSION MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS
EQ 42MG BASE CAPLYTA INTRA-CELLULAR N209500 Dec. 20, 2019 RX CAPSULE ORAL 11690842 Aug. 30, 2039 TREATMENT OF SCHIZOPHRENIA MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 42MG BASE CAPLYTA INTRA-CELLULAR N209500 Dec. 20, 2019 RX CAPSULE ORAL Dec. 17, 2024 INDICATED FOR DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I OR II DISORDER (BIPOLAR DEPRESSION) IN ADULTS, AS MONOTHERAPY AND AS ADJUNCTIVE THERAPY WITH LITHIUM OR VALPROATE
EQ 10.5MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL Dec. 20, 2024 NEW CHEMICAL ENTITY
EQ 21MG BASE CAPLYTA INTRA-CELLULAR N209500 April 22, 2022 RX CAPSULE ORAL Dec. 20, 2024 NEW CHEMICAL ENTITY
EQ 42MG BASE CAPLYTA INTRA-CELLULAR N209500 Dec. 20, 2019 RX CAPSULE ORAL Dec. 20, 2024 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
D(2) dopamine receptor GPCR ANTAGONIST Ki 7.49 DRUG LABEL DRUG LABEL
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 9.26 DRUG LABEL DRUG LABEL
Alpha-1A adrenergic receptor GPCR Ki 7.14 CHEMBL
D(4) dopamine receptor GPCR Ki 6.97 CHEMBL
Alpha-1B adrenergic receptor GPCR Ki 7.51 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 5.83 CHEMBL
D(1A) dopamine receptor GPCR ANTAGONIST Ki 7.38 DRUG LABEL
Sodium-dependent serotonin transporter Transporter Ki 7.48 DRUG LABEL
5-hydroxytryptamine receptor 2C GPCR Ki 6.76 CHEMBL
D(2) dopamine receptor GPCR Ki 7.50 CHEMBL

External reference:

IDSource
92S PDB_CHEM_ID
CHEMBL3306803 ChEMBL_ID
D11169 KEGG_DRUG
C000705749 MESH_SUPPLEMENTAL_RECORD_UI
9099 IUPHAR_LIGAND_ID
1187020-80-9 SECONDARY_CAS_RN
DB06077 DRUGBANK_ID
018246 NDDF
018247 NDDF
838463000 SNOMEDCT_US
838474009 SNOMEDCT_US
4039112 VANDF
C4305843 UMLSCUI
CHEMBL3233142 ChEMBL_ID
10156 INN_ID
21302490 PUBCHEM_CID
2275602 RXNORM
328648 MMSL
37890 MMSL
d09477 MMSL
70BSQ12069 UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
CAPLYTA HUMAN PRESCRIPTION DRUG LABEL 1 70518-3497 CAPSULE 42 mg ORAL NDA 32 sections
CAPLYTA HUMAN PRESCRIPTION DRUG LABEL 1 72060-110 CAPSULE 10.50 mg ORAL NDA 32 sections
CAPLYTA HUMAN PRESCRIPTION DRUG LABEL 1 72060-110 CAPSULE 10.50 mg ORAL NDA 32 sections
CAPLYTA HUMAN PRESCRIPTION DRUG LABEL 1 72060-121 CAPSULE 21 mg ORAL NDA 32 sections
CAPLYTA HUMAN PRESCRIPTION DRUG LABEL 1 72060-121 CAPSULE 21 mg ORAL NDA 32 sections
CAPLYTA HUMAN PRESCRIPTION DRUG LABEL 1 72060-142 CAPSULE 42 mg ORAL NDA 32 sections
CAPLYTA HUMAN PRESCRIPTION DRUG LABEL 1 72060-142 CAPSULE 42 mg ORAL NDA 32 sections
CAPLYTA HUMAN PRESCRIPTION DRUG LABEL 1 72060-142 CAPSULE 42 mg ORAL NDA 32 sections
CAPLYTA HUMAN PRESCRIPTION DRUG LABEL 1 72060-142 CAPSULE 42 mg ORAL NDA 32 sections