Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
tranquillizers, neuroleptics, 4'-fluoro-4-piperidinobutyrophenone derivatives	5358	313368-91-1

Description:

Molecule	Description
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

Molecule

Description

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:

Property	Value	Reference
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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value
kinase-safety-class	ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK	52
kinase-selectivity-class	AKT3,AXL,CAMK2D,EIF2AK3,PDK4,PRKCD,SIK2,STK33	8
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

Date	Agency	Company	Orphan
Dec. 20, 2019	FDA	INTRA-CELLULAR

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Mania	408.63	45.29	108	5792	14016	90608531
Dizziness	401.86	45.29	319	5581	588965	90033582
Tardive dyskinesia	342.15	45.29	89	5811	10841	90611706
Sedation	310.69	45.29	117	5783	48054	90574493
Akathisia	264.70	45.29	73	5827	11086	90611461
Burning sensation	239.73	45.29	105	5795	63347	90559200
Somnolence	208.37	45.29	143	5757	208941	90413606
Suicidal ideation	141.81	45.29	77	5823	73778	90548769
Skin burning sensation	138.55	45.29	51	5849	19560	90602987
Nausea	132.70	45.29	248	5652	1110068	89512479
Electric shock sensation	123.73	45.29	27	5873	1543	90621004
Headache	121.14	45.29	207	5693	862539	89760008
Performance status decreased	106.06	45.29	29	5871	4251	90618296
Irritability	99.89	45.29	48	5852	35614	90586933
Hypomania	89.07	45.29	30	5870	8867	90613680
Tremor	88.70	45.29	76	5824	153097	90469450
Dyskinesia	86.91	45.29	44	5856	36490	90586057
Feeling abnormal	80.98	45.29	75	5825	167160	90455387
Tachyphrenia	73.72	45.29	18	5882	1688	90620859
Temperature regulation disorder	71.18	45.29	29	5871	14550	90607997
Unevaluable event	70.21	45.29	44	5856	54804	90567743
Psychotic disorder	63.89	45.29	34	5866	31196	90591351
Feeling drunk	63.70	45.29	20	5880	4738	90617809
Migraine	62.13	45.29	69	5831	190323	90432224
Feeling hot	60.59	45.29	46	5854	77962	90544585
Hallucination, auditory	55.58	45.29	25	5875	15950	90606597
Pseudostroke	55.32	45.29	9	5891	100	90622447
Anxiety	54.93	45.29	83	5817	309689	90312858
Extrapyramidal disorder	48.85	45.29	23	5877	16280	90606267
Dystonia	48.17	45.29	23	5877	16796	90605751
Neuroleptic malignant syndrome	47.41	45.29	22	5878	15074	90607473

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Mania	195.56	52.83	54	2141	10493	42608647
Akathisia	168.61	52.83	48	2147	10403	42608737
Tardive dyskinesia	144.79	52.83	39	2156	6885	42612255
Sedation	118.25	52.83	48	2147	30427	42588713
Dizziness	113.66	52.83	97	2098	249157	42369983
Burning sensation	102.21	52.83	39	2156	20974	42598166
Suicidal ideation	88.32	52.83	45	2150	48116	42571024
Headache	77.36	52.83	77	2118	239292	42379848
Somnolence	64.11	52.83	55	2140	141050	42478090
Hypomania	61.30	52.83	16	2179	2492	42616648
Hallucination, auditory	56.14	52.83	23	2172	14841	42604299
Psychotic disorder	55.54	52.83	28	2167	29180	42589960
Anxiety	55.41	52.83	47	2148	118513	42500627

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Tardive dyskinesia	304.34	42.34	77	4424	13502	110571296
Dizziness	262.84	42.34	220	4281	697973	109886825
Mania	253.81	42.34	73	4428	20723	110564075
Akathisia	208.45	42.34	60	4441	17053	110567745
Burning sensation	184.49	42.34	78	4423	69134	110515664
Suicidal ideation	146.66	42.34	73	4428	93864	110490934
Sedation	145.00	42.34	66	4435	69617	110515181
Headache	110.67	42.34	156	4345	882221	109702577
Somnolence	105.36	42.34	91	4410	297358	110287440
Nausea	92.73	42.34	173	4328	1235517	109349281
Irritability	89.15	42.34	42	4459	47767	110537031
Psychotic disorder	83.61	42.34	41	4460	50896	110533902
Performance status decreased	77.49	42.34	23	4478	7243	110577555
Skin burning sensation	76.57	42.34	30	4471	21795	110563003
Hypomania	69.79	42.34	23	4478	10187	110574611
Feeling abnormal	69.42	42.34	58	4443	180653	110404145
Tremor	65.73	42.34	59	4442	202173	110382625
Hallucination, auditory	61.20	42.34	27	4474	26370	110558428
Anxiety	56.83	42.34	70	4431	345008	110239790
Insomnia	54.38	42.34	70	4431	360520	110224278
Electric shock sensation	53.42	42.34	13	4488	1931	110582867
Feeling hot	49.65	42.34	36	4465	91070	110493728
Dyskinesia	49.40	42.34	29	4472	51417	110533381
Temperature regulation disorder	46.28	42.34	18	4483	12808	110571990

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N05AD10	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Butyrophenone derivatives
FDA EPC	N0000175430	Atypical Antipsychotic
CHEBI has role	CHEBI:35476	antipsychotic agent
CHEBI has role	CHEBI:35469	antidepressant

Related Drugs by ATC class:

N05AD Butyrophenone derivatives 8 drugs

benperidol bromperidol droperidol haloperidol melperone moperone pipamperone trifluperidol

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

Disease	Relation	SNOMED_ID	DOID
Schizophrenia	indication	58214004	DOID:5419

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.98	Basic
pKa2	4.65	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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 MAJOR DEPRESSIVE DISORDER ADJUNCTIVE TO ANTIDEPRESSANT THERAPY
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 MAJOR DEPRESSIVE DISORDER ADJUNCTIVE TO ANTIDEPRESSANT THERAPY
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 MAJOR DEPRESSIVE DISORDER ADJUNCTIVE TO ANTIDEPRESSANT THERAPY
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 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	8598119	Dec. 28, 2029	TREATMENT OF SCHIZOPHRENIA
EQ 10.5MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	RE48839	Aug. 19, 2033	TREATMENT OF BIPOLAR DEPRESSION
EQ 10.5MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	RE48839	Aug. 19, 2033	TREATMENT OF MAJOR DEPRESSIVE DISORDER ADJUNCTIVE TO ANTIDEPRESSANT TREATMENT
EQ 10.5MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	RE48839	Aug. 19, 2033	TREATMENT OF SCHIZOPHRENIA
EQ 21MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	RE48839	Aug. 19, 2033	TREATMENT OF BIPOLAR DEPRESSION
EQ 21MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	RE48839	Aug. 19, 2033	TREATMENT OF MAJOR DEPRESSIVE DISORDER ADJUNCTIVE TO ANTIDEPRESSANT TREATMENT
EQ 21MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	RE48839	Aug. 19, 2033	TREATMENT OF SCHIZOPHRENIA
EQ 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	RE48839	Aug. 19, 2033	TREATMENT OF BIPOLAR DEPRESSION
EQ 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	RE48839	Aug. 19, 2033	TREATMENT OF MAJOR DEPRESSIVE DISORDER ADJUNCTIVE TO ANTIDEPRESSANT TREATMENT
EQ 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	RE48839	Aug. 19, 2033	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	12409176	March 15, 2039	TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR DISORDER
EQ 21MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	12409176	March 15, 2039	TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR DISORDER
EQ 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	12409176	March 15, 2039	TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR DISORDER
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 MAJOR DEPRESSIVE DISORDER MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS, ADJUNCTIVE TO ANTIDEPRESSANT TREATMENT
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 MAJOR DEPRESSIVE DISORDER MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS, ADJUNCTIVE TO ANTIDEPRESSANT TREATMENT
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 10.5MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	11806348	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	11806348	Aug. 30, 2039	TREATMENT OF MAJOR DEPRESSIVE DISORDER MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS, ADJUNCTIVE TO ANTIDEPRESSANT TREATMENT
EQ 10.5MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	11806348	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 MAJOR DEPRESSIVE DISORDER MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS, ADJUNCTIVE TO ANTIDEPRESSANT TREATMENT
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 MAJOR DEPRESSIVE DISORDER MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS, ADJUNCTIVE TO ANTIDEPRESSANT TREATMENT
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 21MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	11806348	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	11806348	Aug. 30, 2039	TREATMENT OF MAJOR DEPRESSIVE DISORDER MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS, ADJUNCTIVE TO ANTIDEPRESSANT TREATMENT
EQ 21MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	11806348	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 MAJOR DEPRESSIVE DISORDER MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS, ADJUNCTIVE TO ANTIDEPRESSANT TREATMENT
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
EQ 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	11806348	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	11806348	Aug. 30, 2039	TREATMENT OF MAJOR DEPRESSIVE DISORDER MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS, ADJUNCTIVE TO ANTIDEPRESSANT TREATMENT
EQ 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	11806348	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	12070459	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	12070459	Aug. 30, 2039	TREATMENT OF MAJOR DEPRESSIVE DISORDER MEDIATED BY THE 5-HT2A RECEPTOR, SEROTONIN TRANSPORTER, AND/OR DOPAMINE D1/D2 SIGNALING PATHWAYS, ADJUNCTIVE TO ANTIDEPRESSANT TREATMENT
EQ 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	12070459	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	12128043	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	12128043	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	11980617	Oct. 27, 2039	TREATMENT OF BIPOLAR DISORDER OR BIPOLAR DEPRESSION, INCLUDING ASSOCIATED DEPRESSIVE EPISODES
EQ 10.5MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	11980617	Oct. 27, 2039	TREATMENT OF MAJOR DEPRESSIVE DISORDER ADJUNCTIVE TO ANTIDEPRESSANT THERAPY, INCLUDING TREATMENT RESISTANT MAJOR DEPRESSIVE DISORDER
EQ 21MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	11980617	Oct. 27, 2039	TREATMENT OF BIPOLAR DISORDER OR BIPOLAR DEPRESSION, INCLUDING ASSOCIATED DEPRESSIVE EPISODES
EQ 21MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	11980617	Oct. 27, 2039	TREATMENT OF MAJOR DEPRESSIVE DISORDER ADJUNCTIVE TO ANTIDEPRESSANT THERAPY, INCLUDING TREATMENT RESISTANT MAJOR DEPRESSIVE DISORDER
EQ 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	11980617	Oct. 27, 2039	TREATMENT OF BIPOLAR DISORDER OR BIPOLAR DEPRESSION, INCLUDING ASSOCIATED DEPRESSIVE EPISODES
EQ 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	11980617	Oct. 27, 2039	TREATMENT OF MAJOR DEPRESSIVE DISORDER ADJUNCTIVE TO ANTIDEPRESSANT THERAPY, INCLUDING TREATMENT RESISTANT MAJOR DEPRESSIVE DISORDER
EQ 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	12090155	July 7, 2040	TREATMENT OF DEPRESSIVE EPISODES OR MAJOR DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR II DISORDER
EQ 10.5MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	12122792	Dec. 10, 2040	TREATMENT OF BIPOLAR DEPRESSION BY INHIBITING THE 5-HT2A RECEPTOR, INHIBITING THE SEROTONIN TRANSPORTER, AND/OR MODULATING DOPAMINE D2 RECEPTOR FUNCTION, OR TREATMENT OF BIPOLAR DISORDER
EQ 10.5MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	12122792	Dec. 10, 2040	TREATMENT OF MAJOR DEPRESSIVE DISORDER, ADJUNCTIVE TO ANTIDEPRESSANT THERAPY, OR ADJUNCTIVE TO ANTIDEPRESSANT THERAPY BY INHIBITING THE 5-HT2A RECEPTOR AND/OR SEROTONIN TRANSPORTER, AND/OR MODULATING DOPAMINE D2 RECEPTOR FUNCTION
EQ 10.5MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	12122792	Dec. 10, 2040	TREATMENT OF SCHIZOPHRENIA BY INHIBITING THE 5-HT2A RECEPTOR, INHIBITING THE SEROTONIN TRANSPORTER, AND/OR MODULATING DOPAMINE D2 RECEPTOR FUNCTION, OR TREATMENT OF SCHIZOPHRENIA
EQ 21MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	12122792	Dec. 10, 2040	TREATMENT OF BIPOLAR DEPRESSION BY INHIBITING THE 5-HT2A RECEPTOR, INHIBITING THE SEROTONIN TRANSPORTER, AND/OR MODULATING DOPAMINE D2 RECEPTOR FUNCTION, OR TREATMENT OF BIPOLAR DISORDER
EQ 21MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	12122792	Dec. 10, 2040	TREATMENT OF MAJOR DEPRESSIVE DISORDER, ADJUNCTIVE TO ANTIDEPRESSANT THERAPY, OR ADJUNCTIVE TO ANTIDEPRESSANT THERAPY BY INHIBITING THE 5-HT2A RECEPTOR AND/OR SEROTONIN TRANSPORTER, AND/OR MODULATING DOPAMINE D2 RECEPTOR FUNCTION
EQ 21MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	12122792	Dec. 10, 2040	TREATMENT OF SCHIZOPHRENIA BY INHIBITING THE 5-HT2A RECEPTOR, INHIBITING THE SEROTONIN TRANSPORTER, AND/OR MODULATING DOPAMINE D2 RECEPTOR FUNCTION, OR TREATMENT OF SCHIZOPHRENIA
EQ 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	12122792	Dec. 10, 2040	TREATMENT OF BIPOLAR DEPRESSION BY INHIBITING THE 5-HT2A RECEPTOR, INHIBITING THE SEROTONIN TRANSPORTER, AND/OR MODULATING DOPAMINE D2 RECEPTOR FUNCTION, OR TREATMENT OF BIPOLAR DISORDER
EQ 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	12122792	Dec. 10, 2040	TREATMENT OF MAJOR DEPRESSIVE DISORDER, ADJUNCTIVE TO ANTIDEPRESSANT THERAPY, OR ADJUNCTIVE TO ANTIDEPRESSANT THERAPY BY INHIBITING THE 5-HT2A RECEPTOR AND/OR SEROTONIN TRANSPORTER, AND/OR MODULATING DOPAMINE D2 RECEPTOR FUNCTION
EQ 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	12122792	Dec. 10, 2040	TREATMENT OF SCHIZOPHRENIA BY INHIBITING THE 5-HT2A RECEPTOR, INHIBITING THE SEROTONIN TRANSPORTER, AND/OR MODULATING DOPAMINE D2 RECEPTOR FUNCTION, OR TREATMENT OF SCHIZOPHRENIA

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 10.5MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	Nov. 5, 2028	ADJUNCTIVE THERAPY TO ANTIDEPRESSANTS FOR THE TREATMENT OF MAJOR DEPRESSIVE DISORDER IN ADULTS
EQ 21MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	Nov. 5, 2028	ADJUNCTIVE THERAPY TO ANTIDEPRESSANTS FOR THE TREATMENT OF MAJOR DEPRESSIVE DISORDER IN ADULTS
EQ 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	Nov. 5, 2028	ADJUNCTIVE THERAPY TO ANTIDEPRESSANTS FOR THE TREATMENT OF MAJOR DEPRESSIVE DISORDER IN ADULTS
EQ 10.5MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	April 24, 2029	UPDATES TO SECTION 14 OF THE PRESCRIBING INFORMATION BASED ON RESULTS OF A CLINICAL STUDY
EQ 21MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	April 22, 2022	RX	CAPSULE	ORAL	April 24, 2029	UPDATES TO SECTION 14 OF THE PRESCRIBING INFORMATION BASED ON RESULTS OF A CLINICAL STUDY
EQ 42MG BASE	CAPLYTA	INTRA-CELLULAR	N209500	Dec. 20, 2019	RX	CAPSULE	ORAL	April 24, 2029	UPDATES TO SECTION 14 OF THE PRESCRIBING INFORMATION BASED ON RESULTS OF A CLINICAL STUDY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	Ki	7.49	DRUG LABEL	DRUG LABEL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	9.26	DRUG LABEL	DRUG LABEL
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	7.14	CHEMBL
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		Ki	6.97	CHEMBL
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	7.51	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	5.83	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN	ANTAGONIST	Ki	7.38	DRUG LABEL
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	7.48	DRUG LABEL
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	6.76	CHEMBL
D(2) dopamine receptor	GPCR		DRD2_RAT		Ki	7.50	CHEMBL

External reference:

ID	Source
4039112	VANDF
CHEBI:755315	CHEBI
92S	PDB_CHEM_ID
CHEMBL3306803	ChEMBL_ID
D11169	KEGG_DRUG
C000705749	MESH_SUPPLEMENTAL_RECORD_UI
9099	IUPHAR_LIGAND_ID
DB06077	DRUGBANK_ID
838463000	SNOMEDCT_US
838474009	SNOMEDCT_US
C4305843	UMLSCUI
CHEMBL3233142	ChEMBL_ID
10156	INN_ID
1187020-80-9	SECONDARY_CAS_RN
328648	MMSL
37890	MMSL
d09477	MMSL
21302490	PUBCHEM_CID
018246	NDDF
018247	NDDF
70BSQ12069	UNII
2275602	RXNORM
70BSQ12069	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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	72060-142	CAPSULE	42 mg	ORAL	NDA	32 sections

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lumateperone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products: