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

Stem definition	Drug id	CAS RN
psychoactive	4115	65576-45-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: Org-5222 Org 5222 asenapine saphris asenapine maleate sycrest	Molecular weight: 285.77 Formula: C17H16ClNO CLOGP: 4.28 LIPINSKI: 0 HAC: 2 HDO: 0 TPSA: 12.47 ALOGS: -3.96 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

Org-5222
Org 5222
asenapine
saphris
asenapine maleate
sycrest

Molecular weight: 285.77
Formula: C17H16ClNO
CLOGP: 4.28
LIPINSKI: 0
HAC: 2
HDO: 0
TPSA: 12.47
ALOGS: -3.96
ROTB: 0

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
20	mg	O

ADMET properties:

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Property	Value	Reference
S (Water solubility)	3.70 mg/mL	Bocci G, Oprea TI, Benet LZ
Vd (Volume of distribution)	23 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	12.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	1 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.71 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.05 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Aug. 13, 2009	FDA	FOREST LABS INC

FDA Adverse Event Reporting System (Female)

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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
Anosognosia	1260.76	33.07	241	9314	2955	63476512
Blood prolactin abnormal	1257.18	33.07	239	9316	2840	63476627
Disturbance in social behaviour	1201.20	33.07	240	9315	3753	63475714
Sexual dysfunction	1174.28	33.07	239	9316	4120	63475347
Metabolic disorder	1073.47	33.07	238	9317	6265	63473202
Dystonia	1020.44	33.07	264	9291	13555	63465912
Personality change	1002.66	33.07	228	9327	6745	63472722
Sedation	911.99	33.07	305	9250	38504	63440963
Dyskinesia	858.23	33.07	278	9277	31724	63447743
Suicide attempt	635.70	33.07	264	9291	60654	63418813

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FDA Adverse Event Reporting System (Male)

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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
Suicide attempt	507.57	35.88	211	6368	38905	34911447
Akathisia	464.04	35.88	133	6446	7976	34942376
Antipsychotic drug level below therapeutic	387.51	35.88	91	6488	2456	34947896
Sedation	382.79	35.88	145	6434	20861	34929491
Therapeutic product effect variable	374.96	35.88	88	6491	2368	34947984
Disinhibition	371.16	35.88	92	6487	3134	34947218
Anosognosia	364.72	35.88	73	6506	900	34949452
Obsessive-compulsive disorder	344.03	35.88	97	6482	5467	34944885
Blood prolactin abnormal	335.18	35.88	68	6511	901	34949451
Increased appetite	324.86	35.88	99	6480	7330	34943022

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FDA Adverse Event Reporting System (Geriatric)

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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
Anosognosia	1487.47	28.88	282	11132	3482	79729492
Blood prolactin abnormal	1449.42	28.88	274	11140	3327	79729647
Disturbance in social behaviour	1367.30	28.88	275	11139	4695	79728279
Sexual dysfunction	1283.90	28.88	282	11132	7481	79725493
Metabolic disorder	1199.45	28.88	275	11139	8895	79724079
Dystonia	1119.28	28.88	308	11106	21091	79711883
Personality change	1118.66	28.88	265	11149	9905	79723069
Sedation	1101.15	28.88	373	11041	51522	79681452
Dyskinesia	965.87	28.88	326	11088	44447	79688527
Suicide attempt	916.69	28.88	369	11045	82563	79650411

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N05AH05	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Diazepines, oxazepines, thiazepines and oxepines
CHEBI has role	CHEBI:35471	psychotropic drugs
CHEBI has role	CHEBI:35530	beta-adrenergic blockers
CHEBI has role	CHEBI:37890	alpha-adrenergic receptor blockaders
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:48561	dopaminergic antagonists
CHEBI has role	CHEBI:65191	atypical antipsychotic agent
FDA EPC	N0000175430	Atypical Antipsychotic
MeSH PA	D014150	Antipsychotic Agents
MeSH PA	D002491	Central Nervous System Agents

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

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Disease	Relation	SNOMED_ID	DOID
Mixed bipolar I disorder	indication	16506000	DOID:3312
Schizophrenia	indication	58214004	DOID:5419
Bipolar affective disorder, current episode manic	indication	191618007
Depression Treatment Adjunct	off-label use
Suicidal thoughts	contraindication	6471006
Weight gain finding	contraindication	8943002
Neuroleptic malignant syndrome	contraindication	15244003	DOID:14464
Agranulocytosis	contraindication	17182001	DOID:12987
Lowered convulsive threshold	contraindication	19260006
Myocardial infarction	contraindication	22298006	DOID:5844

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.13	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
3.8MG/24HR	SECUADO	HISAMITSU	N212268	Oct. 11, 2019	RX	SYSTEM	TRANSDERMAL	10583121	July 25, 2033	METHOD OF TREATING ADULTS WITH SCHIZOPHRENIA COMPRISING ADMINISTERING ASENAPINE VIA A TRANSDERMAL PATCH
3.8MG/24HR	SECUADO	HISAMITSU	N212268	Oct. 11, 2019	RX	SYSTEM	TRANSDERMAL	10814002	July 25, 2033	METHOD OF TREATING ADULTS WITH SCHIZOPHRENIA COMPRISING ADMINISTERING ASENAPINE VIA A TRANSDERMAL PATCH
5.7MG/24HR	SECUADO	HISAMITSU	N212268	Oct. 11, 2019	RX	SYSTEM	TRANSDERMAL	10583121	July 25, 2033	METHOD OF TREATING ADULTS WITH SCHIZOPHRENIA COMPRISING ADMINISTERING ASENAPINE VIA A TRANSDERMAL PATCH
5.7MG/24HR	SECUADO	HISAMITSU	N212268	Oct. 11, 2019	RX	SYSTEM	TRANSDERMAL	10814002	July 25, 2033	METHOD OF TREATING ADULTS WITH SCHIZOPHRENIA COMPRISING ADMINISTERING ASENAPINE VIA A TRANSDERMAL PATCH
7.6MG/24HR	SECUADO	HISAMITSU	N212268	Oct. 11, 2019	RX	SYSTEM	TRANSDERMAL	10583121	July 25, 2033	METHOD OF TREATING ADULTS WITH SCHIZOPHRENIA COMPRISING ADMINISTERING ASENAPINE VIA A TRANSDERMAL PATCH
7.6MG/24HR	SECUADO	HISAMITSU	N212268	Oct. 11, 2019	RX	SYSTEM	TRANSDERMAL	10814002	July 25, 2033	METHOD OF TREATING ADULTS WITH SCHIZOPHRENIA COMPRISING ADMINISTERING ASENAPINE VIA A TRANSDERMAL PATCH
EQ 10MG BASE	SAPHRIS	ALLERGAN	N022117	Aug. 13, 2009	RX	TABLET	SUBLINGUAL	7741358	April 6, 2026	TREATMENT OF BIPOLAR DISORDER AND SCHIZOPHRENIA
EQ 10MG BASE	SAPHRIS	ALLERGAN	N022117	Aug. 13, 2009	RX	TABLET	SUBLINGUAL	7741358	April 6, 2026	USE OF THE ATYPICAL ANTIPSYCHOTIC ASENAPINE FOR TREATMENT OF MANIC OR MIXED EPISODES OF BIPOLAR I DISORDER: ACUTE MONOTHERAPY OF MANIC OR MIXED EPISODES (AGES 10 TO ADULT)
EQ 10MG BASE	SAPHRIS	ALLERGAN	N022117	Aug. 13, 2009	RX	TABLET	SUBLINGUAL	7741358	April 6, 2026	USE OF THE ATYPICAL ANTIPSYCHOTIC ASENAPINE FOR TREATMENT OF MANIC OR MIXED EPISODES OF BIPOLAR I DISORDER: AS ADJUNCTIVE TREATMENT TO LITHIUM OR VALPROATE IN ADULTS
EQ 10MG BASE	SAPHRIS	ALLERGAN	N022117	Aug. 13, 2009	RX	TABLET	SUBLINGUAL	7741358	April 6, 2026	USE OF THE ATYPICAL ANTIPSYCHOTIC ASENAPINE FOR TREATMENT OF MANIC OR MIXED EPISODES OF BIPOLAR I DISORDER: MAINTENANCE MONOTHERAPY IN ADULTS

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	9.61	WOMBAT-PK	CHEMBL
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	Ki	8.75	WOMBAT-PK	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	8.70	WOMBAT-PK
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	8.19	PDSP
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	7.97	WOMBAT-PK
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	9.80	WOMBAT-PK
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	9.93	WOMBAT-PK
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	9.22	WOMBAT-PK
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	9.47	WOMBAT-PK
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	8.92	WOMBAT-PK

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External reference:

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ID	Source
013233	NDDF
013234	NDDF
163091	PUBCHEM_CID
167374	MMSL
22	IUPHAR_LIGAND_ID
26689	MMSL
341671	MMSL
4029058	VUID
4029058	VANDF
443374004	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ASENAPINE	HUMAN PRESCRIPTION DRUG LABEL	1	42794-016	TABLET	5 mg	SUBLINGUAL	ANDA	21 sections
ASENAPINE	HUMAN PRESCRIPTION DRUG LABEL	1	42794-016	TABLET	5 mg	SUBLINGUAL	ANDA	21 sections
ASENAPINE	HUMAN PRESCRIPTION DRUG LABEL	1	42794-017	TABLET	10 mg	SUBLINGUAL	ANDA	21 sections
ASENAPINE	HUMAN PRESCRIPTION DRUG LABEL	1	42794-017	TABLET	10 mg	SUBLINGUAL	ANDA	21 sections
Asenapine	Human Prescription Drug Label	1	46708-198	TABLET	5 mg	SUBLINGUAL	ANDA	29 sections
Asenapine	Human Prescription Drug Label	1	46708-198	TABLET	5 mg	SUBLINGUAL	ANDA	29 sections
Asenapine	Human Prescription Drug Label	1	46708-199	TABLET	10 mg	SUBLINGUAL	ANDA	29 sections
Asenapine	Human Prescription Drug Label	1	46708-199	TABLET	10 mg	SUBLINGUAL	ANDA	29 sections
Asenapine	Human Prescription Drug Label	1	46708-544	TABLET	2.50 mg	SUBLINGUAL	ANDA	29 sections
Asenapine	Human Prescription Drug Label	1	46708-544	TABLET	2.50 mg	SUBLINGUAL	ANDA	29 sections

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