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

Stem definition	Drug id	CAS RN
psychoactive	1982	132539-06-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: olanzapine pamoate olanzapine embonate zyprexa relprevv olanzapine pamoate monohydrate olanzapine zyprexa LY 170053 LY-170053	The mechanism of action of olanzapine, as with other drugs having efficacy in schizophrenia, is unknown. However, it has been proposed that this drug’s efficacy in schizophrenia is mediated through a combination of dopamine and serotonin type 2 (5HT2) antagonism. The mechanism of action of olanzapine in the treatment of acute manic or mixed episodes associated with bipolar I disorder is unknown. Molecular weight: 312.44 Formula: C17H20N4S CLOGP: 2.86 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 30.87 ALOGS: -3.52 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

olanzapine pamoate
olanzapine embonate
zyprexa relprevv
olanzapine pamoate monohydrate
olanzapine
zyprexa
LY 170053
LY-170053

The mechanism of action of olanzapine, as with other drugs having efficacy in schizophrenia, is unknown. However, it has been proposed that this drug’s efficacy in schizophrenia is mediated through a combination of dopamine and serotonin type 2 (5HT2) antagonism. The mechanism of action of olanzapine in the treatment of acute manic or mixed episodes associated with bipolar I disorder is unknown.

Molecular weight: 312.44
Formula: C17H20N4S
CLOGP: 2.86
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 30.87
ALOGS: -3.52
ROTB: 0

Status: OFP

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

Drug dosage:

Dose	Unit	Route
10	mg	O
10	mg	P
10	mg	P

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	7 %	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	60 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.69 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	0.01 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Sept. 27, 1996	EMA	Eli Lilly Nederland B.V.
Sept. 30, 1996	FDA	LILLY

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
Neuroleptic malignant syndrome	1591.83	11.92	638	104877	11418	63372089
Suicide attempt	1304.19	11.92	960	104555	59958	63323549
Sedation	1186.42	11.92	762	104753	38047	63345460
Intentional overdose	995.67	11.92	890	104625	73262	63310245
Extrapyramidal disorder	893.50	11.92	438	105077	12846	63370661
Dystonia	891.88	11.92	443	105072	13376	63370131
Sexual dysfunction	877.21	11.92	314	105201	4045	63379462
Blood prolactin abnormal	870.18	11.92	286	105229	2793	63380714
Akathisia	804.61	11.92	363	105152	8783	63374724
Sopor	774.70	11.92	474	105041	21690	63361817

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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
Neuroleptic malignant syndrome	1945.72	12.12	998	107124	16936	34831873
Sedation	1235.89	12.12	784	107338	20222	34828587
Post-injection delirium sedation syndrome	1160.10	12.12	276	107846	218	34848591
Psychotic disorder	895.17	12.12	682	107440	23770	34825039
Akathisia	744.58	12.12	404	107718	7705	34841104
Extrapyramidal disorder	701.11	12.12	458	107664	12422	34836387
Agitation	698.86	12.12	874	107248	56525	34792284
Suicide attempt	693.99	12.12	724	107398	38392	34810417
Weight increased	664.54	12.12	1099	107023	91934	34756875
Overdose	629.36	12.12	1060	107062	89999	34758810

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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
Neuroleptic malignant syndrome	3287.26	11.74	1482	178205	26077	79538624
Sedation	1985.79	11.74	1314	178373	50581	79514120
Suicide attempt	1602.25	11.74	1396	178291	81536	79483165
Post-injection delirium sedation syndrome	1450.06	11.74	322	179365	263	79564438
Extrapyramidal disorder	1412.11	11.74	785	178902	21894	79542807
Agitation	1259.57	11.74	1328	178359	98387	79466314
Psychotic disorder	1253.32	11.74	908	178779	40494	79524207
Akathisia	1239.72	11.74	603	179084	12656	79552045
Sopor	1140.63	11.74	785	178902	32225	79532476
Dystonia	1066.65	11.74	641	179046	20758	79543943

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FDA Adverse Event Reporting System (Pediatric)

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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
Exposure during pregnancy	31.88	24.96	40	523	1294	87935
Fever neonatal	26.71	24.96	8	555	9	89220

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Pharmacologic Action:

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Source	Code	Description
ATC	N05AH03	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Diazepines, oxazepines, thiazepines and oxepines
ATC	N05AH53	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Diazepines, oxazepines, thiazepines and oxepines
CHEBI has role	CHEBI:37956	antihistamines
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:48561	dopaminergic antagonists
CHEBI has role	CHEBI:48876	muscarinic antagonists
CHEBI has role	CHEBI:50919	antiemetico
CHEBI has role	CHEBI:50949	SSRI
CHEBI has role	CHEBI:65191	atypical antipsychotic agent
FDA EPC	N0000175430	Atypical Antipsychotic

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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 disorder in remission	indication	85248005
Bipolar affective disorder, current episode manic	indication	191618007
Bipolar affective disorder, current episode depression	indication	191627008	DOID:3312
Major depressive disorder	indication	370143000
Depression Treatment Adjunct	indication
Agitation associated with Bipolar Mania	indication
Agitation associated with Schizophrenia	indication
Nausea and vomiting	off-label use	16932000

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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	7.59	Basic
pKa2	5.72	Basic
pKa3	0.66	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
10MG;EQ 10MG BASE	LYBALVI	ALKERMES INC	N213378	May 28, 2021	RX	TABLET	ORAL	10300054	Aug. 23, 2031	METHOD OF TREATING BIPOLAR DISORDER BY ADMINISTERING THE ATYPICAL ANTIPSYCHOTIC OLANZAPINE AND SAMIDORPHAN
10MG;EQ 10MG BASE	LYBALVI	ALKERMES INC	N213378	May 28, 2021	RX	TABLET	ORAL	10300054	Aug. 23, 2031	METHOD OF TREATING SCHIZOPHRENIA BY ADMINISTERING THE ATYPICAL ANTIPSYCHOTIC OLANZAPINE AND SAMIDORPHAN
10MG;EQ 10MG BASE	LYBALVI	ALKERMES INC	N213378	May 28, 2021	RX	TABLET	ORAL	10716785	Aug. 23, 2031	METHOD OF TREATING BIPOLAR DISORDER BY ADMINISTERING THE ATYPICAL ANTIPSYCHOTIC OLANZAPINE AND SAMIDORPHAN, WITH REDUCED ANTIPSYCHOTIC INDUCED WEIGHT GAIN
10MG;EQ 10MG BASE	LYBALVI	ALKERMES INC	N213378	May 28, 2021	RX	TABLET	ORAL	10716785	Aug. 23, 2031	METHOD OF TREATING SCHIZOPHRENIA BY ADMINISTERING THE ATYPICAL ANTIPSYCHOTIC OLANZAPINE AND SAMIDORPHAN, WITH REDUCED ANTIPSYCHOTIC INDUCED WEIGHT GAIN
10MG;EQ 10MG BASE	LYBALVI	ALKERMES INC	N213378	May 28, 2021	RX	TABLET	ORAL	11185541	Aug. 23, 2031	METHOD OF TREATING SCHIZOPHRENIA BY ADMINISTERING THE ATYPICAL ANTIPSYCHOTIC OLANZAPINE AND SAMIDORPHAN
10MG;EQ 10MG BASE	LYBALVI	ALKERMES INC	N213378	May 28, 2021	RX	TABLET	ORAL	11241425	Aug. 23, 2031	METHOD OF TREATING BIPOLAR DISORDER BY ADMINISTERING THE ATYPICAL ANTIPSYCHOTIC OLANZAPINE AND SAMIDORPHAN, WITH REDUCED ANTIPSYCHOTIC INDUCED WEIGHT GAIN
10MG;EQ 10MG BASE	LYBALVI	ALKERMES INC	N213378	May 28, 2021	RX	TABLET	ORAL	11351166	Aug. 23, 2031	METHOD OF TREATING BIPOLAR DISORDER BY ADMINISTERING THE ATYPICAL ANTIPSYCHOTIC OLANZAPINE AND SAMIDORPHAN
10MG;EQ 10MG BASE	LYBALVI	ALKERMES INC	N213378	May 28, 2021	RX	TABLET	ORAL	11351166	Aug. 23, 2031	METHOD OF TREATING SCHIZOPHRENIA BY ADMINISTERING THE ATYPICAL ANTIPSYCHOTIC OLANZAPINE AND SAMIDORPHAN
10MG;EQ 10MG BASE	LYBALVI	ALKERMES INC	N213378	May 28, 2021	RX	TABLET	ORAL	9126977	Aug. 23, 2031	METHOD OF TREATING BIPOLAR DISORDER BY ADMINISTERING THE ATYPICAL ANTIPSYCHOTIC OLANZAPINE AND SAMIDORPHAN, WITH REDUCED ANTIPSYCHOTIC INDUCED WEIGHT GAIN
10MG;EQ 10MG BASE	LYBALVI	ALKERMES INC	N213378	May 28, 2021	RX	TABLET	ORAL	9126977	Aug. 23, 2031	METHOD OF TREATING SCHIZOPHRENIA BY ADMINISTERING THE ATYPICAL ANTIPSYCHOTIC OLANZAPINE AND SAMIDORPHAN, WITH REDUCED ANTIPSYCHOTIC INDUCED WEIGHT GAIN

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
10MG;EQ 10MG BASE	LYBALVI	ALKERMES INC	N213378	May 28, 2021	RX	TABLET	ORAL	May 28, 2026	NEW CHEMICAL ENTITY
15MG;EQ 10MG BASE	LYBALVI	ALKERMES INC	N213378	May 28, 2021	RX	TABLET	ORAL	May 28, 2026	NEW CHEMICAL ENTITY
20MG;EQ 10MG BASE	LYBALVI	ALKERMES INC	N213378	May 28, 2021	RX	TABLET	ORAL	May 28, 2026	NEW CHEMICAL ENTITY
5MG;EQ 10MG BASE	LYBALVI	ALKERMES INC	N213378	May 28, 2021	RX	TABLET	ORAL	May 28, 2026	NEW CHEMICAL ENTITY

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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	8.32	WOMBAT-PK	CHEMBL
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	Ki	8.52	WOMBAT-PK	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	7.40	WOMBAT-PK
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.49	WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.74	WOMBAT-PK
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	6.26	DRUG MATRIX
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Kd	5.90	CHEMBL
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	7.92	WOMBAT-PK
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	ANTAGONIST	Ki	7.96	WOMBAT-PK
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	8.10	WOMBAT-PK

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External reference:

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ID	Source
006204	NDDF
013309	NDDF
108441004	SNOMEDCT_US
1294588	RXNORM
135398745	PUBCHEM_CID
169390	MMSL
172501	MMSL
221373-18-8	SECONDARY_CAS_RN
386849001	SNOMEDCT_US
39248	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Symbyax	HUMAN PRESCRIPTION DRUG LABEL	2	0002-3230	CAPSULE	3 mg	ORAL	NDA	34 sections
Symbyax	HUMAN PRESCRIPTION DRUG LABEL	2	0002-3230	CAPSULE	3 mg	ORAL	NDA	34 sections
Symbyax	HUMAN PRESCRIPTION DRUG LABEL	2	0002-3231	CAPSULE	6 mg	ORAL	NDA	34 sections
Symbyax	HUMAN PRESCRIPTION DRUG LABEL	2	0002-3231	CAPSULE	6 mg	ORAL	NDA	34 sections
Zyprexa	HUMAN PRESCRIPTION DRUG LABEL	1	0002-4112	TABLET	2.50 mg	ORAL	NDA	36 sections
Zyprexa	HUMAN PRESCRIPTION DRUG LABEL	1	0002-4112	TABLET	2.50 mg	ORAL	NDA	36 sections
Zyprexa	HUMAN PRESCRIPTION DRUG LABEL	1	0002-4112	TABLET	2.50 mg	ORAL	NDA	36 sections
Zyprexa	HUMAN PRESCRIPTION DRUG LABEL	1	0002-4115	TABLET	5 mg	ORAL	NDA	36 sections
Zyprexa	HUMAN PRESCRIPTION DRUG LABEL	1	0002-4115	TABLET	5 mg	ORAL	NDA	36 sections
Zyprexa	HUMAN PRESCRIPTION DRUG LABEL	1	0002-4115	TABLET	5 mg	ORAL	NDA	36 sections

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