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

Stem definition	Drug id	CAS RN
serotonin and/or norepinephrine reuptake inhibitors, fluoxetine derivatives	4806	508233-74-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: vortioxetine-DL-lactate vortioxetine DL-lactate brintellix Lu AA21004 vortioxetine vortioxetine hydrobromide	A piperazine derivative that acts as a serotonin reuptake inhibitor, as a 5-HT3 receptor antagonist, and 5-HT1A receptor agonist. It is used for the treatment of anxiety and depression. Molecular weight: 298.45 Formula: C18H22N2S CLOGP: 4.72 LIPINSKI: 0 HAC: 2 HDO: 1 TPSA: 15.27 ALOGS: -4.92 ROTB: 3 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

vortioxetine-DL-lactate
vortioxetine DL-lactate
brintellix
Lu AA21004
vortioxetine
vortioxetine hydrobromide

A piperazine derivative that acts as a serotonin reuptake inhibitor, as a 5-HT3 receptor antagonist, and 5-HT1A receptor agonist. It is used for the treatment of anxiety and depression.

Molecular weight: 298.45
Formula: C18H22N2S
CLOGP: 4.72
LIPINSKI: 0
HAC: 2
HDO: 1
TPSA: 15.27
ALOGS: -4.92
ROTB: 3

Status: ONP

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

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	35.30 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	5.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	72 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company
Sept. 20, 2019	PMDA	Takeda Pharmaceutical Company Limited
Sept. 30, 2013	FDA	TAKEDA PHARMS USA
Dec. 18, 2013	EMA

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
Suicidal ideation	512.50	17.42	271	16086	62150	63410515
Nausea	357.51	17.42	717	15640	853754	62618911
Serotonin syndrome	200.19	17.42	112	16245	28570	63444095
Suicide attempt	184.73	17.42	141	16216	60777	63411888
No adverse event	159.98	17.42	111	16246	41294	63431371
Pruritus	146.59	17.42	301	16056	361152	63111513
Anxiety	132.24	17.42	216	16141	217325	63255340
Reaction to excipient	128.52	17.42	36	16321	1428	63471237
Irritability	122.48	17.42	85	16272	31609	63441056
Sopor	101.35	17.42	66	16291	22098	63450567
Somnolence	98.59	17.42	170	16187	178515	63294150
Intentional overdose	96.69	17.42	107	16250	74045	63398620
Feeling abnormal	96.42	17.42	152	16205	148240	63324425
Mania	90.91	17.42	50	16307	12317	63460348
Anger	90.58	17.42	50	16307	12406	63460259
Tremor	75.77	17.42	128	16229	132111	63340554
Nightmare	75.36	17.42	52	16305	19142	63453523
Intentional self-injury	74.60	17.42	58	16299	25629	63447036
Agitation	74.07	17.42	84	16273	59673	63412992
Libido increased	69.68	17.42	22	16335	1323	63471342
Decompression sickness	63.02	17.42	12	16345	78	63472587
Depression	62.77	17.42	149	16208	196343	63276322
Drug abuse	62.60	17.42	85	16272	72433	63400232
Abnormal dreams	62.47	17.42	37	16320	10479	63462186
Product administered to patient of inappropriate age	60.63	17.42	25	16332	3243	63469422
Sedation	59.39	17.42	61	16296	38748	63433917
Akathisia	59.14	17.42	34	16323	9112	63463553
Wrong technique in product usage process	58.30	17.42	76	16281	62264	63410401
Soft tissue injury	57.44	17.42	20	16337	1632	63471033
Insomnia	57.00	17.42	152	16205	215100	63257565
Sexual dysfunction	56.84	17.42	26	16331	4333	63468332
Crying	55.70	17.42	47	16310	23296	63449369
Hostility	54.99	17.42	20	16337	1852	63470813
Urinary retention	54.47	17.42	52	16305	30249	63442416
Post-traumatic neck syndrome	53.00	17.42	20	16337	2054	63470611
Vomiting	51.95	17.42	282	16075	559335	62913330
Sternal fracture	51.38	17.42	20	16337	2234	63470431
Bradykinesia	49.57	17.42	25	16332	5163	63467502
Electrocardiogram QT prolonged	48.69	17.42	68	16289	59462	63413203
Myoglobinuria	48.62	17.42	12	16345	288	63472377
Overdose	47.76	17.42	97	16260	114981	63357684
Parkinsonism	47.50	17.42	31	16326	10408	63462257
Weight increased	47.16	17.42	161	16196	260631	63212034
Peripheral circulatory failure	46.71	17.42	15	16342	953	63471712
Joint swelling	45.42	17.42	14	16343	327652	63145013
Hallucination, auditory	43.99	17.42	32	16325	12792	63459873
Product use in unapproved indication	43.93	17.42	123	16234	178957	63293708
Drug interaction	43.66	17.42	144	16213	228987	63243678
Drug intolerance	43.11	17.42	13	16344	308648	63164017
Pneumonia	42.94	17.42	33	16324	456734	63015931
Inappropriate antidiuretic hormone secretion	42.91	17.42	34	16323	15428	63457237
Hyperhidrosis	42.51	17.42	89	16268	107747	63364918
Hyponatraemia	40.27	17.42	89	16268	111811	63360854
Rheumatoid arthritis	38.64	17.42	9	16348	253810	63218855
Neuroglycopenia	38.54	17.42	11	16346	467	63472198
Maternal exposure during pregnancy	37.30	17.42	6	16351	220056	63252609
Infusion related reaction	36.80	17.42	9	16348	245512	63227153
Multiple drug therapy	36.10	17.42	18	16339	3628	63469037
Dizziness	36.05	17.42	211	16146	429714	63042951
Muscle twitching	35.81	17.42	34	16323	19634	63453031
Restlessness	35.79	17.42	41	16316	29412	63443253
Glossodynia	34.95	17.42	3	16354	178873	63293792
Systemic lupus erythematosus	34.73	17.42	6	16351	208912	63263753
Hepatic infiltration eosinophilic	34.57	17.42	6	16351	21	63472644
Swelling	34.33	17.42	14	16343	275364	63197301
Personality disorder	33.35	17.42	20	16337	5791	63466874
Psychomotor hyperactivity	32.97	17.42	25	16332	10638	63462027
Arthropathy	32.57	17.42	10	16347	234782	63237883
Muscle rigidity	31.30	17.42	25	16332	11475	63461190
Completed suicide	30.86	17.42	95	16262	145578	63327087
Stupor	30.63	17.42	17	16340	4258	63468407
Pain	30.55	17.42	94	16263	740534	62732131
Treatment failure	30.40	17.42	7	16350	199036	63273629
Pregnancy	29.99	17.42	42	16315	36794	63435871
Infection	29.63	17.42	11	16346	229162	63243503
Middle insomnia	29.22	17.42	25	16332	12618	63460047
Major depression	27.48	17.42	20	16337	7998	63464667
Migraine	27.32	17.42	73	16284	103273	63369392
Antipsychotic drug level above therapeutic	26.44	17.42	10	16347	1033	63471632
Hyperaldosteronism	26.00	17.42	7	16350	239	63472426
Dementia	26.00	17.42	28	16329	18766	63453899
Energy increased	25.55	17.42	13	16344	2734	63469931
Dyspnoea	25.12	17.42	87	16270	661226	62811439
Concussion	24.95	17.42	20	16337	9224	63463441
Dissociation	24.81	17.42	13	16344	2906	63469759
Headache	24.61	17.42	260	16097	632981	62839684
Drug screen false positive	24.32	17.42	9	16348	875	63471790
Vertigo	24.25	17.42	50	16307	59837	63412828
Contraindicated product administered	24.13	17.42	13	16344	217635	63255030
Prescription form tampering	24.02	17.42	8	16349	570	63472095
Hypersensitivity	24.01	17.42	24	16333	292661	63180004
Body temperature increased	23.96	17.42	38	16319	37154	63435511
Tachyphrenia	23.77	17.42	10	16347	1364	63471301
Hallucination	23.67	17.42	47	16310	54770	63417895
Mental disorder	23.29	17.42	31	16326	25888	63446777
Anaemia	23.01	17.42	25	16332	293405	63179260
Gastric polyps	22.93	17.42	13	16344	3392	63469273
Restless legs syndrome	22.85	17.42	26	16331	18505	63454160
Antipsychotic drug level increased	22.82	17.42	13	16344	3422	63469243
Haemoglobin decreased	22.44	17.42	5	16352	145480	63327185
Labelled drug-drug interaction issue	22.40	17.42	9	16348	1092	63471573
Product name confusion	22.36	17.42	5	16352	77	63472588
Miosis	22.21	17.42	17	16340	7336	63465329
Tardive dyskinesia	22.11	17.42	18	16339	8484	63464181
Drug hypersensitivity	21.68	17.42	29	16328	310658	63162007
Lymphocytic hypophysitis	21.61	17.42	6	16351	230	63472435
Drug titration error	21.26	17.42	8	16349	815	63471850
General physical health deterioration	20.94	17.42	13	16344	201389	63271276
Memory impairment	20.24	17.42	66	16291	104192	63368473
Self-injurious ideation	20.23	17.42	11	16346	2648	63470017
Dysgeusia	20.10	17.42	40	16317	46670	63425995
Thrombocytopenia	19.96	17.42	7	16350	151150	63321515
Polydipsia	19.77	17.42	12	16345	3552	63469113
Bacterial toxaemia	19.71	17.42	3	16354	3	63472662
Poor quality sleep	19.71	17.42	25	16332	19910	63452755
Death	19.63	17.42	42	16315	374339	63098326
Aggression	19.44	17.42	27	16330	23471	63449194
Panic attack	18.98	17.42	26	16331	22305	63450360
Mydriasis	18.66	17.42	19	16338	11937	63460728
Cor pulmonale acute	18.42	17.42	6	16351	399	63472266
Withdrawal syndrome	18.09	17.42	24	16333	19973	63452692
Initial insomnia	18.08	17.42	14	16343	6143	63466522
Acute kidney injury	17.96	17.42	25	16332	263390	63209275
Constipation	17.89	17.42	109	16248	224834	63247831
Hypomania	17.74	17.42	14	16343	6316	63466349
Lower respiratory tract infection	17.69	17.42	6	16351	132301	63340364
Contraindicated product prescribed	17.58	17.42	8	16349	1317	63471348
Libido decreased	17.45	17.42	10	16347	2662	63470003

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
Suicidal ideation	339.15	25.57	158	6069	40230	34910474
Completed suicide	178.39	25.57	144	6083	98024	34852680
Nausea	101.11	25.57	200	6027	339708	34610996
Sexual dysfunction	90.06	25.57	36	6191	6267	34944437
Suicide attempt	89.64	25.57	66	6161	39050	34911654
Erectile dysfunction	81.75	25.57	49	6178	20588	34930116
Dystonic tremor	80.32	25.57	16	6211	203	34950501
Anxiety	72.81	25.57	89	6138	99339	34851365
Intentional overdose	72.63	25.57	61	6166	43613	34907091
Intentional self-injury	52.71	25.57	32	6195	13739	34936965
Dissociation	52.22	25.57	17	6210	1641	34949063
Product use in unapproved indication	51.20	25.57	82	6145	117417	34833287
Mania	49.50	25.57	27	6200	9484	34941220
Urinary retention	46.97	25.57	44	6183	36244	34914460
Depressed mood	45.12	25.57	33	6194	19284	34931420
Feeling abnormal	43.63	25.57	55	6172	63180	34887524
Serotonin syndrome	41.97	25.57	32	6195	19901	34930803
Drug ineffective	41.11	25.57	175	6052	456576	34494128
No adverse event	38.02	25.57	32	6195	22895	34927809
Product administered to patient of inappropriate age	34.23	25.57	15	6212	3276	34947428
Irritability	33.99	25.57	31	6196	24659	34926045
Sopor	33.58	25.57	23	6204	12113	34938591
Agitation	33.50	25.57	46	6181	57353	34893351
Disturbance in attention	32.68	25.57	31	6196	25914	34924790
Vomiting	32.25	25.57	107	6120	247514	34703190
Arterial disorder	32.05	25.57	11	6216	1248	34949456
Anorgasmia	31.98	25.57	10	6217	847	34949857
Anger	31.65	25.57	22	6205	11862	34938842
Tremor	31.06	25.57	54	6173	82533	34868171
Abulia	31.01	25.57	9	6218	591	34950113
Thinking abnormal	30.76	25.57	17	6210	6120	34944584
Feeling of despair	30.69	25.57	10	6217	967	34949737
Restlessness	29.37	25.57	29	6198	25453	34925251
Prescribed overdose	29.04	25.57	20	6207	10627	34940077
Tardive dyskinesia	28.92	25.57	16	6211	5774	34944930
Reaction to excipient	27.84	25.57	8	6219	507	34950197
Insomnia	26.88	25.57	58	6169	103849	34846855
Akathisia	26.38	25.57	17	6210	8092	34942612
Depression	26.04	25.57	55	6172	97043	34853661

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
Suicidal ideation	598.71	17.83	306	17398	76034	79650650
Nausea	237.49	17.83	598	17106	956598	78770086
Suicide attempt	233.66	17.83	173	17531	82759	79643925
Serotonin syndrome	201.13	17.83	125	17579	44902	79681782
Anxiety	147.26	17.83	225	17479	248287	79478397
Intentional overdose	144.48	17.83	146	17558	105814	79620870
Sopor	140.74	17.83	89	17615	32921	79693763
Completed suicide	139.28	17.83	218	17486	245549	79481135
Irritability	118.39	17.83	87	17617	41057	79685627
Intentional self-injury	108.11	17.83	75	17629	32344	79694340
Product administered to patient of inappropriate age	93.55	17.83	38	17666	5515	79721169
Urinary retention	88.26	17.83	84	17620	56546	79670138
Tremor	85.49	17.83	143	17561	169940	79556744
Pruritus	83.11	17.83	233	17471	394415	79332269
Feeling abnormal	80.20	17.83	134	17570	159065	79567619
Mania	79.73	17.83	50	17654	18210	79708474
Sexual dysfunction	78.22	17.83	37	17667	7726	79718958
Dystonic tremor	76.80	17.83	16	17688	203	79726481
Product use in unapproved indication	73.77	17.83	168	17536	250191	79476493
Sedation	69.73	17.83	71	17633	51824	79674860
Depression	67.80	17.83	149	17555	216641	79510043
Somnolence	67.79	17.83	158	17546	238823	79487861
Anger	67.50	17.83	44	17660	17118	79709566
Agitation	67.13	17.83	96	17608	99619	79627065
Libido increased	64.31	17.83	22	17682	1979	79724705
Decompression sickness	64.28	17.83	12	17692	82	79726602
Nightmare	64.01	17.83	50	17654	25811	79700873
No adverse event	63.39	17.83	58	17646	37134	79689550
Dissociation	59.22	17.83	25	17679	3996	79722688
Soft tissue injury	58.88	17.83	20	17684	1761	79724923
Restlessness	57.77	17.83	61	17643	46431	79680253
Insomnia	56.75	17.83	150	17554	245020	79481664
Post-traumatic neck syndrome	55.71	17.83	20	17684	2074	79724610
Akathisia	54.62	17.83	35	17669	13224	79713460
Drug abuse	54.48	17.83	115	17589	162576	79564108
Erectile dysfunction	53.80	17.83	36	17668	14628	79712056
Hostility	53.79	17.83	20	17684	2290	79724394
Inappropriate antidiuretic hormone secretion	52.76	17.83	45	17659	26268	79700416
Sternal fracture	52.02	17.83	20	17684	2510	79724174
Drug interaction	51.40	17.83	205	17499	414978	79311706
Bradykinesia	50.87	17.83	28	17676	8015	79718669
Hyperhidrosis	50.62	17.83	107	17597	151385	79575299
Electrocardiogram QT prolonged	49.43	17.83	79	17625	90307	79636377
Peripheral circulatory failure	46.41	17.83	15	17689	1131	79725553
Hyponatraemia	44.41	17.83	112	17592	177736	79548948
Abnormal dreams	44.25	17.83	29	17675	11383	79715301
Pneumonia	44.16	17.83	49	17655	660197	79066487
Vomiting	44.00	17.83	275	17429	665553	79061131
Personality disorder	43.35	17.83	23	17681	6123	79720561
Crying	41.35	17.83	37	17667	23006	79703678
Antipsychotic drug level increased	41.19	17.83	22	17682	5935	79720749
Hallucination, auditory	40.69	17.83	35	17669	20658	79706026
Dizziness	40.25	17.83	226	17478	526215	79200469
Neuroglycopenia	40.03	17.83	11	17693	473	79726211
Tardive dyskinesia	38.89	17.83	26	17678	10545	79716139
Weight increased	37.56	17.83	141	17563	277245	79449439
Multiple drug therapy	36.73	17.83	18	17686	4060	79722624
Parkinsonism	36.64	17.83	30	17674	16554	79710130
Labelled drug-drug interaction issue	35.73	17.83	13	17691	1400	79725284
Acute kidney injury	35.30	17.83	38	17666	519366	79207318
Myoglobinuria	34.98	17.83	12	17692	1088	79725596
Drug intolerance	34.77	17.83	8	17696	264111	79462573
Dyspnoea	34.71	17.83	88	17616	856937	78869747
Disturbance in attention	34.30	17.83	49	17655	50752	79675932
Wrong technique in product usage process	34.28	17.83	60	17644	73815	79652869
Underdose	33.42	17.83	39	17665	33112	79693572
Overdose	33.15	17.83	103	17601	184103	79542581
Major depression	32.83	17.83	22	17682	8958	79717726
Mental disorder	31.85	17.83	37	17667	31265	79695419
Migraine	31.79	17.83	64	17640	87429	79639255
Haemoglobin decreased	30.73	17.83	6	17698	222113	79504571
Vertigo	30.62	17.83	55	17649	69027	79657657
Panic attack	30.48	17.83	32	17672	24184	79702500
Febrile neutropenia	30.40	17.83	7	17697	230992	79495692
Psychomotor hyperactivity	30.12	17.83	27	17677	16822	79709862
Anorgasmia	29.72	17.83	11	17693	1243	79725441
Libido decreased	29.52	17.83	17	17687	5304	79721380
Concussion	29.38	17.83	21	17683	9482	79717202
Anaemia	28.65	17.83	34	17670	444981	79281703
Poor quality sleep	28.55	17.83	30	17674	22692	79703992
Infusion related reaction	28.33	17.83	8	17696	230229	79496455
Headache	27.64	17.83	243	17461	653529	79073155
Joint swelling	27.37	17.83	15	17689	288631	79438053
Depressed mood	27.35	17.83	43	17661	48437	79678247
Dystonia	26.44	17.83	28	17676	21371	79705313
Muscle twitching	26.42	17.83	30	17674	24734	79701950
Bipolar disorder	26.08	17.83	18	17686	7689	79718995
Stupor	25.52	17.83	17	17687	6855	79719829
Infection	25.28	17.83	11	17693	241701	79484983
Arterial disorder	24.81	17.83	11	17693	1979	79724705
Death	24.60	17.83	56	17648	566458	79160226
Muscle rigidity	24.53	17.83	26	17678	19856	79706828
Abulia	24.37	17.83	9	17695	1011	79725673
Tachyphrenia	24.34	17.83	11	17693	2069	79724615
Prescription form tampering	23.80	17.83	7	17697	385	79726299
Gastric polyps	23.57	17.83	13	17691	3734	79722950
Hallucination	23.50	17.83	56	17648	85689	79640995
Middle insomnia	23.44	17.83	23	17681	16046	79710638
Hyperaldosteronism	22.70	17.83	7	17697	453	79726231
Drug hypersensitivity	22.44	17.83	20	17684	298896	79427788
Arthropathy	22.07	17.83	6	17698	177105	79549579
Body temperature increased	21.81	17.83	37	17667	44383	79682301
Disease progression	21.60	17.83	7	17697	184355	79542329
Sepsis	21.48	17.83	17	17687	269411	79457273
Activation syndrome	21.38	17.83	6	17698	279	79726405
Antipsychotic drug level above therapeutic	21.22	17.83	10	17694	2070	79724614
Lymphocytic hypophysitis	21.20	17.83	7	17697	565	79726119
Rheumatoid arthritis	21.00	17.83	10	17694	208460	79518224
Dysgeusia	20.97	17.83	42	17662	57135	79669549
Swelling	20.92	17.83	11	17693	216700	79509984
Hypersensitivity	20.34	17.83	17	17687	262222	79464462
Stomatitis	20.22	17.83	4	17700	146753	79579931
General physical health deterioration	19.96	17.83	19	17685	275219	79451465
Mydriasis	19.89	17.83	22	17682	17621	79709063
Drug titration error	19.73	17.83	8	17696	1154	79725530
Energy increased	19.59	17.83	11	17693	3271	79723413
Thinking abnormal	19.50	17.83	19	17685	13142	79713542
Restless legs syndrome	19.20	17.83	23	17681	20069	79706615
Dissociative disorder	18.72	17.83	7	17697	814	79725870
Self-injurious ideation	18.54	17.83	11	17693	3627	79723057
Renal impairment	18.47	17.83	6	17698	157777	79568907
Initial insomnia	18.44	17.83	14	17690	6924	79719760
Feeling of despair	18.33	17.83	10	17694	2811	79723873
Negative thoughts	18.30	17.83	8	17696	1391	79725293
Feeling jittery	18.03	17.83	18	17686	12823	79713861
Blood creatinine increased	17.97	17.83	6	17698	155051	79571633
Apathy	17.87	17.83	18	17686	12959	79713725
Memory impairment	17.84	17.83	60	17644	111674	79615010

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N06AX26	NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Other antidepressants
MeSH PA	D014151	Anti-Anxiety Agents
MeSH PA	D000928	Antidepressive Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D014179	Neurotransmitter Uptake Inhibitors
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D017367	Selective Serotonin Reuptake Inhibitors
MeSH PA	D058825	Serotonin 5-HT1 Receptor Agonists
MeSH PA	D058831	Serotonin 5-HT3 Receptor Antagonists
MeSH PA	D018490	Serotonin Agents
MeSH PA	D012702	Serotonin Antagonists
MeSH PA	D017366	Serotonin Receptor Agonists
MeSH PA	D014149	Tranquilizing Agents
CHEBI has role	CHEBI:35469	antidepressants
CHEBI has role	CHEBI:35474	anti-anxiety agents
CHEBI has role	CHEBI:35941	serotonin agonists
CHEBI has role	CHEBI:48279	serotonin antagonists

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

Disease	Relation	SNOMED_ID	DOID
Major depressive disorder	indication	370143000
Monoamine oxidase inhibitors	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.02	Basic
pKa2	1.85	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 10MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	7144884	June 17, 2026	METHOD OF TREATING AN AFFECTIVE DISORDER SUCH AS DEPRESSION
EQ 15MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	DISCN	TABLET	ORAL	7144884	June 17, 2026	METHOD OF TREATING AN AFFECTIVE DISORDER SUCH AS DEPRESSION
EQ 20MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	7144884	June 17, 2026	METHOD OF TREATING AN AFFECTIVE DISORDER SUCH AS DEPRESSION
EQ 5MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	7144884	June 17, 2026	METHOD OF TREATING AN AFFECTIVE DISORDER SUCH AS DEPRESSION
EQ 10MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	11458134	June 15, 2027	USE OF TRINTELLIX FOR THE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD) IN ADULTS
EQ 10MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	8969355	June 15, 2027	METHOD OF TREATING DEPRESSION OR MAJOR DEPRESSIVE DISORDER
EQ 10MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9125908	June 15, 2027	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE PROCESSING SPEED, AN ASPECT OF COGNITIVE FUNCTION
EQ 10MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9125909	June 15, 2027	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE PROCESSING SPEED, AN ASPECT OF COGNITIVE FUNCTION
EQ 10MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9125910	June 15, 2027	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE PROCESSING SPEED, AN ASPECT OF COGNITIVE FUNCTION
EQ 10MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9227946	June 15, 2027	METHOD OF TREATING DEPRESSION OR MAJOR DEPRESSIVE DISORDER
EQ 10MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9861630	June 15, 2027	METHOD OF TREATING DEPRESSION OR MAJOR DEPRESSIVE DISORDER
EQ 15MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	DISCN	TABLET	ORAL	11458134	June 15, 2027	USE OF TRINTELLIX FOR THE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD) IN ADULTS
EQ 15MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	DISCN	TABLET	ORAL	8969355	June 15, 2027	METHOD OF TREATING DEPRESSION OR MAJOR DEPRESSIVE DISORDER
EQ 15MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	DISCN	TABLET	ORAL	9125908	June 15, 2027	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE PROCESSING SPEED, AN ASPECT OF COGNITIVE FUNCTION
EQ 15MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	DISCN	TABLET	ORAL	9125909	June 15, 2027	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE PROCESSING SPEED, AN ASPECT OF COGNITIVE FUNCTION
EQ 15MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	DISCN	TABLET	ORAL	9125910	June 15, 2027	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE PROCESSING SPEED, AN ASPECT OF COGNITIVE FUNCTION
EQ 15MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	DISCN	TABLET	ORAL	9227946	June 15, 2027	METHOD OF TREATING DEPRESSION OR MAJOR DEPRESSIVE DISORDER
EQ 15MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	DISCN	TABLET	ORAL	9861630	June 15, 2027	METHOD OF TREATING DEPRESSION OR MAJOR DEPRESSIVE DISORDER
EQ 20MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	11458134	June 15, 2027	USE OF TRINTELLIX FOR THE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD) IN ADULTS
EQ 20MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	8969355	June 15, 2027	METHOD OF TREATING DEPRESSION OR MAJOR DEPRESSIVE DISORDER
EQ 20MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9125908	June 15, 2027	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE PROCESSING SPEED, AN ASPECT OF COGNITIVE FUNCTION
EQ 20MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9125909	June 15, 2027	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE PROCESSING SPEED, AN ASPECT OF COGNITIVE FUNCTION
EQ 20MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9125910	June 15, 2027	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE PROCESSING SPEED, AN ASPECT OF COGNITIVE FUNCTION
EQ 20MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9227946	June 15, 2027	METHOD OF TREATING DEPRESSION OR MAJOR DEPRESSIVE DISORDER
EQ 20MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9861630	June 15, 2027	METHOD OF TREATING DEPRESSION OR MAJOR DEPRESSIVE DISORDER
EQ 5MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	11458134	June 15, 2027	USE OF TRINTELLIX FOR THE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD) IN ADULTS
EQ 5MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	8969355	June 15, 2027	METHOD OF TREATING DEPRESSION OR MAJOR DEPRESSIVE DISORDER
EQ 5MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9125908	June 15, 2027	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE PROCESSING SPEED, AN ASPECT OF COGNITIVE FUNCTION
EQ 5MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9125909	June 15, 2027	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE PROCESSING SPEED, AN ASPECT OF COGNITIVE FUNCTION
EQ 5MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9125910	June 15, 2027	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE PROCESSING SPEED, AN ASPECT OF COGNITIVE FUNCTION
EQ 5MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9227946	June 15, 2027	METHOD OF TREATING DEPRESSION OR MAJOR DEPRESSIVE DISORDER
EQ 5MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9861630	June 15, 2027	METHOD OF TREATING DEPRESSION OR MAJOR DEPRESSIVE DISORDER
EQ 10MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9278096	March 21, 2032	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE TREATMENT EMERGENT SEXUAL DYSFUNCTION (TESD) INDUCED BY PRIOR SEROTONIN REUPTAKE INHIBITOR TREATMENT
EQ 15MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	DISCN	TABLET	ORAL	9278096	March 21, 2032	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE TREATMENT EMERGENT SEXUAL DYSFUNCTION (TESD) INDUCED BY PRIOR SEROTONIN REUPTAKE INHIBITOR TREATMENT
EQ 20MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9278096	March 21, 2032	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE TREATMENT EMERGENT SEXUAL DYSFUNCTION (TESD) INDUCED BY PRIOR SEROTONIN REUPTAKE INHIBITOR TREATMENT
EQ 5MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	9278096	March 21, 2032	USE IN THE TREATMENT OF MAJOR DEPRESSIVE DISORDER TO IMPROVE TREATMENT EMERGENT SEXUAL DYSFUNCTION (TESD) INDUCED BY PRIOR SEROTONIN REUPTAKE INHIBITOR TREATMENT

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 10MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	Nov. 13, 2023	INFORMATION ADDED TO THE LABELING REGARDING THE RESULT OF STUDY LUAA21004-402
EQ 15MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	DISCN	TABLET	ORAL	Nov. 13, 2023	INFORMATION ADDED TO THE LABELING REGARDING THE RESULT OF STUDY LUAA21004-402
EQ 20MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	Nov. 13, 2023	INFORMATION ADDED TO THE LABELING REGARDING THE RESULT OF STUDY LUAA21004-402
EQ 5MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	Nov. 13, 2023	INFORMATION ADDED TO THE LABELING REGARDING THE RESULT OF STUDY LUAA21004-402
EQ 10MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	Jan. 22, 2024	ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING
EQ 15MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	DISCN	TABLET	ORAL	Jan. 22, 2024	ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING
EQ 20MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	Jan. 22, 2024	ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING
EQ 5MG BASE	TRINTELLIX	TAKEDA PHARMS USA	N204447	Sept. 30, 2013	RX	TABLET	ORAL	Jan. 22, 2024	ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN	INHIBITOR	Ki	8.80	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN	AGONIST	Ki	7.82	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN	ANTAGONIST	Ki	7.72	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN	AGONIST	Ki	7.48	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 3A	Ion channel	P46098	5HT3A_HUMAN	ANTAGONIST	Ki	8.43	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN	ANTAGONIST	Ki	7.27	DRUG LABEL	DRUG LABEL
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	6.74	CHEMBL
5-hydroxytryptamine receptor 5A	GPCR	P47898	5HT5A_HUMAN		Ki	6.66	CHEMBL
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN		Ki	7.34	CHEMBL
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Ki	6.25	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	6.74	CHEMBL
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	6.74	CHEMBL
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	6.48	CHEMBL
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	6.74	CHEMBL
Sodium-dependent serotonin transporter	Transporter		SC6A4_RAT		IC50	8.28	CHEMBL
5-hydroxytryptamine receptor 3A	Ion channel		5HT3A_RAT		Ki	6.64	CHEMBL
5-hydroxytryptamine receptor 1D	GPCR		5HT1D_RAT	ANTAGONIST	IC50	5.40	IUPHAR
5-hydroxytryptamine receptor 7	GPCR		5HT7R_RAT		Ki	6.70	SCIENTIFIC LITERATURE
Sodium-dependent dopamine transporter	Transporter		SC6A3_RAT		IC50	6.05	CHEMBL

External reference:

ID	Source
3O2K1S3WQV	UNII
D10184	KEGG_DRUG
1253056-29-9	SECONDARY_CAS_RN
960203-27-4	SECONDARY_CAS_RN
4032784	VANDF
C3661282	UMLSCUI
CHEBI:76016	CHEBI
CHEMBL2104993	ChEMBL_ID
9966051	PUBCHEM_CID
DB09068	DRUGBANK_ID
CHEMBL2107387	ChEMBL_ID
D000078784	MESH_DESCRIPTOR_UI
9279	INN_ID
7351	IUPHAR_LIGAND_ID
1439824	RXNORM
206222	MMSL
235694	MMSL
29689	MMSL
d08125	MMSL
015226	NDDF
015227	NDDF
708717008	SNOMEDCT_US
712748004	SNOMEDCT_US
768282000	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	55154-0256	TABLET, FILM COATED	10 mg	ORAL	NDA	29 sections
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	55154-0256	TABLET, FILM COATED	10 mg	ORAL	NDA	29 sections
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	55154-0256	TABLET, FILM COATED	10 mg	ORAL	NDA	29 sections
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	55154-0256	TABLET, FILM COATED	10 mg	ORAL	NDA	29 sections
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	55154-0257	TABLET, FILM COATED	20 mg	ORAL	NDA	29 sections
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	55154-0257	TABLET, FILM COATED	20 mg	ORAL	NDA	29 sections
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	55154-0257	TABLET, FILM COATED	20 mg	ORAL	NDA	29 sections
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	55154-0257	TABLET, FILM COATED	20 mg	ORAL	NDA	29 sections
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	64764-720	TABLET, FILM COATED	5 mg	ORAL	NDA	31 sections
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	64764-720	TABLET, FILM COATED	5 mg	ORAL	NDA	31 sections
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	64764-730	TABLET, FILM COATED	10 mg	ORAL	NDA	31 sections
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	64764-730	TABLET, FILM COATED	10 mg	ORAL	NDA	31 sections
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	64764-750	TABLET, FILM COATED	20 mg	ORAL	NDA	31 sections
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	64764-750	TABLET, FILM COATED	20 mg	ORAL	NDA	31 sections
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	70518-2642	TABLET, FILM COATED	20 mg	ORAL	NDA	30 sections
Trintellix	HUMAN PRESCRIPTION DRUG LABEL	1	70518-2642	TABLET, FILM COATED	20 mg	ORAL	NDA	30 sections