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

Stem definitionDrug idCAS RN
serotonin and/or norepinephrine reuptake inhibitors, fluoxetine derivatives 4806 508233-74-7

Description:

MoleculeDescription

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:

DoseUnitRoute
10 mg O

ADMET properties:

PropertyValueReference
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:

DateAgencyCompanyOrphan
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 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
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 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
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 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
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:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 9.02 Basic
pKa2 1.85 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sodium-dependent serotonin transporter Transporter INHIBITOR Ki 8.80 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 1A GPCR AGONIST Ki 7.82 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 7 GPCR ANTAGONIST Ki 7.72 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 1B GPCR AGONIST Ki 7.48 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 3A Ion channel ANTAGONIST Ki 8.43 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 1D GPCR ANTAGONIST Ki 7.27 DRUG LABEL DRUG LABEL
Histamine H2 receptor GPCR Ki 6.74 CHEMBL
5-hydroxytryptamine receptor 5A GPCR Ki 6.66 CHEMBL
Beta-1 adrenergic receptor GPCR Ki 7.34 CHEMBL
Beta-2 adrenergic receptor GPCR Ki 6.25 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 6.74 CHEMBL
5-hydroxytryptamine receptor 2C GPCR Ki 6.74 CHEMBL
5-hydroxytryptamine receptor 6 GPCR Ki 6.48 CHEMBL
Histamine H1 receptor GPCR Ki 6.74 CHEMBL
Sodium-dependent serotonin transporter Transporter IC50 8.28 CHEMBL
5-hydroxytryptamine receptor 3A Ion channel Ki 6.64 CHEMBL
5-hydroxytryptamine receptor 1D GPCR ANTAGONIST IC50 5.40 IUPHAR
5-hydroxytryptamine receptor 7 GPCR Ki 6.70 SCIENTIFIC LITERATURE
Sodium-dependent dopamine transporter Transporter IC50 6.05 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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