brexpiprazole šŸ¶ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
psychotropics, phenylpiperazine derivatives 5014 913611-97-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • brexpiprazole
  • rexulti
  • OPC-34712
  • OPC 34712
an atypical antipsychotic the efficacy of brexpiprazole may be mediated through a combination of partial agonist activity at serotonin 5-HT1A and dopamine D2 receptors, and antagonist activity at serotonin 5-HT2A receptors
  • Molecular weight: 433.57
  • Formula: C25H27N3O2S
  • CLOGP: 4.90
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 44.81
  • ALOGS: -5.28
  • ROTB: 7
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
3 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution) 1.46 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.34 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 54.37 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 0.00 mg/mL Bocci G, Oprea TI, Benet LZ
BA (Bioavailability) 1 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,KIT,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1 55
kinase-selectivity-class AXL,GRK2,MAPK7,SIK2,STK33,TEK 6
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
July 27, 2018 EMA OTSUKA PHARM CO LTD
Jan. 19, 2018 PMDA Otsuka Pharmaceutical Co., Ltd.
July 10, 2015 FDA OTSUKA PHARM CO LTD

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
Akathisia 890.80 21.27 220 11426 10939 90605862
Tardive dyskinesia 770.02 21.27 195 11451 10735 90606066
Schizoaffective disorder 676.11 21.27 152 11494 4995 90611806
Weight increased 480.56 21.27 409 11237 417518 90199283
Drug level increased 422.82 21.27 152 11494 27610 90589191
Electrocardiogram QT prolonged 351.83 21.27 176 11470 72280 90544521
Suicidal ideation 345.71 21.27 175 11471 73680 90543121
Product use in unapproved indication 270.19 21.27 270 11376 335966 90280835
Tremor 223.72 21.27 173 11473 153000 90463801
Drug interaction 210.82 21.27 216 11430 276237 90340564
Extrapyramidal disorder 181.44 21.27 71 11575 16232 90600569
Restlessness 176.79 21.27 88 11558 35632 90581169
Hallucination, auditory 172.26 21.27 68 11578 15907 90600894
Sinus rhythm 160.68 21.27 37 11609 1349 90615452
Suicide attempt 152.91 21.27 104 11542 75295 90541506
Oculogyric crisis 144.08 21.27 38 11608 2441 90614360
Mania 111.11 21.27 48 11598 14076 90602725
Therapy cessation 108.32 21.27 64 11582 36297 90580504
Underdose 105.90 21.27 73 11573 53944 90562857
Parkinsonism 92 21.27 42 11604 14023 90602778
Inability to afford medication 91.33 21.27 29 11617 3593 90613208
Off label use 89.73 21.27 327 11319 1101925 89514876
Dyskinesia 87.63 21.27 56 11590 36478 90580323
Anger 86.70 21.27 40 11606 13680 90603121
Hallucination 84.32 21.27 69 11577 65890 90550911
Sedation 82.60 21.27 60 11586 48111 90568690
Discoloured vomit 82.51 21.27 21 11625 1171 90615630
Dystonia 78.95 21.27 40 11606 16779 90600022
Agitation 77.09 21.27 66 11580 67032 90549769
Hyperprolactinaemia 76.09 21.27 28 11618 5405 90611396
Insomnia 75.06 21.27 145 11501 333329 90283472
Compulsive shopping 70.62 21.27 17 11629 752 90616049
Anxiety 68.84 21.27 134 11512 309638 90307163
Product administered to patient of inappropriate age 65.24 21.27 24 11622 4629 90612172
Blood prolactin increased 63.22 21.27 22 11624 3615 90613186
Product use issue 62.97 21.27 134 11512 329785 90287016
Drug effective for unapproved indication 59.30 21.27 26 11620 7892 90608909
Neuroleptic malignant syndrome 56.89 21.27 31 11615 15065 90601736
Depression 53.80 21.27 119 11527 300482 90316319
Dissociation 53.39 21.27 23 11623 6692 90610109
Delusion 50.99 21.27 28 11618 13812 90602989
Internal haemorrhage 48.46 21.27 21 11625 6199 90610602
Feeling abnormal 48.12 21.27 81 11565 167154 90449647
Irritability 47.01 21.27 38 11608 35624 90581177
Treatment noncompliance 45.87 21.27 44 11602 51683 90565118
Distributive shock 45.57 21.27 17 11629 3407 90613394
Somnolence 44.63 21.27 89 11557 208995 90407806
Collagen-vascular disease 43.49 21.27 8 11638 92 90616709
Muscle twitching 43.42 21.27 31 11615 24171 90592630
Adverse drug reaction 42.52 21.27 63 11583 116638 90500163
Lactation disorder 41.50 21.27 10 11636 444 90616357
Infusion related reaction 39.29 21.27 4 11642 416776 90200025
Serotonin syndrome 38.95 21.27 35 11611 37852 90578949
Completed suicide 38.75 21.27 68 11578 144990 90471811
Food craving 38.48 21.27 13 11633 1954 90614847
Hypomania 38.40 21.27 20 11626 8877 90607924
Wrong technique in product usage process 37.30 21.27 46 11600 71525 90545276
Psychiatric symptom 36.56 21.27 18 11628 7100 90609701
Eye movement disorder 35.84 21.27 17 11629 6181 90610620
Increased appetite 35.78 21.27 21 11625 11744 90605057
Gambling disorder 35.64 21.27 11 11635 1241 90615560
Drug hypersensitivity 35.63 21.27 8 11638 463601 90153200
Hunger 34.92 21.27 17 11629 6546 90610255
Swelling 34.78 21.27 6 11640 419052 90197749
Joint swelling 34.31 21.27 11 11635 503289 90113512
Suicidal behaviour 33.80 21.27 13 11633 2831 90613970
Parakeratosis 33.50 21.27 8 11638 342 90616459
Paranoia 31.47 21.27 20 11626 12888 90603913
Tic 31.07 21.27 11 11635 1900 90614901
Crying 31.02 21.27 26 11620 25619 90591182
Contraindicated product administered 30.35 21.27 3 11643 320136 90296665
Impulsive behaviour 28.29 21.27 10 11636 1720 90615081
Aggression 28.13 21.27 25 11621 26643 90590158
Intentional overdose 27.70 21.27 46 11600 93788 90523013
Galactorrhoea 27.58 21.27 13 11633 4659 90612142
Abnormal behaviour 27.49 21.27 23 11623 22605 90594196
Arthralgia 27.43 21.27 36 11610 778486 89838315
Drug dose titration not performed 27.22 21.27 8 11638 764 90616037
Compulsions 26.37 21.27 6 11640 207 90616594
Nightmare 26.22 21.27 22 11624 21703 90595098
Bruxism 25.33 21.27 12 11634 4351 90612450
Electrocardiogram abnormal 25.21 21.27 16 11630 10282 90606519
Psychotic disorder 24.77 21.27 25 11621 31205 90585596
Death 24.70 21.27 120 11526 456431 90160370
Seborrhoeic dermatitis 24.59 21.27 9 11637 1711 90615090
Blood glucose increased 24.58 21.27 44 11602 95202 90521599
Binge eating 24.58 21.27 7 11639 598 90616203
Rheumatoid arthritis 24.56 21.27 8 11638 362606 90254195
Systemic lupus erythematosus 24.49 21.27 8 11638 361888 90254913
Panic attack 24.46 21.27 23 11623 26342 90590459
Hepatic enzyme increased 24.36 21.27 8 11638 360728 90256073
Pain 24.32 21.27 58 11588 996283 89620518
Insurance issue 24.30 21.27 16 11630 10942 90605859
Restless legs syndrome 23.57 21.27 21 11625 22449 90594352
Hyperphagia 23.55 21.27 10 11636 2808 90613993
Pyrexia 22.78 21.27 31 11615 660454 89956347
Altered state of consciousness 22.76 21.27 24 11622 31508 90585293
Stomatitis 22.63 21.27 4 11642 274694 90342107
Dyspnoea 22.52 21.27 50 11596 880905 89735896
Self-injurious ideation 22.32 21.27 10 11636 3193 90613608
Bipolar disorder 22.10 21.27 14 11632 8971 90607830
Therapeutic response unexpected 22.06 21.27 20 11626 21860 90594941
Cutaneous T-cell lymphoma 21.40 21.27 8 11638 1612 90615189

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
Akathisia 459.39 30.05 129 5491 10322 42605393
Tardive dyskinesia 192.35 30.05 60 5560 6864 42608851
Weight increased 168.50 30.05 128 5492 107855 42507860
Hallucination, auditory 144.12 30.05 59 5561 14805 42600910
Product use in unapproved indication 139.51 30.05 145 5475 184311 42431404
Suicidal ideation 129.52 30.05 80 5540 48081 42567634
Neuroleptic malignant syndrome 88.05 30.05 47 5573 21425 42594290
Sedation 85.36 30.05 52 5568 30423 42585292
Restlessness 82.16 30.05 50 5570 29199 42586516
Dissociation 81.22 30.05 27 5593 3771 42611944
Psychotic disorder 77.12 30.05 48 5572 29160 42586555
Social anxiety disorder 74.23 30.05 17 5603 589 42615126
Persecutory delusion 70.92 30.05 24 5596 3540 42612175
Dysphemia 67.86 30.05 20 5600 1882 42613833
Extrapyramidal disorder 64.68 30.05 35 5585 16377 42599338
Treatment noncompliance 63.75 30.05 47 5573 37625 42578090
Anxiety 61.74 30.05 77 5543 118483 42497232
Pneumonia aspiration 60.04 30.05 51 5569 50027 42565688
Paranoia 52.74 30.05 29 5591 13997 42601718
Apathy 50.96 30.05 24 5596 8382 42607333
Tremor 50.50 30.05 63 5557 96866 42518849
Spasmodic dysphonia 50.04 30.05 12 5608 509 42615206
Product administered to patient of inappropriate age 49.89 30.05 20 5600 4741 42610974
Delusion 48.71 30.05 28 5592 14706 42601009
Hallucination, tactile 48.59 30.05 12 5608 576 42615139
Mental disorder 48.50 30.05 30 5590 17999 42597716
Thinking abnormal 48.25 30.05 22 5598 7139 42608576
Oculogyric crisis 47.74 30.05 15 5605 1750 42613965
Activation syndrome 44.99 30.05 9 5611 161 42615554
Gambling 43.01 30.05 9 5611 203 42615512
Mania 42.96 30.05 23 5597 10524 42605191
Parkinsonism 42.81 30.05 23 5597 10600 42605115
Anger 41.07 30.05 24 5596 12994 42602721
Inability to afford medication 41.02 30.05 14 5606 2116 42613599
Somnolence 40.27 30.05 69 5551 141036 42474679
Gambling disorder 39.47 30.05 13 5607 1763 42613952
Marasmus 38.96 30.05 11 5609 888 42614827
Hypomania 38.79 30.05 14 5606 2494 42613221
Schizoaffective disorder 38.14 30.05 13 5607 1957 42613758
Loss of libido 36.03 30.05 14 5606 3056 42612659
Drug level below therapeutic 34.56 30.05 17 5603 6528 42609187
Depression 33.80 30.05 56 5564 111307 42504408
Dystonia 33.68 30.05 21 5599 12769 42602946
Drug level decreased 33.08 30.05 19 5601 9958 42605757
Alcohol abuse 32.28 30.05 14 5606 4035 42611680
Off label use 30.83 30.05 165 5455 638170 41977545
Dyskinesia 30.69 30.05 26 5594 25364 42590351

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
Akathisia 600.91 20.50 170 11830 16943 110560356
Tardive dyskinesia 536.59 20.50 148 11852 13431 110563868
Suicidal ideation 410.02 20.50 201 11799 93736 110483563
Product use in unapproved indication 308.71 20.50 306 11694 447071 110130228
Hallucination, auditory 294.64 20.50 110 11890 26287 110551012
Weight increased 224.76 20.50 251 11749 419393 110157906
Suicide attempt 190.52 20.50 126 11874 103268 110474031
Oculogyric crisis 175.71 20.50 47 11953 3785 110573514
Restlessness 163.99 20.50 92 11908 56167 110521132
Tremor 153.27 20.50 146 11854 202086 110375213
Extrapyramidal disorder 144.59 20.50 68 11932 28799 110548500
Neuroleptic malignant syndrome 139.77 20.50 70 11930 33989 110543310
Dissociation 135.82 20.50 48 11952 9794 110567505
Sedation 107.14 20.50 76 11924 69607 110507692
Pneumonia aspiration 103.27 20.50 79 11921 81154 110496145
Underdose 101.62 20.50 71 11929 63483 110513816
Parkinsonism 98.14 20.50 48 11952 22139 110555160
Persecutory delusion 95.71 20.50 33 11967 6258 110571041
Delusion 95.03 20.50 48 11952 23707 110553592
Product administered to patient of inappropriate age 91.47 20.50 34 11966 8002 110569297
Dystonia 88.45 20.50 47 11953 25758 110551541
Treatment noncompliance 88.44 20.50 69 11931 72921 110504378
Hallucination 87.91 20.50 79 11921 101353 110475946
Anxiety 83.85 20.50 141 11859 344937 110232362
Discoloured vomit 75.08 20.50 21 11979 1996 110575303
Psychotic disorder 72.43 20.50 53 11947 50884 110526415
Anger 71.93 20.50 37 11963 18970 110558329
Social anxiety disorder 69.63 20.50 17 11983 949 110576350
Paranoia 69.00 20.50 38 11962 22336 110554963
Inability to afford medication 68.34 20.50 23 11977 4053 110573246
Dyskinesia 67.49 20.50 51 11949 51395 110525904
Schizoaffective disorder 65.93 20.50 21 11979 3115 110574184
Apathy 62.58 20.50 32 11968 16207 110561092
Depression 59.60 20.50 116 11884 317219 110260080
Serotonin syndrome 59.14 20.50 50 11950 59103 110518196
Therapy cessation 57.80 20.50 44 11956 44813 110532486
Irritability 57.47 20.50 45 11955 47764 110529535
Spasmodic dysphonia 56.48 20.50 13 11987 562 110576737
Somnolence 56.18 20.50 109 11891 297340 110279959
Completed suicide 56.11 20.50 97 11903 242284 110335015
Marasmus 55.69 20.50 16 11984 1675 110575624
Agitation 54.10 20.50 64 11936 112987 110464312
Insomnia 52.76 20.50 119 11881 360471 110216828
Adverse drug reaction 52.58 20.50 61 11939 105498 110471801
Mania 49.91 20.50 30 11970 20766 110556533
Off label use 49.51 20.50 304 11696 1499881 109077418
Blood prolactin increased 46.89 20.50 18 11982 4624 110572675
Rhabdomyolysis 46.16 20.50 61 11939 120340 110456959
Collagen-vascular disease 45.86 20.50 8 11992 80 110577219
Hypomania 44.88 20.50 22 11978 10188 110567111
Drug ineffective 44.52 20.50 299 11701 1520241 109057058
Hallucination, tactile 44.41 20.50 12 11988 1003 110576296
Hyperprolactinaemia 44.09 20.50 19 11981 6556 110570743
Psychiatric symptom 43.96 20.50 21 11979 9192 110568107
Internal haemorrhage 42.18 20.50 21 11979 10050 110567249
Feeling abnormal 40.08 20.50 71 11929 180640 110396659
Activation syndrome 39.52 20.50 9 11991 371 110576928
Distributive shock 39.39 20.50 17 11983 5887 110571412
Altered state of consciousness 38.69 20.50 39 11961 57587 110519712
Schizophrenia 38.69 20.50 26 11974 21800 110555499
Loss of libido 38.40 20.50 14 11986 3119 110574180
Mental disorder 37.15 20.50 32 11968 38759 110538540
Compulsive shopping 36.75 20.50 10 11990 858 110576441
Thinking abnormal 36.74 20.50 22 11978 15118 110562181
Manic symptom 36.18 20.50 8 11992 288 110577011
Gambling disorder 35.30 20.50 12 11988 2179 110575120
Aggression 34.24 20.50 37 11963 59173 110518126
Urinary retention 34.24 20.50 40 11960 69643 110507656
Suicidal behaviour 33.33 20.50 13 11987 3484 110573815
Alcohol abuse 32.25 20.50 14 11986 4915 110572384
Muscle rigidity 31.90 20.50 24 11976 24007 110553292
Parakeratosis 31.53 20.50 8 11992 523 110576776
Salivary hypersecretion 31.47 20.50 21 11979 17400 110559899
Hunger 31.34 20.50 15 11985 6589 110570710
Hallucination, visual 30.69 20.50 29 11971 39576 110537723
Drug effective for unapproved indication 30.32 20.50 19 11981 14148 110563151
Wrong technique in product usage process 30.05 20.50 42 11958 87306 110489993
Bradykinesia 29.67 20.50 17 11983 10771 110566528
Bruxism 28.86 20.50 13 11987 4981 110572318
Anaemia 28.27 20.50 12 11988 547074 110030225
Intentional self-injury 28.23 20.50 27 11973 37402 110539897
Electrocardiogram abnormal 27.80 20.50 20 11980 18689 110558610
Swelling 27.52 20.50 3 11997 351038 110226261
Self-injurious ideation 27.32 20.50 12 11988 4334 110572965
Torticollis 27.30 20.50 11 11989 3210 110574089
Muscle twitching 27.27 20.50 24 11976 29911 110547388
Impulsive behaviour 26.99 20.50 11 11989 3304 110573995
Panic attack 25.95 20.50 23 11977 28917 110548382
Infusion related reaction 25.85 20.50 5 11995 381157 110196142
Intentional overdose 25.51 20.50 49 11951 132452 110444847
Abnormal behaviour 25.43 20.50 26 11974 39013 110538286
Thrombocytopenia 24.92 20.50 4 11996 348881 110228418
Dysphemia 24.90 20.50 11 11989 4026 110573273
Condition aggravated 24.73 20.50 150 11850 734686 109842613
Arthralgia 24.68 20.50 29 11971 779603 109797696
Product use issue 24.54 20.50 82 11918 311613 110265686
Egocentrism 24.39 20.50 3 11997 0 110577299
Electrocardiogram QT prolonged 24.38 20.50 43 11957 108917 110468382
Obsessive-compulsive disorder 24.27 20.50 13 11987 7228 110570071
General physical health deterioration 24.19 20.50 8 11992 425287 110152012
Gambling 24.05 20.50 6 11994 366 110576933
Joint swelling 24.04 20.50 9 11991 442836 110134463
Dyspnoea 23.94 20.50 53 11947 1106819 109470480
Flat affect 22.77 20.50 9 11991 2496 110574803
Increased appetite 22.23 20.50 16 11984 14961 110562338
Intracranial pressure increased 22.22 20.50 14 11986 10521 110566778
Insurance issue 22.13 20.50 14 11986 10598 110566701
Seborrhoeic dermatitis 22.10 20.50 9 11991 2698 110574601
Soliloquy 22.10 20.50 7 11993 1020 110576279
Pyrexia 21.98 20.50 40 11960 898225 109679074
Drug hypersensitivity 21.84 20.50 11 11989 454079 110123220
Troponin increased 21.56 20.50 21 11979 29745 110547554
Fall 21.45 20.50 125 11875 603357 109973942
Blood triglycerides increased 21.43 20.50 19 11981 23907 110553392
Drug effect less than expected 21.38 20.50 12 11988 7308 110569991
Hypersexuality 21.31 20.50 8 11992 1932 110575367
Abdominal pain 21.06 20.50 15 11985 512974 110064325
Delusion of reference 21.01 20.50 5 11995 250 110577049

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AX16 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Other antipsychotics
MeSH PA D015259 Dopamine Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018490 Serotonin Agents
MeSH PA D018491 Dopamine Agonists
FDA EPC N0000175430 Atypical Antipsychotic
CHEBI has role CHEBI:35469 antidepressant
CHEBI has role CHEBI:35476 antipsychotic agent

Related Drugs by ATC class:

N05AX Other antipsychotics 11 drugs
aripiprazolecariprazineiloperidonemosapraminepaliperidonepimavanserinprothipendylrisperidonetrospiumxanomelinezotepine

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

DiseaseRelationSNOMED_IDDOID
Schizophrenia indication 58214004 DOID:5419
Major depressive disorder indication 370143000




šŸ¶ Veterinary Drug Use

None

šŸ¶ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.14 acidic
pKa2 8.07 Basic
pKa3 0.9 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8349840 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 8618109 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD)
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL 9839637 April 12, 2026 TREATMENT OF SCHIZOPHRENIA IN ADULTS AND PEDIATRIC PATIENTS AGES 13 YEARS AND OLDER

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 10, 2026 TREATMENT OF AGITATION ASSOCIATED WITH DEMENTIA DUE TO ALZHEIMERā€™S DISEASE
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 10, 2026 TREATMENT OF AGITATION ASSOCIATED WITH DEMENTIA DUE TO ALZHEIMERā€™S DISEASE
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 10, 2026 TREATMENT OF AGITATION ASSOCIATED WITH DEMENTIA DUE TO ALZHEIMERā€™S DISEASE
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 10, 2026 TREATMENT OF AGITATION ASSOCIATED WITH DEMENTIA DUE TO ALZHEIMERā€™S DISEASE
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 10, 2026 TREATMENT OF AGITATION ASSOCIATED WITH DEMENTIA DUE TO ALZHEIMERā€™S DISEASE
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 10, 2026 TREATMENT OF AGITATION ASSOCIATED WITH DEMENTIA DUE TO ALZHEIMERā€™S DISEASE
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Nov. 10, 2026 PEDIATRIC EXCLUSIVITY
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Nov. 10, 2026 PEDIATRIC EXCLUSIVITY
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Nov. 10, 2026 PEDIATRIC EXCLUSIVITY
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Nov. 10, 2026 PEDIATRIC EXCLUSIVITY
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Nov. 10, 2026 PEDIATRIC EXCLUSIVITY
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Nov. 10, 2026 PEDIATRIC EXCLUSIVITY
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 8, 2027 ADDITIONAL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 8, 2027 ADDITIONAL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 8, 2027 ADDITIONAL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 8, 2027 ADDITIONAL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 8, 2027 ADDITIONAL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 8, 2027 ADDITIONAL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Nov. 8, 2027 PEDIATRIC EXCLUSIVITY
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Nov. 8, 2027 PEDIATRIC EXCLUSIVITY
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Nov. 8, 2027 PEDIATRIC EXCLUSIVITY
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Nov. 8, 2027 PEDIATRIC EXCLUSIVITY
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Nov. 8, 2027 PEDIATRIC EXCLUSIVITY
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL Nov. 8, 2027 PEDIATRIC EXCLUSIVITY
0.25MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 9, 2028 INFORMATION ADDED TO SECTION 14 OF THE LABELING TO DESCRIBE STUDY 6 (NCT03198078), TO FULFILL POSTMARKETING REQUIREMENT 4205-1
0.5MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 9, 2028 INFORMATION ADDED TO SECTION 14 OF THE LABELING TO DESCRIBE STUDY 6 (NCT03198078), TO FULFILL POSTMARKETING REQUIREMENT 4205-1
1MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 9, 2028 INFORMATION ADDED TO SECTION 14 OF THE LABELING TO DESCRIBE STUDY 6 (NCT03198078), TO FULFILL POSTMARKETING REQUIREMENT 4205-1
2MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 9, 2028 INFORMATION ADDED TO SECTION 14 OF THE LABELING TO DESCRIBE STUDY 6 (NCT03198078), TO FULFILL POSTMARKETING REQUIREMENT 4205-1
3MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 9, 2028 INFORMATION ADDED TO SECTION 14 OF THE LABELING TO DESCRIBE STUDY 6 (NCT03198078), TO FULFILL POSTMARKETING REQUIREMENT 4205-1
4MG REXULTI OTSUKA N205422 July 10, 2015 RX TABLET ORAL May 9, 2028 INFORMATION ADDED TO SECTION 14 OF THE LABELING TO DESCRIBE STUDY 6 (NCT03198078), TO FULFILL POSTMARKETING REQUIREMENT 4205-1

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
D(2) dopamine receptor GPCR AGONIST Ki 9.52 SCIENTIFIC LITERATURE DRUG LABEL
5-hydroxytryptamine receptor 1A GPCR AGONIST Ki 9.92 SCIENTIFIC LITERATURE DRUG LABEL
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 9.33 SCIENTIFIC LITERATURE DRUG LABEL
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.34 CHEMBL
D(1B) dopamine receptor GPCR Ki 6.46 CHEMBL
5-hydroxytryptamine receptor 1D GPCR Ki 7.62 CHEMBL
5-hydroxytryptamine receptor 3A Ion channel Ki 5.82 CHEMBL
5-hydroxytryptamine receptor 1E GPCR Ki 6.32 CHEMBL
Histamine H3 receptor GPCR Ki 5.58 CHEMBL
Transmembrane protein 97 Enzyme Ki 7.20 CHEMBL
Beta-1 adrenergic receptor GPCR Ki 7.23 SCIENTIFIC LITERATURE
Beta-2 adrenergic receptor GPCR Ki 7.17 SCIENTIFIC LITERATURE
D(1A) dopamine receptor GPCR AGONIST Ki 6.80 SCIENTIFIC LITERATURE
Alpha-2A adrenergic receptor GPCR Ki 7.82 SCIENTIFIC LITERATURE
Histamine H1 receptor GPCR ANTAGONIST Ki 7.72 SCIENTIFIC LITERATURE
Sodium-dependent noradrenaline transporter Transporter INHIBITOR IC50 6.86 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 2B GPCR ANTAGONIST Ki 8.72 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 2C GPCR Ki 7.47 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 6 GPCR Ki 7.24 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 7 GPCR ANTAGONIST Ki 8.43 SCIENTIFIC LITERATURE
Alpha-1A adrenergic receptor GPCR Ki 8.42 SCIENTIFIC LITERATURE
Alpha-2B adrenergic receptor GPCR Ki 7.77 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 1B GPCR Ki 7.50 SCIENTIFIC LITERATURE
Alpha-2C adrenergic receptor GPCR ANTAGONIST Ki 9.23 SCIENTIFIC LITERATURE
Sodium-dependent dopamine transporter Transporter INHIBITOR IC50 6.03 SCIENTIFIC LITERATURE
D(4) dopamine receptor GPCR AGONIST Ki 8.20 SCIENTIFIC LITERATURE
Alpha-1D adrenergic receptor GPCR ANTAGONIST Ki 8.59 SCIENTIFIC LITERATURE
Alpha-1B adrenergic receptor GPCR ANTAGONIST Ki 9.77 SCIENTIFIC LITERATURE
Sodium-dependent serotonin transporter Transporter INHIBITOR IC50 7.54 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 5A GPCR Ki 6.85 SCIENTIFIC LITERATURE
D(3) dopamine receptor GPCR AGONIST Ki 8.96 SCIENTIFIC LITERATURE
D(2) dopamine receptor GPCR Ki 9.70 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 10.05 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 8.64 CHEMBL

External reference:

IDSource
D10309 KEGG_DRUG
4034625 VUID
N0000191737 NUI
4034625 VANDF
CHEBI:134716 CHEBI
CHEMBL2105760 ChEMBL_ID
C000591922 MESH_SUPPLEMENTAL_RECORD_UI
7672 IUPHAR_LIGAND_ID
DB09128 DRUGBANK_ID
1658314 RXNORM
234913 MMSL
31120 MMSL
d08373 MMSL
016270 NDDF
716069007 SNOMEDCT_US
781292006 SNOMEDCT_US
C3885614 UMLSCUI
9552 INN_ID
11978813 PUBCHEM_CID
2J3YBM1K8C UNII
2J3YBM1K8C INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Brexpiprazole Human Prescription Drug Label 1 27241-204 TABLET 0.25 mg ORAL ANDA 32 sections
Brexpiprazole Human Prescription Drug Label 1 27241-205 TABLET 0.50 mg ORAL ANDA 32 sections
Brexpiprazole Human Prescription Drug Label 1 27241-206 TABLET 1 mg ORAL ANDA 32 sections
Brexpiprazole Human Prescription Drug Label 1 27241-207 TABLET 2 mg ORAL ANDA 32 sections
Brexpiprazole Human Prescription Drug Label 1 27241-208 TABLET 3 mg ORAL ANDA 32 sections
Brexpiprazole Human Prescription Drug Label 1 27241-209 TABLET 4 mg ORAL ANDA 32 sections
Rexulti HUMAN PRESCRIPTION DRUG LABEL 1 59148-035 TABLET 0.25 mg ORAL NDA 28 sections
Rexulti HUMAN PRESCRIPTION DRUG LABEL 1 59148-036 TABLET 0.50 mg ORAL NDA 28 sections
Rexulti HUMAN PRESCRIPTION DRUG LABEL 1 59148-037 TABLET 1 mg ORAL NDA 28 sections
Rexulti HUMAN PRESCRIPTION DRUG LABEL 1 59148-038 TABLET 2 mg ORAL NDA 28 sections
Rexulti HUMAN PRESCRIPTION DRUG LABEL 1 59148-039 TABLET 3 mg ORAL NDA 28 sections
Rexulti HUMAN PRESCRIPTION DRUG LABEL 1 59148-040 TABLET 4 mg ORAL NDA 28 sections
Rexulti HUMAN PRESCRIPTION DRUG LABEL 1 70518-3548 TABLET 2 mg ORAL NDA 27 sections
Rexulti HUMAN PRESCRIPTION DRUG LABEL 1 70518-4608 TABLET 1 mg ORAL NDA 27 sections