esketamine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
4468 33643-46-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • spravato
  • esketamine HCl
  • esketamine hydrochloride
  • esketamine
  • l-Ketamine
Esketamine is the S-enantiomer of racemic ketamine. It is a non-selective, non-competitive, antagonist of the N-methyl-D-aspartate (NMDA) receptor, an ionotropic glutamate receptor. Through NMDA receptor antagonism, esketamine produces a transient increase in glutamate release leading to increases in alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) stimulation and subsequently to increases in neurotrophic signalling which may contribute to the restoration of synaptic function in these brain regions involved with the regulation of mood and emotional behaviour. Restoration of dopaminergic neurotransmission in brain regions involved in the reward and motivation, and decreased stimulation of brain regions involved in anhedonia, may contribute to the rapid response.
  • Molecular weight: 237.73
  • Formula: C13H16ClNO
  • CLOGP: 2.93
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 29.10
  • ALOGS: -3.71
  • ROTB: 2
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
8 mg N

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.509 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.855 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 30.479 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 21.577 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 59.770 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 51.320 % High 1
herg hERG pIC50 4.472 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 4.634 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 17.179 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 57.650 % High 1
kinase-safety-class ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,NTRK2,PDK1,PDK2,PDK4,TGFBR1 15
kinase-selectivity-class AXL,EIF2AK3,GRK2,PDK4 4
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.711 High 1
mh-clint Mouse hepatocyte intrinsic clearance 66.374 High 1
mppb Mouse plasma protein binding (% unbound) 50.810 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.918 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 65.840 % High 1
rh-clint Rat hepatocyte intrinsic clearance 56.364 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 89.290 % High 1
rppb Rat plasma protein binding (% unbound) 58.210 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 820.352 uM High 1

Approvals:

DateAgencyCompanyOrphan
May 3, 2019 FDA JANSSEN PHARMS
Dec. 18, 2019 EMA Janssen-Cilag International N.V.

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
Dissociation 13234.84 39.64 1993 11947 4722 90609785
Sedation 7074.65 39.64 1595 12345 46576 90567931
Suicidal ideation 1264.92 39.64 461 13479 73394 90541113
Hospitalisation 754.07 39.64 375 13565 127725 90486782
Suicide attempt 342.84 39.64 186 13754 75213 90539294
Physical examination abnormal 335.52 39.64 50 13890 96 90614411
Surgery 294.93 39.64 142 13798 44745 90569762
Hypertension 286.27 39.64 351 13589 457181 90157326
Panic attack 274.16 39.64 115 13825 26250 90588257
Dissociative disorder 255.79 39.64 49 13891 587 90613920
Blood pressure increased 241.56 39.64 217 13723 197000 90417507
Anxiety 213.54 39.64 250 13690 309522 90304985
Incorrect dose administered by device 202.65 39.64 62 13878 5675 90608832
Device issue 168.74 39.64 85 13855 29452 90585055
Adverse event 159.17 39.64 137 13803 117281 90497226
Device malfunction 124.61 39.64 62 13878 20915 90593592
Dizziness 120.97 39.64 274 13666 589010 90025497
Oxygen saturation abnormal 120.82 39.64 39 13901 4249 90610258
Feeling abnormal 105.11 39.64 129 13811 167106 90447401
Euphoric mood 93.02 39.64 34 13906 5375 90609132
Arthralgia 90.55 39.64 8 13932 778514 89835993
Product dose omission issue 90.07 39.64 161 13779 291526 90322981
Nausea 89.07 39.64 371 13569 1109945 89504562
Vomiting 84.29 39.64 289 13651 788004 89826503
Crying 78.47 39.64 49 13891 25596 90588911
Diarrhoea 77.91 39.64 24 13916 939166 89675341
Hallucination 75.48 39.64 70 13870 65889 90548618
Pain 74.88 39.64 30 13910 996311 89618196
Underdose 71.02 39.64 62 13878 53955 90560552
Hallucination, visual 67.84 39.64 43 13897 23049 90591458
Rash 66.59 39.64 20 13920 796080 89818427
Pyrexia 66.43 39.64 11 13929 660474 89954033
Product delivery mechanism issue 63.71 39.64 15 13925 501 90614006
Major depression 57.63 39.64 29 13911 10006 90604501
Device defective 56.57 39.64 21 13919 3465 90611042
Alopecia 55.08 39.64 6 13934 495065 90119442
Seizure 53.24 39.64 89 13851 152540 90461967
Abdominal discomfort 52.56 39.64 6 13934 477322 90137185
Psychogenic seizure 51.39 39.64 17 13923 1999 90612508
Nasal discomfort 50.36 39.64 22 13918 5526 90608981
Self-destructive behaviour 48.90 39.64 12 13928 479 90614028
Pain in extremity 48.76 39.64 6 13934 450523 90163984
Spinal operation 48.60 39.64 26 13914 10170 90604337
Feeling drunk 46.90 39.64 20 13920 4738 90609769
Peripheral swelling 45.95 39.64 5 13935 413101 90201406
Completed suicide 45.87 39.64 81 13859 144977 90469530
Systemic lupus erythematosus 44.00 39.64 3 13937 361893 90252614
Derealisation 43.85 39.64 14 13926 1471 90613036
Condition aggravated 42.91 39.64 19 13921 595526 90018981
Pruritus 42.75 39.64 15 13925 541510 90072997
Anaemia 42.68 39.64 3 13937 352799 90261708
Hallucination, auditory 42.61 39.64 28 13912 15947 90598560
Drug hypersensitivity 41.80 39.64 10 13930 463599 90150908
Respiratory depression 40.82 39.64 27 13913 15548 90598959
Unresponsive to stimuli 40.80 39.64 39 13901 38082 90576425
Neoplasm malignant 40.77 39.64 37 13903 33843 90580664

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
Dissociation 6153.78 45.81 950 5564 2848 42611973
Sedation 2729.45 45.81 676 5838 29799 42585022
Suicidal ideation 545.19 45.81 222 6292 47939 42566882
Hypertension 377.73 45.81 262 6252 166942 42447879
Hospitalisation 306.01 45.81 171 6343 74159 42540662
Blood pressure increased 188.63 45.81 142 6372 101786 42513035
Panic attack 159.78 45.81 61 6453 10984 42603837
Anxiety 141.30 45.81 128 6386 118432 42496389
Completed suicide 134.68 45.81 114 6400 96351 42518470
Suicide attempt 124.27 45.81 81 6433 46019 42568802
Adverse event 123.85 45.81 64 6450 23576 42591245
Surgery 107.82 45.81 53 6461 17563 42597258
Physical examination abnormal 104.47 45.81 22 6492 439 42614382
Oxygen saturation abnormal 94.74 45.81 27 6487 1944 42612877
Incorrect dose administered by device 94.21 45.81 29 6485 2727 42612094
Device issue 92.81 45.81 44 6470 13465 42601356
Dissociative disorder 90.87 45.81 21 6493 651 42614170
Hallucination, visual 71.88 45.81 43 6471 20977 42593844
Underdose 67.34 45.81 38 6476 16628 42598193
Nausea 63.69 45.81 167 6347 396632 42218189
Device malfunction 63.44 45.81 33 6481 12294 42602527
Vomiting 58.17 45.81 133 6381 289590 42325231
Dizziness 57.47 45.81 121 6393 249133 42365688
Diarrhoea 49.98 45.81 6 6508 460843 42153978

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
Dissociation 18357.11 44.55 2791 14688 7051 110564769
Sedation 9771.02 44.55 2230 15249 67453 110504367
Suicidal ideation 1459.80 44.55 550 16929 93387 110478433
Hospitalisation 946.64 44.55 457 17022 142036 110429784
Hypertension 644.36 44.55 576 16903 509508 110062312
Physical examination abnormal 413.88 44.55 72 17407 464 110571356
Suicide attempt 377.37 44.55 223 17256 103171 110468649
Panic attack 361.31 44.55 145 17334 28795 110543025
Blood pressure increased 349.10 44.55 304 17175 258069 110313751
Surgery 324.23 44.55 149 17330 41134 110530686
Dissociative disorder 306.22 44.55 64 17415 1187 110570633
Incorrect dose administered by device 257.29 44.55 78 17401 6736 110565084
Adverse event 255.93 44.55 178 17301 108631 110463189
Anxiety 254.09 44.55 292 17187 344786 110227034
Oxygen saturation abnormal 219.45 44.55 66 17413 5545 110566275
Device issue 187.82 44.55 97 17382 34438 110537382
Dizziness 154.47 44.55 340 17139 697853 109873967
Device malfunction 148.29 44.55 75 17404 25483 110546337
Completed suicide 120.63 44.55 169 17310 242212 110329608
Feeling abnormal 119.53 44.55 145 17334 180566 110391254
Hallucination, visual 117.65 44.55 75 17404 39530 110532290
Nausea 112.77 44.55 438 17041 1235252 109336568
Diarrhoea 104.47 44.55 26 17453 1139479 109432341
Pyrexia 103.33 44.55 11 17468 898254 109673566
Vomiting 99.93 44.55 343 17136 910332 109661488
Product delivery mechanism issue 98.31 44.55 19 17460 232 110571588
Rash 97.16 44.55 9 17470 820955 109750865
Underdose 94.11 44.55 79 17400 63475 110508345
Arthralgia 86.01 44.55 11 17468 779621 109792199
Hallucination 81.46 44.55 90 17389 101342 110470478
Major depression 76.07 44.55 36 17443 10585 110561235
Pain 74.53 44.55 29 17450 954926 109616894
Product dose omission issue 71.15 44.55 157 17322 321625 110250195
Acute kidney injury 69.96 44.55 9 17470 635421 109936399
Euphoric mood 66.55 44.55 31 17448 8796 110563024
Device defective 64.99 44.55 24 17455 3798 110568022
Respiratory depression 62.88 44.55 47 17432 31954 110539866
Rehabilitation therapy 61.75 44.55 20 17459 2141 110569679
Self-destructive behaviour 60.53 44.55 16 17463 839 110570981
Crying 60.32 44.55 42 17437 25586 110546234
Psychogenic seizure 59.99 44.55 20 17459 2344 110569476
Pruritus 59.93 44.55 10 17469 581550 109990270
Spinal operation 57.28 44.55 30 17449 10942 110560878
Nasal discomfort 57.05 44.55 25 17454 6156 110565664
Condition aggravated 56.15 44.55 23 17456 734813 109837007
Seizure 52.37 44.55 111 17368 221074 110350746
Peripheral swelling 51.79 44.55 3 17476 404031 110167789
Feeling drunk 46.76 44.55 21 17458 5479 110566341
Pneumonia 46.70 44.55 42 17437 876672 109695148
Weight decreased 46.14 44.55 9 17470 468048 110103772
Derealisation 45.92 44.55 16 17463 2142 110569678

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N01AX14 NERVOUS SYSTEM
ANESTHETICS
ANESTHETICS, GENERAL
Other general anesthetics
ATC N06AX27 NERVOUS SYSTEM
PSYCHOANALEPTICS
ANTIDEPRESSANTS
Other antidepressants
MeSH PA D000928 Antidepressive Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D011619 Psychotropic Drugs
CHEBI has role CHEBI:35469 antidepressant
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:38877 intravenous anaesthetic
CHEBI has role CHEBI:60643 NMDA receptor antagonist
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

N01AX Other general anesthetics 8 drugs
alfaxaloneetomidateketaminenitrous oxidepropanididpropofolsodium oxybatexenon
N06AX Other antidepressants 28 drugs
agomelatinebifemelanebrexanolonebupropiondesvenlafaxinedextromethorphanduloxetinegepironelevomilnacipranmedifoxaminemianserinmilnacipran show all 28 →

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

DiseaseRelationSNOMED_IDDOID
Depressive disorder indication 35489007
Arteriovenous malformation contraindication 24551003
Aneurysm contraindication 432119003 DOID:178




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.65 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 9592207 March 20, 2027 TREATMENT OF TREATMENT-RESISTANT DEPRESSION IN ADULT IN CONJUNCTION WITH AN ORAL ANTIDEPRESSANT
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 9592207 March 20, 2027 TREATMENT OF TREATMENT-RESISTANT DEPRESSION IN ADULTS
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 8785500 March 5, 2033 TREATMENT OF TREATMENT-RESISTANT DEPRESSION IN ADULT IN CONJUNCTION WITH AN ORAL ANTIDEPRESSANT
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 8785500 March 5, 2033 TREATMENT OF TREATMENT-RESISTANT DEPRESSION IN ADULTS
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11446260 March 14, 2034 TREATMENT OF DEPRESSIVE SYMPTOMS IN ADULTS WITH MDD WITH ACUTE SUICIDAL IDEATION OR BEHAVIOR BY NASALLY ADMINISTERING 56MG OR 84MG OF ESKETAMINE AS A PHARMACEUTICAL COMPOSITION TWICE PER WEEK IN CONJUNCTION WITH AN ORAL ANTIDEPRESSANT
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11446260 March 14, 2034 TREATMENT OF TREATMENT RESISTANT DEPRESSION IN ADULTS BY NASALLY ADMINISTERING 56MG OR 84MG OF ESKETAMINE AS A PHARMACEUTICAL COMPOSITION
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11446260 March 14, 2034 TREATMENT OF TREATMENT-RESISTANT DEPRESSION IN ADULTS BY NASALLY ADMINISTERING 56MG OR 84MG OF ESKETAMINE AS A PHARMACEUTICAL COMPOSITION IN CONJUNCTION WITH AN ORAL ANTIDEPRESSANT
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11446260 March 14, 2034 TREATMENT OF TREATMENT RESISTANT DEPRESSION IN ADULTS BY NASALLY ADMINISTERING 56MG OR 84MG OF ESKETAMINE TWICE PER WEEK AS A PHARMACEUTICAL COMPOSITION
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11446260 March 14, 2034 TREATMENT OF TREATMENT-RESISTANT DEPRESSION IN ADULTS BY NASALLY ADMINISTERING 56MG OR 84MG OF ESKETAMINE TWICE PER WEEK AS A PHARMACEUTICAL COMPOSITION IN CONJUNCTION WITH AN ORAL ANTIDEPRESSANT
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 10869844 Sept. 10, 2035 TREATMENT OF DEPRESSIVE SYMPTOMS IN ADULTS WITH MDD WITH ACUTE SUICIDAL IDEATION OR BEHAVIOR BY NASALLY ADMINISTERING 56MG OR 84 MG OF ESKETAMINE 2X WEEKLY FOR 4 WEEKS IN CONJUNCTION WITH AN ORAL ANTIDEPRESSANT
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 10869844 Sept. 10, 2035 TREATMENT OF TRD IN ADULTS BY NASALLY ADMINISTERING 56MG OR 84MG OF ESKETAMINE 2X WEEKLY FOR 4 WEEKS DURING THE INDUCTION PHASE FOLLOWED BY A MAINTENANCE PHASE OF 56MG OR 84 MG WEEKLY OR 1X EVERY TWO WEEKS IN CONJUNCTION WITH AN ORAL ANTIDEPRESSANT
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 10869844 Sept. 10, 2035 TREATMENT OF TRD IN ADULTS BY NASALLY ADMINISTERING 56MG OR 84MG OF ESKETAMINE 2X WEEKLY FOR 4 WEEKS DURING THE INDUCTION PHASE IN CONJUNCTION WITH AN ORAL ANTIDEPRESSANT
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 10869844 Sept. 10, 2035 TREATMENT OF TREATMENT RESISTANT DEPRESSION IN ADULTS BY NASALLY ADMINISTERING 56MG OR 84MG 2X WEEKLY FOR 4 WEEKS DURING THE INDUCTION PHASE
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 10869844 Sept. 10, 2035 TREATMENT OF TREATMENT RESISTANT DEPRESSION IN ADULTS BY NASALLY ADMINISTERING 56MG OR 84MG 2X WEEKLY FOR 4 WEEKS DURING THE INDUCTION PHASE FOLLOWED BY A MAINTENANCE PHASE OF 56MG OR 84MG WEEKLY OR 1X EVERY TWO WEEKS
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11173134 Sept. 10, 2035 TREATMENT OF DEPRESSION IN ADULTS WITH MOD AND ACUTE SUICIDAL IDEATION OR BEHAVIOR IN CONJUNCTION WITH AN ORAL ANTIDEPRESSANT BY NASALLY ADMINISTERING 56MG OR 84MG OF ESKETAMINE IN A MAINTENANCE PHASE WEEKLY OR LX EVERY 2 WEEKS AFTER INDUCTION PHASE
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11173134 Sept. 10, 2035 TREATMENT OF TRD IN CONJUNCTION WITH AN ORAL ANTIDEPRESSANT BY NASALLY ADMINISTERING 56MG OR 84MG OF ESKETAMINE IN A MAINTENANCE PHASE WEEKLY OR 1X EVERY TWO WEEKS TO ADULTS WHO HAVE BEEN ADMINISTERED ESKETAMINE IN A INDUCTION PHASE FOR ABOUT 4 WEEKS
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11173134 Sept. 10, 2035 TREATMENT OF TREATMENT RESISTANT DEPRESSION BY NASALLY ADMINISTERING 56MG OR 84MG OF ESKETAMINE IN A MAINTENANCE PHASE WEEKLY OR 1X EVERY TWO WEEKS TO ADULTS WHO HAVE BEEN ADMINISTERED ESKETAMINE IN A INDUCTION PHASE FOR ABOUT 4 WEEKS
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11311500 Sept. 10, 2035 TREATMENT OF DEPRESSIVE SYMPTOMS IN ADULTS WITH MDD WITH ACUTE SUICIDAL IDEATION OR BEHAVIOR BY NASALLY ADMINISTERING 56MG OR 84 MG OF ESKETAMINE 2X WEEKLY FOR 4 WEEKS IN CONJUNCTION WITH AN ORAL ANTIDEPRESSANT
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11311500 Sept. 10, 2035 TREATMENT OF TRD IN ADULTS BY NASALLY ADMINISTERING 56MG OR 84MG OF ESKETAMINE 2X WEEKLY FOR 4 WEEKS DURING THE INDUCTION PHASE FOLLOWED BY A MAINTENANCE PHASE OF 56MG OR 84 MG WEEKLY OR 1X EVERY TWO WEEKS IN CONJUNCTION WITH AN ORAL ANTIDEPRESSANT
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11311500 Sept. 10, 2035 TREATMENT OF TRD IN ADULTS BY NASALLY ADMINISTERING 56MG OR 84MG OF ESKETAMINE 2X WEEKLY FOR 4 WEEKS DURING THE INDUCTION PHASE IN CONJUNCTION WITH AN ORAL ANTIDEPRESSANT
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11311500 Sept. 10, 2035 TREATMENT OF TREATMENT RESISTANT DEPRESSION IN ADULTS BY NASALLY ADMINISTERING 56MG OR 84MG OF ESKETAMINE 2X WEEKLY FOR 4 WEEKS DURING THE INDUCTION PHASE
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11311500 Sept. 10, 2035 TREATMENT OF TREATMENT-RESISTANT DEPRESSION IN ADULTS BY NASALLY ADMINISTERING 56MG OR 84MG OF ESKETAMINE 2X WEEKLY FOR 4 WEEKS DURING THE INDUCTION PHASE FOLLOWED BY A MAINTENANCE PHASE OF 56MG OR 84MG WEEKLY OR 1X EVERY TWO WEEKS
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11883526 Feb. 18, 2040 TREATMENT OF DEPRESSION IN MDD WITH ACUTE SUICIDAL IDEATION/BEHAVIOR WITH NASALLY ADMINISTERED ESKETAMINE WITH OAD IN A PATIENT WHO HAS MISSED A DOSE IN THE MAINTENANCE PHASE AND HAD WORSENING DEPRESSION SYMPTOMS BY RETURN TO HIGHER DOSING SCHEDULE
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11883526 Feb. 18, 2040 TREATMENT OF TRD WITH NASALLY ADMINISTERED ESKETAMINE IN CONJUNCTION WITH AN OAD IN A PATIENT WHO HAS MISSED A DOSE DURING THE MAINTENANCE PHASE AND HAD WORSENING OF DEPRESSION SYMPTOM BY RETURNING TO HIGHER DOSING SCHEDULE
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL 11883526 Feb. 18, 2040 TREATMENT OF TREATMENT-RESISTANT DEPRESSION WITH NASALLY ADMINISTERED ESKETAMINE IN A PATIENT WHO HAS MISSED A DOSE DURING THE MAINTENANCE PHASE AND HAD WORSENING OF DEPRESSION SYMPTOMS BY RETURNING TO A HIGHER DOSING SCHEDULE

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 28MG BASE SPRAVATO JANSSEN PHARMS N211243 March 5, 2019 RX SPRAY NASAL Jan. 17, 2028 EXPANSION OF THE INDICATION TO INCLUDE MONOTHERAPY OF ESKETAMINE FOR TREATMENT-RESISTANT DEPRESSION (TRD)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Glutamate NMDA receptor Ion channel ANTAGONIST Ki 6.16 SCIENTIFIC LITERATURE

External reference:

IDSource
D07283 KEGG_DRUG
33643-47-9 SECONDARY_CAS_RN
4038229 VANDF
4038230 VANDF
CHEBI:60799 CHEBI
JC9 PDB_CHEM_ID
CHEMBL395091 ChEMBL_ID
CHEMBL2364609 ChEMBL_ID
C000629870 MESH_SUPPLEMENTAL_RECORD_UI
9152 IUPHAR_LIGAND_ID
7884 INN_ID
DB11823 DRUGBANK_ID
50LFG02TXD UNII
2119365 RXNORM
309966 MMSL
36280 MMSL
d09174 MMSL
015448 NDDF
015449 NDDF
1217154004 SNOMEDCT_US
785816006 SNOMEDCT_US
789486001 SNOMEDCT_US
C2825616 UMLSCUI
182137 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Spravato HUMAN PRESCRIPTION DRUG LABEL 1 50458-028 SOLUTION 28 mg NASAL NDA 38 sections