rasagiline ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
monoamine oxydase (MAO)-inhibitors type B 3521 136236-51-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • TVP-1022
  • rasagiline hydrochloride
  • rasagiline
  • azilect
  • (R)-(+)-Rasagiline
  • rasagiline mesylate
  • TV-1030
  • rasagiline mesilate
Rasagiline is a selective, irreversible MAO-B inhibitor indicated for the treatment of idiopathic Parkinson's disease. The results of a clinical trial designed to examine the effects of rasagiline tablets on blood pressure when it is administered with increasing doses of tyramine indicates the functional selectivity can be incomplete when healthy subjects ingest large amounts of tyramine while receiving recommended doses of rasagiline tablets. The selectivity for inhibiting MAO-B diminishes in a dose-related manner. One mechanism is believed to be related to its MAO-B inhibitory activity, which causes an increase in extracellular levels of dopamine in the striatum. The elevated dopamine level and subsequent increased dopaminergic activity are likely to mediate rasagilineโ€™s beneficial effects seen in models of dopaminergic motor dysfunction.
  • Molecular weight: 171.24
  • Formula: C12H13N
  • CLOGP: 2.34
  • LIPINSKI: 0
  • HAC: 1
  • HDO: 1
  • TPSA: 12.03
  • ALOGS: -3.84
  • ROTB: 2

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
1 mg O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 36 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
May 16, 2006 FDA TEVA
March 23, 2018 PMDA Takeda Pharmaceutical Company Limited

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
Hallucination 222.89 22.18 102 4726 46555 50553741
Dyskinesia 195.64 22.18 80 4748 27781 50572515
Hallucination, visual 189.78 22.18 68 4760 16514 50583782
Serotonin syndrome 124.05 22.18 56 4772 24657 50575639
Fall 113.80 22.18 149 4679 334783 50265513
On and off phenomenon 90.29 22.18 22 4806 1390 50598906
Bradykinesia 76.17 22.18 24 4804 3919 50596377
Delusion 72.88 22.18 30 4798 10539 50589757
Pleurothotonus 66.79 22.18 17 4811 1284 50599012
Drug interaction 63.16 22.18 86 4742 199535 50400761
Freezing phenomenon 60.76 22.18 15 4813 1000 50599296
Tremor 56.66 22.18 62 4766 114841 50485455
Confusional state 52.67 22.18 76 4752 185852 50414444
Gambling disorder 48.72 22.18 13 4815 1181 50599115
Orthostatic hypotension 48.71 22.18 32 4796 29449 50570847
Sudden onset of sleep 48.23 22.18 11 4817 521 50599775
Muscle rigidity 42.18 22.18 20 4808 9809 50590487
Impulse-control disorder 40.60 22.18 10 4818 660 50599636
Compulsive shopping 39.91 22.18 10 4818 708 50599588
Hypersexuality 39.08 22.18 9 4819 445 50599851
Stoma site discharge 38.68 22.18 11 4817 1264 50599032
Labelled drug-drug interaction medication error 35.06 22.18 18 4810 10459 50589837
Coronary artery dissection 34.87 22.18 9 4819 718 50599578
Stoma site erythema 33.05 22.18 9 4819 882 50599414
Altered state of consciousness 31.91 22.18 22 4806 21888 50578408
Psychotic symptom 30.32 22.18 9 4819 1203 50599093
Choking 29.60 22.18 15 4813 8483 50591813
Serum serotonin increased 29.47 22.18 6 4822 165 50600131
Compulsive hoarding 28.79 22.18 5 4823 56 50600240
Agitation 28.36 22.18 30 4798 53354 50546942
Anxiety 28.05 22.18 56 4772 177550 50422746
Stoma site extravasation 27.05 22.18 6 4822 250 50600046
Stoma site hypergranulation 26.33 22.18 6 4822 283 50600013
Dementia 25.53 22.18 17 4811 15980 50584316
Resting tremor 25.38 22.18 7 4821 719 50599577
Cerebral atrophy 24.88 22.18 11 4817 4590 50595706
Fracture 24.74 22.18 17 4811 16816 50583480
Gait disturbance 24.52 22.18 48 4780 149957 50450339
Parkinsonian gait 23.79 22.18 6 4822 436 50599860
Nocturia 23.79 22.18 12 4816 6718 50593578
Sleep talking 23.63 22.18 7 4821 929 50599367
Balance disorder 23.12 22.18 31 4797 70559 50529737
Dystonia 22.29 22.18 14 4814 11912 50588384

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
Hallucination 453.83 24.75 224 7446 44488 29522369
Impulse-control disorder 286.80 24.75 66 7604 1159 29565698
Dyskinesia 247.00 24.75 115 7555 19946 29546911
Hypersexuality 208.33 24.75 52 7618 1304 29565553
Hallucination, visual 178.31 24.75 84 7586 14931 29551926
Fall 155.29 24.75 209 7461 176969 29389888
On and off phenomenon 153.63 24.75 44 7626 1884 29564973
Gambling disorder 153.11 24.75 42 7628 1533 29565324
Freezing phenomenon 124.25 24.75 34 7636 1229 29565628
Orthostatic hypotension 122.27 24.75 75 7595 22554 29544303
Confusional state 121.27 24.75 157 7513 127720 29439137
Dopamine dysregulation syndrome 117.13 24.75 25 7645 304 29566553
Delusion 92.43 24.75 49 7621 11167 29555690
Serotonin syndrome 74.61 24.75 50 7620 17462 29549395
Abnormal behaviour 73.03 24.75 55 7615 23072 29543785
Resting tremor 67.19 24.75 18 7652 599 29566258
Somnolence 63.11 24.75 98 7572 93857 29473000
Dystonia 59.57 24.75 35 7635 9714 29557143
Bradykinesia 59.21 24.75 25 7645 3422 29563435
Muscle rigidity 55.44 24.75 33 7637 9378 29557479
Compulsive shopping 55.00 24.75 14 7656 380 29566477
Tremor 52.59 24.75 79 7591 73459 29493398
Cogwheel rigidity 50.75 24.75 17 7653 1226 29565631
Sudden onset of sleep 50.58 24.75 13 7657 367 29566490
Stereotypy 47.86 24.75 14 7656 645 29566212
Stoma site discharge 47.42 24.75 15 7655 902 29565955
Cognitive disorder 45.25 24.75 42 7628 23457 29543400
Balance disorder 44.85 24.75 51 7619 36119 29530738
Supine hypertension 43.12 24.75 11 7659 301 29566556
Akinesia 42.94 24.75 17 7653 1973 29564884
Marasmus 42.59 24.75 12 7658 483 29566374
Jealous delusion 42.19 24.75 10 7660 200 29566657
Psychomotor hyperactivity 41.22 24.75 26 7644 8187 29558670
Embedded device 40.86 24.75 10 7660 230 29566627
Stoma site erythema 39.66 24.75 12 7658 622 29566235
Hyperkinesia 39.25 24.75 15 7655 1584 29565273
Sleep disorder 38.34 24.75 39 7631 24347 29542510
Oesophageal achalasia 37.64 24.75 10 7660 322 29566535
Anticholinergic syndrome 35.60 24.75 12 7658 882 29565975
Rapid eye movement sleep behaviour disorder 35.55 24.75 8 7662 126 29566731
Mesenteric artery thrombosis 35.34 24.75 10 7660 409 29566448
Dementia 35.18 24.75 27 7643 11631 29555226
Obsessive-compulsive personality disorder 34.50 24.75 8 7662 145 29566712
Gait disturbance 34.03 24.75 65 7605 73284 29493573
Paraphilia 33.60 24.75 7 7663 75 29566782
Device dislocation 32.33 24.75 18 7652 4509 29562348
Agitation 32.28 24.75 52 7618 51252 29515605
Hyperthermia 31.02 24.75 23 7647 9407 29557450
Psychotic disorder 30.99 24.75 32 7638 20322 29546535
Thunderclap headache 30.96 24.75 6 7664 43 29566814
Autonomic nervous system imbalance 30.35 24.75 14 7656 2362 29564495
Therapeutic product effect variable 30.20 24.75 13 7657 1864 29564993
Nocturia 28.87 24.75 21 7649 8341 29558516
Restlessness 28.76 24.75 32 7638 22113 29544744
Blood lactic acid 28.02 24.75 8 7662 338 29566519
Disturbance in attention 27.89 24.75 31 7639 21393 29545464
Fracture 27.50 24.75 18 7652 6035 29560822
Toxicity to various agents 27.04 24.75 6 7664 173655 29393202
Micturition disorder 26.81 24.75 12 7658 1889 29564968
Aggression 26.53 24.75 39 7631 35502 29531355
Binge eating 26.52 24.75 6 7664 97 29566760
Dysphagia 25.86 24.75 49 7621 54877 29511980

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
Hallucination 509.26 19.41 245 10358 72543 64415586
Dyskinesia 367.20 19.41 162 10441 39226 64448903
Hallucination, visual 323.90 19.41 134 10469 27700 64460429
Impulse-control disorder 261.24 19.41 59 10544 1529 64486600
On and off phenomenon 219.35 19.41 56 10547 2463 64485666
Fall 215.57 19.41 301 10302 416525 64071604
Orthostatic hypotension 177.70 19.41 105 10498 46633 64441496
Hypersexuality 169.56 19.41 41 10562 1438 64486691
Gambling disorder 154.61 19.41 40 10563 1854 64486275
Serotonin syndrome 153.90 19.41 90 10513 39192 64448937
Freezing phenomenon 152.60 19.41 38 10565 1508 64486621
Delusion 129.70 19.41 62 10541 17952 64470177
Dopamine dysregulation syndrome 124.90 19.41 26 10577 453 64487676
Confusional state 121.83 19.41 180 10423 260964 64227165
Bradykinesia 109.32 19.41 41 10562 6519 64481610
Resting tremor 92.21 19.41 25 10578 1389 64486740
Muscle rigidity 90.14 19.41 48 10555 17425 64470704
Dystonia 86.69 19.41 48 10555 18817 64469312
Tremor 86.64 19.41 114 10489 148116 64340013
Sudden onset of sleep 75.75 19.41 18 10585 585 64487544
Stoma site discharge 61.66 19.41 19 10584 1663 64486466
Akinesia 61.51 19.41 22 10581 3057 64485072
Compulsive shopping 61.43 19.41 16 10587 761 64487368
Nocturia 61.35 19.41 32 10571 11133 64476996
Jealous delusion 57.32 19.41 12 10591 215 64487914
Abnormal behaviour 54.97 19.41 45 10558 33577 64454552
Rapid eye movement sleep behaviour disorder 52.46 19.41 12 10591 329 64487800
Dementia 52.27 19.41 36 10567 20730 64467399
Cogwheel rigidity 51.82 19.41 19 10584 2834 64485295
Supine hypertension 51.78 19.41 12 10591 349 64487780
Agitation 51.62 19.41 68 10535 88299 64399830
Drug interaction 51.38 19.41 153 10450 361930 64126199
Balance disorder 51.23 19.41 66 10537 83860 64404269
Stereotypy 50.78 19.41 14 10589 828 64487301
Marasmus 50.36 19.41 14 10589 854 64487275
Autonomic nervous system imbalance 48.35 19.41 20 10583 4112 64484017
Hyperthermia 46.47 19.41 30 10573 15520 64472609
Hyperkinesia 46.40 19.41 17 10586 2529 64485600
Psychotic disorder 45.75 19.41 41 10562 34537 64453592
Disturbance in attention 45.29 19.41 44 10559 41030 64447099
Pleurothotonus 44.30 19.41 16 10587 2286 64485843
Somnolence 44.22 19.41 101 10502 203544 64284585
Mesenteric artery thrombosis 42.01 19.41 11 10592 534 64487595
Gait disturbance 41.45 19.41 89 10514 172066 64316063
Stoma site erythema 41.24 19.41 13 10590 1226 64486903
Choking 40.84 19.41 24 10579 10514 64477615
Anxiety 40.17 19.41 97 10506 202552 64285577
Sleep talking 39.48 19.41 12 10591 1003 64487126
Obsessive-compulsive personality disorder 39.43 19.41 8 10595 122 64488007
Fracture 39.11 19.41 29 10574 18726 64469403
Paraphilia 38.41 19.41 7 10596 58 64488071
Compulsive hoarding 37.60 19.41 7 10596 66 64488063
Oesophageal achalasia 34.91 19.41 10 10593 680 64487449
Micturition urgency 33.48 19.41 21 10582 10338 64477791
Dysphagia 32.61 19.41 61 10542 106751 64381378
Impulsive behaviour 31.53 19.41 13 10590 2650 64485479
Abnormal dreams 30.99 19.41 20 10583 10336 64477793
Aggression 30.80 19.41 38 10565 46194 64441935
Therapeutic product effect variable 30.05 19.41 11 10592 1633 64486496
Altered state of consciousness 29.96 19.41 34 10569 37868 64450261
Neuroleptic malignant syndrome 29.87 19.41 28 10575 24968 64463161
Device dislocation 29.78 19.41 26 10577 21152 64466977
Speech disorder 29.39 19.41 38 10565 48403 64439726
Psychomotor hyperactivity 29.36 19.41 22 10581 14429 64473700
Middle insomnia 29.32 19.41 21 10582 12856 64475273
Blood lactic acid 29.32 19.41 8 10595 455 64487674
Hyperpyrexia 29.18 19.41 15 10588 5062 64483067
Parkinsonian gait 28.64 19.41 9 10594 840 64487289
Presyncope 28.63 19.41 32 10571 35057 64453072
Syncope 28.62 19.41 73 10530 157562 64330567
Cognitive disorder 28.52 19.41 40 10563 55047 64433082
Anticholinergic syndrome 28.15 19.41 12 10591 2657 64485472
Coronary artery dissection 28.03 19.41 9 10594 901 64487228
Nightmare 27.98 19.41 25 10578 20968 64467161
Toxicity to various agents 27.03 19.41 13 10590 363500 64124629
Obsessive-compulsive disorder 27.01 19.41 14 10589 4804 64483325
Disorientation 26.65 19.41 39 10564 55789 64432340
Pneumonia aspiration 26.28 19.41 40 10563 59231 64428898
Micturition disorder 26.25 19.41 12 10591 3136 64484993
Gastrointestinal motility disorder 26.06 19.41 14 10589 5165 64482964
Sleep attacks 25.77 19.41 6 10597 178 64487951
Drooling 25.71 19.41 14 10589 5305 64482824
Sleep disorder 24.66 19.41 39 10564 59670 64428459
Thunderclap headache 24.55 19.41 6 10597 220 64487909
Hip fracture 24.34 19.41 26 10577 27073 64461056
Intermittent claudication 23.46 19.41 11 10592 3043 64485086
Serum serotonin increased 23.31 19.41 6 10597 272 64487857
Prescribed underdose 23.11 19.41 21 10582 17994 64470135
Insomnia 22.85 19.41 78 10525 197758 64290371
Diarrhoea 22.43 19.41 54 10549 722650 63765479
Device occlusion 22.19 19.41 16 10587 9897 64478232
Compulsions 22.01 19.41 6 10597 340 64487789
Delirium 21.71 19.41 40 10563 69154 64418975
Off label use 21.48 19.41 45 10558 632761 63855368
Reduced facial expression 20.64 19.41 9 10594 2104 64486025
Psychotic symptom 20.54 19.41 9 10594 2129 64486000
Poor quality sleep 20.32 19.41 20 10583 18931 64469198
Death 20.17 19.41 142 10461 482563 64005566
Underdose 20.12 19.41 23 10580 25806 64462323
Hyperhidrosis 19.78 19.41 55 10548 124865 64363264
Anosmia 19.63 19.41 11 10592 4406 64483723
Parkinsonism hyperpyrexia syndrome 19.46 19.41 5 10598 225 64487904

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N04BD02 NERVOUS SYSTEM
ANTI-PARKINSON DRUGS
DOPAMINERGIC AGENTS
Monoamine oxidase B inhibitors
FDA MoA N0000000184 Monoamine Oxidase Inhibitors
MeSH PA D002491 Central Nervous System Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D008996 Monoamine Oxidase Inhibitors
MeSH PA D018696 Neuroprotective Agents
MeSH PA D020011 Protective Agents
FDA EPC N0000175744 Monoamine Oxidase Inhibitor
CHEBI has role CHEBI:38623 monoamine oxidase inhibitors
CHEBI has role CHEBI:63726 neuroprotective agents

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

DiseaseRelationSNOMED_IDDOID
Parkinson's disease indication 49049000 DOID:14330
Dyskinesia contraindication 9748009
Bipolar disorder contraindication 13746004 DOID:3312
Orthostatic hypotension contraindication 28651003
Hypertensive disorder contraindication 38341003 DOID:10763
Epilepsy contraindication 84757009 DOID:1826
Disease of liver contraindication 235856003 DOID:409
Pheochromocytoma contraindication 302835009
Malignant melanoma contraindication 372244006




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.54 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 0.5MG BASE AZILECT TEVA N021641 May 16, 2006 RX TABLET ORAL 7815942 Aug. 27, 2027 TREATMENT OF PARKINSONS DISEASE
EQ 1MG BASE AZILECT TEVA N021641 May 16, 2006 RX TABLET ORAL 7815942 Aug. 27, 2027 TREATMENT OF PARKINSONS DISEASE

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Amine oxidase [flavin-containing] B Enzyme INHIBITOR Ki 6.15 CHEMBL CHEMBL
Acetylcholinesterase Enzyme IC50 7.72 CHEMBL
5-hydroxytryptamine receptor 6 GPCR Ki 8.85 CHEMBL
Amine oxidase [flavin-containing] A Enzyme Ki 5.01 CHEMBL
Cholinesterase Enzyme IC50 5.32 CHEMBL
Amine oxidase [flavin-containing] B Enzyme IC50 8.36 CHEMBL
Amine oxidase [flavin-containing] A Enzyme IC50 6.39 CHEMBL

External reference:

IDSource
4025261 VUID
N0000179514 NUI
D02562 KEGG_DRUG
136236-50-5 SECONDARY_CAS_RN
161735-79-1 SECONDARY_CAS_RN
4025261 VANDF
4025262 VANDF
C0525678 UMLSCUI
CHEBI:63620 CHEBI
RAU PDB_CHEM_ID
CHEMBL887 ChEMBL_ID
DB01367 DRUGBANK_ID
CHEMBL1201142 ChEMBL_ID
CHEMBL1235738 ChEMBL_ID
3052776 PUBCHEM_CID
7151 INN_ID
C031967 MESH_SUPPLEMENTAL_RECORD_UI
6641 IUPHAR_LIGAND_ID
003N66TS6T UNII
134748 RXNORM
162358 MMSL
20417 MMSL
70623 MMSL
d05612 MMSL
010775 NDDF
010776 NDDF
418734001 SNOMEDCT_US
419010007 SNOMEDCT_US
734664007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Rasagiline HUMAN PRESCRIPTION DRUG LABEL 1 0093-3060 TABLET 0.50 mg ORAL NDA authorized generic 29 sections
Rasagiline HUMAN PRESCRIPTION DRUG LABEL 1 0093-3060 TABLET 0.50 mg ORAL NDA authorized generic 29 sections
Rasagiline HUMAN PRESCRIPTION DRUG LABEL 1 0093-3061 TABLET 1 mg ORAL NDA authorized generic 29 sections
Rasagiline HUMAN PRESCRIPTION DRUG LABEL 1 0093-3061 TABLET 1 mg ORAL NDA authorized generic 29 sections
Rasagiline Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0378-1270 TABLET 0.50 mg ORAL ANDA 30 sections
Rasagiline Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0378-1270 TABLET 0.50 mg ORAL ANDA 30 sections
Rasagiline Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0378-1271 TABLET 1 mg ORAL ANDA 30 sections
Rasagiline Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0378-1271 TABLET 1 mg ORAL ANDA 30 sections
Rasagiline Human Prescription Drug Label 1 16714-770 TABLET 0.50 mg ORAL ANDA 29 sections
Rasagiline Human Prescription Drug Label 1 16714-771 TABLET 1 mg ORAL ANDA 29 sections
Rasagiline Mesylate Human Prescription Drug Label 1 23155-746 TABLET 0.50 mg ORAL ANDA 29 sections
Rasagiline Mesylate Human Prescription Drug Label 1 23155-747 TABLET 1 mg ORAL ANDA 29 sections
Rasagiline HUMAN PRESCRIPTION DRUG LABEL 1 42291-779 TABLET 0.50 mg ORAL NDA authorized generic 29 sections
Rasagiline HUMAN PRESCRIPTION DRUG LABEL 1 42291-780 TABLET 1 mg ORAL NDA authorized generic 29 sections
RASAGILINE HUMAN PRESCRIPTION DRUG LABEL 1 42571-220 TABLET 0.50 mg ORAL ANDA 29 sections
RASAGILINE HUMAN PRESCRIPTION DRUG LABEL 1 42571-221 TABLET 1 mg ORAL ANDA 29 sections
Azilect HUMAN PRESCRIPTION DRUG LABEL 1 43353-015 TABLET 1 mg ORAL NDA 30 sections
Rasagiline HUMAN PRESCRIPTION DRUG LABEL 1 47781-683 TABLET 0.50 mg ORAL ANDA 27 sections
Rasagiline HUMAN PRESCRIPTION DRUG LABEL 1 47781-690 TABLET 1 mg ORAL ANDA 27 sections
Azilect HUMAN PRESCRIPTION DRUG LABEL 1 54868-6206 TABLET 1 mg ORAL NDA 30 sections
Rasagiline Human Prescription Drug Label 1 67877-259 TABLET 0.50 mg ORAL ANDA 29 sections
Rasagiline Human Prescription Drug Label 1 67877-260 TABLET 1 mg ORAL ANDA 29 sections
Azilect HUMAN PRESCRIPTION DRUG LABEL 1 68546-142 TABLET 0.50 mg ORAL NDA 30 sections
Azilect HUMAN PRESCRIPTION DRUG LABEL 1 68546-142 TABLET 0.50 mg ORAL NDA 30 sections
Azilect HUMAN PRESCRIPTION DRUG LABEL 1 68546-229 TABLET 1 mg ORAL NDA 30 sections
Azilect HUMAN PRESCRIPTION DRUG LABEL 1 68546-229 TABLET 1 mg ORAL NDA 30 sections