◎ Sugi Atlas

Atlas / Drug / Rasagiline

Rasagiline

drug
On this page

Also known as AGN-1135NSC-759639RasagilinaTV-1030rasR(+)RasagilineRasaglineAzilectRASAGILINE MESILATERasagiline mesylate[N-Propargyl-1R(+)-aminoindan]

Summary

Rasagiline (CHEMBL887) is an approved small-molecule EC 1.4.3.4 (monoamine oxidase) inhibitor (ATC N04BD02) targeting MAOB; indicated across 5 conditions including parkinson disease and progressive supranuclear palsy.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N04BD02
  • Targets: 1 (MAOB)
  • Indications: 5 conditions
  • Clinical trials: 51
  • Chemistry: 171.24 Da · C12H13N

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL887
NameRasagiline
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID3052776
ChEBICHEBI:63620
ATCN04BD02
Molecular formulaC12H13N
Molecular weight171.24
InChIKeyRUOKEQAAGRXIBM-GFCCVEGCSA-N

SMILES: C#CCN[C@@H]1CCC2=CC=CC=C12

IUPAC name: (1R)-N-prop-2-ynyl-2,3-dihydro-1H-inden-1-amine

ChEBI definition: An indane that consists of 1-aminoindane bearing an N-propargyl substituent. A selective, irreversible monoamine oxidase-B inhibitor.

Pharmacological roles (ChEBI): EC 1.4.3.4 (monoamine oxidase) inhibitor, neuroprotective agent.

Also known as: AGN-1135, NSC-759639, Rasagilina, Rasagiline, TV-1030, ras, R(+)Rasagiline, RASAGILINE, rasagiline, Rasagline, Azilect, RASAGILINE MESILATE

Parent form; salt/anhydrous children: CHEMBL1201142, CHEMBL6067988

Patent coverage: 3,464 distinct patent families (12,978 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
MAOBMonoamine oxidase BInhibition7.850%P27338

Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: Cholinesterase, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Amine oxidase [flavin-containing] A, Amine oxidase [flavin-containing] B, Acetylcholinesterase, Alpha-1A adrenergic receptor, Amine oxidase [flavin-containing] B, Amine oxidase [flavin-containing] A, 5-hydroxytryptamine receptor 6.

Bioactivity

ChEMBL activities: 122 potent at pChembl ≥ 5 of 136 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P213969IC501nMCHEMBL_ACT_15220946
HTR68.85Ki1.4nMCHEMBL_ACT_22798737
MAOB8.4IC504nMCHEMBL_ACT_16308822
MAOB8.4IC504nMCHEMBL_ACT_26595827
P196438.37IC504.31nMCHEMBL_ACT_19171910
P196438.36IC504.4nMCHEMBL_ACT_1263327
P196438.36IC504.4nMCHEMBL_ACT_18916400
P196438.36IC504.4nMCHEMBL_ACT_19241113
MAOB8.36IC504.4nMCHEMBL_ACT_2077436
MAOB8.36IC504.4nMCHEMBL_ACT_24995271
MAOB8.22IC506nMCHEMBL_ACT_23163314
MAOB8.12Ki7.6nMCHEMBL_ACT_15163795
MAOB8.1IC507.87nMCHEMBL_ACT_16766896
MAOB8.08IC508.4nMCHEMBL_ACT_19030125
MAOB8IC509.97nMCHEMBL_ACT_17961022
MAOB8IC5010nMCHEMBL_ACT_18387223
MAOB7.94IC5011.6nMCHEMBL_ACT_20706657
MAOB7.89IC5013nMCHEMBL_ACT_19048933
MAOB7.89IC5013nMCHEMBL_ACT_19171925
MAOB7.85IC5014nMCHEMBL_ACT_12135692
MAOB7.85IC5014nMCHEMBL_ACT_14545550
MAOB7.85Ki14.2nMCHEMBL_ACT_15163802
MAOB7.85IC5014nMCHEMBL_ACT_18052500
MAOB7.85IC5014nMCHEMBL_ACT_18942344
MAOB7.85IC5014nMCHEMBL_ACT_729190
MAOB7.81IC5015.4nMCHEMBL_ACT_22798757
MAOB7.81IC5015.4nMCHEMBL_ACT_24914024
MAOB7.77IC5017nMCHEMBL_ACT_26132687
ACHE7.72IC5019nMCHEMBL_ACT_18222961
MAOB7.72IC5019.05nMCHEMBL_ACT_25659814

Target pathways

Aggregated over 1 target gene(s): MAOB.

Top Reactome pathways

5 total, by targets touching each:

PathwayTargetsGenes
Amine Oxidase reactions1MAOB
Biogenic amines are oxidatively deaminated to aldehydes by MAOA and MAOB1MAOB
Metabolism1MAOB
Biological oxidations1MAOB
Phase I - Functionalization of compounds1MAOB

Dominant GO biological processes

GO termTargets
substantia nigra development1
dopamine catabolic process1
hydrogen peroxide biosynthetic process1

Indications & clinical

Indications

5 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
Parkinson disease4MONDO:0005180MONDO:0005180
progressive supranuclear palsy3MONDO:0019037MONDO:0019037
restless legs syndrome2MONDO:0005391EFO:0004270
Alzheimer disease2MONDO:0004975MONDO:0004975
amyotrophic lateral sclerosis2MONDO:0004976MONDO:0004976

Clinical trials

Total trials: 51.

Phase distribution

PhaseTrials
PHASE418
PHASE312
PHASE28
Not specified6
PHASE15
PHASE2/PHASE32

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00399477PHASE4COMPLETEDA Non-Blinded Study Demonstrating the Effectiveness and Safety of Azilect Alone or in Combination Therapy in Parkinson’s Disease
NCT00492336PHASE4COMPLETEDRasagiline in the Treatment of Persistent Negative Symptoms of Schizophrenia
NCT00696215PHASE4UNKNOWNThe Effects of Rasagiline on Cognitive Deficits Associated With Parkinson’s Disease
NCT00755027PHASE4COMPLETEDRasagiline and Apathy in Parkinson’s Disease
NCT00902941PHASE4COMPLETEDOlfaction in Patients With Parkinson’s Disease Following Treatment With Rasagiline
NCT01007630PHASE4UNKNOWNA Study Assessing Change in Sense of Smell After Rasagiline Use in Parkinson’s Patients
NCT01048229PHASE4TERMINATEDEvaluation of the Tolerance and Acceptability of Rasagiline in the Treatment of Early-stage Parkinson’s Disease
NCT01049984PHASE4COMPLETEDRasagiline as Add on to Dopamine Agonists in the Treatment of Parkinson’s Disease
NCT01055379PHASE4COMPLETEDRasagiline in Cognitive-impairment Related Depression: AzileCt in COgnitive-impairment Related DepressiOn
NCT01168596PHASE4COMPLETEDRasagiline for the Symptomatic Treatment of Fatigue in Parkinson’s Disease
NCT01178047PHASE4TERMINATEDMulticenter Placebo Controlled Study to Assess the Effect of Rasagiline on Sleep-wake Disturbances in Patients With Parkinson’s Disease
NCT01382342PHASE4COMPLETEDThe Effect of Rasagiline on Cognition in Parkinson’s Disease
NCT01385735PHASE4UNKNOWNEmotion, Mood and Executive Function in Parkinson’s Disease (PD)
NCT01442610PHASE4COMPLETEDEffects of Rasagiline on Sleep Disturbances in Parkinson’s Disease
NCT01497652PHASE4COMPLETEDA Double Blind Placebo Controlled Trial Evaluating Rasagiline Effects on Cognition in Parkinson’s Disease Patients With Mild Cognitive Impairment Receiving Dopaminergic Therapy
NCT01723228PHASE4COMPLETEDParallel-Group Study to Assess the Effect of Rasagiline on Cognition in Patients With Parkinson’s Disease
NCT02068625PHASE4TERMINATEDRasagiline (Azilect) - Neuroprotection for Macula-off Retinal Detachment
NCT04525729PHASE4COMPLETEDRituximab and RASi in Patients with IgAN
NCT00203034PHASE3COMPLETEDMulticenter Study of Rasagiline in Parkinson’s Disease Patients Using Levodopa and Experiencing Motor Fluctuations
NCT00203060PHASE3COMPLETEDEffectiveness, Tolerability and Safety of Rasagiline in Early Parkinson’s Disease Patients Not Treated With Levodopa
NCT00203125PHASE3COMPLETEDA Study to Evaluate the Effects of Tyramine in Patients Who Completed the PRESTO Study.
NCT00203138PHASE3COMPLETEDSafety, Tolerability, and Effectiveness of Rasagiline Mesylate in Patients With Parkinson’s Disease
NCT00203164PHASE3COMPLETEDStudy to Evaluate the Safety and Tolerability of Rasagiline in Advanced Parkinson’s Disease Patients
NCT00203177PHASE3COMPLETEDRasagiline in Advanced Parkinson’s Disease Patients With Motor Fluctuations Treated With Levodopa/Carbidopa Therapy.
NCT00256204PHASE3COMPLETEDA Randomized Placebo Controlled Study to Show That Rasagiline May Slow Disease Progression for Parkinson’s Disease
NCT01187888PHASE3TERMINATEDEfficacy, Tolerability and Safety of Azilect in Subjects With Progressive Supranuclear Palsy
NCT01192503PHASE2/PHASE3TERMINATEDSafety and Efficacy of Rasagiline in Restless Legs Syndrome
NCT01215227PHASE3TERMINATEDAn Active-Controlled Extension Study to NCT01155466 [P04938] and NCT01227265 [P07037] (P06153)
NCT01556165PHASE3COMPLETEDRasagiline in Early Parkinson’s Disease Patients Not Treated With Levodopa in China
NCT01736891PHASE3COMPLETEDClinical Trial of Rasagiline in Levodopa-Treated Parkinson’s Disease Patients With Motor Fluctuations
NCT03329508PHASE3COMPLETEDA Phase 3 Study With P2B001 in Subjects With Early Parkinson’s
NCT05611372PHASE2/PHASE3WITHDRAWNEfficacy and Safety of Rasagiline in Prodromal Parkinson’s Disease
NCT00104273PHASE2COMPLETEDRasagiline 1 mg and 2 mg Added to Aricept 10 mg Daily in Patients With Mild to Moderate Alzheimer’s Disease (AD)
NCT00737152PHASE2UNKNOWNEvaluate the Side Effects and Benefits of RAS 130 With or Without Diet and Exercise in Type II Diabetes Mellitus
NCT00977665PHASE2COMPLETEDClinical Trial to Assess Efficacy, Safety, and Tolerability of Rasagiline Mesylate 1 mg in Patients With Multiple System Atrophy of the Parkinsonian Subtype (MSA-P)
NCT01232738PHASE2COMPLETEDTrial of Safety and Efficacy of Rasagiline in Patients With Amyotrophic Lateral Sclerosis (ALS)
NCT01786603PHASE2COMPLETEDRasagiline in Subjects With Amyotrophic Lateral Sclerosis (ALS)
NCT01879241PHASE2COMPLETEDStudy of Rasagiline in Patients With Amyotrophic Lateral Sclerosis
NCT02359552PHASE2COMPLETEDRasagiline Rescue in Alzheimer’s Disease Clinical Trial
NCT02789020PHASE2COMPLETEDImage Parkinson’s Disease Progression Study

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 2 clinical and 8 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

48 molecules share ≥1 primary target. Top 48 by shared-target count:

MoleculeSourceStatusShared targets
TEDIZOLIDChEMBL + PubChemPhase 4 (approved)MAOB
CLOTRIMAZOLEChEMBLPhase 4 (approved)MAOB
DANTHRONChEMBLPhase 4 (approved)MAOB
DONEPEZILChEMBLPhase 4 (approved)MAOB
FENTANYLChEMBLPhase 4 (approved)MAOB
IPRONIAZIDChEMBLPhase 4 (approved)MAOB
ISTRADEFYLLINEChEMBLPhase 4 (approved)MAOB
LINEZOLIDChEMBLPhase 4 (approved)MAOB
MENADIONEChEMBLPhase 4 (approved)MAOB
METHYLENE BLUE CATIONChEMBLPhase 4 (approved)MAOB
MICONAZOLEChEMBLPhase 4 (approved)MAOB
MOCLOBEMIDEChEMBLPhase 4 (approved)MAOB
PARGYLINEChEMBLPhase 4 (approved)MAOB
PHENELZINEChEMBLPhase 4 (approved)MAOB
PIOGLITAZONEChEMBLPhase 4 (approved)MAOB
PRIMAQUINEChEMBLPhase 4 (approved)MAOB
ROSIGLITAZONEChEMBLPhase 4 (approved)MAOB
SAFINAMIDEChEMBLPhase 4 (approved)MAOB
SELEGILINEChEMBLPhase 4 (approved)MAOB
TOLOXATONEChEMBLPhase 4 (approved)MAOB
TRANYLCYPROMINEChEMBLPhase 4 (approved)MAOB
TROGLITAZONEChEMBLPhase 4 (approved)MAOB
ZONISAMIDEChEMBLPhase 4 (approved)MAOB
CURCUMINChEMBLPhase 3MAOB
IDAZOXANChEMBLPhase 3MAOB
QUERCETINChEMBLPhase 3MAOB
RESVERATROLChEMBLPhase 3MAOB
ATIBEPRONEChEMBLPhase 2MAOB
BROFAROMINEChEMBLPhase 2MAOB
CIGLITAZONEChEMBLPhase 2MAOB
CLORGILINEChEMBLPhase 2MAOB
DAIDZEINChEMBLPhase 2MAOB
FORMONONETINChEMBLPhase 2MAOB
GENISTEINChEMBLPhase 2MAOB
HYMECROMONEChEMBLPhase 2MAOB
LADOSTIGILChEMBLPhase 2MAOB
LAZABEMIDEChEMBLPhase 2MAOB
LOFLUCARBANChEMBLPhase 2MAOB
LUTEOLINChEMBLPhase 2MAOB
MOFEGILINEChEMBLPhase 2MAOB
MOLIBRESIBChEMBLPhase 2MAOB
PHENAMAZOLINEChEMBLPhase 2MAOB
PIPERINEChEMBLPhase 2MAOB
SEMBRAGILINEChEMBLPhase 2MAOB
SUTEZOLIDChEMBLPhase 2MAOB
TIOXOLONEChEMBLPhase 2MAOB
VAFIDEMSTATChEMBLPhase 2MAOB
MedroxyprogesteronePubChemApprovedMAOB

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot