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Atlas / Drug / Methylphenidate

Methylphenidate

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Also known as Cotempla xr-odtDaytranaMethylphenidate extended releaseMetilfenidatoPrc-063Threo-dl-methylphenidate(+/-)-methylphenidate

Summary

Methylphenidate (CHEMBL796) is an approved small molecule (ATC N06BA04) targeting SLC6A2 and SLC6A3; indicated across 31 conditions including attention deficit-hyperactivity disorder and narcolepsy.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N06BA04
  • Targets: 2 (SLC6A2, SLC6A3)
  • Indications: 31 conditions
  • Clinical trials: 265
  • Chemistry: 233.31 Da · C14H19NO2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL796
NameMethylphenidate
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID4158
ChEBICHEBI:84276
ATCN06BA04
Molecular formulaC14H19NO2
Molecular weight233.31
InChIKeyDUGOZIWVEXMGBE-UHFFFAOYSA-N

SMILES: COC(=O)C(C1CCCCN1)C2=CC=CC=C2

IUPAC name: methyl 2-phenyl-2-piperidin-2-ylacetate

ChEBI definition: A amino acid ester that is methyl phenylacetate in which one of the hydrogens α to the carbonyl group is replaced by a piperidin-2-yl group.

Also known as: Cotempla xr-odt, Daytrana, Methylphenidate, Methylphenidate extended release, Metilfenidato, Prc-063, Threo-dl-methylphenidate, methylphenidate, METHYLPHENIDATE, (+/-)-methylphenidate

Parent form; salt/anhydrous children: CHEMBL1722

Patent coverage: 9,000 distinct patent families (31,999 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
SLC6A2NETInhibition7.210.4%P23975
SLC6A3DATInhibition7.10.2%Q01959

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Sodium-dependent noradrenaline transporter, Sodium-dependent serotonin transporter, Sodium-dependent dopamine transporter, Sodium-dependent dopamine transporter.

Bioactivity

ChEMBL activities: 9 potent at pChembl ≥ 5 of 10 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
SLC6A37.77IC5017nMCHEMBL_ACT_1146651
SLC6A37.47Ki34nMCHEMBL_ACT_15029274
SLC6A27.21IC5061nMCHEMBL_ACT_1801934
SLC6A37.1IC5079nMCHEMBL_ACT_1801932
P239777.08IC5083nMCHEMBL_ACT_1146653
SLC6A36.96Ki110nMCHEMBL_ACT_1801929
SLC6A26.47Ki340nMCHEMBL_ACT_15029275
SLC6A26.18Ki660nMCHEMBL_ACT_1801931
SLC6A45.29IC505100nMCHEMBL_ACT_1801933

Target pathways

Aggregated over 2 target gene(s): SLC6A2, SLC6A3.

Top Reactome pathways

14 total, by targets touching each:

PathwayTargetsGenes
Disease2SLC6A2, SLC6A3
Transport of small molecules2SLC6A2, SLC6A3
R-HSA-4253662SLC6A2, SLC6A3
SLC-mediated transmembrane transport2SLC6A2, SLC6A3
SLC-mediated transport of neurotransmitters2SLC6A2, SLC6A3
SLC transporter disorders2SLC6A2, SLC6A3
Disorders of transmembrane transporters2SLC6A2, SLC6A3
Neurotransmitter clearance1SLC6A3
Transmission across Chemical Synapses1SLC6A3
Neuronal System1SLC6A3
Dopamine clearance from the synaptic cleft1SLC6A3
Defective neurotransmitter clearance by SLC6A3 causes Parkinsonism-dystonia infantile (PKDYS)1SLC6A3
Defective SLC6A2 causes orthostatic intolerance (OI)1SLC6A2
Defective transport of neurotransmitters by SLC6A3 causes Parkinsonism-dystonia infantile (PKDYS)1SLC6A3

Dominant GO biological processes

GO termTargets
neurotransmitter transport2
amino acid transport2
response to xenobiotic stimulus2
obsolete monoamine transport2
sodium ion transmembrane transport2
dopamine uptake involved in synaptic transmission2
norepinephrine uptake2
transmembrane transport2
chemical synaptic transmission1
obsolete norepinephrine transport1
response to pain1
neuron cellular homeostasis1
catecholamine uptake1
neurotransmitter reuptake1
chloride transmembrane transport1

Indications & clinical

Indications

31 indications (2 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
attention deficit-hyperactivity disorder4MONDO:0007743EFO:0003888
narcolepsy4MONDO:0021107MONDO:0016158
brain neoplasm3MONDO:0021211EFO:0003833
nicotine dependence3MONDO:0008575EFO:0003768
lymphoid neoplasm3MONDO:0005157EFO:0001642
dementia3MONDO:0001627HP:0000726
delirium3MONDO:0045057EFO:0009267
major depressive disorder3MONDO:0002009MONDO:0002009
depressive disorder3MONDO:0002050MONDO:0002050
Alzheimer disease3MONDO:0004975MONDO:0004975
multiple sclerosis3MONDO:0005301MONDO:0005301
sickle cell disease3MONDO:0011382MONDO:0011382
bipolar disorder3MONDO:0004985MONDO:0004985
neoplasm3MONDO:0005070MONDO:0004992
methamphetamine dependence2MONDO:0005419EFO:0004701
eating disorder2MONDO:0005451EFO:0005203
post-traumatic stress disorder2MONDO:0005146EFO:0001358
prostate carcinoma2MONDO:0005159EFO:0001663
cocaine dependence2MONDO:0005186EFO:0002610
drug dependence2MONDO:0005303EFO:0003890
brain injury2MONDO:0043510MONDO:0043510
Parkinson disease2MONDO:0005180MONDO:0005180
orthostatic hypotension1MONDO:0005469EFO:0005252
opiate dependence1MONDO:0005530EFO:0005611
alcohol abuse1MONDO:0002046MONDO:0007079

6 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 265.

Phase distribution

PhaseTrials
PHASE484
Not specified57
PHASE341
PHASE231
PHASE125
EARLY_PHASE112
PHASE2/PHASE311
PHASE1/PHASE24

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00768820PHASE4RECRUITINGThe Psychiatric and Cognitive Phenotypes in Velocardiofacial Syndrome
NCT02951754PHASE4RECRUITINGMethylphenidate in Adults With Attention Deficit/Hyperactivity Disorder
NCT03781752PHASE4RECRUITINGCarboxylesterase 1 Genetic Variation and Methylphenidate in ADHD
NCT03781765PHASE4RECRUITINGStimulant vs. Non-stimulant Treatments and Reward Processing in Drug-naive Youth at SUD Risk
NCT04419272PHASE4RECRUITINGMethylphenidate for the Treatment of Epilepsy-related Cognitive Deficits
NCT04421248PHASE4RECRUITINGBiomarker Validation in Motor System Physiology in Attention Deficit Hyperactivity Disorder
NCT04781972PHASE4RECRUITINGMultimodal Brain Imaging of the Neural Effects of Methylphenidate in Patients With ADHD
NCT05469386PHASE4ACTIVE_NOT_RECRUITINGSingle and Combined Effects of Behavioral, Academic, and Medication Treatments for ADHD in the Classroom
NCT05776056PHASE4RECRUITINGMethylphenidate for the Treatment of PTSD With Associated Neurocognitive Complaints
NCT06577779PHASE4RECRUITINGAn Open-Label Treatment With Randomization Observation, Investigator-Initiated Study, on the Duration and Efficacy of Jornay PM (Methylphenidate Hydrochloride Extended-Release Capsules) on Adult ADHD Symptoms and Executive Function and Emotional Regulation Throughout the Day Into Early Evening
NCT06580041PHASE4ENROLLING_BY_INVITATIONPrecision Care for Major Depressive Disorder
NCT07300956PHASE4NOT_YET_RECRUITINGTreating Young Children With Attention Deficit Hyperactivity Disorder
NCT07594652PHASE4RECRUITINGMedication Treatment of ADHD in Pediatric Epilepsy
NCT00015301PHASE4COMPLETEDMethylphenidate Raclopride Positron Emission Tomography (PET) Test - 11
NCT00035139PHASE4COMPLETEDPediatric Traumatic Brain Injury: Methylphenidate Effects on Early Recovery
NCT00169611PHASE4COMPLETEDNF1-Attention: Study of Children With Neurofibromatosis Type 1 Treated by Methylphenidate
NCT00181571PHASE4COMPLETEDA Double-Blind Comparison of Concerta and Placebo in Adults With Attention Deficit Hyperactivity Disorder
NCT00181714PHASE4COMPLETEDPrevention of Cigarette Smoking in Attention Deficit Hyperactivity Disorder (ADHD) Youth With Concerta
NCT00181987PHASE4COMPLETEDConcerta in the Treatment of ADHD in Youth and Adults With Bipolar Disorder
NCT00183391PHASE4COMPLETEDStimulant Versus Nonstimulant Medication for Attention Deficit Hyperactivity Disorder in Children
NCT00223561PHASE4COMPLETEDMethylphenidate and Driving Ability in Adult Patients With Attention-Deficit Hyperactivity Disorder
NCT00228046PHASE4COMPLETEDMedication Strategies for Treating Aggressive Behavior in Youth With Attention Deficit Hyperactivity Disorder
NCT00254033PHASE4COMPLETEDApathy Associated With Alzheimer’s Disease
NCT00261872PHASE4COMPLETEDTreatment of Patients With Alcoholism and Attention Deficit Disorder
NCT00381758PHASE4COMPLETEDThe COMACS Study: A Comparison of Methylphenidates in an Analog Classroom Setting
NCT00396058PHASE4TERMINATEDThe Effect of Methylphenidate on Motor Learning in Stroke Patients
NCT00429273PHASE4COMPLETEDSingle Versus Combination Medication Treatment for Children With Attention Deficit Hyperactivity Disorder
NCT00434213PHASE4COMPLETEDCharacterization of Dermal Reactions in Pediatric Patients With ADHD Using DAYTRANA
NCT00495820PHASE4COMPLETEDMethylphenidate for Apathy in Alzheimer’s Dementia: A Controlled Study
NCT00517504PHASE4COMPLETEDMethylphenidate Study in Young Children With Developmental Disorders
NCT00526630PHASE4COMPLETEDMethylphenidate for the Treatment of Gait Impairment in Parkinson’s Disease
NCT00536419PHASE4UNKNOWNImpact of Attention Deficit/Hyperactivity Disorder and Substance Use Disorder on Motorcycle Traffic Accidents
NCT00552266PHASE4UNKNOWNMethylphenidate in ADHD With Trichotillomania
NCT00576472PHASE4COMPLETEDLearning Impairments Among Survivors of Childhood Cancer
NCT00586157PHASE4COMPLETEDStudy of Medication Patch to Treat Children Ages 6-12 With ADHD
NCT00593112PHASE4COMPLETEDProton Magnetic Spectroscopy in Children and Adolescents With ADHD Before and After Treatment With OROS Methylphenidate
NCT00602290PHASE4COMPLETEDEffectiveness of Methylphenidate in Improving Cognition and Function in Older Adults With Depression
NCT00663442PHASE4COMPLETEDBasic and Clinical Research on Attention Deficit Hyperactivity Disorder (ADHD)
NCT00754208PHASE4COMPLETEDLong Acting Stimulant Treatment of Attention Deficit Hyperactivity Disorder (ADHD) in Young Children
NCT00758160PHASE4COMPLETEDThe Impact of Osmotic Release Oral Delivery System Methylphenidate (OROS MPH) Upon Family of Children and Adolescents With Attention Deficit Hyperactivity Disorder (ADHD)

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (2) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

GuidelineSourceGene(s)DosingRecommendation
Annotation of DPWG Guideline for methylphenidate and CYP2D6DPWGCYP2D6
Annotation of DPWG Guideline for methylphenidate and COMTDPWGCOMT

PharmGKB also curates 50 clinical and 194 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.

585 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
AfatinibChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3
AMITRIPTYLINEChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3
DACOMITINIBChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3
GENTIAN VIOLETChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3
IdelalisibChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3
OlodaterolChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3
PIMAVANSERINChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3
REGORAFENIBChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3
TAFENOQUINEChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3
UMECLIDINIUMChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3
VORAPAXARChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3
ACETOPHENAZINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
AMINOCAPROIC ACIDChEMBLPhase 4 (approved)SLC6A2, SLC6A3
AMIODARONEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
AMLODIPINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
AMODIAQUINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
AMOXAPINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
ARIPIPRAZOLEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
ASENAPINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
ASTEMIZOLEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
ATOMOXETINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
AZELASTINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BAZEDOXIFENEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BENFLUOREXChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BENOXINATEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BENPERIDOLChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BENZIODARONEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BENZPHETAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BENZTROPINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BENZYDAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BENZYL BENZOATEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BEPRIDILChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BEXAROTENEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BITHIONOLChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BOSUTINIBChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BREXPIPRAZOLEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BROMHEXINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BROMODIPHENHYDRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BROMPERIDOLChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BROMPHENIRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
BUPROPIONChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CABERGOLINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CALCITRIOLChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CANNABIDIOLChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CARBINOXAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CARVEDILOLChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CASPOFUNGINChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CELECOXIBChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CETIRIZINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CHLORHEXIDINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CHLORPHENIRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CHLORPHENTERMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CHLORPROMAZINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CHLORPROTHIXENEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CINACALCETChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CINNARIZINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CITALOPRAMChEMBLPhase 4 (approved)SLC6A2, SLC6A3
CLEMASTINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3

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