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Milnacipran

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Also known as ImpulsorMilnacipran pierre fabre medicamentrel-MilnacipranN-diethylcyclopropane carboxamidel-milnacipran

Summary

Milnacipran (CHEMBL259209) is an approved small molecule (ATC N06AX17) targeting SLC6A2 and SLC6A4; indicated across 7 conditions including depressive disorder and fibromyalgia.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N06AX17
  • Targets: 2 (SLC6A2, SLC6A4)
  • Indications: 7 conditions
  • Clinical trials: 38
  • Chemistry: 246.35 Da · C15H22N2O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL259209
NameMilnacipran
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID11622909
ATCN06AX17
Molecular formulaC15H22N2O
Molecular weight246.35
InChIKeyGJJFMKBJSRMPLA-UHFFFAOYSA-N

SMILES: CCN(CC)C(=O)C1(CC1CN)C2=CC=CC=C2

IUPAC name: 2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropane-1-carboxamide

Also known as: Impulsor, Milnacipran, Milnacipran pierre fabre medicament, milnacipran, rel-Milnacipran, MILNACIPRAN, N-diethylcyclopropane carboxamide, l-milnacipran

Parent form; salt/anhydrous children: CHEMBL3527085, CHEMBL4297064

Patent coverage: 145 distinct patent families (408 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
SLC6A2NETInhibition9.10.4%P23975
SLC6A4SERTInhibition7.30.7%P31645

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Sodium-dependent noradrenaline transporter, 5-hydroxytryptamine receptor 2C, Sodium-dependent serotonin transporter, Sodium-dependent dopamine transporter, Cytochrome P450 2D6, Sodium-dependent serotonin transporter, Sodium-dependent dopamine transporter.

Bioactivity

ChEMBL activities: 28 potent at pChembl ≥ 5 of 30 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
SLC6A29.1IC500.79nMCHEMBL_ACT_12668750
SLC6A48.19Ki6.5nMCHEMBL_ACT_13325669
SLC6A47.7AC5020nMCHEMBL_ACT_25150248
SLC6A47.66IC5022nMCHEMBL_ACT_13325588
SLC6A47.66Ki22nMCHEMBL_ACT_16817150
P316527.57Ki27nMCHEMBL_ACT_13325637
SLC6A27.39IC5041nMCHEMBL_ACT_13325583
P316527.33IC5047nMCHEMBL_ACT_2397307
SLC6A47.3IC5050.12nMCHEMBL_ACT_12668698
SLC6A47.19IC5064nMCHEMBL_ACT_16817102
SLC6A27.11IC5077nMCHEMBL_ACT_2100138
SLC6A27.11IC5077nMCHEMBL_ACT_2169310
SLC6A27.11IC5077nMCHEMBL_ACT_2397322
SLC6A27.07Ki85nMCHEMBL_ACT_13325660
SLC6A47IC50100nMCHEMBL_ACT_1616152
P316526.69IC50203nMCHEMBL_ACT_2397434
SLC6A26.51AC50310nMCHEMBL_ACT_25144913
SLC6A46.38IC50420nMCHEMBL_ACT_2100139
SLC6A46.38IC50420nMCHEMBL_ACT_2169311
SLC6A46.38IC50420nMCHEMBL_ACT_2397354
HTR2C6.23AC50590nMCHEMBL_ACT_25131719
SLC6A45.46IC503500nMCHEMBL_ACT_2169394
SLC6A45.46IC503500nMCHEMBL_ACT_2170824
SLC6A25.26IC505500nMCHEMBL_ACT_2169348
SLC6A25.26IC505500nMCHEMBL_ACT_2170791
SLC6A35.21IC506100nMCHEMBL_ACT_2100140
SLC6A35.21IC506100nMCHEMBL_ACT_2169312
SLC6A35.21IC506100nMCHEMBL_ACT_2397379

Target pathways

Aggregated over 2 target gene(s): SLC6A2, SLC6A4.

Top Reactome pathways

12 total, by targets touching each:

PathwayTargetsGenes
SLC-mediated transport of neurotransmitters2SLC6A2, SLC6A4
Neurotransmitter clearance1SLC6A4
Transmission across Chemical Synapses1SLC6A4
Neuronal System1SLC6A4
Disease1SLC6A2
Serotonin clearance from the synaptic cleft1SLC6A4
Transport of small molecules1SLC6A2
R-HSA-4253661SLC6A2
SLC-mediated transmembrane transport1SLC6A2
SLC transporter disorders1SLC6A2
Defective SLC6A2 causes orthostatic intolerance (OI)1SLC6A2
Disorders of transmembrane transporters1SLC6A2

Dominant GO biological processes

GO termTargets
neurotransmitter transport2
amino acid transport2
response to xenobiotic stimulus2
obsolete monoamine transport2
sodium ion transmembrane transport2
transmembrane transport2
neurotransmitter reuptake2
chemical synaptic transmission1
obsolete norepinephrine transport1
response to pain1
dopamine uptake involved in synaptic transmission1
norepinephrine uptake1
neuron cellular homeostasis1
catecholamine uptake1
chloride transmembrane transport1

Indications & clinical

Indications

1 approved indication. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

IndicationPhaseMONDOEFO
depressive disorder4MONDO:0002050MONDO:0002050

4 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)PhaseMONDOEFO
fibromyalgia3MONDO:0005546EFO:0005687
peripheral neuropathy3MONDO:0005244EFO:0003100
neuralgia2MONDO:0021667EFO:0005762
irritable bowel syndrome2MONDO:0005052EFO:0000555

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

Clinical trials

Total trials: 38.

Phase distribution

PhaseTrials
PHASE415
PHASE39
PHASE27
Not specified4
PHASE2/PHASE32
PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT01014585PHASE4COMPLETEDDiscontinuation Study of the Durability of Effect of Milnacipran for the Treatment of Fibromyalgia
NCT01038323PHASE4COMPLETEDDrug and Talk Therapy for Fibromyalgia
NCT01077375PHASE4COMPLETEDStudy of Milnacipran in Patients With Inadequate Response to Duloxetine for the Treatment of Fibromyalgia
NCT01125423PHASE4COMPLETEDStudy of Fibromyalgia Treated With Milnacipran
NCT01173055PHASE4COMPLETEDA Study to Evaluate the Effects of Milnacipran on Pain Processing and Functional MRI in Patients With Fibromyalgia
NCT01207453PHASE4COMPLETEDMilnacipran in the Treatment of Widespread, Non-Joint Pain in Rheumatoid Arthritis
NCT01225991PHASE4COMPLETEDMilnacipran for Treatment of Pain in Older Adults With Rheumatoid Arthritis
NCT01234675PHASE4COMPLETEDThe Effects of Milnacipran on Sleep Disturbance in Fibromyalgia
NCT01289236PHASE4COMPLETEDMILNACIPRAN in Subjects With Chronic Shoulder Pain
NCT01319825PHASE4UNKNOWNPreventive Treatment of Episodic and Chronic Migraine
NCT01329406PHASE4UNKNOWNStudy to Evaluate the Efficacy of Milnacipran in the Treatment of Pain Due to Osteoarthritis
NCT01337700PHASE4COMPLETEDMilnacipran in Autism and the Functional Locus Coeruleus and Noradrenergic Model of Autism
NCT01359826PHASE4WITHDRAWNThe Effect of Milnacipran on Fatigue and Quality of Life in Lupus Patients
NCT01510457PHASE4COMPLETEDMilnacipran for Chronic Pain in Knee Osteoarthritis
NCT01777581PHASE4COMPLETEDMilnacipran for Lumbosacral Radicular Pain
NCT00225511PHASE3COMPLETEDStudy Evaluating Effexor XR for Major Depression.
NCT00314249PHASE3COMPLETEDStudy of Milnacipran for the Treatment of Fibromyalgia
NCT00436033PHASE3COMPLETEDA Multicentre Trial to Determine the Efficacy and Safety of Milnacipran in the Treatment of Fibromyalgia Syndrome
NCT00757731PHASE3COMPLETEDFMS European Long-Term Study
NCT00793520PHASE3TERMINATEDEffect of Milnacipran on Pain Processing and Functional Magnetic Resonance Imaging (fMRI) Activation Patterns in Patients With Fibromyalgia
NCT00797797PHASE3COMPLETEDStudy of Milnacipran Added to Pregabalin for Treatment of Fibromyalgia
NCT01108731PHASE2/PHASE3COMPLETEDThe Effect of Milnacipran in Patients With Fibromyalgia
NCT01288937PHASE3TERMINATEDA Placebo Controlled, Randomized, Double Blind Trial of Milnacipran for the Treatment of Idiopathic Neuropathy Pain
NCT01304589PHASE3COMPLETEDSavella in Treatment for Provoked Vestibulodynia
NCT01829243PHASE3COMPLETEDMilnacipran and Neurocognition, Pain and Fatigue in Fibromyalgia : A 13-week Randomized, Placebo Controlled Cross Over Trial
NCT02783430PHASE2/PHASE3COMPLETEDEvaluation of the Initial Prescription of Ketamine and Milnacipran in Depression in Patients With a Progressive Disease
NCT00757679PHASE2COMPLETEDEvaluation of the Antinociceptive and Analgesic Effects of Milnacipran
NCT01225068PHASE2COMPLETEDEffect of Milnacipran in Chronic Neuropathic Low Back Pain
NCT01328002PHASE2TERMINATEDSafety and Efficacy of Milnacipran in Pediatric Patients With Primary Fibromyalgia
NCT01331109PHASE2TERMINATEDLong-Term Safety and Efficacy Study of Milnacipran in Pediatric Patients With Primary Fibromyalgia
NCT01471379PHASE2TERMINATEDMilnacipran (Savella) in Irritable Bowel Syndrome (IBS)
NCT01747044PHASE2UNKNOWNProspective Study of the Influence of the Diffuse Noxious Inhibitory Controls of the Pain on the Efficacy of Milnacipran in Fibromyalgia Therapy
NCT01914042PHASE2UNKNOWNPrediction of Inter-individual Differences in the Response to Morphine Versus Milnacipran in Patients With Sciatica
NCT01294059PHASE1COMPLETEDEffects of Milnacipran on Widespread Mechanical and Thermal Hyperalgesia of Fibromyalgia Patients
NCT00606203Not specifiedUNKNOWNDose Milnacipran Prevent Depressive Symptoms in Patients With Acute Stroke?
NCT01393522Not specifiedCOMPLETEDStudy Evaluated the Effectiveness of Milnacipran to Reduce Pain Levels in Individuals With Chronic Migraine
NCT02687165Not specifiedTERMINATEDUncovering Neural and Immune Mechanisms of Chronic Pain in Post Treatment Lyme Syndrome
NCT05384210Not specifiedUNKNOWNEffect of Milnacipran / Gabapentin in Fibromyalgia

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

592 molecules share ≥1 primary target. Top 100 by shared-target count:

MoleculeSourceStatusShared targets
AMITRIPTYLINEChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A4
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A4
GENTIAN VIOLETChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A4
OlodaterolChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A4
PIMAVANSERINChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A4
REGORAFENIBChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A4
TadalafilChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A4
TAFENOQUINEChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A4
UMECLIDINIUMChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A4
VORAPAXARChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A4
ACETOPHENAZINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
ALECTINIBChEMBLPhase 4 (approved)SLC6A2, SLC6A4
AMBENONIUMChEMBLPhase 4 (approved)SLC6A2, SLC6A4
AMIODARONEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
AMOXAPINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
ARIPIPRAZOLEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
ASENAPINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
ASTEMIZOLEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
ATOMOXETINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
ATRACURIUMChEMBLPhase 4 (approved)SLC6A2, SLC6A4
AZELASTINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
BAZEDOXIFENEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
BENFLUOREXChEMBLPhase 4 (approved)SLC6A2, SLC6A4
BENZPHETAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
BENZTROPINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
BENZYDAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
BEPRIDILChEMBLPhase 4 (approved)SLC6A2, SLC6A4
BOSUTINIBChEMBLPhase 4 (approved)SLC6A2, SLC6A4
BREXPIPRAZOLEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
BROMHEXINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
BROMODIPHENHYDRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
BROMPERIDOLChEMBLPhase 4 (approved)SLC6A2, SLC6A4
BROMPHENIRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
BUPROPIONChEMBLPhase 4 (approved)SLC6A2, SLC6A4
BUTENAFINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CABERGOLINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CALCIPOTRIENEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CALCITRIOLChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CARBINOXAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CARVEDILOLChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CELECOXIBChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CETIRIZINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CHLORHEXIDINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CHLORPHENIRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CHLORPHENTERMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CHLORPROMAZINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CHLORPROTHIXENEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CINACALCETChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CINNARIZINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CITALOPRAMChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CLEMASTINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CLOMIPHENEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CLOMIPRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CLOTRIMAZOLEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CLOZAPINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
COBIMETINIBChEMBLPhase 4 (approved)SLC6A2, SLC6A4
COCAINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CYCLOBENZAPRINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
CYPROHEPTADINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DANAZOLChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DAUNORUBICINChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DELAMANIDChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DEQUALINIUMChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DESIPRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DESLORATADINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DESOGESTRELChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DESVENLAFAXINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DEXBROMPHENIRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DEXCHLORPHENIRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DEXTROAMPHETAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DEXTROMETHORPHANChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DIBENZEPINChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DIETHYLSTILBESTROLChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DIPHENHYDRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DOBUTAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DOMPERIDONEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DOTHIEPINChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DOXAZOSINChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DOXEPINChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DRONEDARONEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
DULOXETINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
EBASTINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
ECONAZOLEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
EPALRESTATChEMBLPhase 4 (approved)SLC6A2, SLC6A4
EPINASTINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
ERDAFITINIBChEMBLPhase 4 (approved)SLC6A2, SLC6A4
ESCITALOPRAMChEMBLPhase 4 (approved)SLC6A2, SLC6A4
ETHINYL ESTRADIOLChEMBLPhase 4 (approved)SLC6A2, SLC6A4
ETHOPROPAZINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
ETHYLESTRENOLChEMBLPhase 4 (approved)SLC6A2, SLC6A4
FEDRATINIBChEMBLPhase 4 (approved)SLC6A2, SLC6A4
FENOLDOPAMChEMBLPhase 4 (approved)SLC6A2, SLC6A4
FENOTEROLChEMBLPhase 4 (approved)SLC6A2, SLC6A4
FENTICONAZOLEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
FIPEXIDEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
FLUOXETINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
FLUPHENAZINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
FLUSPIRILENEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
FLUVOXAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A4
GUANABENZChEMBLPhase 4 (approved)SLC6A2, SLC6A4

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
v1.1.4
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