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Toludesvenlafaxine

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Also known as LPM-570065 FREE BASELPM570065 FREE BASELY-03005Ly03005ODVP2ToludesvenlafaxinaAnsofaxine

Summary

Toludesvenlafaxine (CHEMBL4227736) is a phase-3 clinical-stage small molecule targeting SLC6A2, SLC6A3, and SLC6A4; indicated across 2 conditions including major depressive disorder and depressive disorder.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 3 (SLC6A2, SLC6A3, SLC6A4)
  • Indications: 2 conditions
  • Clinical trials: 12
  • Chemistry: 381.5 Da · C24H31NO3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL4227736
NameToludesvenlafaxine
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID15983287
Molecular formulaC24H31NO3
Molecular weight381.5
InChIKeyQKYBZJLEMOZFFU-UHFFFAOYSA-N

SMILES: CC1=CC=C(C=C1)C(=O)OC2=CC=C(C=C2)C(CN(C)C)C3(CCCCC3)O

IUPAC name: [4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenyl] 4-methylbenzoate

Also known as: LPM-570065 FREE BASE, LPM570065 FREE BASE, LY-03005, Ly03005, LY03005, ODVP2, Toludesvenlafaxina, Toludesvenlafaxine, Ansofaxine, TOLUDESVENLAFAXINE

Parent form; salt/anhydrous children: CHEMBL4650223

Patent coverage: 10 distinct patent families (31 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
SLC6A2NETInhibition6.120.4%P23975
SLC6A3DATInhibition6.310.2%Q01959
SLC6A4SERTInhibition6.140.7%P31645

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Sodium-dependent noradrenaline transporter, Sodium-dependent serotonin transporter, Sodium-dependent dopamine transporter.

Bioactivity

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

TargetpChemblTypeValueUnitActivity ID
SLC6A36.31IC50491nMCHEMBL_ACT_18566375
SLC6A36.31IC50491nMCHEMBL_ACT_18566483
SLC6A46.14IC50723nMCHEMBL_ACT_18566331
SLC6A46.14IC50723nMCHEMBL_ACT_18566481
SLC6A26.12IC50763nMCHEMBL_ACT_18566357
SLC6A26.12IC50763nMCHEMBL_ACT_18566482

Target pathways

Aggregated over 3 target gene(s): SLC6A2, SLC6A3, SLC6A4.

Top Reactome pathways

15 total, by targets touching each:

PathwayTargetsGenes
SLC-mediated transport of neurotransmitters3SLC6A2, SLC6A3, SLC6A4
Neurotransmitter clearance2SLC6A3, SLC6A4
Transmission across Chemical Synapses2SLC6A3, SLC6A4
Neuronal System2SLC6A3, SLC6A4
Disease2SLC6A2, SLC6A3
Transport of small molecules2SLC6A2, SLC6A3
R-HSA-4253662SLC6A2, SLC6A3
SLC-mediated transmembrane transport2SLC6A2, SLC6A3
SLC transporter disorders2SLC6A2, SLC6A3
Disorders of transmembrane transporters2SLC6A2, SLC6A3
Dopamine clearance from the synaptic cleft1SLC6A3
Serotonin clearance from the synaptic cleft1SLC6A4
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 transport3
amino acid transport3
response to xenobiotic stimulus3
obsolete monoamine transport3
sodium ion transmembrane transport3
transmembrane transport3
dopamine uptake involved in synaptic transmission2
norepinephrine uptake2
neurotransmitter reuptake2
chemical synaptic transmission1
obsolete norepinephrine transport1
response to pain1
neuron cellular homeostasis1
catecholamine uptake1
chloride transmembrane transport1

Indications & clinical

Indications

2 indications (0 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
major depressive disorder3MONDO:0002009MONDO:0002009
depressive disorder1MONDO:0002050MONDO:0002050

Clinical trials

Total trials: 12.

Phase distribution

PhaseTrials
PHASE16
PHASE43
Not specified2
PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT06426485PHASE4NOT_YET_RECRUITINGTo Evaluate the Long-term Efficacy and Safety of Toludevenlafaxine Hydrochloride Sustained-release Tablets
NCT05849272PHASE4COMPLETEDEfficacy and Safety of Toluedesvenlafaxine Hydrochloride Extended-release Tablets in Somatic Symptoms of Depression
NCT06026917PHASE4UNKNOWNAssessing Dopamine Transporter Occupancy in the Patients With Depression Brain With Toludesvenlafaxine Hydrochloride Extended-Release Tablets Using 11C-CFT Positron Emission Tomography (PET)
NCT05970510PHASE3UNKNOWNA Study to Evaluate Efficacy and Safety of Toludesvenlafaxine Hydrochloride Sustained-release Tablets in Generalized Anxiety Disorder.
NCT02055300PHASE1COMPLETEDSafety, Tolerability and Pharmacokinetics Study of LY03005
NCT02271412PHASE1COMPLETEDMultiple Ascending Dose Study in Healthy Subjects to Evaluate the Safety, Tolerability, and Pharmacokinetics of LY03005
NCT02988024PHASE1COMPLETEDPilot BA Study of New LY03005 vs Pristiq
NCT03357796PHASE1COMPLETEDRelative Bioavailability (RBA) Study of LY03005 vs Pristiq®
NCT03733574PHASE1COMPLETEDA Study of LY03005 vs Pristiq
NCT03822065PHASE1COMPLETEDA Relative Bioavailability Food Effect Study of LY03005
NCT06270433Not specifiedUNKNOWNEfficacy and Safety of Toludesvenlafaxine Hydrochloride Sustained-release Tablets Versus Desvenlafaxine Succinate Sustained-release Tablets Targeting Anhedonia in Patients With Major Depression Disorder
NCT06278038Not specifiedCOMPLETEDEfficacy and Safety of Toludesvenlafaxine Hydrochloride Sustained-release Tablets Versus Venlafaxine Hydrochloride Sustained-release Tablets in Patients With Major Depression Disorder

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.

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

MoleculeSourceStatusShared targets
AfatinibChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
AMITRIPTYLINEChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
GENTIAN VIOLETChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
IdelalisibChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
OlodaterolChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
PIMAVANSERINChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
REGORAFENIBChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
TadalafilChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
TAFENOQUINEChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
UMECLIDINIUMChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
VORAPAXARChEMBL + PubChemPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
ACETOPHENAZINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
AMIODARONEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
AMOXAPINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
ARIPIPRAZOLEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
ASENAPINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
ASTEMIZOLEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
ATOMOXETINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
AZELASTINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
BAZEDOXIFENEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
BENFLUOREXChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
BENZPHETAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
BENZTROPINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
BENZYDAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
BEPRIDILChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
BOSUTINIBChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
BREXPIPRAZOLEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
BROMHEXINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
BROMODIPHENHYDRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
BROMPERIDOLChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
BROMPHENIRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
BUPROPIONChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CABERGOLINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CALCITRIOLChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CARBINOXAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CARVEDILOLChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CELECOXIBChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CETIRIZINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CHLORHEXIDINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CHLORPHENIRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CHLORPHENTERMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CHLORPROMAZINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CHLORPROTHIXENEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CINACALCETChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CINNARIZINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CITALOPRAMChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CLEMASTINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CLOMIPHENEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CLOMIPRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CLOTRIMAZOLEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
COBIMETINIBChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
COCAINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
CYPROHEPTADINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
DANAZOLChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
DAUNORUBICINChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
DEQUALINIUMChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
DESIPRAMINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
DESLORATADINEChEMBLPhase 4 (approved)SLC6A2, SLC6A3, SLC6A4
DESOGESTRELChEMBLPhase 4 (approved)SLC6A2, SLC6A3, 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
v1.1.2
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