Reboxetine

Summary

Reboxetine (CHEMBL14370) is an approved small molecule (ATC N06AX18) targeting SLC6A2; indicated across 11 conditions including depressive disorder and anxiety.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N06AX18
• Targets: 1 (SLC6A2)
• Indications: 11 conditions
• Clinical trials: 15
• Chemistry: 313.4 Da · C19H23NO3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL14370
Name	Reboxetine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	3022645
ATC	N06AX18
Molecular formula	C19H23NO3
Molecular weight	313.4
InChIKey	CBQGYUDMJHNJBX-UHFFFAOYSA-N

SMILES: CCOC1=CC=CC=C1OC(C2CNCCO2)C3=CC=CC=C3

IUPAC name: 2-[(2-ethoxyphenoxy)-phenylmethyl]morpholine

Also known as: Edronax, Reboxetina, Reboxetine, reboxetine, REBOXETINE

Parent form; salt/anhydrous children: CHEMBL2146087

Patent coverage: 103 distinct patent families (327 SureChEMBL compound mentions), from 2 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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
SLC6A2	NET	Inhibition	8	0.4%	P23975

Broader ChEMBL bioactivity targets: 12 (assay-derived). Sample: Beta-2 adrenergic receptor, Muscarinic acetylcholine receptor M2, Muscarinic acetylcholine receptor M1, Motilin receptor, Sodium-dependent noradrenaline transporter, 5-hydroxytryptamine receptor 2C, Sodium-dependent serotonin transporter, Kappa-type opioid receptor, Sodium-dependent dopamine transporter, Voltage-gated inwardly rectifying potassium channel KCNH2.

Bioactivity

ChEMBL activities: 26 potent at pChembl ≥ 5 of 33 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SLC6A2	8.96	Ki	1.1	nM	CHEMBL_ACT_518019
SLC6A2	8.52	IC50	3	nM	CHEMBL_ACT_2483372
SLC6A2	8.52	IC50	3	nM	CHEMBL_ACT_2522734
SLC6A2	8.52	IC50	3	nM	CHEMBL_ACT_2587126
SLC6A2	8.49	IC50	3.2	nM	CHEMBL_ACT_2699875
SLC6A2	8.49	IC50	3.2	nM	CHEMBL_ACT_3128026
SLC6A2	8.3	Ki	5	nM	CHEMBL_ACT_2119194
SLC6A2	8.3	Ki	5	nM	CHEMBL_ACT_2163955
SLC6A2	8.16	AC50	6.9	nM	CHEMBL_ACT_25145492
SLC6A4	8.05	Ki	9	nM	CHEMBL_ACT_123444
SLC6A2	7.96	IC50	11	nM	CHEMBL_ACT_1753715
SLC6A2	7.96	IC50	11	nM	CHEMBL_ACT_1755278
SLC6A3	7.22	Ki	60	nM	CHEMBL_ACT_123443
SLC6A4	6.89	Ki	129	nM	CHEMBL_ACT_518017
SLC6A4	6.82	AC50	150	nM	CHEMBL_ACT_25150820
SLC6A4	6.62	IC50	242	nM	CHEMBL_ACT_2483390
SLC6A4	6.62	IC50	242	nM	CHEMBL_ACT_2522761
SLC6A4	6.62	IC50	242	nM	CHEMBL_ACT_2587141
SLC6A4	6.62	IC50	242	nM	CHEMBL_ACT_3128049
P31652	6.3	Ki	503	nM	CHEMBL_ACT_13868247
P31652	6.3	Ki	503	nM	CHEMBL_ACT_6192564
SLC6A4	6.23	IC50	590	nM	CHEMBL_ACT_1753741
SLC6A4	6.23	IC50	590	nM	CHEMBL_ACT_1755300
SLC6A4	5.85	Ki	1400	nM	CHEMBL_ACT_2119234
SLC6A4	5.85	Ki	1400	nM	CHEMBL_ACT_2163925
CHRM1	5.07	AC50	8600	nM	CHEMBL_ACT_25135968

Target pathways

Aggregated over 1 target gene(s): SLC6A2.

Top Reactome pathways

8 total, by targets touching each:

Pathway	Targets	Genes
Disease	1	SLC6A2
Transport of small molecules	1	SLC6A2
R-HSA-425366	1	SLC6A2
SLC-mediated transmembrane transport	1	SLC6A2
SLC-mediated transport of neurotransmitters	1	SLC6A2
SLC transporter disorders	1	SLC6A2
Defective SLC6A2 causes orthostatic intolerance (OI)	1	SLC6A2
Disorders of transmembrane transporters	1	SLC6A2

Dominant GO biological processes

GO term	Targets
neurotransmitter transport	1
amino acid transport	1
chemical synaptic transmission	1
response to xenobiotic stimulus	1
obsolete monoamine transport	1
obsolete norepinephrine transport	1
sodium ion transmembrane transport	1
response to pain	1
dopamine uptake involved in synaptic transmission	1
norepinephrine uptake	1
neuron cellular homeostasis	1
transmembrane transport	1
catecholamine uptake	1
neurotransmitter reuptake	1
chloride transmembrane transport	1

Indications & clinical

Indications

11 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).

Indication	Trial phase	MONDO	EFO
depressive disorder	4	MONDO:0002050	MONDO:0002009
anxiety	3	MONDO:0011918	EFO:0005230
fibromyalgia	3	MONDO:0005546	EFO:0005687
dementia	3	MONDO:0001627	HP:0000726
attention deficit-hyperactivity disorder	2	MONDO:0007743	EFO:0003888
diabetic neuropathy	2	MONDO:0006626	EFO:1000783
post-traumatic stress disorder	2	MONDO:0005146	EFO:0001358

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

Clinical trials

Total trials: 15.

Phase distribution

Phase	Trials
Not specified	5
PHASE4	4
PHASE3	3
PHASE1	2
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00209807	PHASE4	UNKNOWN	Effect of Escitalopram vs. Reboxetine on Gastro-intestinal Sensitivity of Patients With Major Depressive Disorder
NCT00426946	PHASE4	UNKNOWN	Reboxetine Treatment in Depressed Children and Adolescents an 8-Week, Open Study
NCT00853866	PHASE4	COMPLETED	Enhancement of Motor Function with Reboxetine and Transcranial Direct Current Stimulation
NCT01300364	PHASE4	UNKNOWN	Reboxetine and Citalopram as an Adjunct Treatment to Second Generation Antipsychotics in the Treatment of Negative Symptoms of Schizophrenia
NCT05880342	PHASE3	RECRUITING	The Role of the Brain in Mental and Physical Fatigue
NCT02179268	PHASE3	COMPLETED	Antidepressants and Bone Mineral Density
NCT02374567	PHASE3	TERMINATED	Pharmacovigilance in Gerontopsychiatric Patients
NCT05133804	PHASE2	RECRUITING	Efficacy of Reboxetine and Methylphenidate Treatment on Attentional, Sensory and Emotional Dysregulation in Adults With PTSD
NCT00886886	PHASE1	COMPLETED	Interaction Between Reboxetine and 3,4-Methylenedioxymethamphetamine: Pharmacodynamics (PD) and Pharmacokinetics (PK)
NCT04097288	PHASE1	COMPLETED	Effects of Single Dose Citalopram and Reboxetine on Urethral and Anal Closure Function on Healthy Female Subjects
NCT00421369	Not specified	COMPLETED	Augmentation of the Antidepressant Action of Sertraline With Triiodothyronine (T3)and Reboxetine: Clinical Efficacy, Adverse Effects and Predictors of Response.
NCT00993876	Not specified	COMPLETED	Cognitive Flexibility in Major Depression in the Course of Pharmacological and Psychotherapeutic Treatment
NCT03957174	Not specified	COMPLETED	Noradrenaline, Acetylcholine and Dynamic Learning in Healthy Humans
NCT04371146	Not specified	COMPLETED	The Role of Dopaminergic and Noradrenergic Neurotransmission in Value- and Salience-based Decision-Making
NCT04384562	Not specified	COMPLETED	Studying the Role of Brain Molecules for Decision Making

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

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.

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

Molecule	Source	Status	Shared targets
AMITRIPTYLINE	ChEMBL + PubChem	Phase 4 (approved)	SLC6A2
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	SLC6A2
DACOMITINIB	ChEMBL + PubChem	Phase 4 (approved)	SLC6A2
GENTIAN VIOLET	ChEMBL + PubChem	Phase 4 (approved)	SLC6A2
PIMAVANSERIN	ChEMBL + PubChem	Phase 4 (approved)	SLC6A2
REGORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	SLC6A2
TAFENOQUINE	ChEMBL + PubChem	Phase 4 (approved)	SLC6A2
UMECLIDINIUM	ChEMBL + PubChem	Phase 4 (approved)	SLC6A2
VORAPAXAR	ChEMBL + PubChem	Phase 4 (approved)	SLC6A2
ACETOPHENAZINE	ChEMBL	Phase 4 (approved)	SLC6A2
ALECTINIB	ChEMBL	Phase 4 (approved)	SLC6A2
ALFACALCIDOL	ChEMBL	Phase 4 (approved)	SLC6A2
ALFUZOSIN	ChEMBL	Phase 4 (approved)	SLC6A2
AMBENONIUM	ChEMBL	Phase 4 (approved)	SLC6A2
AMINOCAPROIC ACID	ChEMBL	Phase 4 (approved)	SLC6A2
AMIODARONE	ChEMBL	Phase 4 (approved)	SLC6A2
AMLODIPINE	ChEMBL	Phase 4 (approved)	SLC6A2
AMODIAQUINE	ChEMBL	Phase 4 (approved)	SLC6A2
AMOXAPINE	ChEMBL	Phase 4 (approved)	SLC6A2
AMPHETAMINE	ChEMBL	Phase 4 (approved)	SLC6A2
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	SLC6A2
ASENAPINE	ChEMBL	Phase 4 (approved)	SLC6A2
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	SLC6A2
ATOMOXETINE	ChEMBL	Phase 4 (approved)	SLC6A2
ATRACURIUM	ChEMBL	Phase 4 (approved)	SLC6A2
AZELASTINE	ChEMBL	Phase 4 (approved)	SLC6A2
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	SLC6A2
BENFLUOREX	ChEMBL	Phase 4 (approved)	SLC6A2
BENOXINATE	ChEMBL	Phase 4 (approved)	SLC6A2
BENPERIDOL	ChEMBL	Phase 4 (approved)	SLC6A2
BENZIODARONE	ChEMBL	Phase 4 (approved)	SLC6A2
BENZPHETAMINE	ChEMBL	Phase 4 (approved)	SLC6A2
BENZTROPINE	ChEMBL	Phase 4 (approved)	SLC6A2
BENZYDAMINE	ChEMBL	Phase 4 (approved)	SLC6A2
BENZYL BENZOATE	ChEMBL	Phase 4 (approved)	SLC6A2
BEPRIDIL	ChEMBL	Phase 4 (approved)	SLC6A2
BEXAROTENE	ChEMBL	Phase 4 (approved)	SLC6A2
BITHIONOL	ChEMBL	Phase 4 (approved)	SLC6A2
BOSUTINIB	ChEMBL	Phase 4 (approved)	SLC6A2
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	SLC6A2
BROMHEXINE	ChEMBL	Phase 4 (approved)	SLC6A2
BROMODIPHENHYDRAMINE	ChEMBL	Phase 4 (approved)	SLC6A2
BROMPERIDOL	ChEMBL	Phase 4 (approved)	SLC6A2
BROMPHENIRAMINE	ChEMBL	Phase 4 (approved)	SLC6A2
BUPROPION	ChEMBL	Phase 4 (approved)	SLC6A2
BUTENAFINE	ChEMBL	Phase 4 (approved)	SLC6A2
CABERGOLINE	ChEMBL	Phase 4 (approved)	SLC6A2
CALCIPOTRIENE	ChEMBL	Phase 4 (approved)	SLC6A2
CALCITRIOL	ChEMBL	Phase 4 (approved)	SLC6A2
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	SLC6A2
CANNABIDIOL	ChEMBL	Phase 4 (approved)	SLC6A2
CARBINOXAMINE	ChEMBL	Phase 4 (approved)	SLC6A2
CARVEDILOL	ChEMBL	Phase 4 (approved)	SLC6A2
CASPOFUNGIN	ChEMBL	Phase 4 (approved)	SLC6A2
CELECOXIB	ChEMBL	Phase 4 (approved)	SLC6A2
CETIRIZINE	ChEMBL	Phase 4 (approved)	SLC6A2
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	SLC6A2
CHLOROXINE	ChEMBL	Phase 4 (approved)	SLC6A2
CHLORPHENIRAMINE	ChEMBL	Phase 4 (approved)	SLC6A2
CHLORPHENTERMINE	ChEMBL	Phase 4 (approved)	SLC6A2