Moxonidine

Summary

Moxonidine (CHEMBL19236) is an approved small molecule (ATC C02AC05) targeting ADRA2A, ADRA2B, and ADRA2C; indicated across 3 conditions including hypertensive disorder and heart disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C02AC05
• Targets: 3 (ADRA2A, ADRA2B, ADRA2C)
• Indications: 3 conditions
• Clinical trials: 18
• Chemistry: 241.68 Da · C9H12ClN5O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL19236
Name	Moxonidine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	4810
ATC	C02AC05
Molecular formula	C9H12ClN5O
Molecular weight	241.68
InChIKey	WPNJAUFVNXKLIM-UHFFFAOYSA-N

SMILES: CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC

IUPAC name: 4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methylpyrimidin-5-amine

Also known as: BDF-5896, BDF5896, BE-5895, BE5895, Cynt, Fisiotens, LY-326869, LY326869, Moxonidina, Moxonidine, Normatens, Physiotens

Parent form; salt/anhydrous children: CHEMBL1256287

Patent coverage: 1,259 distinct patent families (4,405 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 4,145 (94%) of the total. 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
ADRA2A	α2A-adrenoceptor	Agonist	5	0.1%	P08913
ADRA2B	α2B-adrenoceptor	Agonist	4.6	0.2%	P18089
ADRA2C	α2C-adrenoceptor	Agonist	4.8	0%	P18825

Broader ChEMBL bioactivity targets: 14 (assay-derived). Sample: Prelamin-A/C, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Histamine H2 receptor, Alpha-2B adrenergic receptor, Adrenergic receptor alpha-2, 5-hydroxytryptamine receptor 1A, Alpha-1A adrenergic receptor, Alpha-2B adrenergic receptor, 5-hydroxytryptamine receptor 1A.

Bioactivity

ChEMBL activities: 14 potent at pChembl ≥ 5 of 19 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
NISCH	8.45	IC50	3.55	nM	CHEMBL_ACT_19062262
NISCH	8.38	Ki	4.2	nM	CHEMBL_ACT_2564082
NISCH	7.25	Ki	56	nM	CHEMBL_ACT_758354
ADRA2A	7.12	Ki	75	nM	CHEMBL_ACT_15197908
Q4G017	7.11	Ki	77.8	nM	CHEMBL_ACT_15197881
ADRA2A	7.06	AC50	88	nM	CHEMBL_ACT_25220855
ADRA1A	7.05	AC50	90	nM	CHEMBL_ACT_25229620
ADRA2A	6.82	Ki	150	nM	CHEMBL_ACT_758351
LMNA	6.4	Potency	398.1	nM	CHEMBL_ACT_3655025
P19327	6.4	Ki	401.2	nM	CHEMBL_ACT_7773483
P19327	6.15	IC50	702.1	nM	CHEMBL_ACT_7773482
P19328	6	Ki	1000	nM	CHEMBL_ACT_758352
ADRA2C	5.7	Ki	2000	nM	CHEMBL_ACT_758353
HTR1A	5.19	AC50	6500	nM	CHEMBL_ACT_25216789

Target pathways

Aggregated over 3 target gene(s): ADRA2A, ADRA2B, ADRA2C.

Top Reactome pathways

19 total, by targets touching each:

Pathway	Targets	Genes
Hemostasis	3	ADRA2A, ADRA2B, ADRA2C
Signal Transduction	3	ADRA2A, ADRA2B, ADRA2C
Signaling by GPCR	3	ADRA2A, ADRA2B, ADRA2C
Class A/1 (Rhodopsin-like receptors)	3	ADRA2A, ADRA2B, ADRA2C
Amine ligand-binding receptors	3	ADRA2A, ADRA2B, ADRA2C
GPCR downstream signalling	3	ADRA2A, ADRA2B, ADRA2C
Adrenoceptors	3	ADRA2A, ADRA2B, ADRA2C
Adrenaline signalling through Alpha-2 adrenergic receptor	3	ADRA2A, ADRA2B, ADRA2C
G alpha (i) signalling events	3	ADRA2A, ADRA2B, ADRA2C
G alpha (z) signalling events	3	ADRA2A, ADRA2B, ADRA2C
GPCR ligand binding	3	ADRA2A, ADRA2B, ADRA2C
Platelet activation, signaling and aggregation	3	ADRA2A, ADRA2B, ADRA2C
Platelet Aggregation (Plug Formation)	3	ADRA2A, ADRA2B, ADRA2C
Metabolism	2	ADRA2A, ADRA2C
Integration of energy metabolism	2	ADRA2A, ADRA2C
Metabolism of proteins	2	ADRA2A, ADRA2C
Adrenaline,noradrenaline inhibits insulin secretion	2	ADRA2A, ADRA2C
Regulation of insulin secretion	2	ADRA2A, ADRA2C
Surfactant metabolism	2	ADRA2A, ADRA2C

Dominant GO biological processes

GO term	Targets
epidermal growth factor receptor signaling pathway	3
G protein-coupled receptor signaling pathway	3
negative regulation of norepinephrine secretion	3
regulation of vasoconstriction	3
platelet activation	3
negative regulation of epinephrine secretion	3
positive regulation of MAPK cascade	3
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	3
adrenergic receptor signaling pathway	3
adenylate cyclase-inhibiting adrenergic receptor signaling pathway	3
regulation of smooth muscle contraction	3
signal transduction	3
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	2
female pregnancy	2
negative regulation of insulin secretion	2

Indications & clinical

Indications

3 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).

Indication	Trial phase	MONDO	EFO
hypertensive disorder	4	MONDO:0005044	EFO:0000537
heart disorder	3	MONDO:0005267	EFO:0003777
orthostatic hypotension	0	MONDO:0005469	EFO:0005252

Clinical trials

Total trials: 18.

Phase distribution

Phase	Trials
PHASE4	11
PHASE3	2
EARLY_PHASE1	2
PHASE1/PHASE2	1
PHASE1	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01094769	PHASE4	COMPLETED	Sympathetic Nervous System Inhibition for the Treatment of Diabetic Kidney Disease
NCT01138423	PHASE4	COMPLETED	Treatment of Adiposity Related hypErTension (TARGET)
NCT01180231	PHASE4	UNKNOWN	Study of the Effect of Moxonidine and Diet on Sympathetic Functions in Young Adults With Obesity
NCT01360710	PHASE4	UNKNOWN	The Effect of Moxonidine on Blood Pressure and Regression of Early Target Organ Damage in Young Subjects With Abdominal Obesity and Hypertension
NCT01504321	PHASE4	COMPLETED	Polycystic Ovary Syndrome - Improving Outcomes
NCT01567124	PHASE4	WITHDRAWN	Alleviating the Metabolic Side Effects of Antipsychotic Medications
NCT01791699	PHASE4	COMPLETED	Moxonidine for Prevention of Post-ablation AFib Recurrences
NCT04023565	PHASE4	UNKNOWN	Moxonidine + Perindopril in Hypertensive Patients With Metabolic Syndrome
NCT04474899	PHASE4	UNKNOWN	Sympathoinhibition as a Preferred Second Line Treatment of Obesity Related Hypertension
NCT04479813	PHASE4	COMPLETED	Role of Sympathetic Activation in Ischemia Reperfusion Injury
NCT05147753	PHASE4	COMPLETED	Moxonidine Effects on Neuropeptide Y
NCT00160277	PHASE3	COMPLETED	Efficacy and Safety of Moxonidine in Indian Patients
NCT00244504	PHASE3	TERMINATED	Moxonidine in Patients Undergoing Vascular Surgery
NCT05312892	PHASE1/PHASE2	RECRUITING	Sympathetic Mechanisms in Obesity-Crossover Design
NCT04329806	PHASE1	TERMINATED	Sympathetic Mechanisms in the Cardiovascular and Metabolic Alterations of Obesity
NCT04050410	EARLY_PHASE1	ACTIVE_NOT_RECRUITING	Autonomic Determinants of POTS - Pilot1
NCT04140721	EARLY_PHASE1	ACTIVE_NOT_RECRUITING	Autonomic Determinants of POTS - Pilot 2
NCT02355821	Not specified	COMPLETED	Comparative Effects of Moxonidine on Bone Metabolism, Vascular and Cellular Aging in Hypertensive Postmenopausal Women

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.

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

Molecule	Source	Status	Shared targets
ACLIDINIUM BROMIDE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
Afatinib	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
Almotriptan	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CHENODIOL	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CLOZAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
DESLORATADINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
GENTIAN VIOLET	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
NAPHAZOLINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
OLANZAPINE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
OLODATEROL	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
PALIPERIDONE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
PRAMIPEXOLE	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
TAMSULOSIN	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
TEGASEROD	ChEMBL + PubChem	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
ACETOPHENAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
ALFUZOSIN	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
AMISULPRIDE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
AMOXAPINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
APOMORPHINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
APRACLONIDINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
ASENAPINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
AZELASTINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
BENFLUOREX	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
BENPERIDOL	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
BENZBROMARONE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
BENZQUINAMIDE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
BENZTHIAZIDE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
BENZTROPINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
BITHIONOL	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
BRIMONIDINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
BROMPERIDOL	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CABERGOLINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CARIPRAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CARVEDILOL	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CHLOROQUINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CINNARIZINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CISAPRIDE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CLEMASTINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CLONIDINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
DANAZOL	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
DARIFENACIN	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
DEXMEDETOMIDINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
DOBUTAMINE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
DOMPERIDONE	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C
DOTHIEPIN	ChEMBL	Phase 4 (approved)	ADRA2A, ADRA2B, ADRA2C