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Atlas / Drug / Clonidine

Clonidine

drug
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Also known as Catapres-tts-1Catapres-tts-2Catapres-tts-3Catarpres-ttsClonidinaClonidine extended releaseClorpresCombipresNexiclon xrST-155BSSID11110984SID11110985SID11113648SID26751841SID104171138SID90341662SID170464900SID144203669

Summary

Clonidine (CHEMBL134) is an approved small molecule (ATC C02AC01) targeting ADRA2A; indicated across 38 conditions including hypertensive disorder and neuralgia.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C02AC01 (+2 more)
  • Targets: 1 (ADRA2A)
  • Indications: 38 conditions
  • Clinical trials: 176
  • Chemistry: 230.09 Da · C9H9Cl2N3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL134
NameClonidine
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID2803
ChEBICHEBI:3757
ATCC02AC01, N02CX02, S01EA04
Molecular formulaC9H9Cl2N3
Molecular weight230.09
InChIKeyGJSURZIOUXUGAL-UHFFFAOYSA-N

SMILES: C1CN=C(N1)NC2=C(C=CC=C2Cl)Cl

IUPAC name: N-(2,6-dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine

Also known as: Catapres-tts-1, Catapres-tts-2, Catapres-tts-3, Catarpres-tts, Clonidina, Clonidine, Clonidine extended release, Clorpres, Combipres, Nexiclon xr, ST-155BS, clonidine

Parent form; salt/anhydrous children: CHEMBL1705

Patent coverage: 27,244 distinct patent families (97,993 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).

GeneTargetActionpAffinityCancer dependencyUniProt
ADRA2Aα2A-adrenoceptorPartial agonist7.60.1%P08913

Broader ChEMBL bioactivity targets: 36 (assay-derived). Sample: Prelamin-A/C, Inositol monophosphatase 1, Ferritin light chain, Multidrug and toxin extrusion protein 1, Alpha-2A adrenergic receptor, Adrenergic receptor alpha-1, Alpha-2C adrenergic receptor, Histamine H2 receptor, Alpha-2B adrenergic receptor, Solute carrier family 22 member 1.

Bioactivity

ChEMBL activities: 120 potent at pChembl ≥ 5 of 134 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
ADRA2A9.54EC500.29nMCHEMBL_ACT_25982814
ADRA2A9.5EC500.32nMCHEMBL_ACT_25982816
P229099.41Ki0.39nMCHEMBL_ACT_1005004
P229099.41Ki0.39nMCHEMBL_ACT_203998
P193288.82Ki1.5nMCHEMBL_ACT_559502
P193288.77Ki1.7nMCHEMBL_ACT_1079539
ADRA1A8.77AC501.7nMCHEMBL_ACT_25208564
P193288.74Ki1.8nMCHEMBL_ACT_1003012
Q288388.7IC502nMCHEMBL_ACT_644453
P193288.6Ki2.51nMCHEMBL_ACT_15186170
P193288.57Ki2.7nMCHEMBL_ACT_16758669
P193288.51IC503.1nMCHEMBL_ACT_156766
ADRA2A8.42Ki3.8nMCHEMBL_ACT_15197906
ADRA2A8.42Ki3.8nMCHEMBL_ACT_38525
ADRA2A8.42Ki3.8nMCHEMBL_ACT_772445
P193288.41IC503.9nMCHEMBL_ACT_1003013
ADRA2A8.36EC504.4nMCHEMBL_ACT_38529
P193288.24Ki5.7nMCHEMBL_ACT_540834
ADRA2B8.21Ki6.17nMCHEMBL_ACT_1293879
ADRA2A8.1Ki7.94nMCHEMBL_ACT_1293878
ADRA2A8.09EC508.13nMCHEMBL_ACT_1293884
ADRA1A8.08AC508.3nMCHEMBL_ACT_25229712
ADRA2A8.08EC508.32nMCHEMBL_ACT_3556444
P193288.08Ki8.3nMCHEMBL_ACT_38526
P193288.08Ki8.3nMCHEMBL_ACT_772446
ADRA2A8.06Ki8.71nMCHEMBL_ACT_10964098
P193288.06Ki8.7nMCHEMBL_ACT_2488323
P193288.06Ki8.7nMCHEMBL_ACT_5129903
NISCH8.05Ki8.9nMCHEMBL_ACT_772448
ADRA2C8.03Ki9.33nMCHEMBL_ACT_10964112

Target pathways

Aggregated over 1 target gene(s): ADRA2A.

Top Reactome pathways

19 total, by targets touching each:

PathwayTargetsGenes
Hemostasis1ADRA2A
Metabolism1ADRA2A
Signal Transduction1ADRA2A
Integration of energy metabolism1ADRA2A
Signaling by GPCR1ADRA2A
Class A/1 (Rhodopsin-like receptors)1ADRA2A
Amine ligand-binding receptors1ADRA2A
GPCR downstream signalling1ADRA2A
Adrenoceptors1ADRA2A
Adrenaline signalling through Alpha-2 adrenergic receptor1ADRA2A
Metabolism of proteins1ADRA2A
Adrenaline,noradrenaline inhibits insulin secretion1ADRA2A
G alpha (i) signalling events1ADRA2A
G alpha (z) signalling events1ADRA2A
Regulation of insulin secretion1ADRA2A
GPCR ligand binding1ADRA2A
Surfactant metabolism1ADRA2A
Platelet activation, signaling and aggregation1ADRA2A
Platelet Aggregation (Plug Formation)1ADRA2A

Dominant GO biological processes

GO termTargets
positive regulation of cytokine production1
DNA replication1
epidermal growth factor receptor signaling pathway1
G protein-coupled receptor signaling pathway1
adenylate cyclase-activating G protein-coupled receptor signaling pathway1
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway1
Ras protein signal transduction1
Rho protein signal transduction1
female pregnancy1
positive regulation of cell population proliferation1
negative regulation of norepinephrine secretion1
regulation of vasoconstriction1
actin cytoskeleton organization1
platelet activation1
positive regulation of cell migration1

Indications & clinical

Indications

38 indications (5 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
hypertensive disorder4MONDO:0005044EFO:0000537
neuralgia4MONDO:0021667EFO:0005762
migraine disorder4MONDO:0005277MONDO:0005277
neoplasm4MONDO:0005070MONDO:0004992
glaucoma4MONDO:0005041MONDO:0005041
attention deficit-hyperactivity disorder3MONDO:0007743EFO:0003888
cardiovascular disorder3MONDO:0004995EFO:0000319
neonatal abstinence syndrome3MONDO:0005566EFO:0005799
hyperemesis gravidarum3MONDO:0006791EFO:1000971
scoliosis3MONDO:0005392EFO:0004273
delirium3MONDO:0045057EFO:0009267
post-traumatic stress disorder3MONDO:0005146EFO:0001358
male reproductive organ cancer3MONDO:0005836EFO:0007355
pituitary dwarfism3MONDO:0006909EFO:1001109
anxiety2MONDO:0011918EFO:0005230
opiate dependence2MONDO:0005530EFO:0005611
autism spectrum disorder2MONDO:0005258EFO:0003756
diabetic neuropathy2MONDO:0006626EFO:1000783
drug dependence2MONDO:0005303EFO:0003890
cannabis dependence2MONDO:0005689EFO:0007191
brain injury2MONDO:0043510MONDO:0043510
stomatitis2MONDO:0004842EFO:1001904
breast neoplasm2MONDO:0021100MONDO:0007254
musculoskeletal system disorder2MONDO:0002081EFO:0009676
atopic eczema1MONDO:0004980EFO:0000274
heroin dependence1MONDO:0005367EFO:0004240
orthostatic hypotension1MONDO:0005469EFO:0005252
postural orthostatic tachycardia syndrome1MONDO:0011479EFO:1000645
brain ischemia1MONDO:0005299MONDO:0005299

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

Clinical trials

Total trials: 176.

Phase distribution

PhaseTrials
PHASE451
Not specified41
PHASE230
PHASE323
PHASE112
PHASE1/PHASE29
PHASE2/PHASE36
EARLY_PHASE14

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03092011PHASE4ACTIVE_NOT_RECRUITINGTreatment of Neonatal Abstinence Syndrome With Clonidine Versus Morphine as Primary Therapy
NCT03121261PHASE4ACTIVE_NOT_RECRUITINGThe Effect of Local Anesthetic and Clonidine on the Cutaneous Silent Period During Spinal Anesthesia
NCT05824832PHASE4RECRUITINGBuprenorphine, Clonidine, and Dexamethasone on Duration of Brachial Plexus Blocks for Upper Extremity Surgery
NCT07313371PHASE4RECRUITINGEfficacy of Clonidine in Reducing Craving in Inpatients With Cocaine and Crack Use Disorder
NCT07567495PHASE4NOT_YET_RECRUITINGAdding Dexmedetomidine or Clonidine to Spinal Anesthesia for Cesarean Delivery
NCT00370838PHASE4COMPLETEDComparison of Keppra and Clonidine in the Treatment of Tics
NCT00535925PHASE4COMPLETEDNephropathy In Type 2 Diabetes and Cardio-renal Events
NCT00661895PHASE4COMPLETEDBlack Education and Treatment of Hypertension (BEAT HTN)
NCT00858845PHASE4COMPLETEDUsing Clonidine to Improve Leg Weakness in People With Heart Failure
NCT00860899PHASE4COMPLETEDPostoperative Pain and SIRS After Preoperative Analgesia With Clonidine or Levobupivacaine
NCT00860925PHASE4COMPLETEDPeriOperative ISchemic Evaluation-2 Pilot
NCT00959062PHASE4COMPLETEDAdjunctive Clonidine in the Sedation of Mechanically Ventilated Children
NCT00983125PHASE4COMPLETEDSystematic Clonidine for Epidural Analgesia in Labour
NCT01052623PHASE4UNKNOWNStatus of Growth Hormone/ Insulin-like Growth Factor-1 (GH/IGF-1) Axis and Growth Failure in Ataxia Telangiectasia (AT)
NCT01075490PHASE4UNKNOWNNeonatal Spinal Anesthesia: Effects of the Addition of Clonidine
NCT01112878PHASE4WITHDRAWNOral Clonidine & Gabapentin: Improving Recovery and Pain Management After Outpatient With Major Orthopedic Surgery
NCT01139996PHASE4TERMINATEDUse of Transdermal Clonidine in Trauma Patients
NCT01619436PHASE4COMPLETEDThe Effect of Clonidine in Glycemia During Coronary Artery Bypass Graft With Cardiopulmonary By-pass
NCT01643434PHASE4UNKNOWNResistant Hypertension Optimal Treatment
NCT01734551PHASE4COMPLETEDNAS Treatment - Opiate Versus Non-Opiate
NCT01761916PHASE4COMPLETEDClonidine Versus Captopril for Treatment of Postpartum Very High Blood Pressure
NCT01785693PHASE4COMPLETEDInterest of a Bi-truncal Nerve Block (Femoral + Sciatic) Extended, Systematically Associated With General Anesthesia, in the Femoropopliteal Bypass: Study of Post-operative Analgesia and Peripheral Circulation Downstream
NCT01846221PHASE4COMPLETEDComparison of Epidural Fentanyl and Clonidine for Breakthrough Pain
NCT01902108PHASE4COMPLETEDAdded Value of Local Clonidine for Spine Postoperative Pain Control, in Addition to Bupivacaine
NCT01931215PHASE4COMPLETEDTransversus Abdominis Plane (TAP) Block Versus Intrathecal Morphine for Caesarean Section - Randomised Controlled Trial
NCT02067078PHASE4COMPLETEDProtracted Effect of Combined Nerve Blocks After Total Knee Arthroplasty
NCT02177461PHASE4COMPLETEDTelmisartan Compared With Enalapril in Elderly Patients With Blood Hypertension
NCT02361476PHASE4COMPLETEDDoes Intraoperative Clonidine Reduce Post Operative Agitation in Children?
NCT02365727PHASE4WITHDRAWNExparel vs Exparel Plus ACB in TKAs
NCT02365961PHASE4COMPLETEDHip Scope Fascia-iliaca (FI) Block Study
NCT02543801PHASE4COMPLETEDA Clinical Trial of Two Periarticular Multimodal Drug Injections in Total Hip and Knee Arthroplasty
NCT02570503PHASE4TERMINATEDPostoperative Pain Control After Periarticular Injection During Total Knee Arthroplasty
NCT02773602PHASE4UNKNOWNDexamethasone or Clonidine as Adjuncts to Ropivacaine for Caudal Analgesia on Analgesia Duration in Children
NCT03017430PHASE4COMPLETEDPregabalin for Opiate Withdrawal Syndrome
NCT03018171PHASE4UNKNOWNIntrathecal Clonidine Addiction for Combined Spinal Epidural Analgesia During Labor
NCT03057015PHASE4UNKNOWNAddition of Clonidine to Ropivacaine in Adductor Canal Block
NCT03065933PHASE4TERMINATEDAn Extended-Release Form of Clonidine as an Anti-Manic Agent: An Add-on, Open-Label Study
NCT03109795PHASE4TERMINATEDAnxiety-mediated Impairments in Large Elastic Artery Function and the Autonomic Nervous System
NCT03119038PHASE4WITHDRAWNEfficacy of Intraoperative Injections on Postoperative Pain Control During Total Hip Replacement
NCT03124082PHASE4UNKNOWNOFA - Opioid Free Anesthesia

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (1) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

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

PharmGKB also curates 2 clinical and 7 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.

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

MoleculeSourceStatusShared targets
ACLIDINIUM BROMIDEChEMBL + PubChemPhase 4 (approved)ADRA2A
CHENODIOLChEMBL + PubChemPhase 4 (approved)ADRA2A
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)ADRA2A
DESLORATADINEChEMBL + PubChemPhase 4 (approved)ADRA2A
DIHYDROERGOTAMINEChEMBL + PubChemPhase 4 (approved)ADRA2A
GENTIAN VIOLETChEMBL + PubChemPhase 4 (approved)ADRA2A
NAPHAZOLINEChEMBL + PubChemPhase 4 (approved)ADRA2A
OLODATEROLChEMBL + PubChemPhase 4 (approved)ADRA2A
PALIPERIDONEChEMBL + PubChemPhase 4 (approved)ADRA2A
PRAMIPEXOLEChEMBL + PubChemPhase 4 (approved)ADRA2A
TAMSULOSINChEMBL + PubChemPhase 4 (approved)ADRA2A
ACETOPHENAZINEChEMBLPhase 4 (approved)ADRA2A
ALFUZOSINChEMBLPhase 4 (approved)ADRA2A
AMIODARONEChEMBLPhase 4 (approved)ADRA2A
AMISULPRIDEChEMBLPhase 4 (approved)ADRA2A
AMITRIPTYLINEChEMBLPhase 4 (approved)ADRA2A
AMLODIPINEChEMBLPhase 4 (approved)ADRA2A
AMOXAPINEChEMBLPhase 4 (approved)ADRA2A
ANTAZOLINEChEMBLPhase 4 (approved)ADRA2A
APOMORPHINEChEMBLPhase 4 (approved)ADRA2A
APRACLONIDINEChEMBLPhase 4 (approved)ADRA2A
ARIPIPRAZOLEChEMBLPhase 4 (approved)ADRA2A
ASENAPINEChEMBLPhase 4 (approved)ADRA2A
ASTEMIZOLEChEMBLPhase 4 (approved)ADRA2A
ATRACURIUMChEMBLPhase 4 (approved)ADRA2A
AURANOFINChEMBLPhase 4 (approved)ADRA2A
AZELASTINEChEMBLPhase 4 (approved)ADRA2A
BAZEDOXIFENEChEMBLPhase 4 (approved)ADRA2A
BENFLUOREXChEMBLPhase 4 (approved)ADRA2A
BENPERIDOLChEMBLPhase 4 (approved)ADRA2A
BENZBROMARONEChEMBLPhase 4 (approved)ADRA2A
BENZIODARONEChEMBLPhase 4 (approved)ADRA2A
BENZQUINAMIDEChEMBLPhase 4 (approved)ADRA2A
BENZTHIAZIDEChEMBLPhase 4 (approved)ADRA2A
BENZTROPINEChEMBLPhase 4 (approved)ADRA2A
BENZYDAMINEChEMBLPhase 4 (approved)ADRA2A
BEXAROTENEChEMBLPhase 4 (approved)ADRA2A
BISACODYLChEMBLPhase 4 (approved)ADRA2A
BITHIONOLChEMBLPhase 4 (approved)ADRA2A
BOSUTINIBChEMBLPhase 4 (approved)ADRA2A
BREXPIPRAZOLEChEMBLPhase 4 (approved)ADRA2A
BRIMONIDINEChEMBLPhase 4 (approved)ADRA2A
BROMOCRIPTINEChEMBLPhase 4 (approved)ADRA2A
BROMODIPHENHYDRAMINEChEMBLPhase 4 (approved)ADRA2A
BROMPERIDOLChEMBLPhase 4 (approved)ADRA2A
BUFLOMEDILChEMBLPhase 4 (approved)ADRA2A
BUTENAFINEChEMBLPhase 4 (approved)ADRA2A
CABERGOLINEChEMBLPhase 4 (approved)ADRA2A
CABOZANTINIBChEMBLPhase 4 (approved)ADRA2A
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)ADRA2A
CARBENOXOLONEChEMBLPhase 4 (approved)ADRA2A
CARIPRAZINEChEMBLPhase 4 (approved)ADRA2A
CARVEDILOLChEMBLPhase 4 (approved)ADRA2A
CHLORHEXIDINEChEMBLPhase 4 (approved)ADRA2A
CHLOROQUINEChEMBLPhase 4 (approved)ADRA2A
CHLORPROMAZINEChEMBLPhase 4 (approved)ADRA2A
CHLORPROTHIXENEChEMBLPhase 4 (approved)ADRA2A
CHLORZOXAZONEChEMBLPhase 4 (approved)ADRA2A
CINNARIZINEChEMBLPhase 4 (approved)ADRA2A
CISAPRIDEChEMBLPhase 4 (approved)ADRA2A

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