Medetomidine

Summary

Medetomidine (CHEMBL77921) is an approved small molecule.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Clinical trials: 1,388
• Chemistry: 200.28 Da · C13H16N2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL77921
Name	Medetomidine
Type	Small molecule
Max phase	3
FDA approved	yes
PubChem CID	68602
ChEBI	CHEBI:48552
Molecular formula	C13H16N2
Molecular weight	200.28
InChIKey	CUHVIMMYOGQXCV-UHFFFAOYSA-N

SMILES: CC1=C(C(=CC=C1)C(C)C2=CN=CN2)C

IUPAC name: 5-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole

Also known as: Domitor, Medetomidina, Medetomidine, MEDETOMIDINE, dexmedetomidine, MEDETOMIDINE_DEXMEDETOMIDINE, medetomidine

Parent form; salt/anhydrous children: CHEMBL537161

Patent coverage: 1,871 distinct patent families (6,766 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 6,424 (95%) 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

Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: Alpha-2A adrenergic receptor, Adrenergic receptor alpha-1, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Adrenergic receptor alpha-2, Adrenergic receptor alpha-1, Adrenergic receptor alpha-2, Alpha-1A adrenergic receptor, Voltage-gated inwardly rectifying potassium channel KCNH2.

Bioactivity

ChEMBL activities: 17 potent at pChembl ≥ 5 of 18 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ADRA2A	8.52	EC50	3	nM	CHEMBL_ACT_1222279
P19328	7.72	Ki	19	nM	CHEMBL_ACT_1222281
P19328	7.6	Ki	25	nM	CHEMBL_ACT_1047180
P19328	7.6	Ki	25	nM	CHEMBL_ACT_779765
ADRA1A	6.96	AC50	110	nM	CHEMBL_ACT_25137855
ADRA2A	6.76	AC50	172.9	nM	CHEMBL_ACT_25157072
P15823	6.55	EC50	281	nM	CHEMBL_ACT_1047182
P15823	5.96	Ki	1109	nM	CHEMBL_ACT_1047179
P15823	5.96	Ki	1102	nM	CHEMBL_ACT_1222280
P15823	5.96	Ki	1110	nM	CHEMBL_ACT_779764
ADRA1D	5.93	EC50	1165	nM	CHEMBL_ACT_1222278
ADRA2C	5.89	AC50	1300	nM	CHEMBL_ACT_25147746
ADRA2A	5.88	AC50	1334	nM	CHEMBL_ACT_25155899
ADRA2A	5.75	AC50	1780	nM	CHEMBL_ACT_25220962
ADRA2B	5.68	AC50	2100	nM	CHEMBL_ACT_25143575
ADRA2A	5.54	IC50	2900	nM	CHEMBL_ACT_1047183
ADRA2A	5.47	IC50	3400	nM	CHEMBL_ACT_1222277

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

0 indications (0 at ChEMBL trial phase 4).

Clinical trials

Total trials: 1,388.

Phase distribution

Phase	Trials
Not specified	508
PHASE4	470
PHASE3	137
PHASE2	89
PHASE2/PHASE3	73
PHASE1	51
EARLY_PHASE1	36
PHASE1/PHASE2	24

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03384563	PHASE4	RECRUITING	Effect of Dexmedetomidine on the Minimum Alveolar Concentration of Sevoflurane
NCT03480061	PHASE4	ACTIVE_NOT_RECRUITING	Dexmedetomidine to Reduce the Incidence of POCD After Open Cardiac Surgery
NCT04289142	PHASE4	RECRUITING	Cognitive Outcomes After Dexmedetomidine Sedation in Cardiac Surgery Patients
NCT04669457	PHASE4	ENROLLING_BY_INVITATION	Pediatric Delirium
NCT04730609	PHASE4	RECRUITING	Dexmedetomidine for Intraoperative Shivering in Scheduled Elective Cesarean Delivery
NCT05031026	PHASE4	ACTIVE_NOT_RECRUITING	Dexmedetomidine to Prevent Hepatic Ischemia-reperfusion Injury-induced Glycocalyx Degradation and Early Allograft Dysfunction in Liver Transplantation
NCT05466708	PHASE4	RECRUITING	Safety and Efficacy of Esketamine Combined With Dexmedetomidine for Sedation of Mechanically Ventilated Patients
NCT05640453	PHASE4	RECRUITING	Pregabalin Versus Dexmedetomidine for Delirium Treatment After Coronary Artery Bypass Grafting
NCT05934669	PHASE4	RECRUITING	IN Midazolam vs IN Dexmedetomidine vs IN Ketamine During Minimal Procedures in Pediatric ED
NCT05935293	PHASE4	NOT_YET_RECRUITING	Dexmedetomidine and Kidney Transplantation
NCT05950646	PHASE4	RECRUITING	Mini-dose Dexmedetomidine-Esketamine Infusion and Perioperative Sleep Quality
NCT06067893	PHASE4	ENROLLING_BY_INVITATION	Low Dose Dexmedetomidine as a Postoperative Pain Adjunct
NCT06139692	PHASE4	RECRUITING	Comparison of Perioperative Conscious Sedation During Endovascular Thrombectomy in Acute Ischemic Stroke
NCT06251375	PHASE4	NOT_YET_RECRUITING	Early Sedation With Dexmedetomidine vs. Placebo in Older Ventilated Critically Ill Patients
NCT06252662	PHASE4	RECRUITING	Liposomal Bupivacaine Vs Bupivacaine with Dexmedetomidine in Erector Spinae Plane Blocks for Mastectomies
NCT06399185	PHASE4	RECRUITING	Effect of Dexmedetomidine and Esketamine on Catheter-related Bladder Discomfort
NCT06410365	PHASE4	NOT_YET_RECRUITING	Impact of Intrathecal vs Intravenous Dexmedetomidine
NCT06418308	PHASE4	RECRUITING	Intrathecal Dexmedetomidine vs Epinephrine
NCT06480539	PHASE4	RECRUITING	The Effect of Nocturnal Dexmedetomidine on Postoperative Sleep Quality and Fatigue After Major Surgery in Elderly Patients: DEXSLEEP Study
NCT06570187	PHASE4	RECRUITING	The Effect of Dexmedetomidine on the Renal Functions in Septic Critically Ill Patients
NCT06575179	PHASE4	RECRUITING	Dexmedetomidine Reduces Sevoflurane MAC-BAR During Pneumoperitoneum
NCT06631534	PHASE4	RECRUITING	Effect of Dexmedetomidine Supplementation to General Anaesthesia in Paediatric Transcatheter Closure of Atrial Septal Defect
NCT06636578	PHASE4	RECRUITING	Dexmedetomidine Ropivacaine Versus Plain Ropivacaine in Bilateral Pectoralis Nerve (PECS) Block
NCT06690021	PHASE4	NOT_YET_RECRUITING	Comparing The Effect of Adding Dexmedetomidine to Bupivacaine in Classical and Modified Thoracolumbar Interfascial Plane Block on Postoperative Pain in Patients Undergoing Lumbar Disc Surgeries
NCT06695468	PHASE4	NOT_YET_RECRUITING	Efficacy and Safety of Adding Dexmedetomidine to Levobupivacaine in Rectus Sheath Block Compared to Quadratus Lumborum Block in Patients Undergoing Lower Abdominal Cancer Surgery: A Randomized Clinical Trial
NCT06720337	PHASE4	NOT_YET_RECRUITING	Comparative Study Between the Analgesic Effect of Dexmedetomidine and Magnesium Sulfate as Adjuvant to Bupivacaine Using Ultrasound-Guided Transversus Abdominis Plane Block in Abdominal Hysterectomy : A Randomized Double-blinded Study
NCT06734195	PHASE4	NOT_YET_RECRUITING	Comparing the Synergistic Effect of Caudal Dexmedetomidine and Propofol Versus Caudal Dexmedetomidine Only or Propofol Only in Prevention of Sevoflurane Related Emergence Agitation in Pediatric Patients Undergoing Congenital Inguinal Hernia Repair
NCT06736496	PHASE4	NOT_YET_RECRUITING	Comparative Study of Opioid-Free Anesthesia Versus Opioid Anesthesia in Patients Undergoing Laparoscopic Cholecystectomy
NCT06752317	PHASE4	NOT_YET_RECRUITING	Effect of Preoperative Intrathecal Dexamethasone Versus Dexmedetomidine on Paralytic Ileus After Major Abdominal Surgery
NCT06752629	PHASE4	NOT_YET_RECRUITING	Comparison Between Dexmedetomidine and Fentanyl As an Adjuvant to Bupivacaine in the Paravertebral Nerve Block in Laparoscopic Cholecystectomy for Postoperative Analgesia: Randomized Comparative Clinical Trial.
NCT06822088	PHASE4	NOT_YET_RECRUITING	Effects of Esketamine on Oxygenation and Quality of Recovery in Patients Undergoing Thoracoscopic Surgery
NCT06823349	PHASE4	RECRUITING	Comparative Analysis of Analgesic Efficacy: by Single Shot Intrathecal Analgesia (SSSA) in Normal Labor
NCT06837818	PHASE4	NOT_YET_RECRUITING	To Explore the Optimal Dose of Dexmedetomidine for Skull Pin Fixation in Intracranial Surgery
NCT06849466	PHASE4	ENROLLING_BY_INVITATION	Effect of Perioperative Dexmedetomidine on Chronic Post-Surgical Pain
NCT06853431	PHASE4	RECRUITING	Determination of ED50 and ED95 With Clinical Efficacy of Intranasal Dexmedetomidine Combined With Esketamine for Preoperative Sedation in Pediatric General Anesthesia
NCT06958393	PHASE4	NOT_YET_RECRUITING	Effect of Opioid-free Anaesthesia on Postoperative Delirium in Elderly Patients Undergoing Gastrointestinal Surgery
NCT06981949	PHASE4	NOT_YET_RECRUITING	Addition of Dexmedetomidine to Ropivacaine in Bilateral Erector Spinae Plane Block in Patients Undergoing Coronary Artery Bypass Surgery
NCT07022821	PHASE4	RECRUITING	Comparison of Dexmedetomidine + Ketamine for Postoperative Pain in C-Section
NCT07034300	PHASE4	RECRUITING	Lidocaine vs. Lidocaine With Dexmedetomidine for Intravenous Regional Anesthesia (IVRA) in Upper Limb Surgery
NCT07034898	PHASE4	ENROLLING_BY_INVITATION	Dexmedetomidine vs Labetalol for Airway Stress in Hypertensive Craniotomy Patients

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 5 clinical and 40 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).