Chlorhexidine

Summary

Chlorhexidine (CHEMBL790) is an approved small-molecule antiinfective agent (ATC D08AC02) targeting TAS2R2; indicated across 23 conditions including eye infectious disorder and periodontitis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: D08AC02 (+8 more)
• Targets: 1 (TAS2R2)
• Indications: 23 conditions
• Clinical trials: 233
• Chemistry: 505.4 Da · C22H30Cl2N10

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL790
Name	Chlorhexidine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	9552079
ChEBI	CHEBI:3614
ATC	D08AC02, D09AA12, S01AX09, B05CA02, D08AC52, A01AB03, R02AA05, S02AA09, S03AA04
Molecular formula	C22H30Cl2N10
Molecular weight	505.4
InChIKey	GHXZTYHSJHQHIJ-UHFFFAOYSA-N

SMILES: C1=CC(=CC=C1N/C(=N/C(=NCCCCCCN=C(/N=C(/NC2=CC=C(C=C2)Cl)\N)N)N)/N)Cl

IUPAC name: (1E)-2-[6-[[amino-[(E)-[amino-(4-chloroanilino)methylidene]amino]methylidene]amino]hexyl]-1-[amino-(4-chloroanilino)methylidene]guanidine

ChEBI definition: A bisbiguanide compound with a structure consisting of two (p-chlorophenyl)guanide units linked by a hexamethylene bridge.

Pharmacological roles (ChEBI): antiinfective agent, antibacterial agent.

Also known as: Avagard, Chlorhexadine, Chlorhexidine, Clorhexidina, Dentisept, Merfen-incolore, Biguanide derivative, chlorhexidine, oridin, SID11112130, SID17389113, SID26752881

Parent form; salt/anhydrous children: CHEMBL486819, CHEMBL1628, CHEMBL1330113, CHEMBL1484251, CHEMBL2106050, CHEMBL4297088

Patent coverage: 27,517 distinct patent families (85,053 SureChEMBL compound mentions), from 11 matched compound structure(s). One matched structure accounts for 80,588 (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

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
TAS2R2	TAS2R2	Agonist			Q50KZ9

Broader ChEMBL bioactivity targets: 67 (assay-derived). Sample: CAAX prenyl protease 2, Nuclear receptor ROR-gamma, Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, Hexokinase HKDC1, Solute carrier family 22 member 2, Multidrug and toxin extrusion protein 1, Multidrug and toxin extrusion protein 2, Vasopressin V2 receptor, 5-hydroxytryptamine receptor 2B.

Bioactivity

ChEMBL activities: 64 potent at pChembl ≥ 5 of 91 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P67578	9.23	Kd	0.59	nM	CHEMBL_ACT_25857469
P67578	8.92	Kd	1.21	nM	CHEMBL_ACT_25857461
P67578	8.51	Kd	3.1	nM	CHEMBL_ACT_25857453
P67578	8.22	Kd	6	nM	CHEMBL_ACT_25857476
TP53	8.1	Potency	7.9	nM	CHEMBL_ACT_4854900
P67578	7.99	Kd	10.2	nM	CHEMBL_ACT_25857445
LMNA	7.45	Potency	35.5	nM	CHEMBL_ACT_3647276
SLC22A1	6.68	IC50	210	nM	CHEMBL_ACT_12636171
MC4R	6.57	AC50	271	nM	CHEMBL_ACT_25184156
SLC22A2	6.4	IC50	400	nM	CHEMBL_ACT_12636201
SLC22A3	6.39	IC50	410	nM	CHEMBL_ACT_12636159
SLC6A2	6.39	AC50	409	nM	CHEMBL_ACT_25144575
P67578	6.35	Kd	450	nM	CHEMBL_ACT_25857415
MC3R	6.31	AC50	490	nM	CHEMBL_ACT_25182967
SLC47A2	6.3	IC50	500	nM	CHEMBL_ACT_12636232
ADRA1A	6.22	AC50	607.4	nM	CHEMBL_ACT_25137672
ADRA1A	6.22	AC50	600	nM	CHEMBL_ACT_25217774
HTR2B	6.17	AC50	683.2	nM	CHEMBL_ACT_25163999
SLC47A1	6.16	IC50	700	nM	CHEMBL_ACT_12637862
MLNR	6.11	AC50	784	nM	CHEMBL_ACT_25188769
SLC6A4	6	AC50	1000	nM	CHEMBL_ACT_25149914
GHSR	6	AC50	1000	nM	CHEMBL_ACT_25172336
HTR2B	5.9	AC50	1265	nM	CHEMBL_ACT_25227117
ADRB1	5.85	AC50	1400	nM	CHEMBL_ACT_25121355
RAD52	5.77	AC50	1700	nM	CHEMBL_ACT_13173507
ADRA2C	5.75	AC50	1800	nM	CHEMBL_ACT_25147437
LMNA	5.75	Potency	1778	nM	CHEMBL_ACT_3626817
HTR2A	5.74	AC50	1833	nM	CHEMBL_ACT_25224774
P67578	5.72	Kd	1900	nM	CHEMBL_ACT_25857475
P28593	5.7	Ki	2000	nM	CHEMBL_ACT_1485474

Target pathways

Aggregated over 1 target gene(s): TAS2R2.

Indications & clinical

Indications

23 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
eye infectious disorder	4	MONDO:0043885	EFO:1001888
periodontitis	3	MONDO:0005076	EFO:0000649
bacterial infectious disease with sepsis	3	MONDO:0005229	EFO:0003033
pneumonia	3	MONDO:0005249	EFO:0003106
dental caries	3	MONDO:0005276	EFO:0003819
staphylococcus aureus infection	3	MONDO:0005545	EFO:0005681
infectious disease	3	MONDO:0005550	EFO:0005741
bacterial infectious disease	3	MONDO:0005113	EFO:0000771
neutropenia	3	MONDO:0001475	MONDO:0001475
pharyngitis	3	MONDO:0002258	MONDO:0002258
gingivitis	3	MONDO:0002508	MONDO:0002508
chronic obstructive pulmonary disease	2	MONDO:0005002	EFO:0000341
stomatitis	2	MONDO:0004842	EFO:1001904
Acanthamoeba keratitis	2	MONDO:0005629	EFO:0007126
periodontal disorder	2	MONDO:0002635	MONDO:0002635
severe acute respiratory syndrome	2	MONDO:0005091	MONDO:0100096
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060

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

Clinical trials

Total trials: 233.

Phase distribution

Phase	Trials
Not specified	128
PHASE4	36
PHASE3	25
PHASE2	22
PHASE2/PHASE3	8
PHASE1	7
EARLY_PHASE1	4
PHASE1/PHASE2	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06045429	PHASE4	RECRUITING	Oral Care With 3% Hydrogen Peroxide (Oroxid®) in ICU - Effects on the Lower Airway Microbial Colonisation
NCT06598514	PHASE4	ACTIVE_NOT_RECRUITING	Chlorhexidine Lavage for Recurrent Urinary Tract Infection
NCT06633588	PHASE4	RECRUITING	Decolonization Efficacy of Polyhexanide vs. Mupirocin
NCT07048899	PHASE4	ENROLLING_BY_INVITATION	Irrisept in Emergency General Surgery Patients
NCT00198679	PHASE4	COMPLETED	Effect of Chlorhexidine Skin Cleansing on Skin Flora
NCT00248300	PHASE4	COMPLETED	A Peri-intubation Oral Intervention to Reduce Oral Flora and VAP
NCT00731042	PHASE4	COMPLETED	A Two-week Crossover Evaluation of Two Hand Antiseptic Products on Skin Condition in Healthy Human Subjects
NCT01115049	PHASE4	COMPLETED	Hexetidine and Chlorobutanol for Lesions Due to Prostheses
NCT01400308	PHASE4	TERMINATED	Effectiveness of Two Protocols for Corporal Decolonization in Patients Colonized by Methicillin Resistant Staphylococcus Aureus (MRSA)
NCT01841242	PHASE4	COMPLETED	Comparison of Alcoholic Chlorhexidine 2% Versus Alcoholic Povidone Iodine for Infections Prevention With Cardiac Resynchronization Therapy Device Implantation
NCT02018094	PHASE4	COMPLETED	The Amputation Surgical Site Infection Trial (ASSIT)
NCT02032394	PHASE4	UNKNOWN	Effect of Chlorhexidine on Bacteriuria
NCT02033187	PHASE4	COMPLETED	Daily Chlorhexidine Bathing and Infection Rates in Critically-ill Patients
NCT02062047	PHASE4	COMPLETED	Full-mouth and Partial-mouth Scaling and Root Planing in Type 2 Diabetic Subjects
NCT02124655	PHASE4	COMPLETED	Antiplaque Effect of Essential Oils and 0.2% Chlorhexidine on an in Situ Model of Oral Biofilm Growth.
NCT02150031	PHASE4	COMPLETED	Bacteraemia Secondary to Tooth Extraction: Chlorhexidine Prophylaxis Protocols
NCT02202304	PHASE4	WITHDRAWN	The Effects of Chlorhexidine/Thymol Varnish on Partial Denture Patient
NCT02267239	PHASE4	UNKNOWN	Methodology Antiseptic Application, Influence on Oral Biofilm.
NCT02279381	PHASE4	COMPLETED	Neonatal Package Study in Rural District of Pakistan
NCT02479347	PHASE4	COMPLETED	Wound Infections in Breast Cancer Surgery After Preoperative Skin Preparation With Chlorhexidine vs. Povidone-iodine
NCT02566928	PHASE4	UNKNOWN	Patient-Centered Comparative Effectiveness Research (CER) Study of Home-based Interventions to Prevent CA-MRSA Infection Recurrence
NCT02572791	PHASE4	COMPLETED	Staph Household Intervention for Eradication (SHINE)
NCT02911766	PHASE4	UNKNOWN	Efficacy of Different Chlorhexidine Concentrations
NCT02935322	PHASE4	COMPLETED	Interaction Between Chlorhexidine and Fluoride
NCT03142828	PHASE4	COMPLETED	Implant Healing Abutment and Chlorhexidine
NCT03412734	PHASE4	TERMINATED	Vaginal Preparation Prior to Hysterectomy
NCT03741894	PHASE4	UNKNOWN	Examination of the Prevention and Treatment Modalities of Alveolitis in Relation With Impacted Teeth Surgery
NCT03940729	PHASE4	COMPLETED	PWID; Longitudinal S Aureus Colonization Pattern and the Impact on Infection Frequency by Regular Showers With Chlorhexidine
NCT03962907	PHASE4	COMPLETED	Preoperative Decolonization and Surgical Site Infections in Orthopaedic Surgery - 2 Year Outcome in Prosthetic Surgery
NCT04171817	PHASE4	COMPLETED	Animal-Assisted Visitation Program Chlorhexidine Trial
NCT04218799	PHASE4	COMPLETED	Human Microbiome and Healthcare Associated Infections - Nursing Home Dwelling Older Veterans
NCT04223076	PHASE4	UNKNOWN	Clinical Effect of Chlorhexidine Mouthwash After Periodontal Surgery
NCT04376268	PHASE4	UNKNOWN	Comparison of the Efficacy of Boric Acid Mouthwashes in Different Concentrations
NCT04512638	PHASE4	UNKNOWN	Best Treatment Choice for Osteonecrosis of the Jaw
NCT05178823	PHASE4	COMPLETED	Short- and Long Term Antibacterial Effects of a Single Rinse With Different Mouthwashes: a Randomized Clinical Trial
NCT07270952	PHASE4	COMPLETED	Protocol Efficacy of Mouthwashes in Experimental Gingivitis
NCT04256798	PHASE3	RECRUITING	Perioperative Respiratory Care and Outcomes for Patients Undergoing High Risk Abdominal Surgery
NCT04575948	PHASE2/PHASE3	NOT_YET_RECRUITING	Anticariogenic Effect of Moringa Oleifera Mouthwash Compared to Chlorhexidine Mouthwash
NCT05532241	PHASE3	ACTIVE_NOT_RECRUITING	Dental Biofilm Control During Orthodontic Treatment
NCT06489431	PHASE3	ACTIVE_NOT_RECRUITING	Irrisept vs Traditional Antibiotic Irrigation for Virgin Penile Prosthesis Placement

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

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