Bromhexine

Summary

Bromhexine (CHEMBL253376) is an approved small-molecule mucolytic (ATC R05CB02); indicated across 2 conditions including severe acute respiratory syndrome and malaria.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R05CB02
• Indications: 2 conditions
• Clinical trials: 6
• Chemistry: 376.13 Da · C14H20Br2N2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL253376
Name	Bromhexine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	2442
ChEBI	CHEBI:77032
ATC	R05CB02
Molecular formula	C14H20Br2N2
Molecular weight	376.13
InChIKey	OJGDCBLYJGHCIH-UHFFFAOYSA-N

SMILES: CN(CC1=C(C(=CC(=C1)Br)Br)N)C2CCCCC2

IUPAC name: 2,4-dibromo-6-[[cyclohexyl(methyl)amino]methyl]aniline

ChEBI definition: A substituted aniline that is 2,4-dibromoaniline which is substituted at position 6 by a [cyclohexyl(methyl)amino]methyl group. It is used (as the monohydrochloride salt) as a mucolytic for the treatment of respiratory disorders associated with productive cough (i.e. a cough characterised by the production of sputum).

Pharmacological roles (ChEBI): mucolytic.

Also known as: Bromhexina, Bromhexine, Fluibron, bromhexine, BROMHEXINE, SID174006813, BROMHEXINE HYDROCHLORIDE

Parent form; salt/anhydrous children: CHEMBL1319139

Patent coverage: 2,068 distinct patent families (6,504 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 6,433 (99%) 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: 10 (assay-derived). Sample: Androgen receptor, Sodium-dependent noradrenaline transporter, Sodium-dependent serotonin transporter, Sodium-dependent dopamine transporter, Voltage-gated inwardly rectifying potassium channel KCNH2, 3’,5’-cyclic-AMP phosphodiesterase 4A, Adenosine receptor A3, Sigma non-opioid intracellular receptor 1, Cytochrome P450 2D6, Bile salt export pump.

Bioactivity

ChEMBL activities: 6 potent at pChembl ≥ 5 of 13 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SIGMAR1	7.6	Ki	25	nM	CHEMBL_ACT_7607001
SIGMAR1	7.21	IC50	61	nM	CHEMBL_ACT_7607000
CYP2D6	6.71	IC50	195.8	nM	CHEMBL_ACT_7605511
SLC6A4	5.95	Ki	1111	nM	CHEMBL_ACT_7606999
SLC6A4	5.68	IC50	2091	nM	CHEMBL_ACT_7606998
AR	5.32	AC50	4747	nM	CHEMBL_ACT_25203454

Target pathways

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

Indications & clinical

Indications

2 indications (0 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
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
malaria	0	MONDO:0005136	EFO:0001068

Clinical trials

Total trials: 6.

Phase distribution

Phase	Trials
PHASE4	2
PHASE3	1
EARLY_PHASE1	1
PHASE1	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04405999	PHASE4	COMPLETED	Prevention of Infection and Incidence of COVID-19 in Medical Personnel Assisting Patients With New Coronavirus Disease
NCT05087381	PHASE4	COMPLETED	Randomized-controlled Trial of the Effectiveness of COVID-19 Early Treatment in Community
NCT04424134	PHASE3	UNKNOWN	BromhexIne And Spironolactone For CoronаVirUs Infection Requiring HospiTalization
NCT04672707	PHASE1	COMPLETED	Study on the Pharmacokinetics of Bromine Hexane Hydrochloride Tablets in Healthy Adults
NCT04340349	EARLY_PHASE1	UNKNOWN	Low-dose Hydroxychloroquine and Bromhexine: a Novel Regimen for COVID-19 Prophylaxis in Healthcare Professionals
NCT04273763	Not specified	UNKNOWN	Evaluating the Efficacy and Safety of Bromhexine Hydrochloride Tablets Combined With Standard Treatment/ Standard Treatment in Patients With Suspected and Mild Novel Coronavirus Pneumonia (COVID-19)

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

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