Brompheniramine

Summary

Brompheniramine (CHEMBL811) is an approved small-molecule H1-receptor antagonist (ATC R06AB51); indicated across 1 condition including allergic disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R06AB51 (+1 more)
• Indications: 1 condition
• Clinical trials: 2
• Chemistry: 319.24 Da · C16H19BrN2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL811
Name	Brompheniramine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	6834
ChEBI	CHEBI:3183
ATC	R06AB51, R06AB01
Molecular formula	C16H19BrN2
Molecular weight	319.24
InChIKey	ZDIGNSYAACHWNL-UHFFFAOYSA-N

SMILES: CN(C)CCC(C1=CC=C(C=C1)Br)C2=CC=CC=N2

IUPAC name: 3-(4-bromophenyl)-N,N-dimethyl-3-pyridin-2-ylpropan-1-amine

ChEBI definition: Pheniramine in which the hydrogen at position 4 of the phenyl substituent is substituted by bromine. A histamine H1 receptor antagonist, brompheniramine is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.

Pharmacological roles (ChEBI): H1-receptor antagonist, anti-allergic agent.

Also known as: Bpn, Bromfeniramina, Brompheniramine, Brotane, Bromfed, Bromfenex, Dimetapp, Lodrane, SID90341200, brompheniramine, BROMPHENIRAMINE, BROMPHENIRAMINE MALEATE

Parent form; salt/anhydrous children: CHEMBL1200961

Patent coverage: 3,115 distinct patent families (11,547 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 11,522 (100%) 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: 13 (assay-derived). Sample: D(1A) dopamine receptor, Sodium channel alpha subunits; brain (Types I, II, III), Muscarinic acetylcholine receptor M2, Muscarinic acetylcholine receptor M1, Sodium-dependent noradrenaline transporter, 5-hydroxytryptamine receptor 2C, Sodium-dependent serotonin transporter, Histamine H1 receptor, Sodium-dependent dopamine transporter, Voltage-gated inwardly rectifying potassium channel KCNH2.

Bioactivity

ChEMBL activities: 12 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
SLC6A4	7.82	AC50	15	nM	CHEMBL_ACT_25149822
SLC6A4	7.46	AC50	34.6	nM	CHEMBL_ACT_25151026
HRH1	7.28	AC50	52	nM	CHEMBL_ACT_25211979
P31652	6.52	IC50	300	nM	CHEMBL_ACT_115195
KCNH2	6.05	IC50	891.2	nM	CHEMBL_ACT_5219004
SLC6A3	5.76	AC50	1732	nM	CHEMBL_ACT_25124658
SLC6A3	5.68	AC50	2100	nM	CHEMBL_ACT_25123428
KCNH2	5.4	AC50	4000	nM	CHEMBL_ACT_25117074
SLC6A2	5.25	AC50	5640	nM	CHEMBL_ACT_25145699
HRH3	5.11	AC50	7800	nM	CHEMBL_ACT_25200165
CHRM2	5.1	AC50	7947	nM	CHEMBL_ACT_25195435
SLC6A2	5.01	AC50	9700	nM	CHEMBL_ACT_25144486

Target pathways

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

Indications & clinical

Indications

1 indication (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
allergic disease	4	MONDO:0005271	MONDO:0005271

Clinical trials

Total trials: 2.

Phase distribution

Phase	Trials
PHASE3	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01393548	PHASE3	COMPLETED	Efficacy and Safety of Combination of Brompheniramine and Phenylephrine for the Symptoms Relief of Rhinitis
NCT00894634	PHASE1	COMPLETED	Study Evaluating Brompheniramine Maleate Liquid in Children and Adolescents

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).