Betahistine

Summary

Betahistine (CHEMBL24441) is an approved small-molecule vasodilator agent (ATC N07CA01); indicated across 5 conditions including obesity disorder and meniere disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N07CA01
• Indications: 5 conditions
• Clinical trials: 8
• Chemistry: 136.19 Da · C8H12N2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL24441
Name	Betahistine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	2366
ChEBI	CHEBI:35677
ATC	N07CA01
Molecular formula	C8H12N2
Molecular weight	136.19
InChIKey	UUQMNUMQCIQDMZ-UHFFFAOYSA-N

SMILES: CNCCC1=CC=CC=N1

IUPAC name: N-methyl-2-pyridin-2-ylethanamine

ChEBI definition: An aminoalkylpyridine that is pyridine substituted by a 2-(methylamino)ethyl group at position 2. It acts as a histamine agonist and a vasodilator, and is thought to improve the microcirculation of the labyrinth, resulting in reduced endolymphatic pressure. It is used (generally as the hydrochloride or mesylate salt) to reduce the symptoms of vertigo, tinnitus, and hearing loss associated with Ménière’s disease.

Pharmacological roles (ChEBI): vasodilator agent, H1-receptor agonist.

Also known as: Betahistina, Betahistine, Histalean, Vestibo, betahistine, BETAHISTINE

Parent form; salt/anhydrous children: CHEMBL1446813, CHEMBL1451277, CHEMBL1464589, CHEMBL4303472

Patent coverage: 1,658 distinct patent families (4,936 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 4,897 (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: 2 (assay-derived). Sample: Histamine H3 receptor, Histamine H3 receptor.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
Q9QYN8	5.69	Ki	2030	nM	CHEMBL_ACT_2625432

Target pathways

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

Indications & clinical

Indications

5 indications (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
obesity disorder	2	MONDO:0011122	EFO:0001073
Meniere disease	1	MONDO:0007972	EFO:0006862

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

Clinical trials

Total trials: 8.

Phase distribution

Phase	Trials
PHASE2	4
Not specified	2
PHASE1/PHASE2	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06001593	PHASE1/PHASE2	RECRUITING	Modulating Auditory Symptoms and Vertigo of Meniere’s Disease by Non-invasive Mastoid Electric Stimulation
NCT00409305	PHASE2	COMPLETED	The Effect of Betahistine on Body Weight in Obese Subjects
NCT00428168	PHASE2	TERMINATED	Study to Examine the Effect of Betahistine on Body Weight Gain Due to Olanzapine Treatment
NCT00466869	PHASE2	TERMINATED	A Randomized, Double-Blind, Placebo-Controlled Study to Examine the Effect of Betahistine on Plasma Lipids in Patients Treated With Simvastatin
NCT00709202	PHASE2	COMPLETED	Efficacy and Tolerability Study of Betahistine to Ameliorate Antipsychotic Associated Weight Gain
NCT00852956	PHASE1	COMPLETED	Evaluation of Safety, Drug-Drug Interactions and Pharmacokinetic Profiles of Co-Administration of Betahistine With Olanzapine in Healthy Female Subjects
NCT03624283	Not specified	UNKNOWN	Interventions for Residual Dizziness After Successful Repositioning Maneuvers in Patients With BPPV
NCT05309538	Not specified	COMPLETED	Paroxysmal Positional Vertigo & Repositioning Maneuvers

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).