Doxylamine

Summary

Doxylamine (CHEMBL1004) is an approved small-molecule histamine antagonist (ATC R06AA59); indicated across 1 condition including allergic disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R06AA59 (+1 more)
• Indications: 1 condition
• Clinical trials: 4
• Chemistry: 270.37 Da · C17H22N2O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1004
Name	Doxylamine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	3162
ChEBI	CHEBI:51380
ATC	R06AA59, R06AA09
Molecular formula	C17H22N2O
Molecular weight	270.37
InChIKey	HCFDWZZGGLSKEP-UHFFFAOYSA-N

SMILES: CC(C1=CC=CC=C1)(C2=CC=CC=N2)OCCN(C)C

IUPAC name: N,N-dimethyl-2-(1-phenyl-1-pyridin-2-ylethoxy)ethanamine

Pharmacological roles (ChEBI): histamine antagonist, cholinergic antagonist, sedative, antiemetic, H1-receptor antagonist, anti-allergic agent, antitussive.

Also known as: Doxilamina, Doxylamine, SID90340822, DOXYLAMINE, DOXYLAMINE SUCCINATE, doxylamine, rac-Doxylamine

Parent form; salt/anhydrous children: CHEMBL1200392

Patent coverage: 3,359 distinct patent families (12,263 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 12,260 (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: 1 (assay-derived). Sample: Muscarinic acetylcholine receptor M2.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
CHRM2	5.22	AC50	6042	nM	CHEMBL_ACT_25196112

Target pathways

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

Indications & clinical

Indications

1 indication (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
allergic disease	2	MONDO:0005271	MONDO:0005271

Clinical trials

Total trials: 4.

Phase distribution

Phase	Trials
Not specified	2
PHASE3	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00614445	PHASE3	COMPLETED	The Efficacy Of Diclectin® For Nausea And Vomiting Of Pregnancy
NCT06342778	PHASE1	COMPLETED	Pharmacokinetics and Bioequivalence of Doxylamine+Pyridoxine and Diclectin Under Fed Conditions in Healthy Volunteers
NCT05498233	Not specified	COMPLETED	Pharmacokinetics and Bioequivalence of Doxylamine + Pyridoxine, Film-coated, Enteric-soluble Tablets, and Diclectin, Delayed Release Tablets, in Healthy Volunteers
NCT06259747	Not specified	COMPLETED	Therapeutic Implications of Acutaping on Nausea and Vomiting During Pregnancy

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).