Alcaftadine

Summary

Alcaftadine (CHEMBL1201747) is an approved small-molecule H1-receptor antagonist (ATC S01GX11); indicated across 2 conditions including eye allergy and atopic conjunctivitis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: S01GX11
• Indications: 2 conditions
• Clinical trials: 4
• Chemistry: 307.4 Da · C19H21N3O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1201747
Name	Alcaftadine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	19371515
ChEBI	CHEBI:71023
ATC	S01GX11
Molecular formula	C19H21N3O
Molecular weight	307.4
InChIKey	MWTBKTRZPHJQLH-UHFFFAOYSA-N

SMILES: CN1CCC(=C2C3=CC=CC=C3CCN4C2=NC=C4C=O)CC1

IUPAC name: 11-(1-methylpiperidin-4-ylidene)-5,6-dihydroimidazo[2,1-b][3]benzazepine-3-carbaldehyde

ChEBI definition: An imidazobenzazepine that is 6,11-dihydro-5H-imidazo[2,1-b][3]benzazepine substituted at position 3 by a formyl group and at position 11 by a 1-methylpiperidin-4-ylidene group. An antihistamine used for treatment of allergic conjunctivitis.

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

Also known as: Alcaftadina, Alcaftadine, Lastacaft, R 89674, R-89674, ALCAFTADINE

Patent coverage: 163 distinct patent families (420 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 344 (82%) 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

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

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

Indications & clinical

Indications

2 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
eye allergy	4	MONDO:0005551	EFO:0005751
atopic conjunctivitis	4	MONDO:0005642	EFO:0007141

Clinical trials

Total trials: 4.

Phase distribution

Phase	Trials
PHASE4	3
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01470118	PHASE4	COMPLETED	A Study to Evaluate the Duration of LASTACAFT® in Acute Allergic Conjunctivitis
NCT01732757	PHASE4	COMPLETED	A Study to Evaluate the Efficacy of Lastacaft® Compared to Pataday™ and Placebo in Patients With Acute Allergic Conjunctivitis
NCT01808768	PHASE4	UNKNOWN	Ocular Allergy Treatment Practical Impact Trial
NCT00889330	PHASE3	COMPLETED	Safety and Efficacy Study of a Eye Drop for Eye Allergy

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).