Acrivastine

Summary

Acrivastine (CHEMBL1224) is an approved small-molecule H1-receptor antagonist (ATC R06AX18); indicated across 1 condition including allergic disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R06AX18
• Indications: 1 condition
• Chemistry: 348.4 Da · C22H24N2O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1224
Name	Acrivastine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	5284514
ChEBI	CHEBI:83168
ATC	R06AX18
Molecular formula	C22H24N2O2
Molecular weight	348.4
InChIKey	PWACSDKDOHSSQD-IUTFFREVSA-N

SMILES: CC1=CC=C(C=C1)/C(=C\CN2CCCC2)/C3=CC=CC(=N3)/C=C/C(=O)O

IUPAC name: (E)-3-[6-[(E)-1-(4-methylphenyl)-3-pyrrolidin-1-ylprop-1-enyl]-2-pyridinyl]prop-2-enoic acid

ChEBI definition: A member of the class of pyridines that is (pyridin-2-yl)acrylic acid substituted at position 6 by a [(1E)-1-(4-methylphenyl)-3-(pyrrolidin-1-yl)prop-1-en-1-yl group. It is a non-sedating antihistamine used for treatment of hayfever, urticaria, and rhinitis.

Pharmacological roles (ChEBI): H1-receptor antagonist.

Also known as: Acrivastina, Acrivastine, Acrivastine component of semprex-d, Benadryl allgy relief plus decongest, BW 825C, BW-825C, Semprex, ACRIVASTINE, SID144206566, acrivastine

Patent coverage: 2,854 distinct patent families (11,124 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 11,071 (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: 7 (assay-derived). Sample: Sodium-dependent serotonin transporter, Alpha-1A adrenergic receptor, Prostaglandin G/H synthase 2, Histamine H1 receptor, Kappa-type opioid receptor, Histamine H1 receptor, Prostaglandin G/H synthase 1.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 9 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HRH1	7.7	Ki	19.95	nM	CHEMBL_ACT_29118531
HRH1	6.9	Kd	125.9	nM	CHEMBL_ACT_29118597
HRH1	6.77	AC50	170	nM	CHEMBL_ACT_25212307
ADRA1A	6.15	AC50	710	nM	CHEMBL_ACT_25217925
SLC6A4	5.64	AC50	2300	nM	CHEMBL_ACT_25150138
Q63921	5.38	AC50	4200	nM	CHEMBL_ACT_25174200
P31389	5.21	IC50	6120	nM	CHEMBL_ACT_12479900

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: 0.

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).