Levocabastine

Summary

Levocabastine (CHEMBL1615438) is an approved small molecule (ATC R01AC02) targeting NTSR2; indicated across 4 conditions including eye allergy and seasonal allergic rhinitis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R01AC02 (+1 more)
• Targets: 1 (NTSR2)
• Indications: 4 conditions
• Clinical trials: 2
• Chemistry: 420.5 Da · C26H29FN2O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1615438
Name	Levocabastine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	54385
ATC	R01AC02, S01GX02
Molecular formula	C26H29FN2O2
Molecular weight	420.5
InChIKey	ZCGOMHNNNFPNMX-YHYDXASRSA-N

SMILES: C[C@@H]1CN(CC[C@@]1(C2=CC=CC=C2)C(=O)O)C3CCC(CC3)(C#N)C4=CC=C(C=C4)F

IUPAC name: (3S,4R)-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenylpiperidine-4-carboxylic acid

Also known as: Levocabastina, Levocabastine, Livostin direct, levocabastine, LEVOCABASTINE

Parent form; salt/anhydrous children: CHEMBL1237102

Patent coverage: 2,508 distinct patent families (10,790 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
NTSR2	NTS2 receptor	Full agonist	6.8	0.3%	O95665

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Neurotensin receptor type 2.

Bioactivity

ChEMBL activities: 2 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
Q63384	7.55	EC50	28	nM	CHEMBL_ACT_14734726
Q63384	7.48	Ki	33	nM	CHEMBL_ACT_14734774

Target pathways

Aggregated over 1 target gene(s): NTSR2.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
Peptide ligand-binding receptors	1	NTSR2
G alpha (q) signalling events	1	NTSR2

Dominant GO biological processes

GO term	Targets
cell surface receptor signaling pathway	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1
neuropeptide signaling pathway	1
sensory perception	1
regulation of membrane potential	1
signal transduction	1
G protein-coupled receptor signaling pathway	1

Indications & clinical

Indications

4 indications (2 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
eye allergy	4	MONDO:0005551	EFO:0005751
seasonal allergic rhinitis	2	MONDO:0005324	EFO:0003956
perennial allergic rhinitis	2	MONDO:0024332	EFO:1001417

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

Clinical trials

Total trials: 2.

Phase distribution

Phase	Trials
PHASE2	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01949051	PHASE2	COMPLETED	A Study to Assess Intranasal Repeat Dose Effect of Levocabastine in the Subjects With Allergic Rhinitis
NCT01957202	PHASE2	COMPLETED	A Proof of Concept Study to Assess Effect of Fluticasone Furoate (FF)/Levocabastine Fixed Dose Combination (FDC) Compared With Levocabastine and FF Alone in Subjects With Allergic Rhinitis (AR)

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

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

1 molecules share ≥1 primary target. Top 1 by shared-target count:

Molecule	Source	Status	Shared targets
REMINERTANT	ChEMBL	Phase 3	NTSR2