levocabastine

Trade name: livostin

Small moleculeapproved

Approved

Nov 10, 1993

Levocabastine (trade name Livo) is a selective second-generation H1-receptor antagonist used for allergic conjunctivitis. Levocabastine binds the G protein-coupled neurotensin receptor 2 (NTR2), but not NTR1, where it behaves as a weak partial inverse agonist. In an environmental study, LIVOSTIN 0.05% (levocabastine hydrochloride ophthalmic suspension) instilled four times daily was shown to be significantly more effective than its vehicle in reducing ocular itching associated with seasonal allergic conjunctivitis. After instillation in the eye, levocabastine is systemically absorbed. However, the amount of systemically absorbed levocabastine after therapeutic ocular doses is low (mean plasma concentrations in the range of 1-2 ng/mL). Brand name Livostin is no longer available in the U.S., but generic versions may still be available. Common side effects include burning, stinging, itching, or watering of the eyes, eye irritation or discomfort, blurred vision, dry or puffy eyes, headache, nosebleed, nausea, or fatigue. — NCATS

Clinical trial activity

5 trials · 5 clinical orgs · 1 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Oct 1, 2013 (NCT01949051)

Timeline

1990s

Nov 10, 1993
Novartis — Earliest FDA Approval
Nov 10, 1993
Novartis — NDA Organization
Nov 10, 1993
Novartis — NDA Secondary Org

2010s

Jan 1, 2013
Earliest Phase 1 Sponsor(trial)
Jan 1, 2013
Earliest Phase 2 Sponsor(trial)
Jan 1, 2015
Earliest Phase 3 Sponsor(trial)

Indications

Approved for

Conjunctivitis, Allergic (approved 1993)

Studied for

Mechanism of action

Histamine H1 receptorANTAGONIST
HRH1 antagonist
- Histamine H1 receptor (HRH1) ↗

Approval history

approvedPriority reviewNov 10, 1993

Chemistry & pharmacology

Loading structure…

SMILES

C[C@@H]1CN([C@H]2CC[C@](C#N)(c3ccc(F)cc3)CC2)CC[C@]1(C(=O)O)c1ccccc1

Mol. weight: 420.53 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Single Stereoisomer
Inorganic: No
Polymer: No
Delivery: Topical
Availability: Discontinued

Oral

Parenteral

Topical

Yes

Sources

Also known as

1-(4-cyano-4-(4-fluorophenyl)cyclohexyl)-3-methyl-4-phenyl-4-piperidinecarboxylic acid
bilina
chauvin brand of levocabastine hydrochloride
ciba vision brand of levocabastine hydrochloride
esteve brand of levocabastine hydrochloride
iolab brand of levocabastine hydrochloride
janssen brand of levocabastine hydrochloride
levocabastin
levocabastin
levocabastina
levocabastina
levocabastine
levocabastine
levocabastine
levocabastine
levocabastine
levocabastine
levocabastine
levocabastine
levocabastine
levocabastine
levocabastine hcl
levocabastine hcl
levocabastine hcl
levocabastine hydrochloride
levocabastine hydrochloride
levocabastine hydrochloride
levocabastine hydrochloride
levocabastine hydrochloride
levocabastinum
levocabastinum
levophta
levophta
lévophta
livocab
livostin
livostin
livostin
livostin
livostin
livostin
livostin
livostin direct
r-50547
r-50547
taxandria brand of levocabastine hydrochloride
winzer brand of levocabastine hydrochloride

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT04002349	N/A	Jul 1, 2019	Beijing Institute of Otolaryngology, Capital Medical University, Johnson and Johnson
NCT02498509	Phase 3	May 1, 2015	Chong Kun Dang Pharmaceutical
NCT01962467	Phase 1	Oct 11, 2013	GlaxoSmithKline
NCT01949051	Phase 2	Oct 1, 2013	GlaxoSmithKline
NCT01957202	Phase 2	Oct 1, 2013	GlaxoSmithKline

Showing 5 of 5 trials

Page 1 / 1

Organizations

Research & Development (5)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
GlaxoSmithKline	For profit	3	3	2	2013
Beijing Institute of Otolaryngology	Academic/Hospital	1	0	1	2019
Capital Medical University	Academic/Hospital	1	1	1	2019
Chong Kun Dang Pharmaceutical	For profit	1	1	1	2015
Johnson and Johnson	For profit	1	0	1	2019

5 organizations

Page 1 / 1

Marketing (2)

Organization	Org type	Relationship	Date
Novartis	For profit	NDA	Nov 10, 1993
Novartis	For profit	NDA2	Nov 10, 1993