Epinastine: profile and news

Inspire acquires rights to Boehringer's epinastine Feb 22, 2006
...entered into an agreement with Boehringer Ingelheim to acquire certain exclusive rights to develop and market an intranasal dosage form of epinastine in the US ... - Pharmaceutical Business Review

Inspire Announces Development and License Agreement with ... Feb 21, 2006
Inspire will acquire certain exclusive rights to develop and market an intranasal dosage form of epinastine in the United States and Canada for the treatment ... - Genetic Engineering News,

Inspire buys US rights to allergy drug Feb 21, 2006
Inspire officials said Tuesday that the Durham-based pharmaceutical company will develop and license a form of epinastine to treat nasal allergies. ... - Raleigh Triangle Business Journal,

Inspire to Present at 26th Annual Cowen Health Care Conference Feb 28, 2006
Inspire's US specialty sales force promotes Elestat(R) (epinastine HCl ophthalmic solution) 0.05% and Restasis(R) (cyclosporine ophthalmic emulsion) 0.05 ... - Genetic Engineering News,

Inspire Reports Fourth Quarter and Full Year 2005 Financial ... Feb 28, 2006
Our recent development and licensing agreement for intranasal epinastine is an excellent example of our ability to expand our pipeline through the creation of ... - Genetic Engineering News,

Inspire Licenses Drug Development Deal With German Firm Feb 21, 2006
...conditions. Inspire wants to develop an intranasal dosage form of epinastine, the active drug substance it is licensing. Inspire ... - Local Tech Wire,

Inspire buys rights to nasal spray Feb 22, 2006
Inspire Pharmaceuticals bought the rights to develop and market a nasal spray of epinastine, an allergy drug made by German-based Boehringer Ingelheim ... - News & Observer,

Other information

Indication
For the prevention of itching associated with allergic conjunctivitis.

Pharmacology
Epinastine is an antihistamine and an inhibitor of histamine release from the mast cell for topical administration to the eyes. Epinastine is indicated for the prevention of itching associated with allergic conjunctivitis. Epinastine is a topically active, direct H₁-receptor antagonist and an inhibitor of the release of histamine from the mast cell. Epinastine is selective for the histamine H₁-receptor and has affinity for the histamine H2 receptor. Epinastine also possesses affinity for the a1-, a2-, and 5-HT₂ -receptors. Epinastine does not penetrate the blood/brain barrier and, therefore, is not expected to induce side effects of the central nervous system.

Mechanism Of Action
Epinastine has a multiaction effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H₂-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response.

Drug Category
Antihistamines; Ophthalmics; ATC:R06AX24; ATC:S01GX10

Brand Names/Synonyms
CHEMBANK1621; Elestat; Epinastina [Spanish]; Epinastine; Epinastine [Inn]; Epinastinum [Latin]; WAL 801

Dosage Forms
Not Available

Absorption
The absolute bioavailability of epinastine is about 40%.

Interactions
Interactions for Epinastine:

None Reported

Chemical IUPAC Name
Not Available

Chemical Formula
C16H15N3

Half Life
12 hours

Drug Type
Approved Drug

# Accession No
APRD00043

CAS Registry Number
80012-43-7