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Clinical data | |
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Trade names | Bepreve |
AHFS/Drugs.com | International Drug Names |
MedlinePlus | a610012 |
Routes of administration | Oral, eye drops |
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Pharmacokinetic data | |
Bioavailability | High (oral) Minimal (topical) |
Protein binding | ~55% |
Excretion | Renal (75–85 |
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Chemical and physical data | |
Formula | C21H25ClN2O3 |
Molar mass | 388.89 g·mol−1 |
3D model (JSmol) | |
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Bepotastine (Talion, Bepreve) is a 2nd generation antihistamine. [1] It was approved in Japan for use in the treatment of allergic rhinitis and urticaria/pruritus in July 2000, and January 2002, respectively. It is marketed in the United States as an eye drop under the brand name Bepreve, by ISTA Pharmaceuticals, a subsidiary of Bausch + Lomb.[ citation needed ]
Bepotastine is available as an ophthalmic solution and oral tablet. It is a direct H1-receptor antagonist that inhibits the release of histamine from mast cells. [2] The ophthalmic formulation has shown minimal systemic absorption, between 1 and 1.5% in healthy adults. [3] Common side effects are eye irritation, headache, unpleasant taste, and nasopharyngitis. [3] The main route of elimination is urinary excretion, 75-90% excreted unchanged. [3]
It is marketed in Japan by Tanabe Seiyaku under the brand name Talion. Talion was co-developed by Tanabe Seiyaku and Ube Industries, the latter of which discovered bepotastine. In 2001, Tanabe Seiyaku granted Senju, now owned by Allergan, exclusive worldwide rights, with the exception of certain Asian countries, to develop, manufacture and market bepotastine for ophthalmic use. Senju, in turn, has granted the United States rights for the ophthalmic preparation to ISTA Pharmaceuticals.
In 2011, ISTA pharmaceuticals experienced a 2.4% increase in net revenues from 2010, which was driven by the sales of Bepreve. Their net revenue for 2011 was $160.3 million. [4] ISTA Pharmaceuticals was acquired by Bausch & Lomb in March 2012 for $500 million. [5] Bausch & Lomb hold the patent for bepotastine besilate (https://www.accessdata.fda.gov/scripts/cder/ob/docs/temptn.cfm. On November 26, 2014, Bausch & Lomb sued Micro Labs USA for patent infringement. [6] Bausch & Lomb was recently bought out by Valeant Pharmaceuticals in May 2013 for $8.57 billion, Valeant's largest acquisition to date, causing the company's stock to rise 25% when the deal was announced. [7]
A Phase III clinical trial was carried out in 2010 to evaluate the effectiveness of bepotastine besilate ophthalmic solutions 1.0% and 1.5%. [8] These solutions were compared to a placebo and evaluated for their ability to reduce ocular itchiness. The study was carried out with 130 individuals and evaluated after 15 minutes, 8 hours, or 16 hours. There was a reduction in itchiness at all-time points for both ophthalmic solutions. The study concluded that bepotastine besilate ophthalmic formulations reduced ocular itchiness for at least 8 hours after dosing compared to placebo. Phase I and II trials were carried out in Japan.
Studies have been performed in animals and bepotastine besilate was not found to be teratogenic in rats during fetal development, even at 3,300 times more than typical use in humans. [3] Evidence of infertility was seen in rats at 33,000 times the typical ocular dose in humans. [3] The safety and efficacy has not been established in patients under 2 years of age and has been extrapolated from adults for patients under 10 years of age. [3]
Bausch + Lomb is an American-Canadian eye health products company based in Vaughan, Ontario, Canada. It is one of the world's largest suppliers of contact lenses, lens care products, pharmaceuticals, intraocular lenses, and other eye surgery products. The company was founded in Rochester, New York, in 1853 by optician John Bausch and cabinet maker turned financial backer Henry Lomb. Until its sale in 2013, Bausch + Lomb was one of the oldest continually operating companies in the United States.
Fexofenadine, sold under the brand name Allegra among others, is an antihistamine pharmaceutical drug used in the treatment of allergy symptoms, such as hay fever and urticaria.
Allergic conjunctivitis (AC) is inflammation of the conjunctiva due to allergy. Although allergens differ among patients, the most common cause is hay fever. Symptoms consist of redness, edema (swelling) of the conjunctiva, itching, and increased lacrimation. If this is combined with rhinitis, the condition is termed allergic rhinoconjunctivitis (ARC).
Olopatadine, sold under the brand name Opatanol among others, is a medication used to decrease the symptoms of allergic conjunctivitis and allergic rhinitis. It is used as eye drops or as a nasal spray. The eye drops generally result in an improvement within half an hour.
Bausch Health Companies Inc. is an American-Canadian domiciled multinational specialty pharmaceutical company based in Laval, Quebec, Canada. It develops, manufactures and markets pharmaceutical products and branded generic drugs, primarily for skin diseases, gastrointestinal disorders, eye health and neurology. Bausch Health owns Bausch & Lomb, a supplier of eye health products.
Dorzolamide/timolol, sold under the brand name Cosopt among others, is a medication used to treat high pressure inside the eye including glaucoma. It is a combination of dorzolamide hydrochloride and timolol maleate. It may be used when a beta blocker, like timolol, is not sufficient alone. It is used as an eye drop.
Brimonidine is an α2 agonist medication used to treat open-angle glaucoma, ocular hypertension, and rosacea. In rosacea it improves the redness. It is used as eye drops or applied to the skin.
Azelastine, sold under the brand name Optivar among others, is a H1 receptor-blocking medication primarily used as a nasal spray to treat allergic rhinitis (hay fever) and as eye drops for allergic conjunctivitis. Other uses may include asthma and skin rashes for which it is taken by mouth. Onset of effects is within minutes when used in the eyes and within an hour when used in the nose. Effects last for up to 12 hours.
Loteprednol is a topical corticosteroid used to treat inflammations of the eye. It is marketed by Bausch and Lomb as Lotemax and Loterex.
Clocortolone (Cloderm) is a topical steroid. It is used in the form of an ester, clocortolone pivalate, and applied as a cream. It is used for the treatment of dermatitis and is considered a medium-strength corticosteroid. It is unusual among steroids in that it contains a chlorine atom and a fluorine atom.
Ebastine is a H1 antihistamine with low potential for causing drowsiness.
Nicox S.A. is a French ophthalmology company developing treatments to maintain vision and improve ocular health. Nicox is headquartered in Sophia Antipolis, France, and its Chairman and CEO is Michele Garufi.
Bromfenac is a nonsteroidal anti-inflammatory drug (NSAID) marketed in the US as an ophthalmic solution by ISTA Pharmaceuticals for short-term, local use. Prolensa and Bromday are the once-daily formulation of bromfenac, while Xibrom was approved for twice-daily administration. In the European Union, the brand name is Yellox. Bromfenac is indicated for the treatment of ocular inflammation and pain after cataract surgery.
Besifloxacin (INN/USAN) is a fourth-generation fluoroquinolone antibiotic. The marketed compound is besifloxacin hydrochloride. It was developed by SSP Co. Ltd., Japan, and designated SS734. SSP licensed U.S. and European rights to SS734 for ophthalmic use to InSite Vision Incorporated in 2000. InSite Vision developed an eye drop formulation (ISV-403) and conducted preliminary clinical trials before selling the product and all rights to Bausch & Lomb in 2003.
ISTA Pharmaceuticals, Inc, was a US-based pharmaceutical company that specialized in ophthalmic pharmaceutical products and discovers, develops, and markets therapies for inflammation, ocular pain, glaucoma, allergy, and dry eye. ISTA was acquired by Bausch & Lomb, an eye care company, on March 26, 2012. Under the deal, Bausch & Lomb have agreed to pay $9.10 per share for ISTA, bringing the total value of the acquisition to $500 million. In 2012, Valeant Pharmaceuticals withdrew its $360 million offer.
Mapracorat is an anti-inflammatory drug belonging to the experimental class of selective glucocorticoid receptor agonists (SEGRAs). It is in clinical trials for the topical treatment of atopic dermatitis, inflammation following cataract surgery, and allergic conjunctivitis. Preliminary investigation for the treatment of keratoconjunctivitis sicca has been conducted in cellular models.
Alimera Sciences, Inc. is a biopharmaceutical company based in Alpharetta, Georgia that specializes in the commercialization and development of prescription ophthalmic pharmaceuticals. The company's main focus is on diseases affecting the back of the eye, or retina. Its main product is Iluvien, a fluocinolone acetonide intravitreal implant.
Alcaftadine is used to prevent eye irritation brought on by allergic conjunctivitis. It is a H1 histamine receptor antagonist.
Bilastine is an antihistamine medication used to treat hives (urticaria), allergic rhinitis and itchy inflamed eyes (allergic conjunctivitis) caused by an allergy. It is a second-generation antihistamine and takes effect by selectively inhibiting the histamine H1 receptor, preventing these allergic reactions. Bilastine has an effectiveness similar to cetirizine, fexofenadine, and desloratadine.
Lifitegrast, sold under the brand name Xiidra, is a medication for the treatment of signs and symptoms of dry eye, a syndrome called keratoconjunctivitis sicca. Lifitegrast reduces inflammation by inhibiting inflammatory cell binding. It is often used in conjunction with ciclosporin for dry eye treatment including meibomian gland dysfunction and inflammatory dry eye.