Clinical data | |
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Trade names | Nevanac, Ilevro, Amnac, others |
AHFS/ Drugs.com | Monograph |
MedlinePlus | a606007 |
License data | |
Pregnancy category |
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Routes of administration | Topical eye drops |
ATC code | |
Legal status | |
Legal status | |
Identifiers | |
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CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard ( EPA) | |
ECHA InfoCard | 100.207.414 |
Chemical and physical data | |
Formula | C15H14N2O2 |
Molar mass | 254.289 g·mol−1 |
3D model ( JSmol) | |
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(what is this?) (verify) |
Nepafenac, sold under the brand name Nevanac among others, is a nonsteroidal anti-inflammatory drug (NSAID), usually sold as a prescription eye drop 0.1% solution (Nevanac) or 0.3% solution (Ilevro). It is used to treat pain and inflammation associated with cataract surgery. [3] Nepafenac is a prodrug of amfenac, an inhibitor of COX-1 and COX-2 activity. [4] [5]
Nepafenac is indicated for use in the treatment of pain and inflammation following cataract surgery. [3] [6] [7] [8]
In the European Union nepafenac is also indicated for the reduction in the risk of postoperative macular edema associated with cataract surgery in people with diabetes. [8]
Nepafenac is an NSAID, thought to be a prodrug of amfenac after conversion by ocular tissue hydrolases after penetration via the cornea. [6] [7] Amfenac, like other NSAIDs, is thought to inhibit cyclooxygenase action. [6] [7]
Side effects include headache; runny nose; pain or pressure in the face; nausea; vomiting; and dry, itchy, sticky eyes. [9] Serious side effects include red or bloody eyes; foreign body sensation in the eye; sensitivity to light; decreased visual acuity; seeing specks or spots; teary eyes; or eye discharge or crusting. [9]
On February 25, 2005, Alcon filed a New Drug Application (NDA) with the U.S. Food and Drug Administration (FDA) for Nevanac 0.1%. [10] Results from the two trials referenced in the NDA (Phase 2/3 study C-02-53; Phase 3 study C-03-32) have not been published. [11] Study C-02-53 consisted of 228 patients across 10 centers in the United States. [12] Study C-03-32 consisted of 522 patients across 22 centers in the United States. [12] The efficacy results presented were confirmed in a study published in 2007. [13]
Nevanac was approved by the FDA on August 19, 2005, with application number 021–862. [14]
An NDA for Ilevro was filed on December 15, 2011. [15] In a one-month study, no new toxicities arose in the new formulation of nepafenac. [16] Safety and efficacy information was derived from the previous Nevanac application. [16] In June 2010, a confirmatory study began (Study C09055) consisting of over 2000 patients from 49 US sites and 37 European sites. [17] [18] A second phase 3 trial (Study C11003) was conducted in a population of 1,342 patients at 37 sites across the United States which failed to demonstrate superiority over Nevanac in an altered dosing regimen. [17]
Ilevro was approved by the FDA on October 16, 2012, with application number 203–491. [19]
Both Nevanac and Ilevro are manufactured and sold by Alcon, Inc. [6] [7] Alcon is currently a division of Novartis International AG, which is primarily based out of Switzerland. [20] Alcon, Inc. also holds locations in both Switzerland and the United States. [21] The company has gone through several name changes, from Alcon Laboratories, Inc. to Alcon Universal, Ltd., to Alcon, Inc. [21]
Nevanac entered the market in 2005 as a product of Alcon, at the time a subsidiary of Nestlé. [22] On April 6, 2008, Novartis agreed to purchase approximately 74 million shares of Alcon from Nestlé at $143.18 per share. [22] On January 4, 2010, Novartis agreed to purchase all remaining shares of Alcon from Nestlé, totalling 156 million shares or 77% of the shares in the company. [22] At the time of the purchase, a proposal for a merger under Swiss merger law was given to the Alcon board of directors. [22] The merger was agreed upon on December 15, 2010, making Alcon "the second largest division within Novartis." [22] The merger was completed on April 8, 2011. [23]
Ilevro was launched by Alcon on January 21, 2013. [24] In 2014 and 2015, net sales by Alcon grew, contributed to in part by the increased volume in sales of Ilevro. [25] [26] [27] That financial year, Novartis reported $18 billion in total financial debt. [25] That figure has grown steadily since. In 2016, Novartis reported a total debt of $23.8 billion, [28] up from the $21.9 billion reported in 2015 [27] and the $20.4 billion reported in 2014. [26] As of May 2017, Novartis is estimated to be worth $193.2 billion. [29]
On January 27, 2016, Alcon was moved to become a branch of the Innovative Medicines Division at Novartis. [28] Early in 2016, Alcon formed agreements with both TrueVision and PowerVision, and acquired Transcend Medical. [28] As of January 2017, Novartis is weighing options for Alcon in the business structure. [28]
Alcon faced declining growth in 2016, having faced challenges in development and marketing of new products. [28]
Novartis maintains a detailing unit geared toward health professionals consisting of over 3,000 employees within the United States and an additional 21,000 worldwide. [28] Novartis is also seeking to expand direct-to-consumer advertising and entrance into specialty product markets. [28] Novartis also notes the influence of position and preference on US Centers for Medicare & Medicaid formularies in expanding their market value. [28]
Nepafenac, Nevanac, and Ilevro are all absent from the 2016 Annual Report issued from Novartis. [28]
There are currently[ when?] seven U.S. patents filed that are directly associated with the modernized formulations of nepafenac, all stemming from Novartis. [30] There are three patents associated with Nevanac that are still[ when?] active [31] and four associated with Ilevro. [32] The earliest patent related to the modern formulations of nepafenac was approved on June 11, 2002, after being filed in 1999, by Bahram Asgharian. [33] A patent was filed by Warren Wong, associated with Alcon, Inc. based out of Fort Worth, Texas, on December 2, 2005, for aqueous suspensions of nepafenac. [34] Another patent for a nepafenac-based drug was filed on May 8, 2006, by Geoffrey Owen, Amy Brooks, and Gustav Graff. [35] A patent was filed by Masood A. Chowhan and Huagang Chen on February 9, 2007, and approved on May 24, 2011, [36] followed closely by a patent filed by Warren Wong on September 23, 2010, and approved on December 6, 2011. [37] Masood A. Chowhan, Malay Ghosh, Bahram Asgharian, and Wesley Wehsin Han filed another patent on December 1, 2010, and approved on December 30, 2014. [38] The most recent[ when?] patent was filed by Masood A. Chowhan, Malay Ghosh, Bahram Asgharian, and Wesley Weshin Han on November 12, 2014, and approved on May 30, 2017. [39] These patents are in effect until dates ranging between July 17, 2018, and March 31, 2032. [32]
Novartis also maintains patents on nepafenac in 26 countries outside the United States. [40]
Clinical data | |
---|---|
Trade names | Nevanac, Ilevro, Amnac, others |
AHFS/ Drugs.com | Monograph |
MedlinePlus | a606007 |
License data | |
Pregnancy category |
|
Routes of administration | Topical eye drops |
ATC code | |
Legal status | |
Legal status | |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard ( EPA) | |
ECHA InfoCard | 100.207.414 |
Chemical and physical data | |
Formula | C15H14N2O2 |
Molar mass | 254.289 g·mol−1 |
3D model ( JSmol) | |
| |
| |
(what is this?) (verify) |
Nepafenac, sold under the brand name Nevanac among others, is a nonsteroidal anti-inflammatory drug (NSAID), usually sold as a prescription eye drop 0.1% solution (Nevanac) or 0.3% solution (Ilevro). It is used to treat pain and inflammation associated with cataract surgery. [3] Nepafenac is a prodrug of amfenac, an inhibitor of COX-1 and COX-2 activity. [4] [5]
Nepafenac is indicated for use in the treatment of pain and inflammation following cataract surgery. [3] [6] [7] [8]
In the European Union nepafenac is also indicated for the reduction in the risk of postoperative macular edema associated with cataract surgery in people with diabetes. [8]
Nepafenac is an NSAID, thought to be a prodrug of amfenac after conversion by ocular tissue hydrolases after penetration via the cornea. [6] [7] Amfenac, like other NSAIDs, is thought to inhibit cyclooxygenase action. [6] [7]
Side effects include headache; runny nose; pain or pressure in the face; nausea; vomiting; and dry, itchy, sticky eyes. [9] Serious side effects include red or bloody eyes; foreign body sensation in the eye; sensitivity to light; decreased visual acuity; seeing specks or spots; teary eyes; or eye discharge or crusting. [9]
On February 25, 2005, Alcon filed a New Drug Application (NDA) with the U.S. Food and Drug Administration (FDA) for Nevanac 0.1%. [10] Results from the two trials referenced in the NDA (Phase 2/3 study C-02-53; Phase 3 study C-03-32) have not been published. [11] Study C-02-53 consisted of 228 patients across 10 centers in the United States. [12] Study C-03-32 consisted of 522 patients across 22 centers in the United States. [12] The efficacy results presented were confirmed in a study published in 2007. [13]
Nevanac was approved by the FDA on August 19, 2005, with application number 021–862. [14]
An NDA for Ilevro was filed on December 15, 2011. [15] In a one-month study, no new toxicities arose in the new formulation of nepafenac. [16] Safety and efficacy information was derived from the previous Nevanac application. [16] In June 2010, a confirmatory study began (Study C09055) consisting of over 2000 patients from 49 US sites and 37 European sites. [17] [18] A second phase 3 trial (Study C11003) was conducted in a population of 1,342 patients at 37 sites across the United States which failed to demonstrate superiority over Nevanac in an altered dosing regimen. [17]
Ilevro was approved by the FDA on October 16, 2012, with application number 203–491. [19]
Both Nevanac and Ilevro are manufactured and sold by Alcon, Inc. [6] [7] Alcon is currently a division of Novartis International AG, which is primarily based out of Switzerland. [20] Alcon, Inc. also holds locations in both Switzerland and the United States. [21] The company has gone through several name changes, from Alcon Laboratories, Inc. to Alcon Universal, Ltd., to Alcon, Inc. [21]
Nevanac entered the market in 2005 as a product of Alcon, at the time a subsidiary of Nestlé. [22] On April 6, 2008, Novartis agreed to purchase approximately 74 million shares of Alcon from Nestlé at $143.18 per share. [22] On January 4, 2010, Novartis agreed to purchase all remaining shares of Alcon from Nestlé, totalling 156 million shares or 77% of the shares in the company. [22] At the time of the purchase, a proposal for a merger under Swiss merger law was given to the Alcon board of directors. [22] The merger was agreed upon on December 15, 2010, making Alcon "the second largest division within Novartis." [22] The merger was completed on April 8, 2011. [23]
Ilevro was launched by Alcon on January 21, 2013. [24] In 2014 and 2015, net sales by Alcon grew, contributed to in part by the increased volume in sales of Ilevro. [25] [26] [27] That financial year, Novartis reported $18 billion in total financial debt. [25] That figure has grown steadily since. In 2016, Novartis reported a total debt of $23.8 billion, [28] up from the $21.9 billion reported in 2015 [27] and the $20.4 billion reported in 2014. [26] As of May 2017, Novartis is estimated to be worth $193.2 billion. [29]
On January 27, 2016, Alcon was moved to become a branch of the Innovative Medicines Division at Novartis. [28] Early in 2016, Alcon formed agreements with both TrueVision and PowerVision, and acquired Transcend Medical. [28] As of January 2017, Novartis is weighing options for Alcon in the business structure. [28]
Alcon faced declining growth in 2016, having faced challenges in development and marketing of new products. [28]
Novartis maintains a detailing unit geared toward health professionals consisting of over 3,000 employees within the United States and an additional 21,000 worldwide. [28] Novartis is also seeking to expand direct-to-consumer advertising and entrance into specialty product markets. [28] Novartis also notes the influence of position and preference on US Centers for Medicare & Medicaid formularies in expanding their market value. [28]
Nepafenac, Nevanac, and Ilevro are all absent from the 2016 Annual Report issued from Novartis. [28]
There are currently[ when?] seven U.S. patents filed that are directly associated with the modernized formulations of nepafenac, all stemming from Novartis. [30] There are three patents associated with Nevanac that are still[ when?] active [31] and four associated with Ilevro. [32] The earliest patent related to the modern formulations of nepafenac was approved on June 11, 2002, after being filed in 1999, by Bahram Asgharian. [33] A patent was filed by Warren Wong, associated with Alcon, Inc. based out of Fort Worth, Texas, on December 2, 2005, for aqueous suspensions of nepafenac. [34] Another patent for a nepafenac-based drug was filed on May 8, 2006, by Geoffrey Owen, Amy Brooks, and Gustav Graff. [35] A patent was filed by Masood A. Chowhan and Huagang Chen on February 9, 2007, and approved on May 24, 2011, [36] followed closely by a patent filed by Warren Wong on September 23, 2010, and approved on December 6, 2011. [37] Masood A. Chowhan, Malay Ghosh, Bahram Asgharian, and Wesley Wehsin Han filed another patent on December 1, 2010, and approved on December 30, 2014. [38] The most recent[ when?] patent was filed by Masood A. Chowhan, Malay Ghosh, Bahram Asgharian, and Wesley Weshin Han on November 12, 2014, and approved on May 30, 2017. [39] These patents are in effect until dates ranging between July 17, 2018, and March 31, 2032. [32]
Novartis also maintains patents on nepafenac in 26 countries outside the United States. [40]