Positive Interim Phase 2 Data Reported for VEGF Trap-Eye in Age-Related Macular Degeneration
`
`March 27, 2007
`Positive Interim Phase 2 Data Reported for VEGF Trap-Eye in Age-Related Macular DegenerationTARRYTOWN, N.Y. &
`LEVERKUSEN, Germany, Mar 27, 2007 (BUSINESS WIRE) -- Regeneron Pharmaceuticals, Inc. (Nasdaq: REGN) and Bayer
`HealthCare AG (NYSE: BAY) today announced positive preliminary data from a pre-planned interim analysis of a Phase 2
`randomized study of their VEGF Trap-Eye in patients with the neovascular form of age-related macular degeneration (wet AMD).
`The VEGF Trap-Eye met its primary endpoint of a statistically significant reduction in retinal thickness after 12 weeks compared
`with baseline (all groups combined, decrease of 135 microns, p < 0.0001). Mean change from baseline in visual acuity, a key
`secondary endpoint of the study, also demonstrated statistically significant improvement (all groups combined, increase of 5.9
`letters, p < 0.0001). Moreover, patients in the dose groups that received only a single dose, on average, demonstrated a decrease
`in excess retinal thickness (p < 0.0001) and an increase in visual acuity (p = 0.012) at 12 weeks. There were no drug-related
`serious adverse events, and treatment with the VEGF Trap-Eye was generally well-tolerated. The most common adverse events
`were those typically associated with intravitreal injections. Detailed data from this interim analysis will be presented at an
`upcoming scientific conference.
`
`"These data support our efforts to develop the VEGF Trap as a potent blocker of VEGF in various diseases," said George D. Yancopoulos, M.D.,
`Ph.D., President of Regeneron Research Laboratories. "Importantly, the VEGF Trap-Eye may offer the potential to improve vision in patients with wet
`AMD with dosing less frequently than every four weeks. Our Phase 3 program is being designed to test this possibility and further evaluate the safety
`and efficacy of various doses and dosing intervals of the VEGF Trap-Eye."
`
`"We are very pleased with the outcome of this interim analysis and the findings support the potential of the VEGF Trap-Eye to improve the lives of
`patients suffering from wet AMD, which accounts for 90% of AMD related blindness," said Kemal Malik, M.D., member of the Bayer HealthCare
`Executive Committee, responsible for Global Development. "These results encourage us in our plans to foster next steps in development and to
`further study the VEGF Trap-Eye in additional eye diseases."
`
`Based on these results, Regeneron and Bayer HealthCare AG plan to initiate the VEGF Trap-Eye Phase 3 program in the second half of 2007. The
`companies are collaborating on the global development of the VEGF Trap-Eye for the treatment of wet AMD, diabetic eye diseases, and other eye
`diseases and disorders. Bayer HealthCare AG and Regeneron will jointly commercialize the VEGF Trap-Eye outside the United States, and
`Regeneron maintains exclusive rights in the United States.
`
`The Phase 2 study is a 12-week, multi-center trial involving 150 patients who are randomized to 5 groups and treated with the VEGF Trap-Eye in one
`eye. Two groups received either 0.5 or 2.0 mg of VEGF Trap-Eye administered every four weeks, and three groups received a single dose of 0.5, 2.0,
`or 4.0 mg of VEGF Trap-Eye. Patients are monitored for safety, retinal thickness, and visual acuity over 12 weeks. Retinal thickness is determined by
`optical coherence tomography (OCT) scans read at an independent reading center. Visual acuity is defined as the total number of letters read correctly
`on the Early Diabetic Retinopathy Study (ETDRS) chart. Maintenance of vision is defined as losing fewer than 3 lines (equivalent to 15 letters) on the
`ETDRS chart.
`
`The interim analysis was conducted on the first 78 patients who completed 12 weeks of study. As summarized above, overall, patients had a
`statistically significant improvement in retinal thickness and visual acuity. All but one patient maintained or improved vision at 12 weeks. Although the
`improvement in visual acuity was numerically larger in patients receiving injections every 4 weeks, there were no statistically significant differences
`across the five dose groups in either retinal thickness or visual acuity at 12 weeks.
`
`About the VEGF Trap-Eye
`
`Vascular endothelial growth factor (VEGF) is a naturally occurring protein in the body whose normal role is to trigger formation of new blood vessels
`(angiogenesis) to support the growth of the body's tissues and organs. It has also been associated with the abnormal growth and fragility of new blood
`vessels in the eye, which lead to the development of wet AMD. The VEGF Trap-Eye is a fully human, soluble VEGF receptor fusion protein that binds
`all forms of VEGF-A along with the related placental growth factor (PlGF). The VEGF Trap-Eye is a specific and highly potent blocker of these growth
`factors. Blockade of VEGF, which can prevent abnormal blood vessel formation and vascular leak, has proven beneficial in the treatment of wed AMD.
`
`About AMD
`
`Age-related macular degeneration (AMD) is a leading cause of acquired blindness. Patients with condition can experience a loss of vision due to the
`development of abnormal, fragile blood vessels in the back of the eye. A particular type of AMD, called wet AMD, accounts for approximately 90% of
`AMD-related blindness. Wet AMD is the leading cause of blindness for people over the age of 65 in the U.S. and Europe.
`
`Macular degeneration is diagnosed as either dry (nonexudative) or wet (exudative). In wet AMD, new blood vessels grow beneath the retina and leak
`blood and fluid. This leakage causes disruption and dysfunction of the retina creating blind spots in central vision and can account for blindness in wet
`AMD patients.
`
`About Regeneron Pharmaceuticals
`
`Regeneron is a biopharmaceutical company that discovers, develops, and intends to commercialize therapeutic medicines for the treatment of serious
`medical conditions. Regeneron has therapeutic candidates for the potential treatment of cancer, eye diseases, and inflammatory diseases and has
`
`Mylan Exhibit 1053
`Mylan v. Regeneron, IPR2021-00881
`Page 1
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`Joining Petitioner: Apotex
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`preclinical programs in other diseases and disorders.
`
`About Bayer HealthCare
`
`Bayer HealthCare, a subsidiary of Bayer AG, is one of the world's leading, innovative companies in the healthcare and medical products industry and
`is based in Leverkusen, Germany. The company combines the global activities of the Animal Health, Consumer Care, Diabetes Care and
`Pharmaceuticals divisions. The pharmaceuticals business operates under the name Bayer Schering Pharma AG. Bayer HealthCare's aim is to
`discover and manufacture products that will improve human and animal health worldwide.
`
`This news release discusses historical information and includes forward-looking statements about Regeneron and its products, programs, finances,
`and business, all of which involve a number of risks and uncertainties, such as risks associated with preclinical and clinical development of our drug
`candidates, determinations by regulatory and administrative governmental authorities which may delay or restrict our ability to continue to develop or
`commercialize our drug candidates, competing drugs that are superior to our product candidates, unanticipated expenses, the availability and cost of
`capital, the costs of developing, producing, and selling products, the potential for any collaboration agreement, including our agreements with the
`sanofi-aventis Group and Bayer HealthCare, to be canceled or to terminate without any product success, risks associated with third party intellectual
`property, and other material risks. A more complete description of these and other material risks can be found in Regeneron's filings with the United
`States Securities and Exchange Commission (SEC), including its Form 10-K for the year ended December 31, 2006. Regeneron does not undertake
`any obligation to update publicly any forward-looking statement, whether as a result of new information, future events, or otherwise unless required by
`law.
`
`This news release contains forward-looking statements based on current assumptions and forecasts made by Bayer Group management. Various
`known and unknown risks, uncertainties and other factors could lead to material differences between the actual future results, financial situation,
`development or performance of the company and the estimates given here. These factors include those discussed in our public reports filed with the
`Frankfurt Stock Exchange and with the U.S. Securities and Exchange Commission (including our Form 20-F). The company assumes no liability
`whatsoever to update these forward-looking statements or to conform them to future events or developments.
`
`Additional information about Regeneron and recent news releases are available on Regeneron's worldwide web site at www.regeneron.com
`
`SOURCE: Regeneron Pharmaceuticals, Inc.
`
`Regeneron Pharmaceuticals, Inc.(cid:10)
`Charles Poole, 1.914.345.7640(cid:10)
`Vice President, Investor Relations(cid:10)
`charles.poole@regeneron.com(cid:10)
`or(cid:10)
`Media Relations:(cid:10)
`Lauren Tortorete, 1.212.845.5609(cid:10)
`ltortorete@biosector2.com(cid:10)
`or(cid:10)
`Bayer HealthCare AG(cid:10)
`Dr. Jost Reinhard, +49 30 468 15062(cid:10)
`Jost.Reinhard@schering.de(cid:10)
`
`Mylan Exhibit 1053
`Mylan v. Regeneron, IPR2021-00881
`Page 2
`
`Joining Petitioner: Apotex
`
`