March 1, 2018

Case Name: Alcon Research, Ltd. v. Watson Labs., Inc., No. 15-1159, 2018 U.S. Dist. LEXIS 33057 (D. Del. Mar. 1, 2018) (Sleet, J.) 

Drug Product and Patent(s)-in-Suit: Pazeo®(olopatadine HCl); U.S. Patent No. 8,791,154 (“the ’154 patent”)

Nature of Case and Issue(s) Presented: The ’154 patent was directed to aqueous ophthalmic solutions for the treatment of ocular allergic conjunctivitis, wherein the solution contained at least 0.67 w/v% but no greater than 1.0 w/v% olopatadine dissolved in a solution of hydroxypropyl-γ-cyclodextrin (“HPγCD”) and certain amounts of polyethylene glycol (“PEG”) and polyvinylpyrrolidone. Prior to trial, Defendants Watson Laboratories and Lupin Pharmaceuticals (collectively, “Defendants”) maintained defenses of obviousness, lack of written description, and lack of enablement. After opening statements, Defendants dropped all written-description arguments. The Court granted judgment rejecting the non-enablement argument at the close of Defendants’ case. The only issue left to be tried was obviousness. The court found the ’154 patent not invalid.     

Why Alcon Prevailed: Defendants argued that the prior art taught a concentration range of olopatadine from 0.0001 to 5%. Judge Sleet agreed, but explained that these prior-art references encompassed non-solution dosage forms, including suspensions, gels, ointments, emulsions, and bioerodible implants. More specifically, in the context of solutions, the preferred range of olopatadine disclosed in the prior art was between 0.1 and 0.25% w/v, and no prior-art reference taught an ophthalmic solution with at least 0.67% olopatadine.  

Moreover, Judge Sleet found that as of the priority date, the highest olopatadine concentration actually in use was Alcon’s predecessor conjunctivitis product, Pataday®, which was a 0.2% olopatadine solution. And although Defendants argued that a POSA would have been motivated to formulate a solution with a higher concentration of olopatadine, Judge Sleet concluded that no such motivation was present, especially a solution with 0.67 to 1.0 w/v% of olopatadine. The Court went on to explain that because of its known structure, a POSA would have expected HPγCD to reduce bioavailability, thereby making it a poor solubilization candidate. Additionally, Judge Sleet explained that the prior art failed to teach how to formulate a solution containing a high concentration of olopatadine with HPγCD and both PEG and polyvinylpyrrolidone.

Finally, Judge Sleet found evidence of unexpected results and long-felt need.  Specifically, Judge Sleet concluded that Alcon adduced evidence that the claimed invention unexpectedly showed that a 0.7% olopatadine solution decreased eye redness at the onset of action by comparison to Pataday. Alcon also showed that a further reduction in eye redness was a clinically meaningful health benefit.