Alcon Research, Ltd. v. Apotex Inc.

When the prior art discloses a portion of the claimed range, the patent claim at issue is invalid as obvious; the motivation of a person of ordinary skill to combine prior art does not need to be the same as that of the patentee; inherency is considered in an obviousness analysis.

October 16, 2012

GENERICally Speaking

Case Name: Alcon Research, Ltd. v. Apotex Inc., Case No. 2011-1455, 687 F.3d 1362 (Fed. Cir. Aug. 8, 2012) (Circuit Judges Prost, Moore, and O’Malley presiding; Opinion by Moore.) (Appeal from S.D. Ind., Young, J.)

Drug Product and Patent(s)-in-Suit:Patanol® (olopatadine); U.S. Patent No.5,641,805 (“the ’805 patent”)

Nature of the Case and Issue(s) Presented: Alcon asserted that Apotex infringed the ’805 patent, which was directed to a method of treating allergic eye disease in humans by stabilizing conjunctival mast cells with topical administration of an olopatadine compound.  While the independent claims of the ’805 patent did not specify a particular amount of olopatadine to be administered, the dependent claims included specific amounts.  The district court found that the asserted claims of ’805 patent were valid, enforceable, and that Apotex infringed them. 

On appeal, Apotex argued that the asserted claims of the ’805 patent were invalid as obvious.  Apotex asserted that the prior art taught the use of certain amounts of olopatadine as an effective antihistamine in the eye.  While the prior art did not teach that olopatadine affected mast cells, Apotex argued that the skilled artisan would be motivated to use olopatadine to treat allergic eye disease based on prior studies with guinea pigs.

Alcon argued that that prior art did not teach that olopatadine would act as a mast-cell stabilizer.  Moreover, the prior art did not teach that olopatadine would be effective in human eyes because the prior art only tested the effectiveness in guinea pigs.  Alcon asserted that there was no reasonable expectation that olopatadine would be safe for use in human eyes based on results obtained from the guinea pig studies.  The Federal Circuit reversed the opinion below and held the claims invalid.

Why Apotex Prevailed: The Federal Circuit focused its analysis on the fact that olopatadine was not effective at all concentrations, which Alcon admitted.  But the independent claims did not have any limitation directed at a specific amount of olopatadine.  As such, the independent claims were invalid because the claims included concentrations that were not enabled.  Moreover, the Federal Circuit held that when the prior art discloses a portion of the claimed range, the entire claim is invalid.  The prior art included portions of the claimed ranges in the dependent claims, and thus those claims were also invalid.  Alcon argued that a person of ordinary skill would not have been motivated to ascribe the prior art findings concerning efficacy in animal eyes to human eyes, and that art taught away from mast-cell stabilization, the patented method of use.  The Federal Circuit noted that it has repeatedly stated that the motivation of the prior art does not need to be the same as the patentee’s motivation; here, mast-cell stabilization.  Thus, the skilled artisan would have been motivated to use the teachings from the guinea pig prior art to test olopatadine on human eyes. 

Next, the Federal Circuit rejected Alcon’s argument that the prior art did not disclose safety associated with the administration of olopatadine in human eyes.  First, the court found that safety was not a claimed limitation.  Moreover, the ’805 patent was not based on any human testing, but rather in vitro testing of human cells.  Thus, the prior art did not have to explicitly state that using olopatadine in humans would be safe in order for a skilled artisan to have an expectation that olopatadine would, in fact, be safe for use in humans.  Further, citing In re Kubin, the court noted that mast-cell stabilization did not impose an additional limitation to the ‘805 patent invention because mast-cell stabilization is an inherent property that is necessarily present at the disclosed concentrations.

Finally, the Federal Circuit affirmed the validity of two claims of the ’805 patent because the prior art that Apotex relied on did not teach the specific amount claimed.  These claims limited the amount of the olopatadine to 0.1% w/v, and the prior art only taught using up to 0.01%.  Thus, a skilled artisan would not have been motivated to use the higher concentration.  Moreover, it was known that olopatadine could be biphasic at certain increased concentrations, such that there would not have been a motivation to use the higher concentration.  Lastly, the commercial success of Patanol, which uses 0.1% w/v of olopatadine, provided objective evidence of non-obviousness of these claims.

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