When the U. S. Supreme Court established its new obviousness test in KSR Int'l Co. v. Teleflex, Inc., 127 S. Ct. 1727 (2007), legal commentators suggested that the decision changed little for lifescience inventions. Subsequently, the United States Patent and Trademark Office promulgated how it would evaluate lifescience inventions for nonobviousness and this standard has not deviated much from past standards. Now in Bayer Schering Pharma AG v. Barr Laboratories, Inc., No. 05-cv-2308 (D. N.J. Mar. 3, 2008), a Federal District Court has jolted the lifescience community with an expansive application of KSR's "common sense" rule.
Bayer Healthcare Pharmaceuticals, Inc. has been marketing Yasmin®, an oral contraceptive. According to the Orange Book, Yasmin® is protected by U.S. Patent No. 6,787,531 ("the '531 Patent). Claim 1 of the '531 Patent is directed to a new formulation and reads:
1. A pharmaceutical composition comprising from about 2 mg to about 4 mg of micronized drospirenone particles, about 0.01 mg to about 0.05 mg of 17α-ethinylestradiol, and one or more pharmaceutically acceptable carriers, the composition being in an oral dose form exposed to the gastric environment upon dissolution, and the composition being effective for oral contraception in a human female.
When Barr Laboratories, Inc. filed an Abbreviated New Drug Application with the FDA relating to the generic version of Yasmin®, Bayer filed a declaratory action in the Federal District Court for the District of New Jersey to declare the '531 Patent valid and enjoin Barr's generic version from proceeding to market.
In a 96-page opinion, the District Court held that the '531 Patent's asserted claims were obvious. The use of these two compounds - drospirenone and ethinylestradiol - as contraceptives was known. Oral administration of this combination without an enteric coating resulted in isomerization of drospirenone which made the oral administration ineffective. To compound this problem, it was thought that micronizing drospirenone would only exacerbate the isomarization. For four years, Bayer's scientists labored under the notion that an enteric coating was required. Yet, when the scientists at Bayer investigated the bioavailability of drospirenone without the enteric coating, they were surprised to find the opposite – the micronized formulation in those specific concentrations, once delivered orally, did not result in isomarization and did not need enteric coating.
The District Court was not swayed by this evidence of surprising and unexpected result. Instead, the Court noted that had Bayer's scientists performed the in vivo tests "at the outset, then [they] would have known drospirenone [...] possessed good bioavailability." Opinion at 40-41. "Justice Kenedy in KSR observed that in analyzing an obviousness defense, the court must use its common sense." Opinion at 69. And the Court did not find Bayer's assertion of surprising and unexpected result to make sense. Instead, the Court found that the formulation was obvious because the combination of drospirenone and ethinylestradiol was known and because micronization of spirorenone (a related compound to drospirenone) was known.
Some may be concerned about the future of patenting formulations and how such patent applications should be approached, especially if this decision is upheld on appeal. We will keep you updated on the status of this case as it proceeds through appeals.
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