PGR2018-00001 (US 9,539,268 B2)
Final Written Decision
April 29, 2019
Brief summary: GG found to have demonstrated by a preponderance of the evidence that Antecip’s claims related to zoledronic acid and methods for using the same to treat arthritis are unpatentable for lack of enablement.
Summary: Grünenthal GmbH (GG) requested post-grant review (PGR) of Antecip’s claims 3-30 (claims 1 and 2 were statutorily disclaimed) of US 9,539,268 B2 relating to “[a] method of treating arthritis comprising orally administering a dosage form” of zoledronic acid, as well as pharmaceutical oral dosage forms thereof. The FWD explains that FWDs also issued regarding the parent patent of the ‘268 patent (US 9,408,862) (PGR2017-00022 and PGR2017-00008). In this case, GG alleged lack of enablement (§ 112(a)), indefiniteness (§ 112(b)), anticipation in view of “Leonard” (§ 102), and obviousness in view of Leonard, “Aronhime”, and the “Merrion Poster”, or “Fox”, “Laslett”, Leonard, and the Merrion Poster (§ 103), supported by three expert declarations. The Board first agreed with Antecip regarding the level of ordinary skill in the art, noting it “would reach the same conclusion on enablement even under Petitioner’s proposed levels of ordinary skill” and that “the prior art itself demonstrates the level of skill in the art at the time of the invention” (Okajima, FC 2001). The Board also determined that “no claim term requires express construction for the purposes of this decision” (broadest reasonable construction (BRC) in light of the specification (§ 42.200(b) (2018); In re Translogic, FC 2007 (under BRC, claims are assigned their “ordinary and customary meaning”; Vivid, FC 1999 (“[o]nly claims in controversy need be construed”)). On enablement, the Board explained that “[t]he touchstone of enablement is whether undue experimentation would have been required to practice the claimed invention” (In re Wands, FC 1998 (the Wands factors)). GG’s expert testified that “[t]he claimed invention…is within the unpredictable field of pharmaceutical formulations”, which Antecip did not dispute. Regarding the Wands factors, the Board also found that “the ordinary skilled artisan would have expected all dosage forms of zoledronic acid to have relatively low bioavailabilities that fall outside the ranges specified in the challenged claims” (e.g., “about 1.1 to about 4%”), that the “eleven disodium salt forms” (to which the claims are not limited) described in the ‘268 specification “could have different properties, including different solubilities and bioavailabilities”, and that the ‘268 specification does not identify any “bioavailability-enhancing ingredients or provide any “actual data…on any particular dosage form…regarding bioavailability”. On whether “the quantity of experimentation required” would have been undue, the Board “observe[d] that the public reference advanced by Patent Owner describes the bioavailability of zoledronic acid in beagle dogs” and that that study “would not have provided sufficient guidance” regarding bioavailability in humans (“[a]n ordinarily skilled artisan would have recognized that bioavailability in humans differs from…dogs”) (the Board noting that “extrinsic evidence can substitute for disclosure in the specification to provide enabling support”, but also that “the specification…must supply the novel aspects…to constitute adequate enablement” (Genentech, FC 1997)). After balancing the Wands factors, the Board determined that GG had demonstrated by a preponderance of the evidence that claims 3-30 are unpatentable for lack of enablement.