Paliperidone palmitate – USA

Paliperidone palmitate – USA

On Apr. 01, 2024, Federal Circuit affirmed affirmed district court’s indefiniteness determination but vacated and remanded its nonobviousness determination.


Janssen markets and sells INVEGA SUSTENNA which is an extended-release intramuscular injectable of paliperidone palmitate, indicated for the treatment of schizophrenia in adults. Teva filed ANDA challenging validity of US 9,439,906. The 906 patent relates to dosing regimens, specifically first loading dose of about 150 mg-eq. of
paliperidone in deltoid muscle, a second loading dose of about 100 mg-eq on the 6th to about 10th day of treatment in deltoid muscle, and first maintenance dose of about 25 mg-eq. to about 150 mg-eq a month after second loading dose in deltoid or gluteal muscle.



Teva relied on three primary prior-art references at trial: (1) clinical study protocol NCT00210548 (“the ’548 protocol”); (2) the ’544 patent; and (3) WO 2006/114384 (“WO’384”) and argued that all claims are obvious. The district court concluded that Teva had not proven invalidity. Upon appeal, Teva argued that district court’s obviousness analysis, including its analysis of secondary considerations, was legally flawed. Federal circuit agreed with Teva that the claims were not directed to a generalized dosing regimen and therefore the district court asked for a showing of obviousness that went beyond what was claimed. Nothing in the claims requires that the regimen be used for the patient population generally or a certain percentage of the patient population. On their face, the claims only recite a dosing regimen for a psychiatric patient. It seems that the court ended up conflating Janssen’s purported difficulties in generating data to gain approval for a “universal” or “generalized” dosing regimen with the scope of the claims themselves. Given the scope of the claims here, it was important for the court to recognize the distinction and focus its findings on single patient administration. This misunderstanding about the claims impacted the district court’s overall obviousness analysis.

Next, Teva argued that the court’s analysis was impermissibly rigid and does not comport with KSR or otherwise
reflect this court’s obviousness jurisprudence. Federal Circuit said that instead of considering the prior art in context or in combination, the court’s analysis seems to tackle the express statements of each reference one-by-one—identifying each difference or dissimilarity between an individual reference and the claims, but not fully assessing the teachings in toto. This seemingly siloed and inflexible approach left insufficient room for POSA’s understanding of, or motivation to modify, the primary references at issue. Federal Circuit therefore, vacated and remanded case back to district court.

With respect to secondary considerations, Federal Circuit said that on remand, the district court will need to reassess the significance of the secondary considerations as part of its renewed obviousness analysis. The district court will necessarily need to reevaluate nexus because of misunderstanding of claim scope carried throughout its obviousness analysis.



Teva argued that claims 19–21 (particle-size claims) were invalid as indefinite. Claim 19 contains a particle-size limitation for the paliperidone palmitate used in the formulations administered: “paliperidone palmitate having an average particle size (d50) of from about 1600 nm to about 900 nm.” The claims do not specify what measurement technique should be used to determine whether the average particle size d(50) is from 1600 nm to 900 nm. Similarly, the specification states that particle size can be “measured by art known conventional techniques, such as sedimentation field flow fractionation, photon correlation spectroscopy or disk centrifugation. Teva did point to evidence that, for particles in general, different particle-size measurement techniques can yield different results. However, the district court found that the actual discrepancy in particle-size measurement of paliperidone palmitate that Teva relied on was “an outlier measurement taken with a defective device,” i.e., was not based on a discrepancy typical of the measurement technique used. Federal Circuit thus said that Teva has not shown that the court’s outlier finding was clearly erroneous. As a result, the district court correctly determined that Teva did not meet its burden to show that claims 20 and 21 are invalid as indefinite.

“cafc opinion”

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