On Nov. 10, 2022, the High Court (Patent Court) of England & Wales found deferasirox formulation patent invalid and not infringed by Teva.

 

Teva brought action for revocation of two patents, EP 2,964,202 and EP 3,124,018 owned by Novartis. These patents claim swallowable film-coated deferasirox formulation with certain excipients. Both patents have been upheld in the Opposition Division of the EPO with amended claims and appeals are pending. Novartis requested to amend the claims before court to bring them into line with the claims allowed by the Opposition Division. Before the priority date, Exjade (deferasirox) dispersible tablets were available on the market but it had certain disadvantages like unpleasant taste, empty stomach administration to avoid food effect etc.

Claim 1 of EP 202 as representative:

A swallowable film coated tablet for oral administration comprising deferasirox or a pharmaceutically acceptable salt thereof present in an amount from 45% to 60% by weight based on the total weight of the tablet, wherein the tablet is without sodium lauryl sulfate and lactose and comprises i. microcrystalline cellulose; ii. crospovidone; iii. povidone; iv. poloxamer 188; v. colloidal silicon dioxide; vi. magnesium stearate.

 

Inventive concept:

Novartis argued that the inventive concept is the provision of a swallowable film-coated tablet having higher bioavailability and reduced food effect compared to Exjade dispersible formulation. Teva argued that the range of deferasirox is the key feature of the inventive concept. Aside from the formulation being film-coated, there was nothing more to it. Court said that Novartis’ case on the inventive concept of unexpected advantages (higher bioavailability and reduced food effect) is not correct as these features are not a part of the claims. The inventive concept is the new technical insight conveyed by the invention and the invention is that which is claimed. Although the description of the invention and the drawings are to be used to interpret the claims (see art.69 European Patent Convention), features disclosed only in the description are not to imported into a claim to impose a limitation that would not otherwise be there. Where the patentee has chosen the words of his claim such as to exclude mention of a feature referred to in the description, that feature forms no part of the claimed invention as a whole or, therefore, the inventive concept. Therefore, higher bioavailability and reduced food effect cannot be imported into either the claims or the inventive concept.

Thus, the court said that the relevant question for inventive step in the present case is whether it was obvious at the priority date to make a “swallowable tablet” as claimed, nothing more than that. This is a case of the inventive concept consisting of a product having a particular combination of features. Therefore, the inventive concept is:

“A swallowable film-coated tablet containing deferasirox in an amount between 45% and 60% of total tablet weight, containing (i) microcrystalline cellulose, (ii) crospovidone, (iii) povidone, (iv) poloxamer 188, (v) colloidal silicon dioxide and (vi) magnesium stearate and containing no SLS or lactose”.

 

Validity:

Teva cited 3 prior arts – WO 2007/045445 (“Battung”); WO 2009/067557 (“Zadok”) & Séchaud R. et al. (NPL). Court said that based on written evidence that there were public discussions with Novartis before the priority date about how to overcome issues of compliance with the dispersible product by way of a new formulation. Swallowable tablets are the most common oral dosage form, due to its advantages. Therefore, at the priority date, the skilled person would have said that a swallowable tablet was a desirable goal. Maximising dispersibility and minimising grittiness are both improvements that the skilled person would plausibly suggest. The prior arts disclosed most of the claimed features and it would have been obvious to skilled person to optimize the formulation. There was an incentive to create a product which minimised all or any of the known side effects of dispersible deferasirox and  swallowable film-coated tablet would have been obvious choice. Therefore, claims lack inventive step.

 

Infringement:

Court said that the issue of infringement and Teva’s application for a declaration of non-infringement turns solely on the percentage content of deferasirox in Teva DFX. Whether on Novartis’ construction of “total weight” or Teva’s construction, the deferasirox content of Teva DFX is, at its lowest, above the claimed range of 45-60%. The precise figures for Teva DFX are confidential, but on what is sometimes described in Actavis as a normal construction, Teva DFX is outside the claims. Novartis argued that it nonetheless falls within the claim as an equivalent to the invention. Court found that in the present case the inventive concept of the Patents would be seen by the skilled team as requiring strict compliance with the 45-60% range of deferasirox. On that basis a variant will not be substantially the same as the inventive concept unless it strictly complies. Thus, Teva DFX falls outside the claims on both a normal construction and under the doctrine of equivalents.