Friday, October 27, 2017

Glatiramer acetate - UK

On Oct 26, 2017, UK High Court of Justice has issued a decision in favor of Mylan and its European partner Synthon, finding Teva's patent EP (UK) 2949335 (EP’335) relating to Copaxone® 40 mg/mL invalid based on lack of inventive step.

The Claimants ("Mylan" and "Synthon") sought revocation of EP’335 patent entitled "Low frequency glatiramer acetate (GA) therapy." The EP’335 patent is directed to a dosage regimen for the administration of GA for the treatment of relapsing forms of multiple sclerosis ("MS") consisting of three subcutaneous injections of 40 mg GA every seven days with at least one day between each injection ("40 mg TIW"). The Claimants contend that the Patent is invalid on the grounds of lack of novelty, lack of inventive step and insufficiency.

Before the priority of patent ie Aug 2009, both parties agreed that the skilled person would have been aware that the 20 mg QD regimen for GA appeared to have been somewhat arbitrarily selected and that no Phase II dose-ranging studies had been carried to determine the optimum dose of GA for treating MS, and in particular RRMS. Court after analyzing the prior arts concluded the teachings as:
a  a) there was no statistically significant difference in efficacy between the 40 mg dose and the 20 mg dose;
b  b) both were safe and well tolerated;
c  c)  in terms of tolerability, there was a disadvantage in administering a 40 mg dose rather than a 20 mg dose.
The skilled person would be aware from his common general knowledge & literatures that there were investigations on less frequent administration of 20 mg GA.

Obviousness over the prior art:

The sole difference between Pinchasi and claim 1 of the Patent was that Pinchasi discloses a regimen of 40 mg every other day (QOD) while claim 1 requires a regimen of 40 mg every seven days with at least one day between each injection (TIW). The difference amounts to one dose every fortnight. Claimants argued that 40 mg TIW was an obvious alternative to 40 mg QOD because the skilled person would think that missing one dose a fortnight was unlikely to have a detrimental effect on the efficacy of the treatment, and TIW would have the advantages that it was likely to increase the tolerability of the medication and would be more convenient for patients who wanted fixed-day administration and weekends injection-free. Secondly, counsel for the Claimants argued that, if the skilled person considered the matter in more detail in the light of his common general knowledge and his literature search, then 40 mg TIW would be an obvious regimen to try in a Phase III clinical trial and the skilled person would have a fair expectation of success, both in the sense that the regimen would be efficacious compared to placebo and in the sense that it would be comparable in efficacy to 20 mg QD.

As to this, the Defendants contended that it was not obvious to try 40 mg TIW, for a combination of three reasons. First, the Defendants contend that the skilled person would not have been interested in improving the administration of GA, because of the new treatments on the horizon. Secondly, the Defendants contend that the skilled person would not be motivated to consider a 40 mg TIW regimen. If the skilled person was interested in reducing the frequency of administration, then the obvious regimen to consider would be 20 mg QOD as suggested by the Fletcher 2002 and Khan 2008 publications. Thirdly, and most importantly, the Defendants contend that the skilled person would be dissuaded from trying a 40 mg dose because of the increase in the severity of ISRs and IPIRs reported in Cohen 2007 and Comi 2008B, and in particular the increase in early terminations due to adverse events mainly due to ISRs which had been reported in Comi 2008B, given that it had been found that 40 mg QD was no more efficacious than 20 mg QD.

Court after analyzing the all facts & expert testimonies held that the skilled person had a clear motivation to reduce the frequency of administration of GA in order to increase tolerability, adherence and convenience. Moreover, a TIW regimen had the advantages of fixed-day administration and injection-free weekends. Given that Prof Comi's overall conclusion in Comi 2008B was that 40 mg QD was safe and well tolerated, and given that a reduction in the frequency of administration from QD to TIW would be expected to reduce the incidence of ISRs (and IPIRs), therefore the skilled person would not be dissuaded from trying 40 mg TIW in a Phase III trial. Overall, court concluded that 40 mg TIW was obvious to try and that the skilled person would have had a fair expectation of success, both in the sense that the regimen would be efficacious compared to placebo and in the sense that it would be comparable in efficacy to 20 mg QD.

CONCLUSION:
1  1.       claims 1 and 3 of the Patent are novel over Pinchasi;
2  2.       claims 1 and 3 of the Patent are obvious over Pinchasi, and therefore invalid.

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