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Actelion Pharmaceuticals Ltd. v. Icos Corporation, District Court of The Hague, the Netherlands, 26 October 2016, Case number C/09/493389 / HA ZA 15-862

Icos is the holder of the European patent with number 1 200 092 B1 entitled “Beta-carboline drug products”. The patent is directed to tadalafil having specific and defined particle size characteristics, which permits uniform formulation of stable pharmaceutical compositions.

According to claim 1 at least 90% of the tadalafil particles should have a particle size of less than about 40 micron. Tadalafil is used as a drug for the treatment of sexual dysfunction.

The goal of EP ‘092 is to provide a formulation of tadalafil with an improved bioavailability, in particular a faster onset of the therapeutically effect, which can be used for the treatment of sexual disorders.

Prior art document WO 97/03675 discloses the use of tadalafil for treatment of sexual disorders. According to the Court WO ‘675 is a realistic starting point for the assessment of inventive step even though it does not disclose tadalafil’s poor solubility in water. Icos argued that another prior art document, Butler, is the closest prior art. According to the Court this is not relevant, because WO ‘675 is a realistic starting point. This, according to the Court means that EP ‘092 also has to be inventive over WO ‘675 even though WO ‘675 may be a more distant starting point.

According to the Court, the only difference between claim 1 of EP ‘092 and WO 675 is the claimed specific particle size. The objective technical problem is to provide a formulation of tadalafil with a faster onset of the therapeutically effect in relation to the state of the art and thus an improved bioavailability.

According to the court it was common general knowledge for the skilled person that particles of poorly soluble compounds may be reduced by micronisation and that this, in general, leads to quicker dissolution and absorption. Further, the skilled person will realise that quicker dissolution and absorption results in a quicker onset of the therapeutic effect.

Icos had not disputed that micronisation was a routine measure for the skilled person. Icos had argued that micronisation could lead to problems, but Icos had not made clear whether or not in this case this would result in the skilled person not using micronisation.

Considering the common general knowledge, the skilled person would at least try to solve the objective technical problem by micronising the tadafanil particles. As micronisation was common general knowledge the skilled person does not need a pointer to use micronisation in this case.

The Court found that whether or not the skilled person would reduce the particles to the claimed 40 micron or less is not relevant, because there is nothing in the patent that attributes the technical effect to that specific particle size, while Actelion had pointed out that it was normal for the skilled person to micronise particles to between 10 and 40 micron.

According to the court, the skilled person would not know at the beginning whether or not micronisation would lead to the desired result, but he would at least take a neutral position.

It follows from the jurisprudence of the board of appeal of the EPO that when 1) the state of art leads the skilled person in the direction of further investigation and 2) the skilled person can carry out those investigations by performing routine experiments, that the expectation of success is subject to less stringent requirements.

When in such a case the skilled person does not have any expectations with respect to the results of the experiments but a neutral try and see-behavior, a reasonable expectation of success is not absent.

As this applies to case at hand, the Court finds with Actelion that the subject matter of claim 1 of EP ‘092 is not inventive. The same holds true for the dependent claims as Icos had not sufficiently disputed Actelion’s arguments in that regard.

A copy of the judgment (in Dutch) can be read here.

Headnote: Mattie de Koning, Simmons&Simmons LLP