DCT

1:19-cv-00880

Bayer IP GmbH v. Macleods Pharma Ltd

Log In

I. Executive Summary and Procedural Information

  • Parties & Counsel:
  • Case Identification: 1:19-cv-00880, D. Del., 05/10/2019
  • Venue Allegations: Venue is alleged to be proper in Delaware because Defendant Macleods USA is incorporated in Delaware, and Defendant Macleods Ltd. is a foreign entity not resident in the United States.
  • Core Dispute: Plaintiffs allege that Defendants’ submission of an Abbreviated New Drug Application (ANDA) for generic versions of the anticoagulant XARELTO® constitutes an act of infringement of a patent covering a specific method of use.
  • Technical Context: The technology concerns a once-daily oral dosing regimen for rivaroxaban, a direct factor Xa inhibitor, used for preventing and treating thromboembolic disorders such as stroke and deep vein thrombosis.
  • Key Procedural History: The litigation was triggered by a notice letter dated March 28, 2019, in which Macleods informed Plaintiffs it had submitted ANDA No. 213114 with a Paragraph IV certification, asserting that its generic product would not infringe the patent-in-suit or that the patent is invalid. The patent is listed in the FDA's "Orange Book" for XARELTO®, creating the basis for this Hatch-Waxman litigation.

Case Timeline

Date Event
2005-01-31 ’218 Patent Priority Date
2017-01-10 ’218 Patent Issue Date
2019-03-28 Macleods sends Notice Letter regarding ANDA submission
2019-05-10 Complaint Filing Date

II. Technology and Patent(s)-in-Suit Analysis

U.S. Patent No. 9,539,218 - "Prevention and Treatment of Thromboembolic Disorders"

  • Patent Identification: U.S. Patent No. 9,539,218, "Prevention and Treatment of Thromboembolic Disorders," issued January 10, 2017.

The Invention Explained

  • Problem Addressed: The patent describes the disadvantages of prior art anticoagulants. Heparin, administered parenterally, is described as non-selective with a high risk of bleeding, while oral vitamin K antagonists have a very slow onset of action and a narrow therapeutic index requiring time-consuming patient monitoring (’218 Patent, col. 2:1-18).
  • The Patented Solution: The invention is a method of treatment using a specific direct factor Xa inhibitor, rivaroxaban, administered orally no more than once per day (’218 Patent, col. 2:64-col. 3:2). The patent presents as surprising the finding that a once-daily regimen is effective for a compound with a plasma half-life of 10 hours or less, a characteristic that would typically suggest a twice-daily (bid) or thrice-daily (tid) administration schedule (’218 Patent, col. 2:6-10; col. 2:64-col. 3:2).
  • Technical Importance: This approach offers the convenience and improved patient compliance of a once-daily oral medication for treating serious thromboembolic disorders, while seeking to provide an effective and safe alternative to older anticoagulants (’218 Patent, col. 2:35-40).

Key Claims at a Glance

  • The complaint asserts infringement of at least Claim 1 (Compl. ¶33).
  • Independent Claim 1 requires:
    • A method of treating a thromboembolic disorder
    • Comprising administering a specific direct factor Xa inhibitor (rivaroxaban)
    • No more than once daily for at least five consecutive days
    • In a rapid-release tablet
    • To a patient in need thereof
    • Wherein the disorder is selected from pulmonary embolisms, deep vein thromboses, and stroke
  • The complaint does not explicitly reserve the right to assert dependent claims, but the infringement allegations are for "at least claim 1" (Compl. ¶33).

III. The Accused Instrumentality

Product Identification

  • "Macleods’ ANDA Products," which are 10 mg, 15 mg, and 20 mg rivaroxaban tablets submitted for FDA approval under ANDA No. 213114 (Compl. ¶9).

Functionality and Market Context

  • The products are described as generic versions of Plaintiffs' XARELTO® products (Compl. ¶1, ¶28). The infringement allegation is not based on a currently marketed product but on the future product that will be manufactured and sold if the ANDA is approved. The complaint alleges that the proposed labeling for the ANDA products will direct physicians and patients to use the tablets for indications including the treatment of deep vein thrombosis (DVT), pulmonary embolism (PE), and the reduction of stroke risk, in a manner that satisfies the claimed dosing frequency (Compl. ¶31).

IV. Analysis of Infringement Allegations

No probative visual evidence provided in complaint.

Claim Chart Summary

’218 Patent Infringement Allegations

Claim Element (from Independent Claim 1) Alleged Infringing Functionality Complaint Citation Patent Citation
A method of treating a thromboembolic disorder... The proposed labeling for Macleods' ANDA Products directs their use for treating thromboembolic disorders. ¶31 col. 11:1-2
...comprising administering a direct factor Xa inhibitor that is 5-Chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide... Macleods' ANDA Products contain rivaroxaban, which is the chemical compound identified in the claim. ¶29 col. 11:2-5
...no more than once daily for at least five consecutive days... The proposed labeling allegedly directs use in a manner that satisfies the "no more than once daily for at least five consecutive days" requirement. ¶31 col. 11:1-2
...in a rapid-release tablet... The complaint alleges, on information and belief, that the tablet dosage form of Macleods' ANDA Products satisfies this requirement. ¶30 col. 11:2-3
...to a patient in need thereof, wherein the thromboembolic disorder is selected from the group consisting of pulmonary embolisms, deep vein thromboses, and stroke. The proposed labeling directs use for treating or reducing the risk of stroke, deep vein thrombosis, and pulmonary embolism. ¶31 col. 11:5-7

Identified Points of Contention

  • Technical Questions: A primary question will be whether Macleods' formulation constitutes a "rapid-release tablet" as that term is used in the patent. The complaint alleges this on "information and belief" (Compl. ¶30), suggesting Plaintiffs may not have complete information on the generic product's dissolution characteristics, which will be a central issue for discovery and expert testimony.
  • Scope Questions: The infringement analysis hinges on the contents of the proposed label in the ANDA. A question for the court will be whether the instructions in that label, if followed by a physician or patient, would result in direct infringement of the method claim. Any differences between the claimed indications (pulmonary embolism, DVT, stroke) and the indications on the final approved label could be a point of dispute.

V. Key Claim Terms for Construction

  • The Term: "rapid-release tablet"
  • Context and Importance: This term is a specific technical requirement for the claimed method. Infringement under 35 U.S.C. § 271(e)(2) will depend on whether the product described in the ANDA is a "rapid-release tablet." Practitioners may focus on this term because its definition could be case-dispositive.
  • Intrinsic Evidence for Interpretation:
    • Evidence for a Broader Interpretation: A party could argue that, absent an explicit disclaimer, the term should be given its plain and ordinary meaning to a person of ordinary skill in the art, which might encompass a wide range of immediate-release formulations.
    • Evidence for a Narrower Interpretation: The specification provides an explicit definition: "In the context of the present invention, rapid-release tablets are in particular those which, according to the USP release method using apparatus 2 (paddle), have a Q value (30 minutes) of 75%" (’218 Patent, col. 8:20-24). This statement acts as a strong lexicographical guide, suggesting the patentee intended to define the term with this specific dissolution characteristic.

VI. Other Allegations

  • Indirect Infringement: The complaint alleges active inducement of infringement, stating that Macleods plans and intends for its product to be used in an infringing manner once the ANDA is approved (Compl. ¶38). The factual basis for this is the allegation that Macleods' proposed product labeling will instruct physicians and patients to administer the drug in a way that directly infringes the method claimed in the ’218 patent (Compl. ¶31, ¶33).
  • Willful Infringement: The complaint alleges that Macleods has had knowledge of the ’218 patent at least since sending its notice letter and filing its Paragraph IV certification (Compl. ¶28, ¶34, ¶37). The allegation is that despite this knowledge, Macleods intends to engage in infringing activities "immediately and imminently upon approval" of its ANDA (Compl. ¶36, ¶37).

VII. Analyst’s Conclusion: Key Questions for the Case

  • A core issue will be one of technical proof: can Plaintiffs demonstrate that the generic formulation described in Macleods' ANDA meets the specific dissolution profile required to be a "rapid-release tablet," as that term is explicitly defined in the '218 patent's specification?
  • A second central question will be label-based infringement: will the final, FDA-approved label for Macleods' generic rivaroxaban contain instructions that direct a user to practice every element of the patented method for the specific thromboembolic disorders recited in Claim 1? The outcome may depend on whether the defendant is able to "carve out" the patented method of use from its label.