PTAB

IPR2025-00947

Azurity Pharmaceuticals Inc v. Helsinn Healthcare SA

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Petition
petition

1. Case Identification

2. Patent Overview

  • Title: Compositions and methods for treating centrally mediated nausea and vomiting
  • Brief Description: The ’357 patent claims methods for treating chemotherapy-induced nausea and vomiting (CINV) by administering a therapeutic regimen comprising netupitant (a neurokinin-1 (NK₁) antagonist), palonosetron (a 5-HT₃ antagonist), and dexamethasone (a corticosteroid).

3. Grounds for Unpatentability

Ground 1: Obviousness over Herrstedt and Bös - Claims 1, 5-10, and 17 are obvious over Herrstedt in view of Bös.

  • Prior Art Relied Upon: Herrstedt (a 2007 journal article summarizing CINV treatments) and Bös (Patent 6,297,375).
  • Core Argument for this Ground:
    • Prior Art Mapping: Petitioner argued that Herrstedt established the standard of care for preventing CINV was a triple-drug combination: a 5-HT₃ antagonist (like palonosetron), a corticosteroid (dexamethasone), and an NK₁ antagonist (aprepitant). Bös disclosed netupitant as a new, potent, and highly selective NK₁ antagonist useful for treating emesis. Petitioner contended that the claimed method of claim 1, which administers palonosetron, netupitant, and dexamethasone, was rendered obvious by simply substituting Herrstedt's NK₁ antagonist (aprepitant) with the improved one disclosed by Bös (netupitant). Dependent claims add limitations for specific types of chemotherapy (e.g., moderately or highly emetogenic) which Herrstedt also explicitly taught were treatable with this triple-therapy approach.
    • Motivation to Combine: A person of ordinary skill in the art (POSITA) would be motivated to improve the established triple-therapy regimen by replacing an existing drug (aprepitant) with a newer, more potent, and selective alternative from the same therapeutic class (netupitant) to achieve better antiemetic results.
    • Expectation of Success: As both aprepitant and netupitant are NK₁ antagonists that function through the same mechanism, a POSITA would have had a reasonable expectation of success in making the substitution, expecting at least comparable, if not superior, efficacy in preventing CINV.

Ground 2: Obviousness over Herrstedt, Bös, and Herrington - Claims 18-19, 25-27, and 30-32 are obvious over Herrstedt and Bös in view of Herrington.

  • Prior Art Relied Upon: Herrstedt, Bös, and Herrington (a 2008 clinical trial report).
  • Core Argument for this Ground:
    • Prior Art Mapping: This ground builds upon the combination of Herrstedt and Bös. The challenged claims add limitations requiring a single administration of netupitant and palonosetron that is effective for a five-day period. Petitioner asserted that Herrington taught a single, day-one dose of the NK₁ antagonist aprepitant was as effective as a multi-day regimen for preventing both acute and delayed CINV. The long half-life of netupitant, as taught by Bös, further supported the suitability of a single-dose administration.
    • Motivation to Combine: A POSITA would be motivated to add Herrington’s teachings to the base combination to simplify the treatment regimen. Herrington explicitly demonstrated that a single dose of an NK₁ antagonist was as effective as multiple doses, providing a clear reason to adopt this simpler protocol for improved patient compliance and convenience.
    • Expectation of Success: Herrington’s clinical study showed that a single-dose regimen was successful. A POSITA would reasonably expect that another long-acting NK₁ antagonist like netupitant would be similarly effective when administered as a single dose, as confirmed by Herrington’s results with aprepitant.

Ground 7: Obviousness over Herrstedt, Bös, Bonadeo, Herrington, and ALOXI - Claims 21-23, 33-35, 37-39, 43-44, and 46-51 are obvious over Herrstedt, Bös, and Herrington, further in view of Bonadeo and ALOXI.

  • Prior Art Relied Upon: Herrstedt, Bös, Herrington, Bonadeo (WO 2008/049552), and ALOXI (2008 FDA-approved product label).
  • Core Argument for this Ground:
    • Prior Art Mapping: This ground addresses claims reciting specific oral dosages and a single-unit dosage form (e.g., claim 21 requires about 300 mg oral netupitant and 0.50 mg oral palonosetron in a single unit). Petitioner argued that ALOXI, the FDA-approved label for oral palonosetron, taught the claimed 0.5 mg dose. Bös disclosed a broad oral dosage range for netupitant (10-1000 mg) that encompassed the claimed 300 mg, making the selection of this dose a matter of routine optimization. Bonadeo taught oral formulations of palonosetron, including soft-gel capsules containing more than one active ingredient, which would result in the claimed "single unit dosage form."
    • Motivation to Combine: A POSITA would be motivated to create a fixed-dose combination of netupitant and palonosetron, as taught by Bonadeo, to increase convenience, ensure patient compliance, and reduce the risk of medication errors. The ALOXI label provided the precise, FDA-approved oral dose for palonosetron, making it an obvious choice.
    • Expectation of Success: Formulating multiple known, co-administered drugs into a single dosage unit was a well-known and predictable practice in the pharmaceutical arts. Therefore, a POSITA would have a high expectation of success in creating a stable and effective single-unit oral dose containing the specified amounts of netupitant and palonosetron.
  • Additional Grounds: Petitioner asserted additional obviousness challenges based on various combinations of the primary references, including adding Hargreaves (a 2002 journal article) to teach that achieving a certain level of NK₁ receptor occupancy was an inherent and expected result of administering a therapeutically effective dose of netupitant.

4. Relief Requested

  • Petitioner requests institution of an inter partes review and cancellation of claims 1, 5-10, 17-39, and 43-51 of Patent 9,186,357 as unpatentable under 35 U.S.C. §103.