Paragraph IV Patent Certifications

On January 30, 2017, FDA published Paragraph IV patent certifications to the following drugs.

Drug Name Dosage Form Strength RLD Date of Submission
Aprepitant for Oral Suspension 125 mg/Kit Emend 11/23/2016
Liraglutide Injection 18 mg/3 mL prefilled syringe Victoza 12/12/2016

I. The following patents are listed for Emend (Oral Suspension) in Orange Book

Patent No Patent Expiration Remarks
6,096,742 Jul 1, 2018 Relates to polymorphic Forms I and II of Aprepitant
8,258,132 Sep 26, 2027 Relates to composition comprising Aprepitant with a specific particle size diameter

II. The following patents are listed for Victoza in Orange Book

Patent No Patent Expiration Remarks
6,004,297 Jan 28, 2019 Relates to an injection syringe for apportioning set doses of a medicine from a cartridge
6,268,343 Aug 22, 2022 (inclusive of PTE) Relates to product
6,458,924 Aug 22, 2017 Relates to product
7,235,627 Aug 22, 2017  Relates to product
8,114,833 Aug 13, 2025 Relates to Formulation and MOT
8,846,618 Jun 27, 2022 Relates to Formulation and a process for its preparation
9,265,893 Sep 23, 2032  Relates to Technology
RE41956 (6,582,404) Jan 21, 2021  Relates to Technology
RE43834 Jan 28, 2019  Relates to Technology

Apotex Loses its IPR2015-00419 Against Merck’s Fosaprepitant

June 25, 2015 Judges LORA M. GREEN, ZHENYU YANG, and ROBERT A. POLLOCK denied Institution of Apotex IPR against Merck’s US 5,691,336 which claims Fosaprepitant Dimeglumine.

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IPR was filed by Apotex on Dec 11, 2014 against Merck’s US 5,691,336 A which claims Fosaprepitant Dimeglumine and also listed in OB for Fosaprepitant Dimeglumine.

US ‘336 was filed by Merck on Sep 8, 1995 claiming Fosaprepitant Dimeglumine generically which was issued on Nov 25, 1997. US ‘336 is set to expire on March 4, 2019 (including patent term extension of five years).

Fosaprepitant Dimeglumine is a prodrug of Aprepitant and it is a P/neurokinin 1 (NK1) receptor antagonist which is developed and patented (US 5,691,336) by Merck. Fosaprepitant Dimeglumine is approved in US on Nov 12, 2010 which is marketed under the brand name EMEND. The structure of Fosaprepitant is shown below:

Apotex challenged the validity of claims of US ‘336 as it is obvious over the the following documents:
i) Dorn’s US 5,637,699 which discloses Aprepitant and its use as Tachykinin receptor antagonist.
ii) Murdock’s US 5,070,082 which teaches the use of phosphoramidate moiety in the preparation of prodrugs with enhanced aqueous solubility.

Apotex argued that an ordinary skilled person will modify Aprepitant which is well known from Dorn ‘699 with the teachings of Murdock ʼ082 to derive Fosaprepitant. However, on June 25, 2015 Patent Trial And Appeal Board rejected Apotex requisition for an inter partes review of US ’336, stating that Petitioner has failed to sufficiently explain why, at the time of the ’336 patent invention, a skilled artisan would have chosen compound 96 of Dorn ’699 to further develop its prodrug, which is the subject matter of the challenged claims. Therefore, it is concluded that Petitioner has not established a reasonable likelihood it would prevail in showing any of the challenged claims would have been obvious over Dorn ’699 and Murdock ’082.

Finally, the board concluded that Petitioner has not established a reasonable likelihood it would prevail in showing any of the challenged claims would have been obvious on either of these grounds. So the IPR is dismissed.

Thanks to Harshavardhan.K for suggesting me and helping me to post this article.

Harsha.K
Harsha.K