API and IP Newsletter
Contents
Alzheimer’s Drug Market To Hit $13B As FDA Approvals And Insurance Coverage Escalate
Merck lawsuit opens new effort to cripple drug price negotiations
FDA approvals in May 2023
We follow FDA approvals in small molecule segment. We don’t give much emphasis on mechanism of action in this newsletter. But we cover, chemistry, brief intellectual property around the molecule. By studying IP we come to know about active players, what kind of API should be developed for Day-1 launch etc. We further analyse import export database and try to understand who potential early developers will be and who would be in position to file DMF soon.
FDA approved Sotagliflozin on 26 May 2023.
Sotagliflozin (INPEFA ) is an orally administered dual SGLT1/2 inhibitor used alongside insulin to improve glycaemic control in patients with type 1 diabetes mellitus.
The chemical name of sotagliflozin is (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)- 6-(methylthio)tetrahydro-2H-pyran-3,4,5-triol. Its molecular formula is C21H25ClO5S and its molecular weight is 424.94. The structural formula is:
Sotagliflozin is a white to off-white solid. It is practically insoluble in water. Each film-coated tablet of INPEFA contains 200 mg or 400 mg of sotagliflozin. The core of the tablet contains colloidal silicon dioxide, croscarmellose sodium, magnesium stearate, microcrystalline cellulose, and talc. The film coating for the 200 mg tablet contains indigo carmine aluminium lake, polyethene glycol, polyvinyl alcohol (partly hydrolyzed), talc, and titanium dioxide. The film coating for the 400 mg tablet contains hypromellose, lactose monohydrate, titanium dioxide, triacetin, and yellow iron oxide.
Brief IP situation
WO2009014970A1 : Relates to co-crystal of Sotagliflozin, wherein the pharmaceutically acceptable amino acid is L-phenylalanine, L-phenylglycine, or L-arginine.
WO2010009197A1 : Relates to amorphous and crystalline compounds of sotagliflozin.
Synthesis is reported in example 6.8 in WO2009014970A1
The basic raw material required will be 2-Chloro-5-iodobenzoic acid. This is common for Dapagliflozin, Empagliflozin. The same raw material is also used in synthesis of bexagliflozin. Bexagliflozin, sold under the brand name Bexacat, is an antidiabetic medication used to improve glycemic control in cats with diabetes.
So, all DMF holders of dapagliflozin and Empagliflozin will be potential developers of Sotagliflozin. However, lot of work would be needed for development of right polymorph, which would be suitable for Day-1 launch in different jurisdictions.
General information
Alzheimer’s Drug Market To Hit $13B As FDA Approvals And Insurance Coverage Escalate
The Alzheimer's disease (AD) market is projected to experience robust growth at a compound annual growth rate of 20% from $2.2 billion in 2020 to $13.7 billion in 2030 across the eight major markets,” GlobalData said in a new report Wednesday of the markets of the U.S., France, Germany, Italy, Spain, the United Kingdom, Japan and China.
News here.
Merck lawsuit opens new effort to cripple drug price negotiations
Why it matters: At a minimum, the IRA's drug pricing provisions probably won’t start on time, experts say. And a Merck victory could cripple the way the law forces manufacturers to the bargaining table with the threat of steep excise taxes.
News here
Intellectual Property
Amgen USA, Inc.’s Motion To Intervene For The Limited Purpose Of Asserting The Public Interest In Access To Judicial Records
Mylan filed a biosimilar application for aflibercept.
Innovator of aflibercept (Eylea) is Regeneron. In our brief understanding, the patent expiration (or Loss of Exclusivity rights) of aflibercept is in 2027 in the US.
Aflibercept is used to treat neovascular age-related macular degeneration (nAMD), a retinal disease that is one of the commonest causes of blindness throughout the world, affecting more than 200 million people globally.
As regards general litigation of biosimilars, once a biosimilar application is submitted within 60 days FDA confirms that the application is accepted. In the following 20 days applicant should provide confidential access to its application and other information on its manufacturing process. There is a set process established by case law for biosimilar applications under The Biologics Price Competition And Innovation Act (BPCIA).
In this write-up, we don’t intend to go into all aspects of the litigation process under BPCIA. We will stick to this specific case of aflibercept. In this case, the two-week trial is scheduled to start on 12 June 2023 in the District Court of the Northern District of West Virginia. Obviously, this litigation is between Regeneron and Mylan.
Now, Amgen is developing its own biosimilar candidate to Eylea known as ABP 938.
On 23 May 2023, Amgen moved the court Pursuant to Rule 24 of the Federal Rules of Civil Procedure, to intervene in the matter for the limited purpose of invoking rights of public access to judicial records in order to unseal documents that were previously sealed,
Amgen argued, most of the documents are sealed. Amgen criticized Regeneron and Mylan’s sealing practices in the litigation and stated that the parties have filed numerous documents under seal
the docket sheet does not list motions to seal with titles explaining what documents the party seeks to seal and the public cannot access the actual motions or pleadings.
In our understanding, this is the first time there is third-party intervention in BLA litigations where the third party is asking the Court to intervene in sealing practices. It will be interesting how the Court reacts to this request and whether there will be any impact in the hearing starting next week.
Court document here
