API and IP Newsletter

 Contents

• Patent filings by Alembic

• General information

• Seven Trends Shaping the Future of Pharmaceutical Formulation Development

• Making pharmacy more sustainable

• Intellectual Property

• Rifaximin tablet composition patent revoked by EPO

Patent filings by Alembic

We analyse IP portfolio of many Indian companies. This week we analysed patent portfolio of Alembic Pharmaceuticals Limited.

Some of our observations are as below.

Publication Number	Sidvim comments
WO2019150253A1	The invention relates to solid state forms of Venetoclax, particularly relates to alkali metal salt and/or DMF solvate form of Venetoclax or its salt. It claims the process for the preparation Venetoclax crystalline forms. Venetoclax was approved in 2016. Alembic filed DMF in 2019 and must be using this process in their DMF filings
WO2022090953A1	The invention relates to pharmaceutical compositions comprising a solid dispersion of ponatinib. It further claims the process of preparation of such compositions. The concern about reported adverse effects, led the FDA and Ariad Pharmaceuticals to abruptly withdraw ponatinib from the market in October 2013. Two DMFs filed.
WO2021028791A1	The invention relates to the process of preparation of Ivosidenib intermediates. Also provide process of preparation of amorphous form of Ivosidenib. Further, the invention provides process of preparation of pure chiral Ivosidenib  Ivosidenib was approved in 2018, Alembic recently filed DMF, the process protected by this invention must be part of the DMF.
WO2020003196A1	The invention was directed to a stable pharmaceutical composition comprising axitinib in crystalline polymorphic form IV. The composition is bioequivalent to the commercially available axitinib tablets (INLYTA®). Three DMFs filed for axitinib. Alembic might file DMF soon or this API must be part of their ANDA submissions.
WO2019049038A1	The invention was directed to process for characterization of Glatiramer acetate.  It further provides statistical methods for characterizing and classifying Glatiramer acetate, which is very complex API.

General comments:

1. Alembic is working with hard to make molecules

2. Processes filed in DMFs are generally protected by patent families.

3. Lot of research activities around new polymorphs 

4. Main target category seems to be tinibs and other oncology molecules. 

General information

Seven Trends Shaping the Future of Pharmaceutical Formulation Development

1. Continuous manufacturing and moving from powder to tablet

2. Modelling and predictive approaches for solid formulation

3. Additive manufacturing’s impact on production

4. Overcoming solubility challenges of poorly-soluble APIs

5. Improving protein purification

6. Highly concentrated protein formulations for subcutaneous application

7. mRNA technology: status and future potential

News here.

Making pharmacy more sustainable

According to the article, humans are consuming more pharmaceuticals than ever before; in 2020, the volume of medicines used worldwide reached 4.5 billion doses, and consumption continues to rise. What is more, drugs are also administered to a wide range of livestock and domestic animals. Although the use of pharmaceuticals brings enormous benefits to human and animal health, it has also led to the increased pharmaceutical contamination of ecosystems across the world.

News here.

Intellectual Property 

Rifaximin tablet composition patent revoked by EPO

EP2618819 patent relates to rifaximin tablet composition, was issued to Alfasigma S.p.A.

Claim was as follows: 

 

1. Pharmaceutical composition in the form of tablets comprising

i) gastroresistant microgranules containing rifaximin β alone or in a mixture with other crystalline, hydrate, solvate or amorphous forms of rifaximin, in an amount comprised between 100 and 800 mg,

ii) pharmaceutically acceptable extragranular excipients, and optionally iii) a film- forming coating

whereby the total amount of extragranular excipients contained in the tablet does not exceed 30% by weight of the tablet.

Sandoz challenged. At first instance The opposition division upheld the patent. 

 

Sandoz  filed an appeal against this decision, requesting that it be set aside and that the patent be revoked in its entirety. Alfasigma S.p.A. requested that the appeal be dismissed and filed auxiliary requests with the reply to the appeal.

 

In preliminary opinion Board of Appeals was not very positive for Alfasigma S.p.A. The Board of Appeals  remarked that irrespective of which rifaximin form is mentioned in example 7 of  prior art WO 2006/094737 the use of rifaximin in polymorph form beta, as a mixture in the pure form, is explicitly considered on page 14 line 1-7 in prior art WO 2006/094737. Furthermore as per the Boards of Appeals use of tablet is also envisaged in WO 2006/094737. (Here)

 

In view of this written opinion from Board of Appeals, Patentee Alfasigma S.p.A,  by letter dated 22 September 2022 stated that they no longer approved the text in which the patent was granted or of any amendment filed during the opposition/appeal proceedings, and that they would not be submitting any amended text. Furthermore, they  withdrew their request for oral proceedings.

 

It is established case law that, if the patent proprietor states in opposition or appeal proceedings that he no longer approves the text in which the patent was granted and will not be submitting an amended text, the patent is to be revoked.

 

Hence patent was revoked. Decision here.