API and IP Newsletter
Contents
FDA approvals in September 2021
Mobocertinib approved in September 2021 to treat locally advanced or metastatic non-small cell lung cancer with epidermal growth factor receptor.
Example 2 of WO2019222093 family covers (dimethylamino)ethyl) methyl)amino)-2-methoxyphenyl) amino)-4-( 1 -methyl- 1 H-indol-3- yl)pyrimidine-5-carboxylate (Mobocertinib) succinate polymorphic Form-I (92% yield) as an off-white solid. Purity: 99.8%.
This must be the marketed product.
General information
Indian cos asked to bid for molnupiravir deal
Unitaid, a global health initiative that works with partners to bring about innovations to prevent, diagnose, and treat major diseases in low- and middle-income countries, and Unicef have asked eight Indian generic manufacturers to participate in a rolling tender to supply the experimental covid-19 drug molnupiravir to extend access for the antiviral in low- and middle-income countries.
News here.
Optimus Group completes phase 3 clinical trial of anti-COVID drug
Molnupiravir is an affordable option to neutralise the disease in minimum time.
Optimus Group based in Telangana has announced the successful completion of the much-awaited Molnupiravir oral capsule phase 3 clinical trials on Thursday.
News here.
Intellectual Property
Dapagliflozin case in USA
There are several patents listed in OB. Most of these patents were issued to BMS. In February 2014, AstraZeneca announced the acquisition of Bristol-Myers Squibb’s interests in the companies’ diabetes alliance.
Zydus filed ANDA in January 2018 and AstraZeneca sued Zydus. Farxiga (Dapagliflozin) had U.S. sales of $569 million in 2020, about 2.2% of Astra’s total revenue.
During the trial the ligation was narrowed down to validity of claims 1-3, 14, and 16 of the OB listed patent US 6,515,117. The ‘117 patent relates to compounds, composition and MoT of diabetes by inhibition of sodium dependent glucose transporters (SGLT2)
The core pharmaceutical composition recited by the claims is shown below:
Prior art, WO2001027128 (WO '128) has example 12 with structure as below
WO2001027128 (WO '128) does not provide data of comparative biological activity (i.e., SGL T2 inhibition) for any of its listed compounds.
Based on the lack of biological activity data in WO '128 and the teaching away from the use of larger alkoxy groups at the 4-distal position by Hongu and Kees (which were other prior art references cited), a POSA (a person skilled in art) would not have been motivated to swap the distal 4- methoxy in WO '128 's Example 12 with an ethoxy (which would otherwise yield the molecule claimed in the ' 117 patent, ie Dapagliflozin).
Given the lack of available biological data for candidate SGL T2 inhibitors and the unpredictability of changes in biological activity due to modification of chemical structure, a POSA would not have had a basis to expect dapagliflozin to exhibit better glucose-reducing effects than the closest prior art, such as Example 12.
Hence, the Court rejected Zydus’s arguments that the patent shouldn’t have been issued because it covers an obvious variation of an old idea.
Now generics must wait till October 2025 in US!
Court document here.
Disclaimer
Sidvim LifeSciences Private Ltd has taken due care and caution in developing this document. Since the data used for analysis in this document is based on the information available in the public domain, its adequacy or accuracy or completeness cannot be guaranteed. This document is for information only and Sidvim is not responsible for losses that may or may not arise due to any decisions made based on the same. No part of the document shall constitute or be represented as a legal opinion of any kind or nature. No warranties or guarantees, expressed or implied, are included in or intended by the document, except that it has been prepared in accordance with the current generally accepted practices and standards consistent with the level of care and skill exercised under similar circumstances by professional consultants or firms that perform the same or similar services.
