API and IP Newsletter
Contents
Investment in R&D in the pharmaceutical industry achieved its second-best record in 2020
Food and drinks manufacturers come under pressure to make healthier products
FDA approval in November 2021
We follow FDA approvals especially for small molecules.
In November FDA approved Pafolacianine, sold under the brand name Cytalux, is an optical imaging agent.
Pafolacianine marketed as a tetrasodium salt referred to as pafolacianine sodium. Chemically, pafolacianine sodium is (S)-2-(4-(((2-amino-4-oxo-3,4- dihydropteridin-6-yl)methyl)amino)benzamido)-3-(4-(((E)-2-((E)-2-(3,3-dimethyl-5-sulfonato-1-(4- sulfonatobutyl)-3H-indol-1-ium-2-yl)vinyl)-6-((E)-2-(3,3-dimethyl-5-sulfonato-1-(4- sulfonatobutyl)indolin-2-ylidene)ethylidene)cyclohex-1-en-1-yl)oxy)phenyl)propanoate hydrate Tetrasodium. Pafolacianine sodium has a molecular formula of C61H63N9Na4O17S4, a molecular mass of 1414.42 g/mol and has the following structure:
CYTALUX (pafolacianine) injection is a sterile, non-pyrogenic, dark bluish green, clear aqueous solution for intravenous use. Each vial contains 3.2 mg (2 mg/mL) pafolacianine (equivalent to 3.4 mg pafolacianine sodium),14.4 mg sodium chloride, 0.23 mg potassium phosphate monobasic, 1.27 mg sodium phosphate dibasic heptahydrate in 1.6 mL volume. The pH is adjusted with sodium hydroxide and/or hydrochloric acid and is between 7.1 to 7.8.
Over 700,000 patients undergo cancer surgery every year in the US and 40% of surgical patients have a recurrence of locoregional disease within 5 years.
Method of manufacturing of pafolacianine is covered in WO2014149073A1 comprising several steps outlined in paragraph 22.
MSN, Sai, Glenmark, DRL are ordering development quantities of 7-Azabenzotriazole derivatives (HATU) mainly from China, and these companies could file DMF soon.
General information
Investment in R&D in the pharmaceutical industry achieved its second best record in 2020
The investment of the pharmaceutical industry in drug research and development in Spain exceeded 1,160 million euros in 2020, according to the latest Survey on R&D Activities that Pharmaindustry performed among its associates every year. Despite the exceptional difficulties caused by the pandemic, the indicator holds and achieves the second highest figure in history, after the record set in 2019 with 1,211 million euros.
News here.
Food and drinks manufacturers come under pressure to make healthier products
Obesity litigation cases against food and drinks manufacturers and fast-food giants are likely to increase as plaintiffs find new tactics to hold them to account.
Following the successes seen in cases against Big Tobacco and Big Pharma for the opioid crisis we are now seeing a new era of litigation. These mass tort lawsuits have changed the litigation landscape and are changing how social harms are addressed.
News here.
Intellectual Property
T 1875/18 (Apixaban/BRISTOL-MYERS) of 7.5.2021
Article 123 (2) in EPC relates to broadening. The European patent application or European patent may not be amended in such a way that it contains subject-matter which extends beyond the content of the application as filed.
Claims of EP2538925B1 and Auxiliary claims flied were as follows:
"A tablet or capsule comprising a pharmaceutical composition, wherein the pharmaceutical composition comprises apixaban and a pharmaceutically acceptable diluent or carrier, wherein the apixaban is in particulate and crystalline form and the individual apixaban particles, whether the particles exist singly or are agglomerated, have a D90 equal to or less than 89 microns as measured by laser light scattering."
Eleven oppositions were filed against the grant of the patent on the grounds that its subject-matter lacked novelty and inventive step, that the claimed invention was not sufficiently disclosed and that the patent comprised subject-matter extending beyond the content of the application as filed Article 123 (2).
The appeal filed by the patent proprietors lies against the decision of the opposition division posted on 09 May 2018 to revoke the patent. The decision was based on the main request and auxiliary requests 1-5.
Table 3 and paragraph 6 in patent as filed in priority document are as follows:
Considering that Table 3 does not exemplify a tablet composition comprising up to 5 mg apixaban as described in paragraph [0006] of the application as filed and defined in claim 1 of the main request and having regard to the relevant relationship between the ingredients and their amounts listed in Table 3, the Board opined that the skilled person would not directly and unambiguously derive from the application as originally filed that the disclosure in paragraph [0006] of the tablet compositions comprising up to 5 mg apixaban should be combined with the features of the tablet compositions of Table 3, let alone with the ingredients listed in the left column of Table 3 abstracted from their relative amounts.
The application as originally filed makes no other mention of this specific combination of components.
The claims of each of the auxiliary requests involve a similar definition of a tablet composition comprising 5 mg or less apixaban in combination with the ingredients listed in the left column of Table 3 abstracted from their relative amounts as defined in claim 1 of the main request.
No further argument regarding the basis for this combination in the claims of the auxiliary requests was provided by the patentee and no such basis is evident to the Board.
Accordingly, the Board concludes that the claims of the auxiliary request 1-5 do not comply with the requirement of Article 123(2) EPC for the same reason as claim 1 of the main request and the patent was revoked. (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.
