Pharmaceutical Invention 1st Class Flashcards
What investigation carried out by European Commission compared the price of generic companies to pharmaceutical prices.
The investigation carried out by European Commission has shown that the average generic price 2 years after its entry is around 40 % below the price of the former brand name products.
What was Genetech argument when defending Trehalose as part of the formulation.
Professor Arvinte (Genentech skilled person working in biotechnology company) argued that while literature suggest trehalose was common general knowledge its safety when administered in the parenteral form to humans was not common knowledge (e.g. idea of possible toxicity and regulatory issues).
Reference: http://www.bailii.org/ew/cases/EWHC/Patents/2014/3857.html#para36
What was patient compliance like for using creams/ointments in the Teva vs Leo case.
What was the name of the patent that disclosed the use of Arlamol E and the reason for using Arlamol E.
Turi patent (1978) claims that Arlamol E was non-irritating to the skin.
What theory of analysis can be put in place when justify the reason why Arlamol E was an invention worth patenting.
Pozzoli structured analysis.
What were the principles guiding the court of appeals decision in the Teva v Leo case.
Choice of excipient was beneficial and not arbitrary. A skilled person would have no reason to believe that there would’ve success when combining Armalol E with the two active ingredients. Nothing in the previous art pointed towards Arlamol E being the excipient of choice.
There was a long felt want from clinicians and patients for a combination product and no explanation as to why there was no solution to the pH instability issue seen with Betamethasone and Calcipotriol.
What was the guiding principle in the decision made in Hospira v Genentrech case.
A formulator would be motivated based on Phase II trial evidence to make Trastuzumab into a lyophile and the choice of excipients was arbitrary. Prior art (Draber et al. In 1995) state the use of trehalose in IgM antibodies freeze-dried.
There was lack in inventive step: Regular screening methods and excipients were part of CGK and test were routine.
There was a degree of confidence that the screening methods would produce a formulation that would work.
What are the challenges associated with APIs with low solubility (Gedeon v Bayer).
Low solubility APIs run a risk of incomplete absorption due to incomplete dissolution.
What are the challenges are faced regarding APIs unstable in acidic conditions (Gedeon v Bayer).
What are the ways to overcome (a) poor solubility (b) acid labile APIs (Gedeon v Bayer).
What is the desired characteristic of oral contraceptive and what made Drospirenone (DSP) difficult to formulate (Gedeon v Bayer).
Oral contraceptive must attain 100% effectiveness in inhibiting ovulation, given the consequences of an ineffective dose leading to unwanted pregnancy. Therefore DSP poor solubility, acid labile nature and ability to be hydrolysed in alkaline condition presented a challenge for formulating drug with high bioavailability.
What test are carried out to determine in vivo bioavailability (Gedeon v Bayer).
In-vitro testing with dissolution paddle.
How did Bayer actually come to realise that DSP did not need to protected by an enteric coating.
This is where the inventor story emerges. The bioavailability of DSP administered in three forms: (a) intravenously; (b) enteric coated tablets (c) tablets which were not enteric coated at all. Based on the in vitro studies the formulation team clearly had no anticipation of success for the uncoated formulation. Thus it came to them as surprise when the bioavalibiltiy of the uncoated formulation provided to be statistically no different of that enteric coated drug. Despite DSP being acid labile and in fact not degrading in vivo.
What was the underpinning principle in the Gedeon Richter v Bayer Schering case.
The move from prior art to invention was a ‘Speculative jump in the dark’
Also there was no clear explanation of how the claimed formulation worked> success of the claimed formulation was unlikely to be predictable.
How was thalidomide repositioned.
Off‑label usage and pharmacological analysis.
🔘 Thalidomide had anti-tumor necrosis factor alpha activity. Erythema nodosum is a hypersensitivity type of reaction so thalidomide modulates it.
🔘 Whereas, in multiple myeloma, Thalidomide has immunomodulatory effect and found to have powerful anti-angiogenic drug, inhibiting the growth of blood vessels in tumors.
(a) Give an example of drug that failed repurposing. (b) what point did it fail repurposing. (c)What was the outcome of repurposing.
Use an example of drug to describe the potential problems with re purposing drug
