On 22nd November 2016, the guest was Professor John Leonard and lecture

introduced us to Pharmaceutical API Route design and chemical

development. Initially he quoted the definition of drug. The drug is divided
into two parts in the active part and in the formulation. In the active part
researchers see that the studying chemical compound has useful
pharmaceutical properties and thus may be acting as a drug in the future.
In the formulation is the process where a can be moved to the site of
action which is not dissolved in the stomach but then absorbed by the
bloodstream. Example of a chemical compound is the ZD6126 Tubulin
Inhibitor which acts as an anti-cancer drug. Then reported how chemical
compound start to developed. Chemical Development begins once it has
been discovered that a compound has the ability to become a drug. Also
quoted the main steps for API development as well as the basic key
functions of R&B. Professor John emphasized the synthesis campaigns API.
First Campaign normally used 10-100g API .The API used for early
Toxicological and Metabolic studies before drug goes into Development
and the cost is unimportant. Second Campaign use normally ~2-5 Kg API.
Apart of toxicological, metabolic and formulation studies, the compound
has to be pure enough for dosing to people. However speed is critical
importance because other investigations are waiting for material.
Campaign three normally use 50-150 Kg but is much more demanding. In
campaigns 4, 5, 6 Processes must be robust, reliable and predicable all
process parameters must be defined and understood. API must be very
high quality and high specification. Final regulatory documents must be
produced and reliable manufacturing guaranteed. Last part of the lecture
was on the factors underlying route design. The six basic areas are:
Safety, Economic, Legal, Environmental, Control and Throughput. He
emphasised that issues with any of these factors will compromise the
viability of a route and have cost implications. If talk about the best route
design that would be a route which offers the best balance between
operational, environmental, legal and economic factors at the current
state of knowledge. As an example of effective route design: The anti-
cancer (MEK Inhibitor) development drug. Concluded, synthetic Route
Design is the core activity which underpins the rest of chemical
development the process description is recipes that define the
manufacturing processes. The most expensive API is manufactured for use
in clinical trials studies.