The Challenge
A small biotechnology company approached Patheon in search of an outsourcing partner company that could formulate and produce Clinical Trial Materials (CTM) for their relatively unstable small molecule with a very specific release profile requirement. The candidate molecule was preparing to enter Phase I clinical trials. The intention of the Phase I clinical trial, aside from establishing safety and tolerability, was to establish a target release profile and generate data that would contribute to a proof of concept decision for the molecule. Therefore better understanding the release profile and ultimately speed to clinic were key considerations with this project.

The Solution
Patheon worked with the customer to develop a comprehensive staged formulation strategy that would address their compound’s unique physical properties while meeting their aggressive clinical development timetable.

Patheon first formulated the customer’s molecule in a Powder In Bottle (PIB) format specifically for the Phase I trial. This approach reduced excipient compatibility issues and expedited the initiation of Phase I clinical trials which provided valuable insight into the characteristics of the drug in humans.

Patheon’s development team then focused on the development of an immediate release tablet formulation that was intended to allow the prompt initiation of subsequent clinical trials for efficacy. These tablets were also determined to be suitable for dissolution and bioavailability studies. Patheon’s experienced scientists utilized advanced in-house analytical technologies to assess the release profile and molecular properties of the compound.  This information was then used to develop a unique bi-layer tablet formulation that addressed the compound’s instability and complex release profile.

This staged development process was designed by an extensive team of scientists at Patheon using sophisticated in-house analytical tools and formulation experience to arrive at a viable and scalable finished dosage form for this unique molecule.

The Outcome
Only two years after the customer’s preclinical work began, and several clinical trials later, Patheon’s scientific team was formulating a bi-layer tablet dosage form that would overcome the formulation challenges associated with the molecule and would also highlight the product’s uniqueness in the marketplace. The formulation strategy that was implemented allowed the customer to advance quickly through various clinical trials while simultaneously moving towards a dosage form that would address their compound’s specific requirements as it moved towards commercialization.

The clinical and market success of this drug candidate is key to the success of the customer company’s overall growth strategy. Through the generation of positive early phase trial data and the development of a stable formulation , the customer believes that the market value of the drug, now in Phase II clinical trials, has increased dramatically since development began with Patheon.