TRUE GENERICS FOR INJECTABLE controlled RELEASE DRUGS
Xbrane has developed what is expected to become the worlds first generic to a leading GnRH analogue with formulation for controlled release of the active substance through encapsulation in microspheres composed of a biodegradable polymer.
XBRANE MICROSPHERE TECHNOLOGY
Many drugs require frequent administration to have its desired effect in the human body. To make administration of these drugs more convenient for the patients and more cost efficient for the health care systems different technologies to achieve a controlled release of the active substance in the drug over a 1-6 month time-period after injection have been developed. One such technology is based on encapsulation of the active substance in microspheres of a biodegradable polymer. When the microspheres are injected they create a depot and as the polymer degrades over time in the body the active substance is released.
This technology has contributed to significant value to patients and health care systems over time, but also to the originators behind these drugs as the technology has provided certain protection against generic competition. To develop a generic version of these drugs the release pattern of the active substance needs to be imitated closely enough to fall within the strict regulatory requirements. The release pattern depends on the composition and hardness of the microspheres, which is a result of multiple different production process parameters. The difficulty therefore lies in finding the exact formulation and production process that results in microspheres that closely enough imitates the release pattern of the originator drug. This is exactly Xbranes focus and expertise. After more than 5 years of research and development we have developed Spherotide which is expected to become the worlds first generic to a leading GnRH analogue with a formulation for controlled release. In addition to Spherotide we are working on four other generic candidates to important drugs with a controlled release formulation based on microsphere technology.
Why It Is Difficult
The regulatory requirement for market approval of generic drugs in highly regulated markets is related to proving bioequivalence in clinical trials. A generic drug candidate is considered being bioequivalent to an originator drug if the development of the plasma concentration of the active substance over time after administration in humans is similar enough compared to the originator drug according to strict criteria set by the regulatory authorities. In controlled release formulations the plasma concentration of the active substance over time is determined by the release mechanism of the active substance into the circulatory blood system. The release mechanism is determined by the composition of the microspheres, hence the difficulty in developing a generic drug to an originator drug with a controlled release formulation is to closely enough imitate the microsphere composition of the originator drug. This is a difficult task as the composition is determined by the exact quantities of the ingredients, the production process (e.g. coacercvation or emulsion) and multiple production process parameters such as ph, temperature and revolution speed. An experimental development process is required with frequent comparative in-vitro and in-vivo release tests.
Deep expertise and understanding of the production process is required in order to be successful – something Xbrane has built over time and enabled development of what is expected to become the worlds first generic drug to a leading GnRH analogue.
Controlled Release Drugs
Spherotide* Decapeptyl®/ Trelstar®/Pamorelin®
Spherotide Decapeptyl®/ Trelstar®/Pamorelin®
Spherotide 3M Decapeptyl®/ Trelstar®/Pamorelin®
Decapeptyl, Trelstar, Pamorelin, RisperdalConsta, Bydureon, LupronDepot and Sandostatin are registered trademarks of their respective owners.
* Less regulated markets
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