TECHNOLOGY

Novel microcrystal formulation

Historically, one of the greatest barriers preventing long-acting injectable GnRH antagonists from entering the market was the inability to create a suitable formulation for injection. Such a formulation must offer sufficiently sustained release of the drug with good injection site tolerance. This is difficult to achieve with GnRH antagonists because of the low solubility of the drug class coupled with the volume of active substance required to have an effect.

Teverelix TFA is able to overcome these challenges by forming a suspension of microcrystals: these allow a high concentration of drug to be delivered with a low volume compared with other GnRH antagonists. Teverelix TFA is delivered as a depot injection which releases the drug slowly and allows longer intervals between doses. Finally, our clinical data to date indicate good injection site tolerance. These qualities make teverelix TFA an easy to inject, long-acting GnRH antagonist with a novel formulation. We believe that this strongly positions teverelix TFA to become the best in class GnRH antagonist.

Patent information

The formation of a microcrystal suspension is integral to the use of teverelix TFA as a long-acting GnRH antagonist and this is covered by patent protection until 2022/2023. Antev has filed new patents to extend this protection through to 2038. As a new chemical entity, teverelix TFA will be protected by an additional five-year period of data exclusivity. Antev has further pending patent protection covering the use, route of administration, and aspects of manufacturing of teverelix TFA. The specialized team has a significant body of proprietary know-how and technical knowledge and is continuously working to expand the intellectual property estate.