Cristal Therapeutics Highlights Proprietary CriPec Nanomedicine Platform & Promising Data

Cristal Therapeutics recently announced the publication of three articles on CriPec-based nanomedicines in Nano Today, Journal of Controlled Release, and Biomaterials. The publications are co-authored by Dr. Cristianne Rijcken, Founder and CSO of Cristal Therapeutics, and clearly demonstrate the superior therapeutic performance of CriPec nanomedicines in preclinical models as well as the position of the CriPec platform in the overall nanotherapeutics field.

In the first publication by Talleli et al in Nano Today, Dr. Rijcken provides her vision on the translational development of polymeric nanoparticles. Many different micelles have been developed in recent years, and some of them have steadily progressed into clinical evaluation. Increasing evidence suggests that for efficient drug targeting, the micelles need to be stabilized, to prevent premature disintegration. Particularly upon temporarily covalently entrapment of drugs within these nanoparticles (ie, the CriPec platform), promising efficacy in various animal models has been demonstrated. Recent advances in this field, including tailorable drug-release kinetics at the target site as well as potential applications and the clinical development path are described.

The second publication of Hu et al on CriPec docetaxel (the lead candicate of Cristal Therapeutics) in Biomaterials describes the complete regression of breast tumor with a single dose of docetaxel-entrapped core-cross-linked polymeric micelles.
CriPec® docetaxel is a nanoparticle with covalently entrapped docetaxel, designed to have a long blood circulation profile and significantly enhanced tumor accumulation, followed by locally more extended exposure as a result of sustained release of docetaxel over time. In tumor-bearing mice, CriPec docetaxel accumulated at least 20 times more in tumor tissue compared to an equivalent dose of the commercially available docetaxel (Taxotere). A superior survival benefit was demonstrated in tumor xenografts and even complete regression has been achieved upon a single administration of CriPec docetaxel. These remarkable anti-tumor effects are attributed to the enhanced tumor accumulation and anti-stromal activity. In addition, the preclinical data showed that CriPec docetaxel exhibited superior tolerability as compared to Taxotere.

In the third publication of Hu et al in the Journal of Controlled Release article, Dr. Rijcken and colleagues demonstrated the applicability of the CriPec platform for peptides and the ability to achieve therapeutically relevant blood levels for more than 1 week upon only a single intravenous injection to rats. Meanwhile, CriPec has also been successfully combined with larger peptides (>30 amino acids).

The transiently stable entrapment of peptides in CriPec nanoparticles prevents burst release and undesired peak levels, protects peptides against degradation, and enables sustained systemic levels. In addition, since the pharmacokinetic profile of a CriPec nanoparticle is not dependent on the entrapped compound, these CriPec peptide products are also expected to display superior tumor tissue targeting.

“These findings clearly demonstrate the added value of the CriPec platform, being the improved therapeutic index in oncology for various drug molecules. Relative to the worldwide developments in nanomedicine, the CriPec platform is really state-of-the-art and capable of translating the biological requirements into a fully tuneable nanomedicine with superior therapeutic outcome,” said Prof. Dr. Twan Lammers, Head of the Department of Nanomedicine and Theranostics at RWTH Aachen University Clinic (Germany).

Cristal Therapeutics, established in Maastricht, focuses on the development of nanomedicines with improved therapeutic efficacy. The pipeline comprises of products based on drugs in development and also on the market, in combination with the patented CriPec platform, for the treatment of various diseases, including cancer and chronic inflammatory disorders. For more information, visit www.cristaltherapeutics.com

CriPec® transforms drugs into polymeric nanoparticles via an innovative process. These nanoparticles provide improved distribution throughout the body. The substantial improvement of the efficacy and safety of the drugs entrapped in CriPec® nanoparticles has been demonstrated in several preclinical disease models. Cristal Therapeutics has demonstrated the benefits of CriPec® for various molecules, including peptide drugs, as well as for applications such as active targeting. The results to date have contributed to the company’s present innovative product portfolio.