Cristal Therapeutics’ Proprietary CriPec Nanomedicine Platform and Promising Preclinical Data Highlighted in Three Recent Publications

Cristal Therapeutics, has 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 stabilised, to prevent premature disintegration. Particularly upon temporarily covalently entrapment of drugs within these nanoparticles (i.e., 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 tumour 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 tumour accumulation, followed by locally more extended exposure as a result of sustained release of docetaxel over time. In tumour bearing mice, CriPec docetaxel accumulated at least 20 times more in tumour tissue compared to an equivalent dose of the commercially available docetaxel (Taxotere). A superior survival benefit was demonstrated in tumour xenografts and even complete regression has been achieved upon a single administration of CriPec docetaxel. These remarkable antitumour effects are attributed to the enhanced tumour 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 one 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 tumour 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).