THERABULLET - Pt(II) complexes derived from a new class of chlorines: Validation of these theranostic agents for cancer.

Overview

Project Summary

The TheraBullet proposal aims to validate and exploit the scientific and technological developments resulting from the research project "Novel Fused Ring Tetrapyrrolic Macrocycles as Highly Efficient Theranostic Agents for Cancer - PDT-NanoBullet" (PTDC/QEQ-MED/0262/2014). The current development of Clor-Pt1.0 corresponds to the third technology readiness level (TLR 3) at which the experimental proof of concept was carried out. With the TheraBullet proposal we intend to carry out experimental validation, reaching TRL level 4. The ultimate goal of developing this technology is to achieve personalised treatment.

Main Goals

In order to move forward with the Clor-Pt1.0 development process, it is necessary to:

A) Optimise the lead compound; that is, carry out molecular modelling of the chemical structure in order to obtain the desired pharmacokinetic properties, namely absorption, distribution, metabolism and excretion (ADME). Specifically, the aim is to reduce the maximum accumulation time in the tumour (currently 7 days), increase the tumour/skin ratio (evaluated at 2.5) and increase the elimination speed (currently 21 days).

B) Producing quantities on a multi-gramme scale, which is necessary for determining pharmacokinetic parameters in vivo and, above all, for subsequent progression to higher TRL levels. Production on a multi-gramme scale must be carried out in accordance with pharmaceutical industry standards (GMP) and also in accordance with the sustainability requirements currently governing the pharmaceutical industry. This requires optimising the process according to the principles of green chemistry, which aim to reduce waste and the use of substances that are hazardous to the environment or human health.

Project Details