Lead optimization

Starting from a weakly active hit or from a validated lead, usually provided by the customer, Prestwick Chemical (PCI) proposes a research project to be discussed and approved by our partner. Our medicinal chemists then initiate the optimization process in order to identify a pre-clinical drug candidate.
The research strategy implies iterative cycles of design and assessment using:

Systematic SAR study using in-house know-how to identify productive directions for analogue design
Design of new analogues directed towards optimization of potency, selectivity and improvement of the ADME-Tox profile
Consolidation of the IP position
Analogue resynthesis/scale-up to support profiling studies
Scaffold-hopping to identify new chemotypes

A constant dialog with the customer's scientists (project management, chemists, biologists, toxicologists...) insures the fast recognition of structure-activity relationships. Using parallel and/or convergent synthesis as well as traditional approaches, our scientists are able to synthesize quickly a significant variety of compounds.

Even in the early stages we design and synthesize compounds with improved pharmacokinetic (ADME) profiles: increased absorption, modified distribution, modulated sensitivity to metabolism and different elimination kinetics. The compounds we propose are conceived taking in consideration toxicity problems derived from some radicals or substituents.

In all cases, the industrial property of the contract research remains our partner's ownership.