Lead Selection Studies

CXR provide mechanistic assays and screens tailored to address your specific requirements. We provide customised, cost-effective ADME /tox packages, designed to complement in vitro efficacy screens and identify compounds with potential adverse ADMET liabilities, to improve the selection of the most promising clinical candidates more

Predictive in vitro metabolism studies

• Human liver preparations (microsomes & hepatocytes) with all co-factors
• Metabolic stability and metabolite identification, comparison across species
• Metabolising CYP enzyme identification
• Rates and routes of metabolism studies
• CYP inhibition
• CYP induction, nuclear receptor activation

Permeation studies

• Drug transporter assays
• Cell line models of drug transport
• MDR-1 knockout mice

Early ADME and toxicity characteristics of compounds for lead selection and optimization. Determine compound liabilities earlier (select out poor performers)

In vivo ADME studies

• in vivo PK & ADME studies in wild type, transgenic, HRN, and nude mice
• HRN and nude HRN studies to evaluate and optimise compound bioavailability
• animal toxicity studies (Bioavailability, distribution, metabolism, elimination )
• clinical trial design
• analysis of clinical trial samples( eg. to assess ADME parameters)

An appreciation of unforseen adverse effects (eg tissue specific toxicity) can also be determined in vivo using whole genome gene expression studies more