Drug Metabolism and Pharmacokinetics (DMPK)
Objective
Provide in vitro and in vivo absorption, distribution, metabolism, and excretion (ADME) characterization of small molecule ligands including projected human dosing and drug-drug interaction liabilities
Technology/Techniques
Sciex Triple quadrupoles (4500 with Agilent autoinjector & two 4000’s with LEAP autoinjector PAL HTC)
Sciex QTRAP (5500) with LEAP autoinjector PAL HTC
Tecan Freedom EVO and Agilent Bravo robotic liquid handler
In vitro Clearance; plasma and brain homogenate binding assay
Cytochrome P450 inhibition
Bioanalysis of in vivo PK samples (brain and plasma)
Identification of Metabolites (human/rat)
Innovation
DMPK group typically not found in academic institutions that mimics industrial small Biotech
Full in vitro and in vivo ADME profiling to de-risk preclinical candidates and make early “Go/ No-Go” decisions
Understand mechanisms of clearance and pharmacokinetic/pharmacodynamic (PK/PD) relationships for maximal efficacy on target