The Max and Minnie Tomerlin Voelcker Preclinical Pharmacology Core: Accelerating Cancer Drug Discovery in Texas
Introduction
Poor pharmacokinetic (PK) and ADME (absorption, distribution, metabolism, and excerection) properties are two of the most common reasons for early failure of a drug candidate. While the implementation of this data early-on in the the discovery process is incredibly valuable to inform compound design, it is often pushed to later stages due to high cost and the lack of available resources. The Preclinical Pharmacology Core (PPC) at UTSA provides inductry-level expertise and capabilities for both in vitro ADME and in vivo PK studies at competitive rates to CROs. Access to these resources allows drug discovery sceientists to integrate this data much earlier in the discovery process, allowing the parallel optimization of SAR (structure activity relationships) and SPR (structure property relationships).
Methods
The PPC has capabilities spanning common in vitro ADME assays (microsomal clearance, plasma protein binding, Caco-2 permeability, etc.) and more specialized offerings, such as ion channel screening and transporter activity profiling. All in vivo work is conducted in collaboration with the LARC (Laboratory Animal Research Center) at UTSA. Available instrumentation includes a Thermo Scientific Orbitrap Exploris 120 and Thermo Scientific TSQ Altis Plus mass spectrometers (both equipped with a Vanquish UHPLC system) and a Molecular Devices SpectraMax i3x multimodal plate reader and imaging cytometer.
Results
Example studes from multiple collaborations with CPRIT-funded collaborators will be presented.
Conclusion
The PPC has established industy-level resources and expertise in ADME and DMPK (drug metabolism and pharmacokinetics) in south Texas. It is our mission to make these resources available to Texas researchers to enable smarter, more efficient, and more fruitful efforts in cancer drug discovery.