In Vivo PK Evaluation during Drug Discovery

Pharmacology Discovery Services excels in preclinical pharmacokinetics (PK), focusing on in vivo PK evaluations at the early stage of drug discovery. We offer comprehensive assessments across different rodent species, including mice, rats, hamsters, and guinea pigs, as well as humanized mice for advanced translational application. Our discovery PK studies provide in-depth data on PK parameters, oral bioavailability, organ distribution, blood-brain barrier (BBB) permeability, which are crucial for evaluating new molecular entities and prerequisite for interpreting preclinical efficacy and toxicology results.

Let us work with you to understand the physicochemical properties of your test materials, shaping an effective dosing and sampling strategy to ensure the acquisition of meaningful and accurate data. We are equipped to handle various administration routes, including bolus dosing with IV, PO, IP, IM, SC, IN, and ICV, and continuous dosing with short- and long-term infusion, utilizing both serial microsampling and parallel sampling techniques for comprehensive PK data analysis.

We generate thorough concentration versus time profiles, which enables us to provide a complete spectrum of PK parameters, essential for moving drug development projects forward. As a CRO specializing in in vivo preclinical and discovery PK, we are committed to providing precise and in vivo PK profile of your molecules to advance your drug discovery endeavors.

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In Vivo Pharmacokinetic and Blood/Brain Barrier Studies with Pharmacology Discovery Services:

• Extensive experience with multiple routes of administration, including long-term continuous infusion
• Proficient in performing PK and BBB studies
• Combined PK/BBB sampling and bioanalytical studies
• Renal and biliary clearance
• Experience you can trust: 50 years running in vivo preclinical services with a staff averaging 15 years of experience
• Long range of efficacy and toxicity studies can be conducted at the same provider

Publications

• Translational in vitro and in vivo PKPD modelling for apramycin against Gram-negative lung pathogens to facilitate prediction of human efficacious dose in pneumonia. Vincent AC et al. Clin. Microbiol. Infect. 2022 Oct;28(10);1367-1374. https://doi.org/10.1016/j.cmi.2022.05.003
• A selective p53 activator and anticancer agent to improve colorectal cancer therapy. Ramos H et al. Cell Rep. 2021 Apr;35(2):108982. https://doi.org/10.1016/j.celrep.2021.108982
• Betulinic acid hydroxamate prevents colonic inflammation and fibrosis in murine models of inflammatory bowel disease. Prados ME et al. Acta Pharmacol Sin. 2021 Aug;42;1124–1138. https://doi.org/10.1038/s41401-020-0497-0
• Formulation, stability, pharmacokinetic, and modeling studies for tests of synergistic combinations of orally available approved drugs against ebola virus in vivo. Finch CL et al. Microorganisms. 2021 Mar;9(3):566. https://doi.org/10.3390/microorganisms9030566
• Vitamin E Phosphate Nucleoside Prodrugs: A Platform for Intracellular Delivery of Monophosphorylated Nucleosides. Diafuku R et al. Pharmaceuticals. 2018 Feb;11(1). https://doi.org/10.3390/ph11010016
• 5-aza-2',2'-Difluoro Deoxycytidine (NUC013): A Novel Nucleoside DNA Methyl Transferase Inhibitor and Ribonucleotide Reductase Inhibitor for the Treatment of Cancer. Diafuku R et al. Pharmaceuticals. 2017 Jul 20;10(3):65. https://doi.org/10.3390/ph10030065
• BCAT1 controls metabolic reprogramming in activated human macrophages and is associated with inflammatory diseases. Papathanassiu AE et al. Nat Commun. 2017 Jul;8:16040. https://doi.org/10.1038/ncomms16040