Emerging Modalities in DMPK

Emerging Modalities in DMPK

Efficiently adapt to new analytical challenges to determine DMPK properties of emerging therapeutic classes, including PROteolysis-Targeting Chimeras (PROTACs), with Waters UPLC-MS/MS solutions. Stay ahead of the bioanalysis requirements in an evolving DMPK landscape with exceptional sensitivity, accuracy, and reliability from Waters advanced chromatography, mass spectrometry, and sample preparation tools.

Efficiently adapt to new analytical challenges to determine DMPK properties of emerging therapeutic classes, including PROteolysis-Targeting Chimeras (PROTACs), with Waters UPLC-MS/MS solutions. Stay ahead of the bioanalysis requirements in an evolving DMPK landscape with exceptional sensitivity, accuracy, and reliability from Waters advanced chromatography, mass spectrometry, and sample preparation tools.

Peptide molecular structure in blue
Peptide molecular structure in blue

Overview

Next-generation small molecule medicines like PROTACs offer potential solutions for previously untreatable diseases, and accurately measuring their DMPK properties is crucial for drug discovery and development. Due to their long half-lives and low systemic concentrations, high-sensitivity bioanalysis is essential.

Waters UPLC-MS/MS and advanced chromatography solutions, sample preparation kits, standards, and high-sensitivity mass spectrometry systems simplify method development and ensure high-quality quantitative bioanalysis assays across modality types—supporting the evolution of safe and effective medicines. 


Molecular structure of a peptide, sequence of amino acids

Applications

PROTACs molecules are a new class of drug molecules with the potential to treat many diseases. Discover how Waters addresses the challenges associated with PROTACs analysis in DMPK studies with these application notes.

PROTACs molecules are a new class of drug molecules with the potential to treat many diseases. Discover how Waters addresses the challenges associated with PROTACs analysis in DMPK studies with these application notes.




Versatile LC-MS/MS Solutions for the Evolving Bioanalysis Landscape

Expand your capabilities across evolving modalities with Waters compendium of the latest applications in quantitative bioanalysis. The notebook features application notes covering a range of bioanalytical topics, including small molecule therapeutics, oligonucleotide therapeutics, peptide/protein therapeutics, efficiency enabling software, and novel imaging approaches. Learn how Waters can help you overcome the challenges brought by these new and varied drug modalities.

Expand your capabilities across evolving modalities with Waters compendium of the latest applications in quantitative bioanalysis. The notebook features application notes covering a range of bioanalytical topics, including small molecule therapeutics, oligonucleotide therapeutics, peptide/protein therapeutics, efficiency enabling software, and novel imaging approaches. Learn how Waters can help you overcome the challenges brought by these new and varied drug modalities.


DNA helix with glowing plexus and light shining behind

Solutions


Waters UPLC-MS/MS systems deliver absolute performance in separation and sensitivity for bioanalysis of PROTACs and other emerging modality pharmaceuticals. 

Waters UPLC-MS/MS systems deliver absolute performance in separation and sensitivity for bioanalysis of PROTACs and other emerging modality pharmaceuticals. 

Absolute performance for lowest levels of quantification

Absolute performance for lowest levels of quantification

Achieve and maintain high performance and productivity with significantly increased sensitivity for negative ionizing compounds with the Xevo TQ Absolute Triple Quadrupole Mass Spectrometer, Waters compact, sustainable tandem quadrupole mass spectrometer for confident detection and quantification of drugs and metabolites. 

  • PROTACs Bioanalysis

High performance chromatography for new bioanalytical challenges

High performance chromatography for new bioanalytical challenges

Optimize chromatographic resolution and speed while eliminating concerns of non-specific binding for new analytes with the Waters ACQUITY Premier UPLC System and enhance overall quantitative performance in bioanalysis assays.

  • PROTACs Bioanalysis


The data speaks for itself

The data speaks for itself
Comparison of chromatographic peak shape for PROTACs 3 gefitinib using ACQUITY Premier chromatography system/column and Conventional UPLC system/column, with reduced trailing and Peak width at base (Pwb) improvements shown. Comparison of chromatographic peak shape for PROTACs 3 gefitinib using ACQUITY Premier chromatography system/column and Conventional UPLC system/column, with reduced trailing and Peak width at base (Pwb) improvements shown.
Pharmacokinetics elimination curve of PROTACS 3 gefitinib determined  by ACQUITY Premier with Xevo TQ Absolute for  quantitation,  following subcutaneous administration to the male Wistar rat at 10 mg/kg. Pharmacokinetics elimination curve of PROTACS 3 gefitinib determined by ACQUITY Premier with Xevo TQ Absolute for quantitation, following subcutaneous administration to the male Wistar rat at 10 mg/kg.
0.5 pg/mL  PROTACs – 3- gefitinib in rat plasma. 0.5 pg/mL PROTACs – 3- gefitinib in rat plasma.
720008229en-f4 Positive ion LC-MS/MS analysis of gefitinib based PROTACs-3, gefitinib-d6 and gefitinib using a 2.1 x 50 mm ACQUITY HSS T3 1.7 µm C18 Column, maintained at 60 °C and eluted with a 5–95% aqueous – acetonitrile 1 mM ammonium formate, 0.1% formic acid gradient over 2 minutes with a 2 minute hold.

Webinars and Resources


  • On Demand Webinar

High Throughput Quantification of Gefitinib-3-PROTACs and Gefitinib to Support a Subcutaneous Dosing Rodent Study

High Throughput Quantification of Gefitinib-3-PROTACs and Gefitinib to Support a Subcutaneous Dosing Rodent Study

Related

Agilely support the progression of drug candidates throughout the drug development pipeline with Waters versatile quantitative bioanalysis solutions.

Perform peptide, protein and oligonucleotide analysis and overcome quantitation challenges during drug development processes with Waters UPLC-MS/MS solutions for large molecule bioanalysis.

Accurately perform small molecule bioanalysis of drug therapeutics with Waters UPLC-MS/MS solutions, designed to maximize throughput and minimize non-specific absorption.

Develop dependable and robust ADME assays while reducing the risk of any potential non-specific binding sensitive compound with Waters LC-MS/MS technologies and consumables for In Vitro ADME analysis.

Learn more about Emerging Modalities in DMPK Solutions.

Learn more about Emerging Modalities in DMPK Solutions.

Peptide molecular structure in blue