Industry Perspective on the Pharmacokinetic and Absorption, Distribution, Metabolism, and Excretion Characterization of Heterobifunctional Protein Degraders

Protein degraders enter the clinic — a new approach to cancer therapy

(2023) Deborah Chirnomas et al.   Nature Reviews Clinical Oncology

State of the Art and Uses for the Biopharmaceutics Drug Disposition Classification System (BDDCS): New Additions, Revisions, and Citation References

(2022) Giovanni Bocci et al.   AAPS Journal

PROTAC targeted protein degraders: the past is prologue

(2022) Miklós Békés et al.   NATURE REVIEWS DRUG DISCOVERY

Free Drug Theory – No Longer Just a Hypothesis?

(2022) Scott G. Summerfield et al.   PHARMACEUTICAL RESEARCH

Proteolysis-Targeting Chimera (PROTAC): Is the Technology Looking at the Treatment of Brain Tumors?

(2022) Ludovica Lospinoso Severini et al.   Frontiers in Cell and Developmental Biology

Pharmacoproteomics of Brain Barrier Transporters and Substrate Design for the Brain Targeted Drug Delivery

(2022) Kristiina M. Huttunen et al.   PHARMACEUTICAL RESEARCH

Targeted BRD4 protein degradation by dBET1 ameliorates acute ischemic brain injury and improves functional outcomes associated with reduced neuroinflammation and oxidative stress and preservation of blood–brain barrier integrity

(2022) Lei Liu et al.   Journal of Neuroinflammation

Engineered bioorthogonal POLY-PROTAC nanoparticles for tumour-specific protein degradation and precise cancer therapy

(2022) Jing Gao et al.   Nature Communications

Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable, and Blood–Brain Barrier Penetrant PROTAC Degrader of Leucine-Rich Repeat Kinase 2

(2022) Xingui Liu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The drug efflux pump MDR1 promotes intrinsic and acquired resistance to PROTACs in cancer cells

(2022) Alison M. Kurimchak et al.   Science Signaling

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties

(2021) Peter S. Dragovich et al.   JOURNAL OF MEDICINAL CHEMISTRY

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy

(2021) Peter S. Dragovich et al.   JOURNAL OF MEDICINAL CHEMISTRY

Ultrafiltration Method for Plasma Protein Binding Studies and Its Limitations

(2021) Camelia-Maria Toma et al.   Processes

Is PROTAC technology really a game changer for central nervous system drug discovery?

(2021) Kayla Farrell et al.   Expert Opinion on Drug Discovery

Discovery and Characterisation of Highly Cooperative FAK‐Degrading PROTACs

(2021) Robert P. Law et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Prediction of Chameleonic Efficiency

(2021) Laurent David et al.   ChemMedChem

Species selection for nonclinical safety assessment of drug candidates: Examples of current industry practice

(2021) Rostam Namdari et al.   REGULATORY TOXICOLOGY AND PHARMACOLOGY

Proteolysis‐targeting chimeras in drug development: A safety perspective

(2020) Kevin Moreau et al.   BRITISH JOURNAL OF PHARMACOLOGY

Fundamental aspects of DMPK optimization of targeted protein degraders

(2020) Carina Cantrill et al.   DRUG DISCOVERY TODAY

OATP1A2 and OATP2B1 Are Interacting with Dopamine-Receptor Agonists and Antagonists

(2020) Anima M. Schäfer et al.   MOLECULAR PHARMACEUTICS

Optimising proteolysis-targeting chimeras (PROTACs) for oral drug delivery: a drug metabolism and pharmacokinetics perspective

(2020) Andy Pike et al.   DRUG DISCOVERY TODAY

Understanding and Improving the Membrane Permeability of VH032-Based PROTACs

(2020) Victoria G. Klein et al.   ACS Medicinal Chemistry Letters

Systematic Investigation of the Permeability of Androgen Receptor PROTACs

(2020) Duncan E. Scott et al.   ACS Medicinal Chemistry Letters

Understanding the Metabolism of Proteolysis Targeting Chimeras (PROTACs): The Next Step toward Pharmaceutical Applications

(2020) Laura Goracci et al.   JOURNAL OF MEDICINAL CHEMISTRY

Solution Conformations Shed Light on PROTAC Cell Permeability

(2020) Yoseph Atilaw et al.   ACS Medicinal Chemistry Letters

Neuroprotective effects of targeting BET proteins for degradation with dBET1 in aged mice subjected to ischemic stroke

(2019) Kelly M. DeMars et al.   NEUROCHEMISTRY INTERNATIONAL

Mathematical and Experimental Validation of Flux Dialysis Method: An Improved Approach to Measure Unbound Fraction for Compounds with High Protein Binding and Other Challenging Properties

(2018) J. Cory Kalvass et al.   DRUG METABOLISM AND DISPOSITION

Plasma Protein Binding of Highly Bound Drugs Determined With Equilibrium Gel Filtration of Nonradiolabeled Compounds and LC-MS/MS Detection

(2018) John Isbell et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Understanding the Thalidomide Chirality in Biological Processes by the Self-disproportionation of Enantiomers

(2018) Etsuko Tokunaga et al.   Scientific Reports

Beyond the Rule of 5: Lessons Learned from AbbVie’s Drugs and Compound Collection

(2017) David A. DeGoey et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural basis of PROTAC cooperative recognition for selective protein degradation

(2017) Morgan S Gadd et al.   Nature Chemical Biology

Biomimetic reassembled chylomicrons as novel association model for the prediction of lymphatic transportation of highly lipophilic drugs via the oral route

(2015) Yi Lu et al.   INTERNATIONAL JOURNAL OF PHARMACEUTICS

Plasma Protein Binding of Challenging Compounds

(2015) Keith Riccardi et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

From sewer to saviour — targeting the lymphatic system to promote drug exposure and activity

(2015) Natalie L. Trevaskis et al.   NATURE REVIEWS DRUG DISCOVERY

EPSA: A Novel Supercritical Fluid Chromatography Technique Enabling the Design of Permeable Cyclic Peptides

(2014) Gilles H. Goetz et al.   ACS Medicinal Chemistry Letters

Investigation of the Functional Role of P-Glycoprotein in Limiting the Oral Bioavailability of Lumefantrine

(2013) Wahajuddin et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Absorption, metabolism and excretion of [14C]pomalidomide in humans following oral administration

(2012) Matthew Hoffmann et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Demystifying Brain Penetration in Central Nervous System Drug Discovery

(2012) Li Di et al.   JOURNAL OF MEDICINAL CHEMISTRY

Plasma Protein Binding in Drug Discovery and Development

(2010) Monique Howard et al.   COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

Segmental Dependent Transport of Low Permeability Compounds along the Small Intestine Due to P-Glycoprotein: The Role of Efflux Transport in the Oral Absorption of BCS Class III Drugs

(2008) Arik Dahan et al.   MOLECULAR PHARMACEUTICS