Metabolism of bioconjugate therapeutics: why, when, and how?

Nonclinical characterization of the pharmacokinetics and disposition of inotuzumab ozogamicin, a calicheamicin-containing antibody-drug conjugate

(2018) Theodore R. Johnson et al.   Drug Metabolism and Pharmacokinetics

Prevalence of Delta-like protein 3 expression in patients with small cell lung cancer

(2018) Kentaro Tanaka et al.   LUNG CANCER

A Novel NF-κB Inhibitor, Edasalonexent (CAT-1004), in Development as a Disease-Modifying Treatment for Patients With Duchenne Muscular Dystrophy: Phase 1 Safety, Pharmacokinetics, and Pharmacodynamics in Adult Subjects

(2017) Joanne M. Donovan et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Aripiprazole Lauroxil

(2017) Marjie L. Hard et al.   JOURNAL OF CLINICAL PSYCHOPHARMACOLOGY

Polymer therapeutics at a crossroads? Finding the path for improved translation in the twenty-first century

(2017) Ruth Duncan   JOURNAL OF DRUG TARGETING

Modulating Therapeutic Activity and Toxicity of Pyrrolobenzodiazepine Antibody–Drug Conjugates with Self-Immolative Disulfide Linkers

(2017) Thomas H. Pillow et al.   MOLECULAR CANCER THERAPEUTICS

Bioconjugate Therapeutics: Current Progress and Future Perspective

(2017) Feng Li et al.   MOLECULAR PHARMACEUTICS

Lipid–Drug Conjugate for Enhancing Drug Delivery

(2017) Danielle Irby et al.   MOLECULAR PHARMACEUTICS

Strategies and challenges for the next generation of antibody–drug conjugates

(2017) Alain Beck et al.   NATURE REVIEWS DRUG DISCOVERY

Edasalonexent (CAT-1004), an NF-kB inhibitor, enhances myotube formation in vitro, and increases exon-skipped sarcolemmal dystrophin in muscle of mdx mice

(2017) A. Nichols et al.   NEUROMUSCULAR DISORDERS

Conjugation of squalene to gemcitabine as unique approach exploiting endogenous lipoproteins for drug delivery

(2017) Dunja Sobot et al.   Nature Communications

Current Multistage Drug Delivery Systems Based on the Tumor Microenvironment

(2017) Binlong Chen et al.   Theranostics

Preclinical and Clinical Advances of GalNAc-Decorated Nucleic Acid Therapeutics

(2017) Yuanyu Huang   Molecular Therapy-Nucleic Acids

Nanotechnology-based combination therapy for overcoming multidrug-resistant cancer

(2017) Meng Zhang et al.   Cancer Biology & Medicine

A phase I study of the folate-targeted conjugate EC0489 in patients with refractory or advanced metastatic cancer.

(2017) W. A. Harb et al.   JOURNAL OF CLINICAL ONCOLOGY

Custom-Designed Affinity Capture LC-MS F(ab′)2 Assay for Biotransformation Assessment of Site-Specific Antibody Drug Conjugates

(2016) Dian Su et al.   ANALYTICAL CHEMISTRY

From Anthramycin to Pyrrolobenzodiazepine (PBD)-Containing Antibody-Drug Conjugates (ADCs)

(2016) Julia Mantaj et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Determination of Antibody–Drug Conjugate Released Payload Species Using Directed in Vitro Assays and Mass Spectrometric Interrogation

(2016) Andrew J. Bessire et al.   BIOCONJUGATE CHEMISTRY

Antibody-drug conjugates—an emerging class of cancer treatment

(2016) Nikolaos Diamantis et al.   BRITISH JOURNAL OF CANCER

Targeted Drug Delivery with Polymers and Magnetic Nanoparticles: Covalent and Noncovalent Approaches, Release Control, and Clinical Studies

(2016) Karel Ulbrich et al.   CHEMICAL REVIEWS

Antibody-drug conjugates for non-oncological indications

(2016) Renhe Liu et al.   EXPERT OPINION ON BIOLOGICAL THERAPY

Efficacy and safety of entecavir versus tenofovir treatment in chronic hepatitis B patients: A randomized controlled trial

(2016) Tassanee Sriprayoon et al.   HEPATOLOGY RESEARCH

Linkers Having a Crucial Role in Antibody–Drug Conjugates

(2016) Jun Lu et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Targeting of pegylated liposomal mitomycin-C prodrug to the folate receptor of cancer cells: Intracellular activation and enhanced cytotoxicity

(2016) Yogita Patil et al.   JOURNAL OF CONTROLLED RELEASE

Synthesis and Characterization of Fatty Acid Conjugates of Niacin and Salicylic Acid

(2016) Chi B. Vu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fatty Acid Cysteamine Conjugates as Novel and Potent Autophagy Activators That Enhance the Correction of Misfolded F508del-Cystic Fibrosis Transmembrane Conductance Regulator (CFTR)

(2016) Chi B. Vu et al.   JOURNAL OF MEDICINAL CHEMISTRY

PEGylation of Biopharmaceuticals: A Review of Chemistry and Nonclinical Safety Information of Approved Drugs

(2016) Peter L. Turecek et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Discovery of Pyrophosphate Diesters as Tunable, Soluble, and Bioorthogonal Linkers for Site-Specific Antibody–Drug Conjugates

(2016) Jeffrey C. Kern et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Development of Novel Quaternary Ammonium Linkers for Antibody-Drug Conjugates

(2016) P. J. Burke et al.   MOLECULAR CANCER THERAPEUTICS

Optimization of a PEGylated Glucuronide-Monomethylauristatin E Linker for Antibody–Drug Conjugates

(2016) Patrick J. Burke et al.   MOLECULAR CANCER THERAPEUTICS

Lymphatic Transport and Lymphocyte Targeting of a Triglyceride Mimetic Prodrug Is Enhanced in a Large Animal Model: Studies in Greyhound Dogs

(2016) Sifei Han et al.   MOLECULAR PHARMACEUTICS

Targeted drug delivery through the traceless release of tertiary and heteroaryl amines from antibody–drug conjugates

(2016) Leanna R. Staben et al.   Nature Chemistry

Antibody Drug Conjugates: Design and Selection of Linker, Payload and Conjugation Chemistry

(2015) Jessica R. McCombs et al.   AAPS Journal

Effect of Attachment Site on Stability of Cleavable Antibody Drug Conjugates

(2015) Magdalena Dorywalska et al.   BIOCONJUGATE CHEMISTRY

Antibody-targeted drugs and drug resistance—Challenges and solutions

(2015) LeeRon Shefet-Carasso et al.   DRUG RESISTANCE UPDATES

Challenges in SN38 drug delivery: current success and future directions

(2015) Srinath Palakurthi   Expert Opinion on Drug Delivery

Antibody Positron Emission Tomography Imaging in Anticancer Drug Development

(2015) Laetitia E. Lamberts et al.   JOURNAL OF CLINICAL ONCOLOGY

A sensitive multidimensional method for the detection, characterization, and quantification of trace free drug species in antibody-drug conjugate samples using mass spectral detection

(2015) Robert E. Birdsall et al.   mAbs

Metabolites of Antibody–Maytansinoid Conjugates: Characteristics and in Vitro Potencies

(2015) Wayne Widdison et al.   MOLECULAR PHARMACEUTICS

Design, Synthesis, and Evaluation of Linker-Duocarmycin Payloads: Toward Selection of HER2-Targeting Antibody–Drug Conjugate SYD985

(2015) Ronald C. Elgersma et al.   MOLECULAR PHARMACEUTICS

Pharmacologic Studies of a Prodrug of Mitomycin C in Pegylated Liposomes (Promitil®): High Stability in Plasma and Rapid Thiolytic Prodrug Activation in Tissues

(2015) Yasmine Amitay et al.   PHARMACEUTICAL RESEARCH

Antibody–drug conjugates nonclinical support: from early to late nonclinical bioanalysis using ligand-binding assays

(2015) Seema Kumar et al.   Bioanalysis

Bioanalytical approaches for characterizing catabolism of antibody–drug conjugates

(2015) Ola M Saad et al.   Bioanalysis

Aripiprazole long-acting injectable formulations for schizophrenia: aripiprazole monohydrate and aripiprazole lauroxil

(2015) Leslie Citrome   Expert Review of Clinical Pharmacology

Vintafolide: a novel targeted therapy for the treatment of folate receptor expressing tumors

(2015) Ignace Vergote et al.   Therapeutic Advances in Medical Oncology

Phospholipid/deoxycytidine analogue prodrugs for the treatment of cancer

(2015) K.A. Pickin et al.   JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY

Antibody–drug conjugates—A new wave of cancer drugs

(2014) Hervé Bouchard et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A Review of the Pharmacological Properties of Insulin Degludec and Their Clinical Relevance

(2014) Hanne Haahr et al.   CLINICAL PHARMACOKINETICS

A phase I pharmacokinetic and safety analysis of epothilone folate (BMS-753493), a folate receptor targeted chemotherapeutic agent in humans with advanced solid tumors

(2014) P. P. Peethambaram et al.   INVESTIGATIONAL NEW DRUGS

Targeted delivery of a model immunomodulator to the lymphatic system: Comparison of alkyl ester versus triglyceride mimetic lipid prodrug strategies

(2014) Sifei Han et al.   JOURNAL OF CONTROLLED RELEASE

Polypharmacology: Challenges and Opportunities in Drug Discovery

(2014) Andrew Anighoro et al.   JOURNAL OF MEDICINAL CHEMISTRY

Preclinical Profile of the HER2-Targeting ADC SYD983/SYD985: Introduction of a New Duocarmycin-Based Linker-Drug Platform

(2014) W. Dokter et al.   MOLECULAR CANCER THERAPEUTICS

Improving the Therapeutic Index in Cancer Therapy by Using Antibody–Drug Conjugates Designed with a Moderately Cytotoxic Drug

(2014) Serengulam V. Govindan et al.   MOLECULAR PHARMACEUTICS

Synthesis of Doxorubicin α-Linolenic Acid Conjugate and Evaluation of Its Antitumor Activity

(2014) Chun-hui Liang et al.   MOLECULAR PHARMACEUTICS

Profiling the Role of Deacylation-Reacylation in the Lymphatic Transport of a Triglyceride-Mimetic Prodrug

(2014) Sifei Han et al.   PHARMACEUTICAL RESEARCH

Preclinical Pharmacokinetic Considerations for the Development of Antibody Drug Conjugates

(2014) Amrita V. Kamath et al.   PHARMACEUTICAL RESEARCH

Using the Lessons Learned From the Clinic to Improve the Preclinical Development of Antibody Drug Conjugates

(2014) Dowdy Jackson et al.   PHARMACEUTICAL RESEARCH

Radioimmunoconjugates for the Treatment of Cancer

(2014) Françoise Kraeber-Bodéré et al.   SEMINARS IN ONCOLOGY

Vintafolide (EC145) for the treatment of folate-receptor-α positive platinum-resistant ovarian cancer

(2014) Allison J Ambrosio et al.   Expert Review of Clinical Pharmacology

Antibody–drug conjugates: current status and future directions

(2013) Heidi L. Perez et al.   DRUG DISCOVERY TODAY

PRECEDENT: A Randomized Phase II Trial Comparing Vintafolide (EC145) and Pegylated Liposomal Doxorubicin (PLD) in Combination Versus PLD Alone in Patients With Platinum-Resistant Ovarian Cancer

(2013) R. Wendel Naumann et al.   JOURNAL OF CLINICAL ONCOLOGY

CYP3A-Mediated Drug-Drug Interaction Potential and Excretion of Brentuximab Vedotin, an Antibody−Drug Conjugate, in Patients With CD30-Positive Hematologic Malignancies

(2013) Tae H. Han et al.   JOURNAL OF CLINICAL PHARMACOLOGY

The Immunogenicity of Polyethylene Glycol: Facts and Fiction

(2013) Huub Schellekens et al.   PHARMACEUTICAL RESEARCH

Novel Biotinylated Lipid Prodrugs of Acyclovir for the Treatment of Herpetic Keratitis (HK): Transporter Recognition, Tissue Stability and Antiviral Activity

(2013) Aswani Dutt Vadlapudi et al.   PHARMACEUTICAL RESEARCH

Monoclonal antibody-based therapies in cancer: Advances and challenges

(2013) Puja Sapra et al.   PHARMACOLOGY & THERAPEUTICS

Clinical utility of insulin and insulin analogs

(2013) Ahter D. Sanlioglu et al.   Islets

ADME of Antibody–Maytansinoid Conjugates

(2012) Hans K. Erickson et al.   AAPS Journal

Fatty acids as therapeutic auxiliaries for oral and parenteral formulations

(2012) Michael J. Hackett et al.   ADVANCED DRUG DELIVERY REVIEWS

Engineering Folate–Drug Conjugates to Target Cancer: From Chemistry to Clinic

(2012) Iontcho R. Vlahov et al.   BIOCONJUGATE CHEMISTRY

Nanoparticle delivery systems for cancer therapy: advances in clinical and preclinical research

(2012) Susana Patricia Egusquiaguirre et al.   Clinical & Translational Oncology

Design of Non-Standard Insulin Analogs for the Treatment of Diabetes Mellitus

(2012) V. Pandyarajan et al.   Current Diabetes Reports

Degradation of BMS-753493, a novel epothilone folate conjugate anticancer agent

(2012) Madhushree Gokhale et al.   DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY

Antibody–drug conjugates – a perfect synergy

(2012) John R Adair et al.   EXPERT OPINION ON BIOLOGICAL THERAPY

Phase I Study of Folate Conjugate EC145 (Vintafolide) in Patients With Refractory Solid Tumors

(2012) Patricia M. LoRusso et al.   JOURNAL OF CLINICAL ONCOLOGY

Therapeutic Potential of Amanitin-Conjugated Anti-Epithelial Cell Adhesion Molecule Monoclonal Antibody Against Pancreatic Carcinoma

(2012) Gerhard Moldenhauer et al.   JNCI-Journal of the National Cancer Institute

The discovery and development of brentuximab vedotin for use in relapsed Hodgkin lymphoma and systemic anaplastic large cell lymphoma

(2012) Peter D Senter et al.   NATURE BIOTECHNOLOGY

Conjugation site modulates the in vivo stability and therapeutic activity of antibody-drug conjugates

(2012) Ben-Quan Shen et al.   NATURE BIOTECHNOLOGY

Preclinical experimental models of drug metabolism and disposition in drug discovery and development

(2012) Donglu Zhang et al.   Acta Pharmaceutica Sinica B

Design of Antibody−Maytansinoid Conjugates Allows for Efficient Detoxification via Liver Metabolism

(2011) Xiuxia Sun et al.   BIOCONJUGATE CHEMISTRY

Disulfide-Linked Antibody−Maytansinoid Conjugates: Optimization of In Vivo Activity by Varying the Steric Hindrance at Carbon Atoms Adjacent to the Disulfide Linkage

(2011) Brenda A. Kellogg et al.   BIOCONJUGATE CHEMISTRY

Antibody Fusion Proteins: Anti-CD22 Recombinant Immunotoxin Moxetumomab Pasudotox

(2011) R. J. Kreitman et al.   CLINICAL CANCER RESEARCH

Antibody Conjugate Therapeutics: Challenges and Potential

(2011) B. A. Teicher et al.   CLINICAL CANCER RESEARCH

Comparative evaluation of the biological properties of reducible and acid-sensitive folate prodrugs of a highly potent doxorubicin derivative

(2011) Khalid Abu Ajaj et al.   EUROPEAN JOURNAL OF CANCER

Investigational antibody drug conjugates for solid tumors

(2011) Puja Sapra et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Therapeutic efficacy of a lipid-based prodrug of mitomycin C in pegylated liposomes: Studies with human gastro-entero-pancreatic ectopic tumor models

(2011) Alberto Gabizon et al.   JOURNAL OF CONTROLLED RELEASE

Development of Hexadecyloxypropyl Tenofovir (CMX157) for Treatment of Infection Caused by Wild-Type and Nucleoside/Nucleotide-Resistant HIV

(2010) E. R. Lanier et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Tumor-Selective Delivery of Macromolecular Drugs via the EPR Effect: Background and Future Prospects

(2010) Hiroshi Maeda   BIOCONJUGATE CHEMISTRY

PEGylation of therapeutic proteins

(2010) Simona Jevševar et al.   Biotechnology Journal

Metabolism and Excretion of the Once-Daily Human Glucagon-Like Peptide-1 Analog Liraglutide in Healthy Male Subjects and Its In Vitro Degradation by Dipeptidyl Peptidase IV and Neutral Endopeptidase

(2010) M. Malm-Erjefalt et al.   DRUG METABOLISM AND DISPOSITION

Modulation of doxorubicin activity in cancer cells by conjugation with fatty acyl and terpenyl hydrazones

(2010) K. Effenberger et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Antiproliferative activity, mechanism of action and oral antitumor activity of CP-4126, a fatty acid derivative of gemcitabine, in in vitro and in vivo tumor models

(2010) Andries M. Bergman et al.   INVESTIGATIONAL NEW DRUGS

Carbohydrate-Based Synthetic Approach to Control Toxicity Profiles of Folate−Drug Conjugates

(2010) Iontcho R. Vlahov et al.   JOURNAL OF ORGANIC CHEMISTRY

Reducing Undesirable Hepatic Clearance of a Tumor-Targeted Vinca Alkaloid via Novel Saccharopeptidic Modifications

(2010) C. P. Leamon et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

The Activity of the Lipophilic Nucleoside Derivatives Elacytarabine and CP-4126 in a Panel of Tumor Cell Lines Resistant to Nucleoside Analogues

(2010) Marit Liland Sandvold et al.   NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS

Enhanced circulation half-life of site-specific PEGylated rhG-CSF: Optimization of PEG molecular weight

(2009) Yanqin Zhai et al.   JOURNAL OF BIOTECHNOLOGY

Clinical Pharmacokinetics and Exposure-Toxicity Relationship of a Folate-VincaAlkaloid Conjugate EC145 in Cancer Patients

(2009) Jing Li et al.   JOURNAL OF CLINICAL PHARMACOLOGY

In Vivo Structural Activity and Optimization Studies of Folate−Tubulysin Conjugates

(2009) Joseph A. Reddy et al.   MOLECULAR PHARMACEUTICS

Glycoengineered Acid α-Glucosidase With Improved Efficacy at Correcting the Metabolic Aberrations and Motor Function Deficits in a Mouse Model of Pompe Disease

(2009) Yunxiang Zhu et al.   MOLECULAR THERAPY

CP-4055 and CP-4126 are active in ara-C and gemcitabine-resistant lymphoma cell lines

(2008) Carlos M. Galmarini et al.   BRITISH JOURNAL OF HAEMATOLOGY

Targeting HER2-Positive Breast Cancer with Trastuzumab-DM1, an Antibody-Cytotoxic Drug Conjugate

(2008) G. D. Lewis Phillips et al.   CANCER RESEARCH

Folate receptor alpha as a tumor target in epithelial ovarian cancer

(2008) Kimberly R. Kalli et al.   GYNECOLOGIC ONCOLOGY

Immunohistochemical expression of folate receptor α in colorectal carcinoma: patterns and biological significance

(2008) Jinru Shia et al.   HUMAN PATHOLOGY

Pompe's disease

(2008) Ans T van der Ploeg et al.   LANCET

PEG-uricase in the management of treatment-resistant gout and hyperuricemia

(2007) Merry R. Sherman et al.   ADVANCED DRUG DELIVERY REVIEWS