← Back to Search
PEG Drugs: An Overview.
R. B. Greenwald
Published 2001 · Chemistry, Medicine
Save to my Library
Download via 🐼 PaperPanda Download via oaDOI Download via OAB Download via LibKey Download via Google Google ScholarAnalyze on Scholarcy Visualize in Litmaps
Reduce the time it takes to create your bibliography by a factor of 10 by using the world’s favourite reference manager
Time to take this seriously.
No low molecular weight (<20000) poly(ethylene glycol) (PEG) small molecule drug conjugates, prepared over a 20-year period, have led to a clinically approved product. In this area, published studies for these types of compounds have been scrutinized and their properties compared and contrasted to higher molecular weight conjugates where, during the past 5 years, a renaissance in the field of PEG (anticancer) drug conjugates has taken place. This new development has been attributed to the use of higher molecular weight PEGs (>20000), and especially employing PEG 40000 which is estimated to have a plasma circulating half life of approximately 8-9 h in the mouse. This recent resuscitation of small organic molecule delivery by high molecular weight PEG conjugates was founded on meaningful in vivo testing using established tumor models, and has led to a clinical candidate. Recent applications of high molecular weight PEG prodrug strategies to amino containing drugs are also detailed, and potential applications to proteins are proposed.
This paper references
Alkaline Hydrolysis of Some Carbamic Acid Esters.
I. Christenson (1964)
The Mechanism of the Alkaline Hydrolysis of p-Nitrophenyl N-Methylcarbamate1
M. Bender (1965)
Alteration of immunological properties of bovine serum albumin by covalent attachment of polyethylene glycol.
A. Abuchowski (1977)
A novel connector linkage applicable in prodrug design.
P. L. Carl (1981)
Attachment of drugs to polyethylene glycols
S. Zalipsky (1983)
THE 1,4 AND 1,6 ELIMINATIONS FROM HYDROXY‐ AND AMINO‐SUBSTITUTED BENZYL SYSTEMS: CHEMICAL AND BIOCHEMICAL APPLICATIONS
M. Wakselman (1983)
Prodrugs. Do they have advantages in clinical practice?
V. Stella (1985)
Effect of molecular weight (Mw) of N-(2-hydroxypropyl)methacrylamide copolymers on body distribution and rate of excretion after subcutaneous, intraperitoneal, and intravenous administration to rats.
L. Seymour (1987)
The double prodrug concept and its applications
H. Bundgaard (1989)
Synthesis of congeners and prodrugs. 3. Water-soluble prodrugs of taxol with potent antitumor activity.
H. Deutsch (1989)
Modified Taxols, 6. Preparation of Water-Soluble Prodrugs of Taxol
Zhao Zhi-Yang (1991)
Conjugates of anticancer agents and polymers: advantages of macromolecular therapeutics in vivo.
H. Maeda (1992)
Evaluation of a new reagent for covalent attachment of polyethylene glycol to proteins.“
S. Zalipsky (1992)
Synthesis and evaluation of some water-soluble prodrugs and derivatives of taxol with antitumor activity.
A. Mathew (1992)
Plant antitumor agents. 30. Synthesis and structure activity of novel camptothecin analogs.
M. Wall (1993)
Preparation and properties of monomethoxy poly(ethylene glycol) doxorubicin conjugates linked by an amino acid or a peptide as spacer.
P. Caliceti (1993)
Camptothecins: from bench research to hospital wards.
M. Potměšil (1994)
On the suitability of urethane bonds between the carrier and the drug moiety in poly(ethyleneglycol)-based oligomeric prodrugs.
E. Ranucci (1994)
Distribution and tissue uptake of poly(ethylene glycol) with different molecular weights after intravenous administration to mice.
T. Yamaoka (1994)
Highly water soluble taxol derivatives: 2′-polyethyleneglycol esters as potential prodrugs
R. Greenwald (1994)
Poly(Ethylene Glycol) with Reactive Endgroups: I. Modification of Proteins
S. Herman (1995)
Influence of molecular weight on passive tumour accumulation of a soluble macromolecular drug carrier.
L. Seymour (1995)
HIGHLY WATER SOLUBLE TAXOL DERIVATIVES : 7-POLYETHYLENE GLYCOL CARBAMATES AND CARBONATES
R. Greenwald (1995)
Functionalized poly(ethylene glycol) for preparation of biologically relevant conjugates.
S. Zalipsky (1995)
Camptothecin and taxol: discovery to clinic--thirteenth Bruce F. Cain Memorial Award Lecture.
M. Wall (1995)
A branched monomethoxypoly(ethylene glycol) for protein modification.
C. Monfardini (1995)
Targetable drug carriers: present status and a future perspective
M. Yokoyama (1996)
PEG Modified Anticancer Drugs: Synthesis and Biological Activity
A. Pendri (1996)
PEG thiazolidine-2-thione, a novel reagent for facile protein modification: conjugation of bovine hemoglobin.
R. Greenwald (1996)
Drug delivery systems. 2. Camptothecin 20-O-poly(ethylene glycol) ester transport forms.
R. Greenwald (1996)
Drug delivery systems: water soluble taxol 2'-poly(ethylene glycol) ester prodrugs-design and in vivo effectiveness.
R. Greenwald (1996)
Branched poly(ethylene glycol) linkers
Anthony Martínez (1997)
Camptothecin delivery systems: the antitumor activity of a camptothecin-20-0-polyethylene glycol ester transport form.
C. Conover (1997)
Prodrug strategies based on intramolecular cyclization reactions.
D. Shan (1997)
Design of intramolecularly activated prodrugs.
B. Testa (1998)
Camptothecin delivery systems: enhanced efficacy and tumor accumulation of camptothecin following its conjugation to polyethylene glycol via a glycine linker
C. Conover (1998)
The Design of Selectively‐activated Anti‐cancer Prodrugs for use in Antibody‐directed and Gene‐directed Enzyme‐Prodrug Therapies *
W. Denny (1998)
Antitumor activity of paclitaxel-2'-glycinate conjugated to poly(ethylene glycol): a water-soluble prodrug.
A. Pendri (1998)
Camptothecin-20-PEG ester transport forms: the effect of spacer groups on antitumor activity.
R. Greenwald (1998)
Early Phase Tumor Accumulation of Macromolecules: A Great Difference in Clearance Rate between Tumor and Normal Tissues
Youichiro Noguchi (1998)
Prodrug approaches to the improved delivery of peptide drugs.
W. Wang (1999)
Camptothecin delivery systems: the utility of amino acid spacers for the conjugation of camptothecin with polyethylene glycol to create prodrugs.
C. Conover (1999)
Drug delivery systems employing 1,4- or 1,6-elimination: poly(ethylene glycol) prodrugs of amine-containing compounds.
R. Greenwald (1999)
Detection and characterization of antibodies to PEG-IFN-alpha2b using surface plasmon resonance.
M. Takacs (1999)
Enhanced antitumor potency of polyethylene glycolylated tumor necrosis factor-alpha: a novel polymer-conjugation technique with a reversible amino-protective reagent.
S. Tsunoda (1999)
20-O-acylcamptothecin derivatives: evidence for lactone stabilization.
H. Zhao (2000)
Drug delivery systems based on trimethyl lock lactonization: poly(ethylene glycol) prodrugs of amino-containing compounds.
R. Greenwald (2000)
SMANCS and polymer-conjugated macromolecular drugs: advantages in cancer chemotherapy.
H. Maeda (2001)
Drug delivery systems employing 1,6-elimination: releasable poly(ethylene glycol) conjugates of proteins.
Stanford Lee (2001)
This paper is referenced by
Cartilage-targeting Poly(Ethyleneglycol) (PEG)-formononetin (FMN) Nanodrug for Treating Osteoarthritis
Wei Xiong (2021)
Cartilage-targeting poly(ethylene glycol) (PEG)-formononetin (FMN) nanodrug for the treatment of osteoarthritis
Wei Xiong (2021)
Microbial polyesters: synthesis and applications
S. Cammas-Marion (2021)
Advances in Ultra-Trace Analytical Capability for Micro/Nanoplastics and Water-Soluble Polymers in the Environment: Fresh Falling Urban Snow.
Zi Wang (2021)
Premixed tricalcium silicate/sodium phosphate dibasic cements for root canal filling
Meng Wu (2021)
Biological Implications of Polyethylene Glycol and PEGylation: Therapeutic Approaches Based on Biophysical Studies and Protein Structure-Based Drug Design Tools
Neha Raina (2021)
RAFT polymerization mediated core–shell supramolecular assembly of PEGMA-co-stearic acid block co-polymer for efficient anticancer drug delivery
Priyatosh Sarkar (2021)
Schiff-Linked PEGylated Doxorubicin Prodrug Forming pH-Responsive Nanoparticles With High Drug Loading and Effective Anticancer Therapy
Jian Song (2021)
Potential urinary monitoring of the enhanced permeability and retention effect using MMP-2-responsive poly(ethylene glycol) derivatives.
Xiaohan Sun (2020)
Chemical approaches for the enhancement of porphyrin skeleton-based photodynamic therapy
Yuyan Lin (2020)
Solubility and Bioavailability Enhancement of Oridonin: A Review
Yuanyuan Zhang (2020)
Comparative pharmacokinetic study of PEGylated gemcitabine and gemcitabine in rats by LC-MS/MS coupled with pre-column derivatization and MSALL technique.
L. Yin (2020)
Molecular design of a high-performance polymeric carrier for delivery of a variety of boronic acid-containing drugs.
A. Kim (2020)
Lipidomic changes in mouse oocytes vitrified in PEG 8000-supplemented vitrification solutions.
Gun Tae Jung (2020)
A self-assembled polymer therapeutic for simultaneously enhancing solubility and antimicrobial activity and lowering serum albumin binding of fusidic acid.
Mohammed Salih (2020)
Polymer-drug conjugates as nanomedicine: a review
Monika Lotansing Girase (2020)
Enzymes for pharmaceutical and therapeutic applications
G. Meghwanshi (2020)
Synthesis and Biological Evaluation of Water-Soluble Oleanolic Acid Derivatives for use as Melanogenesis Inhibitors
H. An (2020)
Synchrotron UV photoactivation of trapped sodiated ions produced from poly (ethylene glycol) by electrospray ionization.
Inès Aloui (2020)
Development of amphiphile 4-armed PEO-based Ti4+ complex for highly selective enrichment of phosphopeptides.
Y. Huang (2019)
Gold nanoparticles and polyethylene glycol alleviate clinical symptoms and alter cytokine secretion in a mouse model of experimental autoimmune encephalomyelitis
Tayebe Aghaie (2019)
Reduction sensitive CC9-PEG-SSBPEI/miR-148b nanoparticles: Synthesis, characterization, targeting delivery and application for anti-metastasis.
Cui Cheng (2019)
PEG-amino acid-przewaquinone a conjugations: Synthesis, physicochemical properties and protective effect in a rat model of brain ischemia-reperfusion.
Minghui Wang (2019)
Experimental study on the compound system of proanthocyanidin and polyethylene glycol to prevent coal spontaneous combustion
Zhian Huang (2019)
Intestinal targeting of small molecule MMP and TGR5 ligands for inflammatory bowel disease
M. Pigott (2018)
Laser Structuring of Soft Materials: Laser-Induced Forward Transfer and Two-Photon Polymerization
F. Stokker-Cheregi (2018)
Acetal-linked PEGylated paclitaxel prodrugs forming free-paclitaxel-loaded pH-responsive micelles with high drug loading capacity and improved drug delivery.
D. Huang (2018)
Pharmacokinetics and Biodistribution of Pegylated Methotrexate after IV Administration to Mice
G. Yousefi (2018)
An integrated process for enzymatic catalysis allowing product recovery and enzyme reuse by applying thermoreversible aqueous biphasic systems.
A. Ferreira (2018)
A simple, cost-effective emitter for controlled release of fish pheromones: Development, testing, and application to management of the invasive sea lamprey
C. M. Wagner (2018)
Effects of localized interactions and surface properties on stability of protein‐based therapeutics
Brittney J. Mills (2018)
Human Milk Oligosaccharides as a Defense Against Group B Streptococcus
Dorothy LeeAnn Ackerman (2018)See more