History
Around 1970, Frank F. Davis, a professor of biochemistry at Rutgers University, became interested in developing a process to render usable bioactive proteins of potential medical value. After considerable study, he concluded that the attachment of an inert and hydrophilic polymer might extend blood life and control immunogenicity of the proteins. Polyethylene glycol was chosen as the polymer. A team of Davis, Theodorus Van Es and Nicholas C. Palczuk conducted animal studies and found that PEG attachment greatly extended blood life and controlled immunogenicity of the proteins. A patent was obtained. Abraham Abuchowski conducted extensive additional PEGylation studies on various enzymes. Davis and Abuchowski founded Enzon, Inc., which brought three PEGylated drugs to market. Abuchowski later founded and is CEO of Prolong Pharmaceuticals.
PEGylation, is a process of attaching the strands of the polymer PEG to molecules most typically peptides, proteins, and antibody fragments, that can help to meet the challenges of improving the safety and efficiency of many therapeutics It produces alterations in the physiochemical properties including changes in conformation, electrostatic binding, hydrophobicity etc. These physical and chemical changes increase systemic retention of the therapeutic agent. Also, it can influence the binding affinity of the therapeutic moiety to the cell receptors and can alter the absorption and distribution patterns.
PEGylation, by increasing the molecular weight of a molecule, can impart several significant pharmacological advantages over the unmodified form, such as:
- Improved drug solubility
- Reduced dosage frequency, without diminished efficacy with potentially reduced toxicity
- Extended circulating life
- Increased drug stability
- Enhanced protection from proteolytic degradation
PEGylated drugs have the following commercial advantages also:
- Opportunities for new delivery formats and dosing regimens
- Extended patent life of previously approved drugs
Read more about this topic: PEGylation
Famous quotes containing the word history:
“This above all makes history useful and desirable: it unfolds before our eyes a glorious record of exemplary actions.”
—Titus Livius (Livy)
“All history is a record of the power of minorities, and of minorities of one.”
—Ralph Waldo Emerson (1803–1882)
“All objects, all phases of culture are alive. They have voices. They speak of their history and interrelatedness. And they are all talking at once!”
—Camille Paglia (b. 1947)