PEGylation Technology

來源：seebio.cn作者：西寶生物人氣：-發表時間：2012-06-21 08:50:17【大中小】

PEGylation has been a highly effective commercial strategy for the development of blockbuster therapeutics, such as Roche's PEGASYS? (interferon) and Amgen's Neulasta? (G-CSF).

PEG (polyethylene glycol), a versatile technology, is a water soluble, amphiphilic, non-toxic, non-immunogenic compound that is safely cleared from the body. Its primary use to date in currently approved drugs is to favorably alter the pharmacokinetic properties of biologics. Early approaches to PEGylation were tremendously successful in creating blockbuster biologics but these did not fully leverage the flexibility and potential of the technology.

The limitations of older PEGylation approaches used with biologics are:

Sub-optimal bioavailability and bioactivity
Product is altered by PEG remaining attached to parent drug
Limited ability to fine-tune properties of drug
Did not allow for oral administration
Not applicable to small molecules, antibody fragments, and peptides

Related products:

Product	Mw（PEG raw material）	replacement rate	PD
mPEG-OH-10K	10000±1000		≤1.06
mPEG-OH-20K	20000±2000		≤1.06
mPEG-OH-30K	30000±3000		≤1.08
mPEG-NH₂-2K	2000±200	≥95%	≤1.05
mPEG-NH₂-5K	5000±500	≥95%	≤1.05
mPEG-NH₂-10K	10000±1000	≥95%	≤1.06
mPEG-NH₂-20K	20000±2000	≥90%	≤1.08
mPEG-NH₂-30K	30000±3000	≥90%	≤1.08
mPEG-SC-2K	2000±200	≥95%	≤1.05
mPEG-SC-5K	5000±500	≥95%	≤1.05
mPEG-SC-10K	10000±1000	≥95%	≤1.06
mPEG-SC-20K	20000±2000	≥90%	≤1.08
mPEG-SC-30K	30000±3000	≥90%	≤1.08
mPEG-MAL-20K	20000±2000	≥90%	≤1.08
mPEG-MAL-30K	30000±3000	≥90%	≤1.08
mPEG--COOH-2K	2000±200	≥95%	≤1.05
mPEG-COOH-5K	5000±500	≥95%	≤1.05
mPEG-COOH-10K	10000±1000	≥95%	≤1.06
mPEG-COOH-20K	20000±2000	≥90%	≤1.08
mPEG-COOH-30K	30000±3000	≥90%	≤1.08
mPEG-SPA-2K	2000±200	≥95%	≤1.05
mPEG-SPA-5K	5000±500	≥95%	≤1.05
mPEG-PA-2K	～2000	≥95%	≤1.05
mPEG-PA-3.4K	～3400	≥95%	≤1.05
mPEG-NHS-10K	10000±1000	≥90%	≤1.06
mPEG-NHS-20K	20000±2000	≥90%	≤1.08
mPEG-NHS-30K	30000±3000	≥90%	≤1.08
mPEG-AC-2K	2000±200	≥95%	≤1.05
mPEG-AC-5K	5000±500	≥95%	≤1.05
mPEG-AC-10K	10000±1000	≥90%	≤1.06
mPEG-AC-20K	20000±2000	≥90%	≤1.08
mPEG-AC-30K	30000±3000	≥90%	≤1.08
mPEG-Ms-2K	2000±200	≥95%	≤1.05
mPEG- Ms -5K	5000±500	≥95%	≤1.05
mPEG- Ms -10K	10000±1000	≥90%	≤1.06
mPEG- Ms -20K	20000±2000	≥90%	≤1.08
mPEG- Ms -30K	30000±3000	≥90%	≤1.08
Bi-NH₂-2K	2000±200	≥95%	≤1.05
Bi-NH₂-3.4K	3400±340	≥95%	≤1.05
Bi-NH₂-4K	4000±400	≥95%	≤1.05
Bi-NH₂-6K	5000±500	≥95%	≤1.05
Bi-NH₂-10K	10000±1000	≥90%	≤1.06
Bi-NH₂-20K	20000±2000	≥90%	≤1.08
Bi-COOH-2K	2000±200	≥95%	≤1.05
Bi-COOH-3.4K	3400±340	≥95%	≤1.05
Bi-COOH-4K	4000±400	≥95%	≤1.05
Bi-COOH-6K	5000±500	≥95%	≤1.05
Bi-COOH-10K	10000±1000	≥95%	≤1.06
Bi-COOH-20K	20000±2000	≥90%	≤1.08
4-arm-PEG-5K	5000±500		≤1.05
4-arm-PEG-10K	10000±1000		≤1.06
4-arm-PEG-20K	20000±2000		≤1.07
4-arm-NH₂-5K	5000±500		≤1.05
4-arm-NH₂-10K	10000±1000		≤1.06
4-arm-NH₂-20K	20000±2000		≤1.07
HO-PEG-NH₂-2K	2000±200	≥95%	≤1.05
HO-PEG-NH₂-3.4K	3400±340	≥95%	≤1.05
HO-PEG-NH₂-0.6K
HO-PEG-COOH-2K	2000±200	≥95%	≤1.05
HO-PEG-COOH-3.4K	3400±340	≥95%	≤1.05
NH₂-PEG-COOH-2K	2000±200	≥95%	≤1.05
NH2-PEG-MAL-2K	2000±200	≥95%	≤1.05
Acryl-PEG-NHS-2K	2000±200	≥95%	≤1.05