ABSTRACT
OBJECTIVE To comprehensively evaluate four weekly preparations of glucagon-like peptide-1 receptor agonist （GLP-1RA） marketed in China，and to provide evidence for hospitals to optimize drug catalogs and clinical rational drug use. METHODS Mini health technology assessment method was used to establish detailed evaluation rules according to A Quick Guideline for Drug Evaluation and Selection in Chinese Medical Institutions， and conduct comprehensive evaluation of four GLP- 1RA weekly preparations from aspects of pharmaceutical characteristics， effectiveness， safety， economy and other attributes. RESULTS Mini health technology assessment scores of the four GLP-1RA weekly preparations from high to low were dulaglutide 78.60 points， semaglutide 77.35 points，polyethylene glycol loxenatide 67.40 points， and exenatide microspheres 65.50 points， respectively. Dulaglutide had advantages in reducing blood sugar， arteriosclerotic cardiovascular disease， kidney benefits， and cost- effectiveness. Semaglutide had advantages in reducing blood sugar and weight loss， but its cost-effectiveness was lower than that of dulaglutide. Exenatide microspheres had advantages in the use of children， but its daily average treatment cost is the highest. Polyethylene glycol loxenatide needed further clinical evidence. CONCLUSIONS Four GLP-1RA weekly preparations all have high pharmaceutical comprehensive scores. Dulaglutide and semaglutide may have more comprehensive pharmaceutical value among them， while the use of exenatide microspheres for children is unique.
ABSTRACT
OBJECTIVE: To investigate whether there is significant difference between the GLP-1-Fc fusion protein(YD057) that is expressed by gene recombination and the marketed drug dulaglutide(Lilly). METHODS: SDS-PAGE, SEC, CE-SDS and CIEF were used to analyze the differences in molecular weight, purity and charge heterogeneity. The amino acid sequence, biological activity and receptor binding analysis were measured to assess whether the cytological function and molecular binding capacity were consistent. Oligosaccharide distribution was measured to assess whether N-linked glycosylation modification ratio was consistent. RESULTS: There was no significant difference in physicochemical properties, amino acid primary sequence, N-linked glycosylation modification ratio, cell biology function and receptor binding capacity between the biological similar drugs(YD057) and dulaglutide. CONCLUSION: Their critical quality attributes are basically the same.
ABSTRACT
@# Objective To investigate the protective effects of dulaglutide on Alzheimer’s disease (AD)-like neurodegenerativechangesanditsmechanismthereof. Methods Dulaglutide，anewdrugfordiabetes,wasappliedto observeandexploreAD-likeneurodegenerativechangesinducedbyPI3KinhibitorwortmannininSH-SY5Ycells.MTT assaywasusedtoobservethecellvitalityinducedbydulaglutide,wortmanninandglucagon-likepeptide(GLP-1)1receptor antagonistex9-39.WesternblotassaywasusedtodetectthelevelsofphosphorylatedTau,neurofilaments(NFs)andthe proteinsofPI3K/GSK-3βsignalingpathway.Results Dulaglutideimprovedtheimpairedvitality,increasedthelevelsof phosphorylatedPI3KandGSK-3βanddecreasedphosphorylationlevelsoftauandNFsinducedbywortmannininSHSY5Ycells.Ex9-39antagonizedtheeffectsofDulaglutide. Conclusion DulaglutideprotectsSH-SY5YcellsfromADlikeneurodegenerativechangesthroughimprovingPI3K/GSK-3βinsulinsignalingpathway.