159351-81-2Relevant academic research and scientific papers
Enzymic synthesis and biological evaluation of injectable glutathione-everolimus
Wang, Haibo,Zheng, Xiaohe,Mao, Lifei,Qin, Liang,Zhu, Tianmin
, p. 583 - 591 (2018)
An enzymic synthesis of glutathione-everolimus is reported. This process has been optimized and scaled up with high reproducibility and yields, which will facilitate the development of such conjugate. The stability of the conjugate supported that this prodrug can be prepared into lyophilized solid, which is to be reconstituted with 0.9% sodium chloride for injection before intravenous infusion. And the results of species-related drug release experiment displayed that the performance of the conjugate in human plasma, rat and monkey was similar. Moreover, the in vivo efficacy of glutathione-everolimus in the treatment of renal cell carcinoma was investigated in detail. The conjugate was proved to be an effective, safe and well-tolerated injectable prodrug in the treatment of renal cell carcinoma. The results indicated that three times injection with a high dosage in 1 week can achieve much better in vivo efficacy, and no obvious toxic response was observed.
Processes for preparing water-soluble polyethylene glycol conjugates of macrolide immunosuppressants
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Page/Page column 16-17, (2008/06/13)
Processes are described for preparing 42-pegylated rapamycins including reacting a rapamycin with an acylating agent in the presence of a lipase to form an acylated rapamycin and reacting the acylated rapamycin with a methoxy poly(ethylene glycol) derivative in the presence of a base. Also described are processes for preparing 32-pegylated tacrolimus and/or ascomycin using these steps.
