Development of an Oral Form of Azacytidine : 2′3′5′Triacetyl-5-Azacytidine

المؤلفون المشاركون

Hayes, Eugene
Pizzorno, Giuseppe
Ye, Tao
Freeman, Burgess B.
Ziemba, Amy

المصدر

Chemotherapy Research and Practice

العدد

المجلد 2011، العدد 2011 (31 ديسمبر/كانون الأول 2011)، ص ص. 1-9، 9ص.

الناشر

Hindawi Publishing Corporation

تاريخ النشر

2011-12-18

دولة النشر

مصر

عدد الصفحات

9

التخصصات الرئيسية

علم الصيدلة

الملخص EN

Myelodysplastic syndromes (MDSs) represent a group of incurable stem-cell malignancies which are predominantly treated by supportive care.

Epigenetic silencing through promoter methylation of a number of genes is present in poor-risk subtypes of MDS and often predicts transformation to acute myelogenous leukemia (AML).

Azacitidine and decitabine, two FDA-approved DNA methyltransferase (DNMT) inhibitors, are able to improve overall response although their oral bioavailability complicates their clinical use.

This study evaluated 2′,3′,5′-triacetyl-5-azacitidine (TAC) as a potential prodrug for azacitidine.

The prodrug demonstrated significant pharmacokinetic improvements in bioavailability, solubility, and stability over the parent compound.

In vivo analyses indicated a lack of general toxicity coupled with significantly improved survival.

Pharmacodynamic analyses confirmed its ability to suppress global methylation in vivo.

These data indicate that esterified nucleoside derivatives may be effective prodrugs for azacitidine and encourages further investigation of TAC into its metabolism, activity, and possible clinical evaluation.

نمط استشهاد جمعية علماء النفس الأمريكية (APA)

Ziemba, Amy& Hayes, Eugene& Freeman, Burgess B.& Ye, Tao& Pizzorno, Giuseppe. 2011. Development of an Oral Form of Azacytidine : 2′3′5′Triacetyl-5-Azacytidine. Chemotherapy Research and Practice،Vol. 2011, no. 2011, pp.1-9.
https://search.emarefa.net/detail/BIM-512077

نمط استشهاد الجمعية الأمريكية للغات الحديثة (MLA)

Ziemba, Amy…[et al.]. Development of an Oral Form of Azacytidine : 2′3′5′Triacetyl-5-Azacytidine. Chemotherapy Research and Practice No. 2011 (2011), pp.1-9.
https://search.emarefa.net/detail/BIM-512077

نمط استشهاد الجمعية الطبية الأمريكية (AMA)

Ziemba, Amy& Hayes, Eugene& Freeman, Burgess B.& Ye, Tao& Pizzorno, Giuseppe. Development of an Oral Form of Azacytidine : 2′3′5′Triacetyl-5-Azacytidine. Chemotherapy Research and Practice. 2011. Vol. 2011, no. 2011, pp.1-9.
https://search.emarefa.net/detail/BIM-512077

نوع البيانات

مقالات

لغة النص

الإنجليزية

الملاحظات

Includes bibliographical references

رقم السجل

BIM-512077