A cytarabine peptidomimetic prodrug composition and uses thereof

By combining cytarabine peptide prodrugs and chidamide, the problem of low oral bioavailability of cytarabine has been solved, achieving higher oral bioavailability and less injection frequency, thus enhancing the therapeutic effect on cancer.

CN122398840APending Publication Date: 2026-07-17SHENYANG PHARMA UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHENYANG PHARMA UNIV
Filing Date
2025-01-17
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Cytarabine has low oral bioavailability, leading to the need for frequent intravenous infusions or subcutaneous injections. Existing technologies make it difficult to improve its activity and stability in vivo.

Method used

To develop a composition of cytarabine peptide prodrug and dicaruridine, by adjusting the ratio of the two to enhance the membrane permeability of cytarabine and its inhibitory effect on cytidine deaminase, thereby improving oral bioavailability.

Benefits of technology

It significantly improves the oral bioavailability of cytarabine, reduces its metabolism in the body, decreases the frequency of intravenous infusion or subcutaneous injection, and enhances the therapeutic effect on cancer.

✦ Generated by Eureka AI based on patent content.

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Abstract

本发明提供一种阿糖胞苷拟肽类前药和西达尿苷联用的口服给药组合物，属于药物领域。本发明提供了一种阿糖胞苷拟肽类前药组合物，所述组合物包括阿糖胞苷拟肽类前药或其盐，和西达尿苷。本发明涉及的药物组合物，一方面旨在通过提升小肠的通透性，增强阿糖胞苷的口服吸收效率，从而提高其生物利用度。另一方面，该组合物显著提升了抑制胞苷脱氨酶活性的效能，有效减缓阿糖胞苷的代谢速度。相较于非阿糖胞苷拟肽类前药与西达尿苷的联合使用，本发明的药物组合物在特定比例下的疗效更为卓越。
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