Gamma polyglutamine oxoxide antimetabolites and their use

Gamma-polyglutamine oxidized folate antimetabolites delivered via liposomes address the limitations of folate antagonist therapies by enhancing cancer cell cytotoxicity and overcoming resistance, thus improving therapeutic efficacy.

JP7884876B2Active Publication Date: 2026-07-06L E A F HLDG GRP
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Patent Information

Application Number
JP2025070872
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Priority Date
2018-08-17
Filing Date
2025-04-22
Publication Date
2026-07-06
Estimated Expiration
2039-02-07

AI Technical Summary

Technical Problem

Existing folate antagonist therapies for treating diseases such as cancer, immune system disorders, and infectious diseases face challenges with dose-limiting toxicity and therapeutic resistance due to cellular mechanisms like efflux pumps and drug resistance, limiting their clinical efficacy.

Method used

The development of gamma-polyglutamine oxidized folate antimetabolites, delivered via liposomes, which directly target cancer cells while minimizing exposure to normal tissues and overcoming resistance mechanisms, enhancing cytotoxic effects on cancer cells.

Benefits of technology

This approach optimizes the therapeutic efficacy of folate antimetabolites by reducing dose-limiting toxicity and resistance, improving cytotoxicity on cancer cells, and minimizing effects on normal tissues.

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Patent Text Reader

Abstract

To provide gamma polyglutamated antifolate compositions to overcome pharmacological challenges associated with antifolate therapy, the dose-limiting toxicities and treatment resistance.SOLUTION: Disclosed is a liposome composition comprising a gamma polyglutamated antifolate (Lp-γPANTIFOL composition), where the gamma polyglutamated antifolate comprises 2-10 glutamyl groups, the liposome is PEGylated, and the liposome composition comprises a targeting moiety that has a specific affinity to a surface antigen on a target cell of interest.SELECTED DRAWING: None
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Citation Information

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