Invention Grant
US07687473B2 5-amino-4-imidazolecarboxamide riboside and its nucleobase as potentiators of antifolate transport and metabolism
有权
5-氨基-4-咪唑酰胺核苷及其核碱基作为抗叶酸转运和代谢的增效剂
- Patent Title: 5-amino-4-imidazolecarboxamide riboside and its nucleobase as potentiators of antifolate transport and metabolism
- Patent Title (中): 5-氨基-4-咪唑酰胺核苷及其核碱基作为抗叶酸转运和代谢的增效剂
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Application No.: US11327872Application Date: 2006-01-09
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Publication No.: US07687473B2Publication Date: 2010-03-30
- Inventor: John J. McGuire
- Applicant: John J. McGuire
- Applicant Address: US NY Buffalo
- Assignee: Health Research, Inc.
- Current Assignee: Health Research, Inc.
- Current Assignee Address: US NY Buffalo
- Agency: Hodgson Russ LLP
- Main IPC: A01N43/04
- IPC: A01N43/04 ; A61K31/70
Abstract:
The present invention provides a method for increasing the efficacy of antifolates which act via inhibition of dihydrofolate reductase (DHFR). The method comprises the steps of administration of 5-amino-4-imidazolecarboxamide riboside (Z) or its base with the antifolate such that the targeted cells are exposed to both the antifolate and Z simultaneously. This results in increased influx of the antifolate. For MTX, accumulation of the more biologically active polyglutamate forms is also potentiated. This potentiation appears to be mediated by an effect on the RFC.
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