Antiviral prodrugs and pharmaceutical compositions thereof
EFdA diesters with reduced solubility, formulated as crystalline suspensions, address the limitations of EFdA by achieving prolonged plasma levels and viral suppression, effectively extending treatment duration in HIV infection and pre-exposure prophylaxis.
Patent Information
- Application Number
- AU2026204849
- Authority / Receiving Office
- AU · AU
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2026-06-23
- Publication Date
- 2026-07-09
AI Technical Summary
EFdA, a nucleoside analog used as an antiretroviral, has a high water solubility and short plasma concentration, limiting its duration of viral suppression in treating HIV infection and pre-exposure prophylaxis.
Development of EFdA diesters with reduced aqueous solubility, formulated as crystalline compounds for parenteral administration in suspensions with pharmaceutically acceptable carriers, providing extended duration of viral suppression.
The EFdA diesters achieve prolonged plasma levels and viral suppression, with compounds like Compound 3 and 5 exhibiting plasma levels above the lower limit of quantitation for over a week in rats and a month in rhesus macaques, significantly extending the duration of viral suppression compared to EFdA.
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