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Nucleoside Triphosphates - From Synthesis to Biochemical Characterization
Published on: April 3, 2014
The Holý Trinity: the acyclic nucleoside phosphonates.
1Rega Institute for Medical Research, KU Leuven, Leuven, Belgium. erik.declercq@rega.kuleuven.be
Advances in Pharmacology (San Diego, Calif.)
|July 27, 2013
Summary
A new class of antiviral drugs, acyclic nucleoside phosphonates, has revolutionized treatment for DNA virus infections, hepatitis B, and AIDS (HIV infection). These compounds offer effective therapies for various viral diseases.
Area of Science:
- Virology
- Medicinal Chemistry
- Pharmacology
Background:
- A new class of antiviral agents, acyclic nucleoside phosphonates, was pioneered.
- These compounds are based on the work of Dr Antonín Holý, Dr John C. Martin, and the author.
Purpose of the Study:
- To highlight the development and impact of acyclic nucleoside phosphonates in antiviral therapy.
- To showcase the successful application of these compounds in treating significant viral infections.
Main Methods:
- Development of acyclic nucleoside phosphonates.
- Clinical trials and regulatory approval of derived drugs.
- Formulation of prodrugs for improved delivery and efficacy.
Main Results:
- Several approved drugs derived from this class: cidofovir (DNA viruses), adefovir (hepatitis B), and tenofovir (HIV infection).
- Tenofovir disoproxil fumarate, an oral prodrug, is used for hepatitis B and HIV treatment/prophylaxis.
- Combination therapies involving tenofovir, emtricitabine, and other HIV inhibitors (efavirenz, rilpivirine, elvitegravir/cobicistat) are effective for AIDS treatment.
Conclusions:
- Acyclic nucleoside phosphonates represent a major advancement in antiviral drug development.
- These agents have led to transformative treatments for serious viral infections like HIV and hepatitis B.
- The ongoing development and combination therapies underscore the sustained importance of this drug class.
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