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1. Introduction
2. Outline
3. Nucleoside phosphonates definition
4. Modifications of nucleoside phosphonates
5. Beginning of nucleoside phosphonate antivirals
6. ANPs as broad-spectrum antivirals
7. Clinically approved ANPs
8. HIV inhibition mechanism
9. Nucleoside phosphonates and HIV inhibition
10. HIV reverse transcription
11. Intracellular activation
12. Interaction with HIV reverse transcriptase
13. Tenofovir-diphosphate binding
14. Tenofovir-diphosphate mechanism
15. Tenofovir-diphosphate poor selectivity
16. Nucleoside/tide RT inhibitors (NRTIs)
17. Tenofovir prolonged antiviral action
18. HIV resistance to tenofovir
19. Unique features of tenofovir
20. Prodrugs of nucleoside phosphonates
21. Prodrugs usage advantages
22. Antiviral activity of prodrugs
23. GS-7340 compound
24. GS-7340: intracellular activation
25. GS-7340 distribution
26. Clinical use and efficacy
27. Tenofovir disoproxil fumarate (TDF)
28. Key studies with TDF in HIV patients
29. Study GS-935 detailed outcome
30. Studies since TDF approval
31. HIV treatment guidelines
32. Tenofovir and prevention of HIV transmission
33. Nucleoside phosphonates and renal toxicity
34. Nucleoside phosphonates renal transport
35. Novel nucleoside phosphonates
36. Classical acyclic phosphonate
37. Other acyclic phosphonate
38. Cyclic nucleoside phosphonates
39. Tetrahydrofuran core examples
40. d4AP compound
41. GS-9131: amidate prodrug of GS-9148
42. In vivo pharmacokinetics of GS-9131
43. Summary
44. Nucleoside phosphonates summary (1)
45. Nucleoside phosphonates summary (2)
46. Acknowledgements

Topics Covered

• Nucleoside phosphonates and their antiviral spectrum
• Mechanism of action and characteristics of tenofovir
• Prodrugs of nucleoside phosphonates
• Clinical use and efficacy
• Novel classes of nucleoside phosphonates
• Summary of antiviral profiles

Links

Series:

• Antivirals

Categories:

• Biochemistry
• Clinical Practice
• Microbiology
• Pharmaceutical Sciences

Therapeutic Areas:

• Infectious Diseases

Talk Citation

Publication History

• Published on August 30, 2011

Financial Disclosures

• Dr. Tomas Cihlar has not informed HSTalks of any commercial/financial relationship that it is appropriate to disclose.