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Fosalvudine
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Drug Class: Nucleoside Reverse Transcriptase Inhibitors

Drug Description
Fosalvudine, also known as fosalvudine tidoxil, is a prodrug of alovudine, a nucleoside reverse transcriptase inhibitor.[1]

HIV/AIDS-Related Uses
Fosalvudine is being evaluated in Phase II clinical trials for the treatment of HIV-1 infection in patients who have multiple-NRTI-resistant HIV-1 infection.[2][3]

Dosing Information

Mode of Delivery
Oral.[4]

Dosage Form
Fosalvudine 5, 10, 20, and 40 mg have been studied in Phase I and II clinical trials. Fosalvudine 10- to 40-mg doses are being studied in ongoing Phase II trials.[5][6]

Pharmacology
Fosalvudine is an enhanced prodrug (through addition of a single phosphate group) of alovudine, a thymidine-anologue nucleoside reverse transcriptase inhibitor. Fosalvudine is covalently linked to a specific lipid-moiety, which should reduce adverse effects associated with alovudine treatment. Fosalvudine is expected to have altered pharmacokinetics and distribution compared with alovudine.[7][8]

In vitro, fosalvudine inhibits the replication of HIV group M subtypes A through G. In a murine tissue study, low concentrations of fosalvudine were distributed to fat and bone marrow, which suggests a low potential for hematopoetic toxicity.[9]

Fosalvudine is being studied in Phase II trials in treatment-naïve and treatment-experienced patients infected with HIV-1. In a 14-day, dose-finding, Phase II study in treatment-naïve patients, fosalvudine exhibited dose-dependent efficacy across 10- to 40-mg doses. Mean viral load reduction at day 15 was 60% for the 5-mg dose, nearly 80% for the 10-mg dose, 85% for the 20-mg dose, and 90% for the 40-mg dose compared with placebo (nearly 0% change in viral load). Fosalvudine is currently being studied in a Phase II trial in treatment-experienced patients.[10]

Adverse Events/Toxicity
Fosalvudine doses of 5 to 40 mg were well tolerated in treatment-naïve, HIV-infected patients for 14 days. Adverse effects were infrequent and included grade 1 nausea, vomiting, and diarrhea and grade 2 headache.[11]

Clinical Trials
Click here to search ClinicalTrials.gov for trials that use Fosalvudine.

Chemistry

Further Reading
CahnP., et al. A phase-II study of 14 days monotherapy with the nucleoside-analogue Fosalvudine Tidoxil in treatment-naïve HIV-1 infected adults. Poster exhibition: 4th IAS Conference on HIV Pathogenesis, Treatment and Prevention: Abstract no. WEPEB114LB. Available at: http://aids2008.org/Abstracts/A200705533.aspx. Accessed 09/08/08.

Manufacturer Information
Fosalvudine
  Heidelberg Pharma
  Schriesheimer Strasse 101
  D-68526 Ladenburg
  Baden-Wurttemberg,  Germany
  49-6203-1009-40
    

References
[1] Heidelberg Pharma - News: HEIDELBERG PHARMA AG starts second clinical phase II study with FOSALVUDINE [Press Release], November 12, 2007. Available at: http://www.heidelberg-pharma.com/news/popup/20071112.html. Accessed 09/08/08.
[2] Heidelberg Pharma - News: HEIDELBERG PHARMA AG starts second clinical phase II study with FOSALVUDINE [Press Release], November 12, 2007. Available at: http://www.heidelberg-pharma.com/news/popup/20071112.html. Accessed 09/08/08.
[3] Heidelberg - Products - Pipeline: Fosalvudine. Available at: http://www.heidelberg-pharma.com/products/fosalvudine.html. Accessed 09/08/08.
[4] Heidelberg Pharma - News: HEIDELBERG PHARMA AG starts second clinical phase II study with FOSALVUDINE [Press Release], November 12, 2007. Available at: http://www.heidelberg-pharma.com/news/popup/20071112.html. Accessed 09/08/08.
[5] IAS Conf HIV Pathogen, Treat, Prevent- 4th, 2007 - Abstract WEPEB114LB.
[6] Heidelberg Pharma - News: HEIDELBERG PHARMA AG starts second clinical phase II study with FOSALVUDINE [Press Release], November 12, 2007. Available at: http://www.heidelberg-pharma.com/news/popup/20071112.html. Accessed 09/08/08
[7] IAS Conf HIV Pathogen, Treat, Prevent- 4th, 2007 - Abstract WEPEB114LB.
[8] IAS Conf - 16th, 2006 - Abstract ThPE0025.
[9] IAS Conf - 16th, 2006 - Abstract ThPE0025.
[10] Heidelberg - HEIDELBERG PHARMA AG starts second clinical phase II study with FOSALVUDINE [Press Release], November 12, 2007. Available at: http://www.heidelberg-pharma.com/news/popup/20071112.html. Accessed 09/08/08.
[11] IAS Conf HIV Pathogen, Treat, Prevent- 4th, 2007 - Abstract WEPEB114LB.
Updated September 8, 2008