Fosamprenavir

Structural formula
General
Non-proprietary name	Fosamprenavir
other names	GW433908
Molecular formula	C 25 H 36 N 3 O 9 PS
External identifiers / databases
CAS number 226700-79-4 PubChem 131536 ChemSpider 116245 DrugBank DB01319 Wikidata Q1385311
Drug information
ATC code	J05 AE07
Drug class	HIV protease inhibitor
Mechanism of action	Inhibition of HIV proteases
properties
Molar mass	585.61 g mol −1
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed GHS hazard labeling no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Fosamprenavir (fAPV, trade name: Telzir ^® , manufacturer: GlaxoSmithKline ) is a drug that is used in oral dosage forms for the treatment of HIV infections and AIDS . It belongs to the group of HIV protease inhibitors that are usually combined with other antiviral drugs. See HAART , NNRTI , NRTI .

Fosamprenavir-containing tablets and suspensions were developed by Glaxo Wellcome and approved by the European Commission in July 2004 for the treatment of previously treated patients with HIV infection in the EU.

Indication and effectiveness

The medicine is approved for HIV infection in adults. Fosamprenavir itself is not effective; only the metabolite amprenavir , which is itself available as a medicinal substance, develops the antiviral effect. As a rule, fosamprenavir is boosted with ritonavir , which means that a second HIV protease inhibitor in a low dose inhibits the breakdown of fosamprenavir so that a higher active ingredient content remains in the body.

Mechanism of action, pharmacokinetics

Fosamprenavir is a further development of the HIV protease inhibitor amprenavir. By esterification with phosphoric acid a was prepared from amprenavir prodrug with diminished lipophilicity , the better absorption from the gastrointestinal tract allows. Fosamprenavir is hydrolyzed to amprenavir during absorption. This is almost completely bound to plasma proteins in the blood. The effect is to inhibit the viral HIV protease , which means that infectious viruses can no longer be formed in the host cell . Degradation and excretion takes place via the liver and stool, with the cytochrome P450 enzyme system playing the decisive role.

dosage

The recommended dosage for fosamprenavir is 700 mg twice daily (= 1 film-coated tablet ) together with 100 mg ritonavir twice daily. This means a significant reduction in the number of tablets compared to therapy with amprenavir.

Side effects, contraindications

Headache, dizziness, tiredness, nausea, vomiting, diarrhea and exanthema are common . Under certain circumstances, these can lead to life-threatening complications and discontinuation of therapy. The breakdown mechanism via the liver results in numerous interactions with other drugs. The combination of fosamprenavir / ritonavir, both inhibitors of the cytochrome CYP3A4 isoenzyme, aggravates this situation significantly. Treatments with additional medication therefore require careful monitoring.

literature

• JM Gatell: From amprenavir to GW433908 , J HIV Ther., 2001; 6 (4): 95-99.

Web links

• Drug Information (Engl.)
• MEROPS : Page on Fosamprenavir (engl.)

Individual evidence

1. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.

This article is about a health issue. It is not used for self-diagnosis and does not replace a diagnosis by a doctor. Please note the information on health issues !