Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027497 (nausea)
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Agenerase (amprenavir), the first of a new generation of protease inhibitors, manufactured by Glaxo Wellcome, promises to be a powerful drug for salvage therapy and for use in treatment-naive patients. It is the first protease inhibitor to be approved by the Rockville, MD-based Food and Drug Administration in 2 years. The drug does not elevate glucose or triglyceride levels as much as some of the other protease inhibitors do, and resistance to this drug is different from that of other protease inhibitors. Some adverse effects include nausea, diarrhea, and rash, and one percent of patients may experience severe and life-threatening skin conditions. Agenerase has been studied in 1,400 patients, and costs about $6,100 per year.
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PMID:Study: new drug doesn't display cross-resistance. 1136 18

The FDA has approved amprenavir (Agenerase), the fifth protease inhibitor (PI) to be approved and the first PI approved in 2 years. When used in triple combination therapy, amprenavir is effective in viral suppression in treatment-naive patients and some patients who have taken NRTIs and NNRTIs. The drug has also been shown to be effective in about half of the patients who are resistant to other PIs. The standard dose for amprenavir is eight large capsules taken twice a day. Levels of amprenavir may be affected by the concurrent use with efavirenz (Sustiva). Common side effects of amprenavir include nausea, vomiting, diarrhea, and numbness and tingling around the mouth.
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PMID:Amprenavir approved. 1136 53

The FDA has approved Agenerase (generic name amprenavir), a new protease inhibitor which costs about $6,500 per year. Eight 150mg gelatin capsules, twice a day, can be taken without food restrictions. Potential side effects include nausea, fatigue, and headache. About 20 percent of patients developed a rash, that was life-threatening in 1 percent. Early data indicate that the drug does not cause lipodystrophy. Drug interactions are possible with some antihistamines, sedatives, and anti-fungal agents. Website contact information is provided.
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PMID:New protease inhibitor. 1136 64

Fosamprenavir (GW433908, Lexiva, Telzir) is an oral prodrug of the protease inhibitor (PI) amprenavir, with a reduced daily pill burden. Fosamprenavir, in combination with other antiretroviral agents, is indicated for the treatment of patients with HIV infection, particularly those who have not previously received antiretroviral therapy. Viral load reductions were at least as great with fosamprenavir-based regimens as those achieved with nelfinavir-based regimens in two large, 48-week, randomised, multicentre trials in antiretroviral therapy-naive patients with HIV infection. In the NEAT study, more patients receiving twice-daily fosamprenavir in combination with abacavir and lamivudine achieved HIV RNA levels <400 copies/mL than those receiving a similar nelfinavir-based regimen. Results of the SOLO study showed similar reductions in viral load among patients who received once-daily ritonavir-boosted fosamprenavir and those treated with twice-daily nelfinavir, both in combination with twice-daily abacavir and lamivudine. In both trials, virological failure rates were at least twice as high with the nelfinavir-based regimen as they were with the fosamprenavir-based regimen. Fosamprenavir was generally well tolerated in clinical trials. The most common adverse events among patients treated with fosamprenavir, with or without ritonavir, plus abacavir and lamivudine were diarrhoea, nausea, vomiting, abdominal pain, drug hypersensitivity and skin rash. The incidence of diarrhoea was significantly lower with fosamprenavir-based therapy than with nelfinavir-based therapy in the NEAT and SOLO trials. The resistance profile of fosamprenavir is consistent with that of amprenavir. Amprenavir-resistant viral isolates from patients experiencing treatment failure with fosamprenavir-based therapy in the NEAT study showed little or no cross-resistance to several other PIs, and protease mutations commonly selected for by various other PIs were not observed. In the SOLO study, protease resistance mutations were not observed in viral isolates from patients experiencing treatment failure with ritonavir-boosted fosamprenavir-based therapy. In conclusion, fosamprenavir-based regimens have shown good antiviral efficacy and are generally well tolerated in antiretroviral therapy-naive patients with HIV infection. Available data on the resistance profile of the drug suggest that it may be used early in the course of therapy without compromising a range of future treatment options. The relatively low pill burden and lack of food restrictions with fosamprenavir may improve adherence to therapy. Further studies are needed to compare fosamprenavir with other PIs and to establish the long-term efficacy of fosamprenavir-based regimens. In conclusion, fosamprenavir appears to be a promising agent for the treatment of antiretroviral therapy-naive patients with HIV infection.
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PMID:Fosamprenavir: a review of its use in the management of antiretroviral therapy-naive patients with HIV infection. 1534 7