HIV drug fosamprenavir (Lexiva) raises cholesterol; could lead to heart disease

The anti-HIV drug fosamprenavir calcium (Lexiva) could lead to heart disease, warns the maker of the drug GlaxoSmithKline.

Fosamprenavir (Lexiva), which is used in combination with other antiretroviral agents for the treatment of HIV infection has a possible link with heart attacks in HIV-infected adults, the US Food and Drug Administration said.

Taking fosamprenavir (Lexiva) could raise your cholesterol and triglyceride levels, placing the HIV patients at risk for developing heart disease in the future, US FDA warned in a statement.

Doctors who prescribe fosamprenavir (Lexiva) are recommended to check cholesterol levels in patients before treatment, as well as monitor patients for high blood pressure, diabetes and smoking, which can also lead to heart disease.

Fosamprenavir (Lexiva) was approved in US on October 20, 2003.

Lexiva is a prodrug of amprenavir, a protease inhibitor used to treat infection with the human immunodeficiency virus (HIV-1). Lexiva is rapidly converted to amprenavir by cellular or serum phosphatases in the body.

Lexiva is indicated in combination with other antiretroviral agents for the treatment of HIV infection in adults.

The approval of Lexiva was based on two studies in antiretroviral naive patients and one study in protease inhibitor experienced patients.

In study APV30001, Lexiva (1,400 mg twice daily) was compared to nelfinavir (1,250 mg twice daily) in 249 antiretroviral naive patients. Both treatment groups also received abacavir (300 mg twice daily) and lamivudine (150 mg twice daily).

The proportions of patients who achieved and maintained confirmed HIV RNA <400 copies/mL  through week 48 was 66% (57%) for the Lexiva group and 52% (42%) for the nelfinavir group, respectively. Through 48 weeks of therapy, the median increases from baseline in CD4+ cell counts were 201 cells/mm3 in the group receiving Lexiva and 216 cells/mm3 in the nelfinavir group.

In study APV30002, Lexiva (1,400 mg once daily) plus ritonavir (200 mg once daily) was compared to nelfinavir (1,250 mg twice daily) in 649 treatment-naive patients. Both treatment groups also received abacavir (300 mg twice daily) and lamivudine (150 mg twice daily).

In study APV30003, two different regimens of Lexiva plus ritonavir (Lexiva 700 mg twice daily plus ritonavir 100 mg twice daily or Lexiva 1,400 mg once daily plus ritonavir 200 mg once daily) was compared to lopinavir/ritonavir (400 mg/100 mg twice daily) in 315 patients who had experienced virologic failure to 1 or 2 prior protease inhibitor-containing regimens.

The most common adverse events in clinical studies of Lexiva were diarrhea, nausea, vomiting, headache, and rash and were generally mild to moderate in severity.

Lexiva was co-discovered by GlaxoSmithKline and Vertex Pharmaceuticals Incorporated.

Lexiva is the first PI to offer flexible dosing options (for PI-naïve patients) with no food or water restrictions.

Lexiva is indicated in combination with other antiretroviral agents for the treatment of HIV infection in adults.