TPV is given with ritonavir to increase its therapeutic concentration, thereby inhibiting HIV replication. In clinical studies, TPV was an inhibitor of CYP 1A2, CYP 2C9, CYP 2C19, and CYP 2D6, but the net effect in vivo is not known. When given with 200 mg of ritonavir, TPV is an inhibitor of CYP 3A4, and […]
The FDA’s approval of TPV was based on two randomized, controlled, open-label, multicenter phase 3 clinical trials, RESIST-1 and RESIST-2 (Randomized Evaluation of Strategic Intervention in Multidrug-Resistant Patients with Tipranavir). The trials enrolled a combined 1,159 triple antiretroviral class-experienced patients with a history of at least two prior PI-based antiretroviral regimens, including one therapeutic failure […]
Protease inhibitors work at the last stage of the viral reproduction cycle. TPV is an inhibitor of the HIV-1 protease, thereby preventing cleavage of the polyprotein. This inhibition leads to the production of an immature, noninfec-tious virus.
INTRODUCTION Highly active antiretroviral therapy (HAART) has augmented the treatment and outcome of human immunodeficiency virus (HIV-1) infection. The inclusion of protease inhibitors (PIs) with a HAART regimen has been responsible for dramatic reductions in morbidity and mortality in cases of advanced infection. It is estimated that nearly 40 million people worldwide are infected with […]