Aptivus (Tipranavir) - Summary

APTIVUS SUMMARY

Aptivus^®
(tipranavir)
Capsules, 250 mg

APTIVUS^® (tipranavir) is the brand name for tipranavir (TPV), a non-peptidic protease inhibitor (PI) of HIV belonging to the class of 4-hydroxy-5,6-dihydro-2-pyrone sulfonamides. APTIVUS soft gelatin capsules are for oral administration. Each capsule contains 250 mg tipranavir.

APTIVUS (tipranavir), co-administered with 200 mg of ritonavir, is indicated for combination antiretroviral treatment of HIV-1 infected adult patients with evidence of viral replication, who are highly treatment-experienced or have HIV-1 strains resistant to multiple protease inhibitors.

This indication is based on analyses of plasma HIV-1 RNA levels in two controlled studies of APTIVUS/ritonavir of 24 weeks duration. Both studies were conducted in clinically advanced, 3-class antiretroviral (NRTI, NNRTI, PI) treatment-experienced adults with evidence of HIV-1 replication despite ongoing antiretroviral therapy.

The following points should be considered when initiating therapy with APTIVUS/ritonavir:

• The use of other active agents with APTIVUS/ritonavir is associated with a greater likelihood of treatment response (see CLINICAL PHARMACOLOGY, Microbiology and INDICATIONS AND USAGE, Description of Clinical Studies).
• Genotypic or phenotypic testing and/or treatment history should guide the use of APTIVUS/ritonavir (see CLINICAL PHARMACOLOGY, Microbiology). The number of baseline primary protease inhibitor mutations affects the virologic response to APTIVUS/ritonavir (see CLINICAL PHARMACOLOGY, Microbiology).
• Use caution when prescribing APTIVUS/ritonavir in patients who may be at risk of increased bleeding or who are receiving medications known to increase the risk of bleeding (see WARNINGS).
• Liver function tests should be performed at initiation of therapy with APTIVUS/ritonavir and monitored frequently throughout the duration of treatment (see WARNINGS).
• Use caution when prescribing APTIVUS/ritonavir to patients with elevated transaminases, hepatitis B or C co-infection or other underlying hepatic impairment (see WARNINGS).
• The extensive drug-drug interaction potential of APTIVUS/ritonavir when co-administered with multiple classes of drugs must be considered prior to and during APTIVUS/ritonavir use (see CLINICAL PHARMACOLOGY and CONTRAINDICATIONS).
• The risk-benefit of APTIVUS/ritonavir has not been established in treatment-naïve adult patients or pediatric patients.

There are no study results demonstrating the effect of APTIVUS/ritonavir on clinical progression of HIV-1.

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NEWS HIGHLIGHTS

Published Studies Related to Aptivus (Tipranavir)

Effects of boosted tipranavir and lopinavir on body composition, insulin sensitivity and adipocytokines in antiretroviral-naive adults. [2008.11.12]
OBJECTIVES: Thymidine-based nucleoside analogue reverse transcriptase inhibitors and some protease inhibitors of HIV are associated with lipoatrophy, relative central fat accumulation and insulin resistance. The latter associations have not been well evaluated prospectively in adults commencing antiretroviral therapy. We studied the effects of protease inhibitor-based antiretroviral regimens on body composition, insulin sensitivity and adipocytokine levels... CONCLUSION: Unlike many other antiretroviral regimens, TPV/r or LPV/r with tenofovir-lamivudine increased subcutaneous fat without evidence for increasing visceral fat or insulin resistance over 48 weeks.

Effect of ritonavir-boosted tipranavir or darunavir on the steady-state pharmacokinetics of elvitegravir. [2008.10.01]
OBJECTIVE: Elvitegravir (EVG) is in phase 3 development in combination with ritonavir (RTV)-boosted protease inhibitors in treatment-experienced, HIV-infected patients. Two studies evaluated pharmacokinetic (PK) interactions among EVG and RTV-boosted tipranavir (TPV/r) or darunavir (DRV/r)... CONCLUSIONS: The PK of EVG and TPV or DRV were not altered after coadministration of EVG with TPV/r or DRV/r. EVG PK was similar with varied RTV doses of 100 mg once daily, 100 mg twice daily, or 200 mg twice daily. EVG can be added to TPV/r or DRV/r regimens without dose adjustment.

Pharmacokinetics, Safety, and Efficacy of Tipranavir Boosted With Ritonavir Alone or in Combination With Other Boosted Protease Inhibitors as Part of Optimized Combination Antiretroviral Therapy in Highly Treatment-Experienced Patients (BI Study 1182.51). [2008.04.01]
BACKGROUND:: Given the limited treatment options for patients with high-level resistance, antiretroviral (ARV) regimens based on concomitant use of 2 ritonavir (RTV)-boosted protease inhibitors (PIs) were considered a therapeutic option... CONCLUSIONS:: The efficacy of a dual PI regimen depended on the presence of TPV, with additional recycled CPIs having limited activity, even in drug-resistant patient populations with plasma trough concentrations regarded as likely to be adequate in this study. No clear guidelines exist about ARV plasma trough concentrations in treatment-experienced patients, however.

Health-related quality of life and tolerability in treatment-experienced HIV-1-infected patients on tipranavir versus comparator regimens. [2008]
BACKGROUND: Antiretroviral therapy including tipranavir boosted with ritonavir (TPV/r) has shown superior viral suppression and immunological response compared with comparator ritonavir-boosted protease inhibitor (CPI/r) regimens in treatment-experienced HIV-1-infected patients. This study assesses the influence of adverse events (AEs) on health-related quality of life (HRQOL) and change in HRQOL in patients treated with TPV/r versus CPI/r regimens... CONCLUSIONS: HRQOL was maintained across both summary and all subscale scores from baseline to 48 weeks in the TPV/r and CPI/r treatment arms, despite the incidence of treatment-related AEs.

Long-term efficacy and safety of tipranavir boosted with ritonavir in HIV-1-infected patients failing multiple protease inhibitor regimens: 80-week data from a phase 2 study. [2007.08.01]
BACKGROUND: BI 1182.2, an open-label, randomized, multicenter, phase 2 study, evaluated efficacy and tolerability of the protease inhibitor (PI) tipranavir (TPV; 500 mg twice daily or 1000 mg twice daily) administered with ritonavir (100 mg twice daily) in combination with 1 nucleoside reverse transcriptase inhibitor and 1 nonnucleoside reverse transcriptase inhibitor in multiple PI-experienced HIV-1-infected patients... CONCLUSION: TPV/r combined with other active antiretroviral agents can provide a durable treatment response for highly treatment-experienced patients.

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Clinical Trials Related to Aptivus (Tipranavir)

Observational Non-Interventional Study (Anwendungsbeobachtung) With Aptivus (Tipranavir) in HIV-Infected Patients [Recruiting]
This observational study is supposed to assess (under conditions of clinical practice in daily routine) whether treatment with Aptivus (tipranavir) in combination with low-dose Norvir (ritonavir) will durable suppress viral load and may achieve suppression of viral load below the limit of detection.

Pharmaco-Epidemiological Description of the Population Treated With Aptivus Under Market Conditions, Safety & Efficacy [Recruiting]

APost Marketing Surveillance Study Assessing the Long-term Efficacy and Safety of Aptivus Co-administered With Low-dose Ritonavir in Treatment Experienced Patients With HIV-1 Infection in the Daily Clinical Practice. [Not yet recruiting]
The aim of this trial is to evaluate the safety and virological and immunological efficacy of Aptivus in treatment-experienced patients with advanced HIV-1 infection who had developed resistance to more than one protease inhibitor.

Pharmacokinetic Interactions Between Buprenorphine and Tipranavir/Ritonavir [Completed]
The main purpose of this study is to examine the effect of tipranavir combined with ritonavir, medications for the treatment of HIV-infection, on buprenorphine/naloxone (BUP) in people who have been receiving the same dose of buprenorphine/naloxone for at least 3 weeks before study entry.

Pharmacokinetics of Apricitabine and Tipranavir When Dosed Alone or Together [Completed]
The aim of the study is to see if apricitabine or tipranavir affect the levels of each other in the blood (pharmacokinetic interaction) when they are dosed together.

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