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Aptivus (Tipranavir) - Summary




Clinical hepatitis and hepatic decompensation, including some fatalities, have been reported. Extra vigilance is warranted in patients with chronic hepatitis B or hepatitis C co-infection, as these patients have an increased risk of hepatotoxicity [ see Warnings and Precautions ].

Intracranial Hemorrhage:

Both fatal and non-fatal intracranial hemorrhage have been reported [ see Warnings and Precautions ].



APTIVUS is a protease inhibitor of HIV-1 belonging to the class of 4-hydroxy-5,6-dihydro-2-pyrone sulfonamides.

APTIVUS, co-administered with ritonavir, is indicated for combination antiretroviral treatment of HIV-1 infected patients who are treatment-experienced and infected with HIV-1 strains resistant to more than one protease inhibitor (PI).

This indication is based on analyses of plasma HIV-1 RNA levels in two controlled studies of APTIVUS/ritonavir of 48 weeks duration in treatment-experienced adults and one open-label 48-week study in pediatric patients age 2 to 18 years. The adult 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 APTIVUS/ritonavir in treatment-na├»ve patients is not recommended [ see Warnings and Precautions ].
  • The use of other active agents with APTIVUS/ritonavir is associated with a greater likelihood of treatment response [ see Clinical Pharmacology and Clinical Studies ].
  • Genotypic or phenotypic testing and/or treatment history should guide the use of APTIVUS/ritonavir [ see Clinical Pharmacology ]. The number of baseline primary protease inhibitor mutations affects the virologic response to APTIVUS/ritonavir [ see Clinical Pharmacology ].
  • Use caution when prescribing APTIVUS/ritonavir to patients with elevated transaminases, hepatitis B or C co-infection or patients with mild hepatic impairment [ see Warnings and Precautions ].
  • Liver function tests should be performed at initiation of therapy with APTIVUS/ritonavir and monitored frequently throughout the duration of treatment [ see Warnings and Precautions ].
  • The drug-drug interaction potential of APTIVUS/ritonavir when co-administered with other drugs must be considered prior to and during APTIVUS/ritonavir use [ see Contraindications and Drug Interactions (7) ].
  • Use caution when prescribing APTIVUS/ritonavir in patients who may be at risk for increased bleeding or who are receiving medications known to increase the risk of bleeding [ see Warnings and Precautions ].
  • The risk-benefit of APTIVUS/ritonavir has not been established in pediatric patients <2 years of age.

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

See all Aptivus indications & dosage >>


Published Studies Related to Aptivus (Tipranavir)

Effects of tipranavir, darunavir, and ritonavir on platelet function, coagulation, and fibrinolysis in healthy volunteers. [2011.06.01]
The use of HIV protease inhibitors (PIs) as part of antiretroviral therapy in the treatment of HIV-1 infection may be associated with an increased risk of bleeding... There was large inter-patient variability in antiplatelet effect for all PI treatments, ranging from no effect to complete inhibition of AA-induced platelet aggregation.

Lack of a pharmacokinetic interaction between steady-state tipranavir/ritonavir and single-dose valacyclovir in healthy volunteers. [2011.03]
OBJECTIVE: This study assessed the single-dose pharmacokinetics of the herpes antiviral acyclovir (administered as the pro-drug valacyclovir) alone and in combination with twice-daily 200 mg ritonavir-boosted tipranavir (500 mg) at steady state... CONCLUSIONS: When administered as a single dose of valacyclovir with steady-state tipranavir/ritonavir, there were no clinically important changes in acyclovir pharmacokinetics. This result indicates that valacyclovir can be co-administered safely with no dose adjustments.

A phenotype-genotype approach to predicting CYP450 and P-glycoprotein drug interactions with the mixed inhibitor/inducer tipranavir/ritonavir. [2010.06]
The effects of tipranavir/ritonavir (TPV/r) on hepatic and intestinal P-glycoprotein (P-gp) and cytochrome P450 (CYP) enzyme activity were evaluated in 23 volunteers. The subjects received oral (p.o.) caffeine, warfarin + vitamin K, omeprazole, dextromethorphan, and midazolam and digoxin (p.o...

Pharmacokinetic characterization of three doses of tipranavir boosted with ritonavir on highly active antiretroviral therapy in treatment-experienced HIV-1 patients. [2010.01]
PURPOSE: This study characterized the pharmacokinetic effects, safety, and antiretroviral activity of three different doses of the nonpeptidic protease inhibitor tipranavir, in combination with ritonavir administered twice daily for 28 days, on a number of triple-combination regimens containing a nonnucleoside reverse transcriptase inhibitor (efavirenz or nevirapine) plus two nucleoside reverse transcriptase inhibitors (abacavir, didanosine, lamivudine, stavudine, and zidovudine) or a three nucleoside reverse transcriptase inhibitor combination (zidovudine, lamivudine, and abacavir)... CONCLUSIONS: Tipranavir coadministered with ritonavir has been demonstrated to be safe, effective, and pose little potential for clinically meaningful drug interactions when added to the highly active antiretroviral therapy regimens containing nevirapine, efavirenz, lamivudine, stavudine, or didanosine.

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.

more studies >>

Clinical Trials Related to Aptivus (Tipranavir)

Bioavailability of Tipranavir/Ritonavir Paediatric Solution Compared to Tipranavir/Ritonavir Capsules in Healthy Female and Male Subjects [Completed]
Study to determine the relative bioavailability of 500/200 mg of tipranavir/ritonavir (TPV/r) oral solution compared to 500/200 mg of TPV/r capsules following oral administration and to investigate the relative bioavailability of 500/200 mg of TPV/r oral solution with food versus without food.

Effects of Steady State Tipranavir/Ritonavir or Darunavir/Ritonavir or Ritonavir on Platelet Function, Coagulation and Fibrinolysis Biomarkers in Healthy Subjects [Completed]

Pharmacokinetic Interaction Between Tipranavir and BILR 355 BS Plus Ritonavir in Healthy Male Volunteers [Completed]

Study to Determine the Effects of Multiple-dose Omeprazole on the Single-dose Pharmacokinetics of Tipranavir (TPV) Coadministered With Ritonavir (RTV) in Healthy Adult Volunteers [Completed]

Bioequivalence of Two Different Oral Solutions Tipranavir Administered in Combination With Ritonavir to Healthy Volunteers [Completed]
To establish the bioequivalence of the new tipranavir oral solution formulation with the current tipranavir oral solution formulation following single-dose administration. In each case, 500 mg tipranavir was coadministered with 200 mg ritonavir.

more trials >>

Page last updated: 2011-12-09

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