Tipranavir

Tipranavir is an antiretroviral drug [ see Microbiology (12.4) ].

• APTIVUS, co-administered with ritonavir, is indicated for combination antiretroviral treatment of HIV-1 infected adults and pediatric patients weighing 36 kg or higher who are treatment-experienced and infected with HIV-1 strains resistant to more than one protease inhibitor (PI) [see Use in Specific Populations (8.4) ] . 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.ICD-10: B20

• APTIVUS is contraindicated in patients with moderate or severe (Child-Pugh Class B or C, respectively) hepatic impairment [ see Warnings and Precautions (5.2) ]. APTIVUS/ritonavir is contraindicated when co-administered with drugs that are highly dependent on CYP3A for clearance or are potent CYP3A inducers (see Table 1 ) [ see Drug Interactions (7.2) ].contraindicated

Adults: 500 mg APTIVUS, co-administered with 200 mg ritonavir, twice daily ( 2.2 ) Pediatric patients (weighing 36 kg or higher): 500 mg APTIVUS, co-administered with 200 mg ritonavir twice daily. ( 2.2 ) APTIVUS taken with ritonavir tablets must be taken with meals ( 2.1 ) APTIVUS capsules must be swallowed whole and must not be opened or chewed ( 2.1 ) Children should be assessed for their ability to swallow capsules before prescribing APTIVUS capsules. ( 2.1 ) Store unopened bottles of APTIVUS capsules in the refrigerator. ( 16 ) 2.1 Dosage and Administration Overview APTIVUS must be co-administered with ritonavir to exert its therapeutic effect. Failure to correctly co-administer APTIVUS with ritonavir will result in plasma levels of tipranavir that will be insufficient to achieve the desired antiviral effect and will alter some drug interactions [see Warnings and Precautions (5.1) ] . Children should be assessed for their ability to swallow capsules before prescribing APTIVUS capsules [see Use in Specific Populations (8.4) ] . APTIVUS co-administered with ritonavir tablets must only be taken with meals [see Clinical Pharmacology (12.3) ] . APTIVUS is supplied as capsules. APTIVUS capsules must be swallowed whole and must not be opened or chewed. Due to the need for co-administration of APTIVUS with ritonavir, please refer to the ritonavir prescribing information.

Co-administration with Ritonavir: APTIVUS must be co-administered with ritonavir and food to achieve the desired antiviral effect. Failure to administer APTIVUS with ritonavir and food may result in a loss of efficacy of tipranavir. ( 5.1 ) Hepatic Impairment: Discontinue for signs and symptoms of clinical hepatitis or asymptomatic increases in ALT/AST >10 times ULN or asymptomatic increases in ALT/AST 5-10 times ULN with concomitant increases in total bilirubin. Monitor liver function tests prior to therapy and frequently thereafter. ( 5.2 ) Intracranial Hemorrhage/Platelet Aggregation and Coagulation: Use with caution in patients at risk for increased bleeding or who are receiving medications that increase the risk of bleeding. ( 5.3 , 5.5 ) The concomitant use of APTIVUS/ritonavir and certain other drugs may result in known or potentially significant drug interactions. Consult the full prescribing information prior to and during treatment for potential drug interactions. ( 5.4 , 7.2 ) Rash: Discontinue and initiate appropriate treatment if severe skin reaction occurs or is suspected. ( 5.6 ) Use with caution in patients with a known sulfonamide allergy. ( 5.7 ) Patients may develop new onset or exacerbations of diabetes mellitus, hyperglycemia ( 5.8 ), immune reconstitution syndrome ( 5.9 ), redistribution/accumulation of body fat ( 5.10 ), and elevated lipids. ( 5.11 ) Monitor cholesterol and triglycerides prior to therapy and periodically thereafter. Hemophilia: Spontaneous bleeding may occur, and additional factor VIII may be required.

The following adverse reactions are described, in greater detail, in other sections: Hepatic Impairment and Toxicity [ see Warnings and Precautions (5.2) ] Intracranial Hemorrhage [ see Warnings and Precautions (5.3) ] Rash [ see Warnings and Precautions (5.6) ] Due to the need for co-administration of APTIVUS with ritonavir, please refer to ritonavir prescribing information for ritonavir-associated adverse reactions. Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. In adults the most frequent adverse reactions (incidence >4%) were diarrhea, nausea, pyrexia, vomiting, fatigue, headache, and abdominal pain. ( 6.1 ) In pediatric subjects the most frequent adverse reactions were generally similar to those seen in adults. However, rash was more frequent in pediatric subjects than in adults. ( 6.2 ) To report SUSPECTED ADVERSE REACTIONS, contact Boehringer Ingelheim Pharmaceuticals, Inc. at 1-800-542-6257 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials in Adults APTIVUS, co-administered with ritonavir, has been studied in a total of 6308 HIV-1 positive adults as combination therapy in clinical studies. Of these, 1299 treatment-experienced subjects received the dose of 500 mg/200 mg BID.

8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to APTIVUS during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary Prospective pregnancy data from the APR and an Expanded Access program are not sufficient to adequately assess the risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Tipranavir use during pregnancy has been evaluated in a limited number of women as reported by the APR and an Expanded Access program, and available data show no birth defects in 13 first trimester exposures (see Data ) compared with the background rate for major birth defects of 2.7% in the US reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP). The rate of miscarriage is not reported in the APR. The estimated background rate of miscarriage in clinically recognized pregnancies in the U.S. general population is 15-20%. The background risk of birth defects and miscarriage for the indicated population is unknown. Methodological limitations of the APR include the use of MACDP as the external comparator group.

Metabolism

In order to achieve effective tipranavir plasma concentrations and a twice-daily dosing regimen, co-administration of APTIVUS with ritonavir is essential [ see Dosage and Administration (2) ]. Ritonavir inhibits hepatic cytochrome P450 3A (CYP3A), the intestinal P-gp efflux pump and possibly intestinal CYP3A.

There is no known antidote for APTIVUS overdose. Treatment of overdose should consist of general supportive measures, including monitoring of vital signs and observation of the patient's clinical status. If indicated, elimination of unabsorbed tipranavir should be achieved by emesis or gastric lavage. Administration of activated charcoal may also be used to aid in removal of unabsorbed drug. Since tipranavir is highly protein bound, dialysis is unlikely to provide significant removal of the drug.

• Jun 22, 2005NDANDA021814Boehringer Ingelheim

1. 1Nausea28321%
2. 2Vomiting27420%
3. 3Pneumonia26319%
4. 4Cholelithiasis25118%
5. 5Schizophrenia25018%
6. 6Hepatotoxicity17513%
7. 7Hypomania17313%
8. 8Hepatic Enzyme Increased17212%
9. 9Blood Bilirubin Increased16912%
10. 10Condition Aggravated16712%
11. 11Psychotic Disorder16412%
12. 12Jaundice Cholestatic16112%
13. 13Death15011%
14. 14Off Label Use1198.6%
15. 15Oedema Peripheral1097.9%

The 10 most recently updated of 77 ClinicalTrials.gov registrations naming Tipranavir as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Trial to Evaluate the Interest of a Reductive Anti Retroviral Strategy Using Dual Therapy Inspite of Triple Therapy
  Completed · Phase 3 · Interventional · 224 enrolled · University Hospital, Tours
  NCT02302547updated 2025-12-26
• Pharmacokinetic Study of Antiretroviral Drugs and Related Drugs During and After Pregnancy
  Completed · Observational · 1,578 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT00042289updated 2025-12-02
• Study to Compare Bictegravir/Lenacapavir Versus Current Therapy in People With HIV-1 Who Are Successfully Treated With a Complicated Regimen
  Active not recruiting · Phase 2 · Phase 3 · Interventional · 689 enrolled · Gilead Sciences
  NCT05502341updated 2025-10-14
• Study to Determine the Pharmacokinetics on TPV/r in Subjects With Mild and Moderate Hepatic Insufficiency
  Completed · Phase 1 · Interventional · 24 enrolled · Boehringer Ingelheim
  NCT02249442updated 2025-01-23
• Pharmacokinetics (PK) of Tipranavir/Ritonavir, Ribavirin, Pegylated Interferon (Peg INF) in Hepatitis C (HCV) Subjects With Mild Hepatic Impairment and in HCV, Hepatitis B (HBV), Hepatitis D Infected Subjects or Alcoholic Cirrhosis With Moderate Hepatic Impairment
  Completed · Phase 1 · Interventional · 36 enrolled · Boehringer Ingelheim
  NCT02259855updated 2025-01-22
• 3 TPV/RTV Doses in Multiple ARV Experienced Patients - Tipranavir Dose Defining Study
  Completed · Phase 2 · Interventional · 216 enrolled · Boehringer Ingelheim
  NCT00275444updated 2023-12-01
• Dual Boosted - Protease Inhibitor (PI) Pharmacokinetics (PK) Trial (Tipranavir / Ritonavir) in Highly Treatment-experienced HIV-1 Infected Patients
  Completed · Phase 2 · Interventional · 328 enrolled · Boehringer Ingelheim
  NCT00056641updated 2023-12-01
• Optimizing Treatment for Treatment-Experienced, HIV-Infected People
  Completed · Phase 3 · Interventional · 517 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT00537394updated 2021-11-04
• Study to Evaluate Switching From a Regimen of Two Nucleos(t)Ide Reverse Transcriptase Inhibitors (NRTI) Plus a Third Agent to a Fixed Dose Combination (FDC) of Bictegravir/Emtricitabine/Tenofovir Alafenamide (B/F/TAF), in Virologically-Suppressed, HIV-1 Infected African American Participants
  Completed · Phase 3 · Interventional · 496 enrolled · Gilead Sciences
  NCT03631732updated 2021-09-05
• IMPAACT P1080: Psychiatric and Antiretroviral Medication Concentrations in HIV-infected and Uninfected Children and Adolescents
  Completed · Observational · 127 enrolled · International Maternal Pediatric Adolescent AIDS Clinical Trials Group
  NCT01232361updated 2021-08-03

Frequently asked questions

How does Tipranavir work?

Tipranavir is an antiretroviral drug [ see Microbiology (12.4) ].

What is Tipranavir used for?

According to FDA labeling, Tipranavir carries indications including: APTIVUS, co-administered with ritonavir, is indicated for combination antiretroviral treatment of HIV-1 infected adults and pediatric patients weighing 36 kg or higher who are treatment-experienced and infected with HIV-1 strains resistant to more than one protease inhibitor (PI) [see Use in Specific Populations (8.4) ] . 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Tipranavir?

Tipranavir is classified as Protease inhibitors, Protease Inhibitor, Cytochrome P450 3A Inducers, HIV Protease Inhibitors, Decreased Protein Synthesis.

What are the brand names for Tipranavir?

Tipranavir is marketed under brand names including Aptivus.

What are the contraindications for Tipranavir?

Tipranavir labeling lists contraindications including: APTIVUS is contraindicated in patients with moderate or severe (Child-Pugh Class B or C, respectively) hepatic impairment [ see Warnings and Precautions (5.2) ]. APTIVUS/ritonavir is contraindicated when co-administered with drugs that are highly dependent on CYP3A for clearance or are potent CYP3A inducers (see Table 1 ) [ see Drug Interactions (7.2) ].. Always consult the full prescribing information and a clinician.