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UPTRAVI® IV

UPTRAVI®: Available for Intravenous Use

Uninterrupted treatment is key in managing pulmonary arterial hypertension (PAH, WHO Group I), a progressive disease.1

UPTRAVI® IV IS FOR THE TREATMENT OF PAH (WHO GROUP I) IN FC II-III PATIENTS WHO ARE TEMPORARILY UNABLE TO TAKE ORAL THERAPY2

  • Avoid treatment disruptions when your patients are unable to take oral therapy by temporarily transitioning them from their current oral dose to IV treatment and returning to UPTRAVI® Tablets when possible2,3
dosing illustration

Remain confident that your patients can receive UPTRAVI® treatment at home, in the hospital, and after discharge

  • Expected to maintain similar UPTRAVI® efficacy and safety, with the exception of infusion-site reactions, when temporarily using UPTRAVI® IV in the hospital2,3
  • Bypass re-titration when transitioning between UPTRAVI® IV and UPTRAVI® Tablets2
UPTRAVI® Tablets and IV dosing mobile table

Administer UPTRAVI® IV twice daily by intravenous infusion at a dose that corresponds to the patient’s current dose of UPTRAVI® Tablets.

Please see complete UPTRAVI® IV dosing and administration instructions as listed in the full Prescribing Information.

LEARN ABOUT UPTRAVI® IV WITH DR IOANA PRESTON

Watch the video below to hear from Dr Ioana Preston, Director of the Pulmonary Hypertension Center at Tufts Medical Center.

UPTRAVI® IV INSTRUCTIONS FOR USE VIDEO

Watch the video below to learn more about storage, reconstitution, dilution, and administration of UPTRAVI® IV.

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About UPTRAVI® IV
About UPTRAVI® IV
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Important Safety Information
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Downloadable Resources

UPTRAVI® IV Instructions for Use Guide

Use this guide to learn about storage, reconstitution, dilution, and administration of UPTRAVI® IV.

UPTRAVI® IV Frequently Asked Questions

Get the answers to your questions about UPTRAVI® IV.

TEMPORARILY SWITCHING TO UPTRAVI® IV FROM UPTRAVI® TABLETS WAS WELL TOLERATED WITH COMPARABLE EXPOSURE TO THE ACTIVE METABOLITE

Study design3

  • Phase 3, prospective, multicenter, open-label, single-sequence crossover study
  • Twenty patients with PAH in FC I-III† receiving a stable dose of UPTRAVI® Tablets for ≥28 days prior to enrollment were included
  • Patients were monitored to assess the safety, tolerability, and pharmacokinetics (including exposure to the active metabolite ACT-333679) of switching from a stable dose of UPTRAVI® Tablets to a corresponding dose of UPTRAVI® IV and back to UPTRAVI® Tablets
  • The dosing regimen for UPTRAVI® IV was selected to help patients achieve similar exposure to the active metabolite when compared with UPTRAVI® Tablets
Pharmacokinetic and safety mobile study design

Baseline patient characteristics (N=20)3

  • Mean age: 57 years
  • Female: 80%
  • Etiology: idiopathic or heritable PAH (70%), PAH-CTD (20%), PAH-CHD (5%), PoPH (5%)
baseline patient characteristics chart

Results2,3

Comparable exposure to the active metabolite following UPTRAVI® Tablets and UPTRAVI® IV administration

Mean (SD) ACT-333679 concentration (ng/mL) over time (hours) mobile graph
Time to the maximum concentration of the active metabolite was comparable

Safety2,3

  • The transition from UPTRAVI® Tablets to UPTRAVI® IV and back was well tolerated: Patient tolerability was similar between UPTRAVI® IV and Tablets
  • 10% of patients reported infusion-site reactions during UPTRAVI® IV administration, including infusion-site erythema/redness, pain, and swelling

IMPORTANT SAFETY INFORMATION

CONTRAINDICATIONS

Concomitant use of strong inhibitors of CYP2C8 (eg, gemfibrozil) with UPTRAVI® is contraindicated.

Hypersensitivity to the active substance or to any of the excipients is contraindicated.

WARNINGS AND PRECAUTIONS

Pulmonary Edema with Pulmonary Veno-Occlusive Disease (PVOD)

Should signs of pulmonary edema occur, consider the possibility of associated PVOD. If confirmed, discontinue UPTRAVI®.

ADVERSE REACTIONS

Adverse reactions more frequent compared to placebo (≥3%) seen with UPTRAVI® Tablets are headache (65% vs 32%), diarrhea (42% vs 18%), jaw pain (26% vs 6%), nausea (33% vs 18%), myalgia (16% vs 6%), vomiting (18% vs 9%), pain in extremity (17% vs 8%), flushing (12% vs 5%), arthralgia (11% vs 8%), anemia (8% vs 5%), decreased appetite (6% vs 3%), and rash (11% vs 8%).

These adverse reactions are more frequent during the dose titration phase.

Hyperthyroidism was observed in 1% (n=8) of patients on UPTRAVI® Tablets and in none of the patients on placebo.

DRUG INTERACTIONS

CYP2C8 Inhibitors

Concomitant administration with gemfibrozil, a strong inhibitor of CYP2C8, doubled exposure to selexipag and increased exposure to the active metabolite by approximately 11-fold. Concomitant use of UPTRAVI® with strong inhibitors of CYP2C8 is contraindicated.

Concomitant administration of UPTRAVI® with clopidogrel, a moderate inhibitor of CYP2C8, had no relevant effect on the exposure to selexipag and increased the exposure to the active metabolite by approximately 2.7–fold. Reduce the dosing of UPTRAVI® to once daily in patients on a moderate CYP2C8 inhibitor.

CYP2C8 Inducers

Concomitant administration with an inducer of CYP2C8 and UGT 1A3 and 2B7 enzymes (rifampin) halved exposure to the active metabolite. Increase UPTRAVI® dose, up to twice, when co-administered with rifampin. Reduce UPTRAVI® when rifampin is stopped.

DOSAGE AND ADMINISTRATION

Recommended Dosage

Recommended starting dose is 200 mcg twice daily for UPTRAVI® Tablets. Tolerability may be improved when taken with food. Increase by 200 mcg twice daily, usually at weekly intervals, to the highest tolerated dose up to 1600 mcg twice daily. If dose is not tolerated, reduce to the previous tolerated dose.

Patients With Hepatic Impairment

For patients with moderate hepatic impairment (Child-Pugh class B), the starting dose of UPTRAVI® Tablets is 200 mcg once daily. Increase by 200 mcg once daily at weekly intervals, as tolerated. Avoid use of UPTRAVI® in patients with severe hepatic impairment (Child-Pugh class C).

Co-administration With Moderate CYP2C8 Inhibitors

When co-administered with moderate CYP2C8 inhibitors (eg, clopidogrel, deferasirox and teriflunomide), reduce the dosing of UPTRAVI® to once daily.

Dosage Strengths

UPTRAVI® tablet strengths:
200, 400, 600, 800, 1000, 1200, 1400, and 1600 mcg.

Additional Important Safety Information for UPTRAVI® IV

Use UPTRAVI® for injection in patients who are temporarily unable to take oral therapy.

Administer UPTRAVI® for injection twice daily by intravenous infusion at a dose that corresponds to the patient’s current dose of UPTRAVI® Tablets (see Table 1 in full Prescribing Information). Administer UPTRAVI® for injection as an 80-minute intravenous infusion.

Adverse Reactions: Infusion-site reactions (infusion-site erythema/redness, pain and swelling) were reported with UPTRAVI® for injection.

INDICATION

UPTRAVI® (selexipag) is indicated for the treatment of pulmonary arterial hypertension (PAH, WHO Group I) to delay disease progression and reduce the risk of hospitalization for PAH.

Effectiveness of UPTRAVI® Tablets was established in a long-term study in PAH patients with WHO Functional Class II-III symptoms.

Patients had idiopathic and heritable PAH (58%), PAH associated with connective tissue disease (29%), and PAH associated with congenital heart disease with repaired shunts (10%).

Please see full Prescribing Information for UPTRAVI®.

cp-126160v5

*Once daily for patients with moderate hepatic impairment and co-administration with moderate CYP2C8 inhibitors.

†In the study, 1 patient (5%) was in FC I. UPTRAVI® is indicated for the treatment of PAH (WHO Group I, FC II-III) to delay disease progression and reduce the risk of hospitalization for PAH.

AUCt,ss=area under the plasma concentration–time curve during a dose interval at steady state; BID=twice daily; Cmax,ss=maximum concentration at steady state; ERA=endothelin receptor antagonist; FC=Functional Class; IV=intravenous; PAH-CHD=PAH associated with congenital heart disease with repaired shunts; PAH-CTD=PAH associated with connective tissue disease; PDE-5i=phosphodiesterase type-5 inhibitor; PoPH=portopulmonary hypertension; SD=standard deviation; sGC=soluble guanylate cyclase; WHO=World Health Organization.

References: 1. Narechania S, Torbic H, Tonelli AR. Treatment discontinuation or interruption in pulmonary arterial hypertension. J Cardiovasc Pharmacol Ther. 2020;25(2):131-141. 2. UPTRAVI® (selexipag) full Prescribing Information. Actelion Pharmaceuticals US, Inc. 3. Klose H, Chin KM, Ewert R, et al. Temporarily switching from oral to intravenous selexipag in patients with pulmonary arterial hypertension: safety, tolerability, and pharmacokinetic results from an open-label, phase III study. Respir Res. 2021;22(1):34. doi:10.1186/s12931-020-01594-8