selexipag (Rx)

Brand and Other Names:Uptravi

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 200mcg
  • 400mcg
  • 600mcg
  • 800mcg
  • 1000mcg
  • 1200mcg
  • 1400mcg
  • 1600mcg

injection, lyophilized powder for reconstitution

  • 1800mcg/vial
  • Reconstituted concentration of each vial: 225 mcg/mL

Pulmonary Arterial Hypertension

Indicated for pulmonary arterial hypertension (PAH, WHO Group 1) to delay disease progression and reduce risk of hospitalization

Oral

  • 200 mcg PO BID, initially
  • Increase dose by 200 mcg BID, at weekly intervals (usually), to highest tolerated dose; not to exceed 1600 mcg BID
  • If dose not tolerated, reduce to previous tolerated dose
  • PO to IV conversion

    • Use in patients who are temporarily unable to take PO
    • Current dose 200 mg PO BID: Administer 225 mg IV BID
    • Current dose 400 mg PO BID: Administer 450 mg IV BID
    • Current dose 600 mg PO BID: Administer 675 mg IV BID
    • Current dose 800 mg PO BID: Administer 900 mg IV BID
    • Current dose 1000 mg PO BID: Administer 1125 mg IV BID
    • Current dose 1200 mg PO BID: Administer 1350 mg IV BID
    • Current dose 1400 mg PO BID: Administer 1575 mg IV BID
    • Current dose 1600 mg PO BID: Administer 1800 mg IV BID

Dosage Modifications

Renal impairment

  • eGFR >15 mL/min/1.73 m2: No dosage adjustment required
  • eGFR <15 mL/min/1.73 m2 or patients undergoing dialysis: No clinical experience

Hepatic impairment

  • Mild (Child-Pugh A): No dosage adjustment required
  • Moderate (Child-Pugh B): Starting dose is 200 mcg qDay; increase by increments of 200 mcg/day at weekly intervals, as tolerated
  • Severe (Child-Pugh C): Avoid use

Coadministration with moderate CYP2C8 inhibitors

  • Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors (eg, clopidogrel, deferasirox, teriflunomide)
  • Revert to selexipag BID dosing when moderated CYP2C8 inhibitor discontinued

Coadministration with CYP2C8 inducers

  • Increase selexipag dose (up to 2-fold) if coadministered with rifampin

Dosage Considerations

Effectiveness was established in a long-term study in patients with PAH with WHO Functional Class II-III symptoms

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

Chronic Thromboembolic Pulmonary Hypertension (Orphan)

Orphan designation for chronic thromboembolic pulmonary hypertension

Orphan sponsor

  • Janssen Research & Development LLC; 1820 Chapel Ave West, Suite 300; Cherry Hill, New Jersey 08002

Safety and efficacy not established

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Interactions

Interaction Checker

and selexipag

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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             activity indicator 

            Contraindicated (1)

            • gemfibrozil

              gemfibrozil will increase the level or effect of selexipag by decreasing metabolism. Contraindicated. Coadministration of selexipag with strong CYP2C8 inhibitors doubled exposure to selexipag and increased exposure to the active metabolite by about 11-fold.

            Serious - Use Alternative (3)

            • darolutamide

              darolutamide will increase the level or effect of selexipag by Other (see comment). Avoid or Use Alternate Drug. Darolutamide is a BCRP inhibitor. Avoid coadministration with BCRP inhibitors. If use is unavoidable, closely monitor for adverse reactions and consider dose reduction of BCRP substrate drug (refer BCRP substrate prescribing information).

            • lasmiditan

              lasmiditan increases levels of selexipag by Other (see comment). Avoid or Use Alternate Drug. Comment: Lasmiditan inhibits BCRP in vitro. Avoid coadministration of lasmiditan with BCRP substrates.

            • leniolisib

              leniolisib will increase the level or effect of selexipag by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates

            Monitor Closely (67)

            • abiraterone

              abiraterone will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • acalabrutinib

              acalabrutinib increases effects of selexipag by Other (see comment). Use Caution/Monitor. Comment: Acalabrutinib may increase exposure to coadministered BCRP substrates by inhibition of intestinal BCRP.

            • apalutamide

              apalutamide will decrease the level or effect of selexipag by increasing elimination. Use Caution/Monitor. Apalutamide weakly induces BCRP and may decrease systemic exposure of drugs that are BCRP substrates.

            • cannabidiol

              cannabidiol will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • capmatinib

              capmatinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • carbamazepine

              carbamazepine will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Increase selexipag dose (up to 2-fold) if coadministered with strong CYP2C8 inducers.

            • celecoxib

              celecoxib will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • clopidogrel

              clopidogrel will increase the level or effect of selexipag by decreasing metabolism. Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • cobicistat

              cobicistat will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • colchicine

              colchicine will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • cyclosporine

              cyclosporine will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • dabrafenib

              dabrafenib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • deferasirox

              deferasirox will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • dexamethasone

              dexamethasone will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • dipyridamole

              dipyridamole will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • efavirenz

              efavirenz will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • eltrombopag

              eltrombopag will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • eluxadoline

              eluxadoline will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • elvitegravir/cobicistat/emtricitabine/tenofovir DF

              elvitegravir/cobicistat/emtricitabine/tenofovir DF will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • encorafenib

              encorafenib will increase the level or effect of selexipag by Other (see comment). Modify Therapy/Monitor Closely. Encorafenib (a BCRP inhibitor) may increase the concentration and toxicities of BCRP substrates. Closely monitor for signs and symptoms of increased exposure and consider adjusting the dose of these substrates.

            • felodipine

              felodipine will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • fosphenytoin

              fosphenytoin will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Increase selexipag dose (up to 2-fold) if coadministered with strong CYP2C8 inducers.

            • fostamatinib

              fostamatinib will increase the level or effect of selexipag by decreasing metabolism. Use Caution/Monitor. Concomitant use of fostamatinib may increase concentrations of BCRP substrate drugs. Monitor for toxicities of BCRP substrate drug that may require dosage reduction when given concurrently with fostamatinib.

            • fostemsavir

              fostemsavir will increase the level or effect of selexipag by Other (see comment). Modify Therapy/Monitor Closely. Fostemsavir inhibits BCRP transporters. If possible, avoid coadministration or modify dose of BCRP substrate coadministered with fostemsavir.

            • gefitinib

              gefitinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • glecaprevir/pibrentasvir

              glecaprevir/pibrentasvir will increase the level or effect of selexipag by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates.

            • griseofulvin

              griseofulvin will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • ifosfamide

              ifosfamide will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • imatinib

              imatinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • irbesartan

              irbesartan will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • ketoconazole

              ketoconazole will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • lapatinib

              lapatinib will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

              lapatinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • levoketoconazole

              levoketoconazole will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • losartan

              losartan will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • lumacaftor/ivacaftor

              lumacaftor/ivacaftor will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • mifepristone

              mifepristone will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • momelotinib

              momelotinib increases toxicity of selexipag by plasma protein binding competition. Modify Therapy/Monitor Closely. Momelotinib (BCRP inhibitor) may increase exposure of BCRP substrates, which may increase the risk of BCRP substrate adverse reactions. Dose adjustment of other BCRP substrates may necessary.

            • nilotinib

              nilotinib will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • omaveloxolone

              omaveloxolone will decrease the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Omaveloxolone may reduce systemic exposure of sensitive CYP2C8 substrates. Check prescribing information of substrate if dosage modification is needed.

            • osimertinib

              osimertinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • oteseconazole

              oteseconazole will increase the level or effect of selexipag by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.

            • pantoprazole

              pantoprazole will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • phenobarbital

              phenobarbital will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Increase selexipag dose (up to 2-fold) if coadministered with strong CYP2C8 inducers.

            • phenytoin

              phenytoin will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Increase selexipag dose (up to 2-fold) if coadministered with strong CYP2C8 inducers.

            • pioglitazone

              pioglitazone will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • ponatinib

              ponatinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • primidone

              primidone will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Increase selexipag dose (up to 2-fold) if coadministered with strong CYP2C8 inducers.

            • quinine

              quinine will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • rabeprazole

              rabeprazole will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • regorafenib

              regorafenib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • rifampin

              rifampin will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Coadministration of selexipag with rifampin, an inducer of CYP2C8, UGT1A3, and 2B7 enzymes, decreased exposure to selexipag's active metabolite by 50%. Increase selexipag dose up to twice of the typical dose if coadministered with rifampin.

            • rifapentine

              rifapentine will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Increase selexipag dose (up to 2-fold) if coadministered with strong CYP2C8 inducers.

            • rolapitant

              rolapitant will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • rosiglitazone

              rosiglitazone will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • safinamide

              safinamide will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • secobarbital

              secobarbital will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Increase selexipag dose (up to 2-fold) if coadministered with strong CYP2C8 inducers.

            • sofosbuvir/velpatasvir

              sofosbuvir/velpatasvir will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • stiripentol

              stiripentol will increase the level or effect of selexipag by Other (see comment). Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors. Stiripentol is also a BCRP transport inhibitor.

            • sunitinib

              sunitinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • tafamidis

              tafamidis will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.

            • tafamidis meglumine

              tafamidis meglumine will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.

            • tamoxifen

              tamoxifen will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • teriflunomide

              teriflunomide will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • trimethoprim

              trimethoprim will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • vandetanib

              vandetanib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • vemurafenib

              vemurafenib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            • voxilaprevir

              voxilaprevir will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.

            Minor (2)

            • lopinavir

              lopinavir will increase the level or effect of selexipag by decreasing metabolism. Minor/Significance Unknown. Coadministration of selexipag with ritonavir may result in an increase in exposure to selexipag. Despite this pharmacokinetic change, this interaction is likely of little clinical significance.

            • ritonavir

              ritonavir will increase the level or effect of selexipag by decreasing metabolism. Minor/Significance Unknown. Coadministration of selexipag with ritonavir may result in an increase in exposure to selexipag. Despite this pharmacokinetic change, this interaction is likely of little clinical significance

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            Adverse Effects

            >10%

            Headache (65%)

            Diarrhea (42%)

            Jaw pain (26%)

            Nausea (33%)

            Vomiting (18%)

            Pain in extremity (17%)

            Myalgia (16%)

            Flushing (12%)

            Arthralgia (11%)

            Rash (11%)

            1-10%

            Hemoglobin decreased below 10 g/dL (8.6%)

            Anemia (8%)

            Decreased appetite (6%)

            Frequency Not Defined

            TSH reduced (up to −0.3 MU/L from a baseline of 2.5 MU/L)

            Vascular disorders: Symptomatic hypotension

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            Warnings

            Contraindications

            Hypersensitivity to the active substance or to any of the excipients

            Concomitant use of strong CYP2C8 inhibitors (eg, gemfibrozil)

            Cautions

            If signs of pulmonary edema occur, consider the possibility of associated pulmonary veno-occlusive disease (PVOD); if PVOD is confirmed, discontinue selexipag

            Drug interaction overview

            • Contraindicated with strong CYP2C8 inhibitors; coadministration with strong CYP2C8 inhibitors may result in significant increased exposure to selexipag and its active metabolite
            • Concomitant administration with an inducer of CYP2C8 and UGT 1A3 and 2B7 enzymes (rifampin) halved exposure to active metabolite; increase dose up to twice of the normal dose when coadministered with rifampin; reduce therapy dose when rifampin is stopped
            • An increased selexipag dose (up to 2-fold) may be necessary if coadministered with strong CYP2C8 inducers
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            Pregnancy

            Pregnancy

            No adequate and well-controlled studies with selexipag exist in pregnant women

            Animal studies

            • Reproduction studies performed with selexipag showed no clinically relevant effects on embryofetal development and survival
            • A slight reduction in maternal as well as in fetal body weight was observed when pregnant rats were administered selexipag during organogenesis at a dose producing an exposure ~47 times that in humans at the maximum recommended human dose

            Lactation

            Unknown if distributed in human breast milk

            Selexipag or its metabolites were present in the milk of rats

            Because many drugs are present in the human milk and because of the potential for serious adverse reactions in nursing infants, discontinue nursing or discontinue selexipag

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Selectively activates the prostacyclin receptor (ie, IP-receptor), one of 5 types of prostanoid receptors

            Unlike prostacyclin analogs, selexipag is selective for the IP receptor over other prostanoid receptors (ie, EP1-4, DP, FP, TP)

            Activating the IP receptor induces vasodilation and inhibits proliferation of vascular smooth muscle cells

            Absorption

            Peak plasma time: 1-3 hr; 3-4 hr (active metabolite)

            Distribution

            Protein bound: ~99% (albumin and alpha1-acid glycoprotein)

            Metabolism

            Undergoes enzymatic hydrolysis of the acylsulfonamide by hepatic carboxylesterase 1, to yield the active metabolite, which is ~37-fold as potent as selexipag

            Elimination

            Half-life: 0.8-2.5 hr; 6.2-13.5 hr (active metabolite)

            Oral clearance: 35 L/hr

            Excretion: 93% in feces; neither selexipag nor its metabolite were found in urine

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            Administration

            IV Preparation

            Reconstitution

            • Remove vials from refrigerator and for ~30-60 min to reach room temperature (20-25ºC [68-77ºF])
            • Protect vials from light at all times; ensure protective wrap around the label is covering vial
            • Peel back light protective wrap on vial to inspect vial and then immediately close light protective wrap on the vial; contents should appear white-to-almost white broken cake or powder material
            • Reconstitute vial contents using a polypropylene syringe with 8.6 mL of 0.9% NaCl; slowly inject stream directed toward the inside wall of vial to obtain concentration of 225 mcg/mL
            • Gently invert vial and repeat until powder is completely dissolved; do NOT shake
            • Inspect vial for discoloration by peeling back light protect wrap; solution is clear, colorless, and free from foreign material; discard if solution is discolored, cloudy, or contains visible particles

            Dilution

            • Must be diluted in glass containers only
            • Withdraw 100 mL of 0.9% NaCl and transfer into an empty sterile glass container
            • Calculate and withdraw required volume of reconstituted solution from vial using a single, appropriately sized polypropylene syringe; dilute into glass container containing 100 mL 0.9% NaCl to obtain desired final dose
            • Mix diluted infusion solution by gentle inversion of the glass container 5 times; do NOT shake
            • Always protect the diluted solution from light
            • Assign a 4-hr expiration from the time of first vial puncture and wrap the glass container completely with light protective cover
            • Visually inspect solution for particulate matter and discoloration prior to administration; diluted solution is clear and colorless; discard if particulate matter observed

            IV Administration

            Infuse over 80 minutes using an infusion set made of DEHP-free polyvinyl chloride, natural latex rubber-free, microbore tubing protected from light

            Do not use a filter for administration

            Once glass container is empty, continue infusion at the same rate with 0.9% NaCl to ensure that the entire dose has been administered

            Oral Administration

            Swallow tablet whole; do not split, crush, or chew

            Tolerability may be improved when taken with food

            Dose interruptions and discontinuations

            • Missed dose: Take missed dose as soon as possible unless the next dose is within the next 6 hr
            • Missed treatment for ≥3 days: Restart selexipag at a lower dose and then titrate to desired effect and tolerance

            Storage

            Tablet

            • Store at 20-25ºC (68-77ºF); excursions permitted to 15-30°C (59-86°F)
            • Keep out of reach of children

            Unopened vials

            • Refrigerate in the original carton at 2-8ºC (36-46ºF) until use to protect from light

            Diluted solutions

            • Store at room temperature (20-25ºC [68-77ºF]); must complete infusion within 4 hr from the first puncture of the vial stopper
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            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            Uptravi oral
            -
            1,200 mcg tablet
            Uptravi oral
            -
            600 mcg tablet
            Uptravi oral
            -
            200 mcg tablet
            Uptravi oral
            -
            200 mcg (140)- 800 mcg (60) tablet
            Uptravi oral
            -
            1,400 mcg tablet
            Uptravi oral
            -
            1,000 mcg tablet
            Uptravi oral
            -
            800 mcg tablet
            Uptravi oral
            -
            400 mcg tablet
            Uptravi oral
            -
            1,600 mcg tablet

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            Patient Handout

            A Patient Handout is not currently available for this monograph.
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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.