macitentan (Rx)

Brand and Other Names:Opsumit
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 10mg
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Pulmonary Arterial Hypertension

Indicated for the treatment of pulmonary arterial hypertension (WHO Group I) to delay disease progression

10 mg PO qDay

Dosage Modifications

Renal impairment

  • Severe (CrCl 15-29 mL/min): No dosage modification needed
  • Systemic Exposure to macitentan and its active metabolite were increased by 30% and 60% respectively (this increase ise not considered clinically relevant)

Hepatic impairment

  • Mild, moderate, or severe (Child-Pugh Class A, B, and C): No dosage modification needed
  • System exposure decreased by 21%, 34%, and 6% and exposure to the active metabolite was decreased by 20%, 25%, and 25% in subjects with mild, moderate, or severe hepatic impairment respectively (this decrease is not considered clinically relevant)

Pulmonary Arterial Hypertension (Orphan)

Orphan designation of a fixed dose combination of macitentan and tadalafil for treatment of pulmonary arterial hypertension

Sponsor

  • Actelion Clinical Research, Inc; 1820 Chapel Avenue West, Suite 300; Cherry Hill, New Jersey 08002

Safety and efficacy not established

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Interactions

Interaction Checker

and macitentan

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Nasopharyngitis (20%)

            Headache (14%)

            Anemia (13%)

            Bronchitis (12%)

            1-10%

            Urinary tract infection (9%)

            Influenza (6%)

            Postmarketing Reports

            Hypersensitivity reactions (angioedema, pruritus and rash)

            Nasal congestion

            Edema/fluid retention

            Symptomatic hypotension

            Elevations of liver aminotransferases (ALT, AST) and liver injury

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            Warnings

            Black Box Warnings

            Pregnancy contraindication

            • Likely to produce serious birth defects if used by pregnant women; this effect has been seen consistently when administered to animals
            • Negative pregnancy test result required before initiating and prevention of pregnancy required monthly during treatment and for 1 month after treatment by the use of at least 2 reliable methods of contraception (unless tubal sterilization or Copper T 380A IUD or LNg 20 IUD inserted, in which case no other contraception required)
            • If a partner’s vasectomy is the chosen method of contraception, a hormone or barrier method must be used along with this method

            Restricted distribution program

            • Because of risks of birth defects, available only through restricted distribution program called the Opsumit REMS program
            • May be dispensed only to patients enrolled in and meet all conditions of the REMS program

            Contraindications

            Pregnancy

            Cautions

            Other endothelin receptor antagonists (ERAs) have been associated with elevated liver aminotransferases, hepatotoxicity, and liver failure; obtain liver enzymes tests before initiating and repeat as clinically warranted; discontinue if aminotransferase elevations are accompanied by clinical symptoms of hepatoxicity

            ERAs associated with decreased hemoglobin and hematocrit concentrations; initiation not recommended if severe anemia present

            If pulmonary edema occurs, consider the possibility of associated pulmonary veno-occlusive disease, and if confirmed, discontinue drug

            Avoid coadministration with strong CYP3A4 inhibitors

            ERAs associated with adverse effects on spermatogenesis; counsel men about potential effects on fertility

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            Pregnancy & Lactation

            Pregnancy Category: X; consistently shown to have teratogenic effects when administered to animals

            In both rabbits and rats, there were cardiovascular and mandibular arch fusion abnormalities; administration to female rats from late pregnancy through lactation caused reduced pup survival and impairment of the male fertility of the offspring at all dose levels tested

            Lactation: Unknown if distributed in human breast milk; due to presence of macitentan and metabolites in milk of lactating rats and potential for serious adverse effects in nursing infants, do not recommend use while nursing

            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

            Endothelin receptor antagonist (ET); prevents binding of ET-1 to both ET-A and ET-B receptors with high affinity to ET receptors in pulmonary arterial smooth muscle cells; active metabolite 20% as potent as parent compound

            Absorption

            Peak plasma time: 8 hr

            Absolute bioavailability: Unknown

            Distribution

            Protein bound: >99%; mainly to albumin and to a lesser extent alpha-1-glycoprotein

            Vd: 50 L; 40 L (active metabolite)

            Metabolism

            Metabolized by liver: Mainly by CYP3A4, minor amount by CYP2C19; primarily metabolized by oxidative depropylation of the sulfamide to active metabolite

            Active metabolite: At steady state, systemic exposure of active metabolite is 3-times the exposure of macitentan; active metabolite thought to contribute approximately 40% of total pharmacologic activity

            Elimination

            Half-life: 16 hr; 48 hr (active metabolite)

            Excretion: 50% urine; 24% feces

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            Administration

            Oral Administration

            May take with or without food

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            Images

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            Formulary

            FormularyPatient Discounts

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            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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