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Macitentan

Also known as: Opsumit

Endothelin Receptor AntagonistEndothelin Receptor Antagonists

Route: Oral

5 interactions on record⛔ Black Box Warning

Macitentan has 5 known drug interactions based on U.S. FDA drug labeling data. Of these, 5 are contraindicated combinations that should be avoided entirely. Notable interactions include combinations with Amiodarone, Fluconazole, Ketoconazole. Patients taking Macitentan should inform their healthcare provider of all current medications — including over-the-counter drugs and supplements — to avoid potentially harmful combinations. Data sourced from OpenFDA and the NIH National Library of Medicine.

Total: 5
Contraindicated: 5

Contraindicated (5)

Macitentan + Amiodarone— Moderate dual CYP3A4 and CYP2C9 inhibitor may increase macitentan exposure. Avoid co-administration.
Macitentan + Fluconazole— Moderate dual CYP3A4 and CYP2C9 inhibitor predicted to increase macitentan exposure approximately 4-fold. Avoid co-admin…
Macitentan + Ketoconazole— Strong CYP3A4 inhibitor approximately doubles macitentan exposure. Avoid co-administration.
Macitentan + Rifampin— Strong CYP3A4 inducer significantly reduces macitentan exposure. Avoid co-administration.
Macitentan + Ritonavir— Strong CYP3A4 inhibitor increases macitentan exposure. Avoid co-administration; use other PAH treatment options.

Macitentan + Amiodarone⛔Contraindicated

Moderate dual CYP3A4 and CYP2C9 inhibitor may increase macitentan exposure. Avoid co-administration.

Macitentan + Fluconazole⛔Contraindicated

Moderate dual CYP3A4 and CYP2C9 inhibitor predicted to increase macitentan exposure approximately 4-fold. Avoid co-administration.

Macitentan + Ketoconazole⛔Contraindicated

Strong CYP3A4 inhibitor approximately doubles macitentan exposure. Avoid co-administration.

Macitentan + Rifampin⛔Contraindicated

Strong CYP3A4 inducer significantly reduces macitentan exposure. Avoid co-administration.

Macitentan + Ritonavir⛔Contraindicated

Strong CYP3A4 inhibitor increases macitentan exposure. Avoid co-administration; use other PAH treatment options.

⛔ FDA Black Box Warning

WARNING: EMBRYO-FETAL TOXICITY OPSUMIT is contraindicated for use during pregnancy because it may cause fetal harm based on animal data [see Contraindications (4.1) , Warnings and Precautions (5.1) , Use in Specific Populations (8.1) ]. Therefore, for females of reproductive potential, exclude pregnancy before the start of treatment with OPSUMIT. Advise use of effective contraception before the initiation of treatment, during treatment, and for one month after stopping treatment with OPSUMIT [see Dosage and Administration (2.2) , Use in Specific Populations (8.3) ]. When pregnancy is detected, discontinue OPSUMIT as soon as possible [see Warnings and Precautions (5.1) ]. WARNING: EMBRYO-FETAL TOXICITY See full prescribing information for complete boxed warning. Based on animal data, OPSUMIT may cause fetal harm if used during pregnancy ( 4.1 , 5.1 , 8.1 ). Females of reproductive potential: exclude pregnancy before start of treatment. Prevent pregnancy prior to initiation of treatment, during treatment and for one month after treatment by using effective methods of contraception ( 2.2 , 8.3 ). When pregnancy is detected, discontinue OPSUMIT as soon as possible ( 5.1 ).

Contraindications

4 CONTRAINDICATIONS Pregnancy ( 4.1 ) Hypersensitivity ( 4.2 ) 4.1 Pregnancy OPSUMIT may cause fetal harm when administered to a pregnant woman. OPSUMIT is contraindicated in females who are pregnant. OPSUMIT was consistently shown to have teratogenic effects when administered to animals. If OPSUMIT is used during pregnancy, advise the patient of the potential risk to a fetus [see Warnings and Precautions (5.1) and Use in Specific Populations (8.1) ] . 4.2 Hypersensitivity OPSUMIT is contraindicated in patients with a history of a hypersensitivity reaction to macitentan or any component of the product [see Adverse Reactions (6.2) ] .

Pregnancy & Breastfeeding

8.1 Pregnancy Risk Summary Based on data from animal reproduction studies, OPSUMIT may cause embryo-fetal toxicity, including birth defects and fetal death, when administered to a pregnant female and is contraindicated during pregnancy. There are risks to the mother and the fetus associated with pulmonary arterial hypertension in pregnancy [see Clinical Considerations ] . Available data from postmarketing reports and published literature over decades of use with ERAs in the same class as OPSUMIT have not identified an increased risk of major birth defects; however, these data are limited. Methodological limitations of these postmarketing reports and published literature include lack of a control group; limited information regarding dose, duration, and timing of drug exposure; and missing data. These limitations preclude establishing a reliable estimate of the risk of adverse fetal and neonatal outcomes with maternal ERA use. Macitentan was teratogenic in rabbits and rats at all doses tested. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, advise the patient of the risk to a fetus [see Contraindications (4.1) ] . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2–4% and 15–20%, respectively. Clinical Considerations Disease-associated Maternal and/or Embryo/Fetal Risk In patients with pulmonary arterial hypertension, pregnancy is associated with an increased rate of maternal and fetal morbidity and mortality, including spontaneous abortion, intrauterine growth restriction and premature labor. Data Animal Data In both rabbits and rats, there were cardiovascular and mandibular arch fusion abnormalities. Administration of macitentan to

Data sourced from U.S. FDA drug labeling via openFDA and the NIH National Library of Medicine. For informational purposes only. Always consult your pharmacist or physician.