PAGE 2
RIGHT HAND PAGE
OPSUMIT® (macitentan)
OPSUMIT® (macitentan)
DRUG INTERACTIONS
Strong CYP3A4 Inducers
Strong inducers of CYP3A4 such as rifampin significantly reduce macitentan exposure.
Concomitant use of OPSUMIT with strong CYP3A4 inducers should be avoided [see
Clinical Pharmacology (Pharmacokinetics)].
Strong CYP3A4 Inhibitors
Concomitant use of strong CYP3A4 inhibitors like ketoconazole approximately double
macitentan exposure. Many HIV drugs like ritonavir are strong inhibitors of CYP3A4. Avoid
concomitant use of OPSUMIT with strong CYP3A4 inhibitors [see Clinical Pharmacology
(Pharmacokinetics)]. Use other PAH treatment options when strong CYP3A4 inhibitors are
needed as part of HIV treatment [see Clinical Pharmacology (Pharmacokinetics)].
USE IN SPECIFIC POPULATIONS
Pregnancy
Pregnancy Category X.
Risk Summary
OPSUMIT may cause fetal harm when administered to a pregnant woman and is
contraindicated during pregnancy. Macitentan was teratogenic in rabbits and rats at
all doses tested. A no-effect dose was not established in either species. If this drug
is used during pregnancy, or if the patient becomes pregnant while taking this drug,
advise the patient of the potential hazard to a fetus [see Contraindications (Pregnancy)].
Animal Data
In both rabbits and rats, there were cardiovascular and mandibular arch fusion
abnormalities. Administration of macitentan 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.
Nursing Mothers
It is not known whether OPSUMIT is present in human milk. Macitentan and its
metabolites were present in the milk of lactating rats. Because many drugs are
present in human milk and because of the potential for serious adverse reactions
from macitentan in nursing infants, nursing mothers should discontinue nursing or
discontinue OPSUMIT.
Pediatric use
The safety