INDICATION
OPSUMIT® (macitentan) is an endothelin receptor antagonist (ERA) indicated for the treatment of pulmonary arterial hypertension (PAH,
WHO Group I) to delay disease progression. Disease progression included: death, initiation of intravenous (IV) or subcutaneous prostanoids,
or clinical worsening of PAH (decreased 6-minute walk distance, worsened PAH symptoms and need for additional PAH treatment).
OPSUMIT also reduced hospitalization for PAH.
Keep disease progression in mind from the start of therapy: OPSUMIT is the only ERA
approved to delay disease progression in FC II and III patients1
Kaplan-Meier estimates of risk of first primary endpoint event in SERAPHIN
45%
Event-free patients (%)
100
Risk Reduction
p<0.0001
80
OPSUMIT*
63%
Placebo*
47%
60
40
Disease progression included: death,
initiation of IV or SC prostanoids, or clinical
worsening of PAH (decreased 6MWD,
worsened PAH symptoms and need for
additional PAH treatment).1
*Patients on PAH-specific background
therapy at baseline
20
64%
0
1 year
2 years
3 years
61% PDE-5 inhibitors
6%
inhaled or
oral prostanoids
Time from treatment start
PATIENTS AT RISK
OPSUMIT
Placebo
242
250
208
188
187
160
171
135
155
122
91
64
41
23
Summary of primary endpoint events
OPSUMIT 10 mg
(n=242)
n (%)
Placebo
(n=250)
n (%)
76 (31.4)
116 (46.4)
Worsening PAH
59 (24.4)
93 (37.2)
Death
16 (6.6)
17 (6.8)
IV/SC prostanoid
1 (0.4)
6 (2.4)
Patients with a primary endpoint event†
Component as first event
The beneficial effect of OPSUMIT was
primarily attributable to a reduction
in clinical worsening events (decreased
6MWD, worsened PAH symptoms, and
need for additional PAH treatment).1
†No patients experienced an event of lung
transplantation or atrial septostomy in the placebo
or OPSUMIT 10 mg treatment groups.
WARNINGS AND PRECAUTIONS (continued)
Hemoglobin Decrease
Decreases in hemoglobin concentration and hematocrit have occurred following administration of other ERAs and in clinical studies with
OPSUMIT. These decreases occurred early and stabilized thereafter.
In the SERAPHIN study, OPSUMIT caused a mean decrease in hemoglobin (from baseline to 18 months) of about 1.0 g/dL vs no change in the
placebo group. A decrease in hemoglobin to below 10.0 g/dL was reported in 8.7% of the OPSUMIT group vs 3.4% for placebo. Decreases in
hemoglobin seldom require transfusion.
Initiation of OPSUMIT is not recommended in patients with severe anemia. Measure hemoglobin prior to initiation of treatment and repeat
during treatment as clinically indicated.
Pulmonary Edema with Pulmonary Veno-occlusive Disease (PVOD)
Should signs of pulmonary edema occur, consider the possibility of associated PVOD. If confirmed, discontinue OPSUMIT.
Decreased Sperm Counts
Other ERAs have caused adverse effects on spermatogenesis. Counsel men about potential effects on fertility.
Please see Important Safety Information throughout and Brief Summary of Prescribing Information,
including BOXED WARNING for embryo-fetal toxicity, on adjacent pages.