into account and a reduced dose
of dexamethasone (acting as a
CYP3A4 substrate) should be used
when combined with aprepitant
and NEPA. 1,3,42–46
NEPA is approved for prevention
of CINV in patients receiving MEC
and HEC (cisplatin HEC + MEC in
Europe) and is recommended in
international guidelines. 3,42–46
The positive effect in
improvement of quality of life of
patients has been assessed with
NEPA. NEPA plus a single dose of
dexamethasone was superior to
palonosetron plus dexamethasone
in preventing CINV following
MEC in acute, delayed and overall
phases of observation. As a fixed-
dose antiemetic drug combination,
NEPA along with a single dose of
dexamethasone on day 1 offers
guideline-based prophylaxis with
a convenient, single-day treatment
in MEC. 46 In HEC, dexamethasone
should be administered for four
days as per guidelines.
Intravenous formulation
In addition to the oral fixed
combination, the intravenous
equivalent (IV NEPA) consisting of
235mg fosnetupitant free-base, a
prodrug of netupitant, plus 0.25mg
palonosetron, has been approved
by the FDA (in 2018) for prevention
of CINV in patients receiving
cisplatin HEC.
A Phase IIIb study of safety
and efficacy of oral NEPA vs IV
NEPA in the AC setting has been
60 | 2019 | hospitalpharmacyeurope.com
published. 47 No infusion-site
AEs related to IV NEPA and no
anaphylaxis were reported. The
safety profile of NEPA IV was
consistent with the pivotal study,
and the outcomes of this study are
currently under FDA evaluation.
The fosnetupitant solution does
not require a surfactant, emulsifier,
or solubility enhancer and contains
no allergenic excipients.
The bioequivalence and safety
of intravenous versus oral NEPA
has been demonstrated. Netupitant
has a half-life of 90 hours and a
high binding affinity.
Rolapitant
Oral formulation
Rolapitant is a potent and selective
NK1 inhibitor, approved in