combination with other agents,
for prevention of delayed CINV.
Rolapitant has a long plasma
half-life (approximately 180 hours)
and is metabolised primarily
by CYP3A4. Unlike aprepitant,
fosaprepitant and netupitant, it
does not inhibit CYP3A4, so no
dose adjustment of dexamethasone
is required.
Rolapitant moderately inhibits
CYP2D6, breast-cancer resistance
protein and P-glycoprotein.
Caution should be exercised when
rolapitant is combined with a
medicinal product metabolised by
CYP2D6, notably those having a
narrow therapeutic margin. It is
approved in adults, in combination
with other antiemetic agents (5-HT 3
RAs and corticosteroid) to prevent
delayed CINV and effectively
prevents nausea during the overall
and delayed phases in patients
receiving HEC and MEC. 48–50
The most common side
effects are fatigue and headache.
Rolapitant improves the quality
of life in courses of HEC and
MEC. 1,3,50,51
Intravenous formulation
Despite pharmacological and
formulation advantages (for
example, faster time to onset,
and lack of first-pass hepatic
metabolism) a significant risk of
infusion-related hypersensitivity
reactions associated with the
administration of intravenous
rolapitant has been reported
in post-marketing surveillance,
including anaphylaxis, anaphylactic
shock due to rolapitant injection
formulation occurred. 3,52,53
Following their approval, all
the mentioned NK 1 RAs have been
incorporated into international
guidelines .1,3,6–9
Although there are no data
available to support the possibly
switch to different NK 1 RAs
with different pharmacokinetic/
pharmacodynamic profiles, it may
be helpful in some cases. 7
In the 2019 NCCN guidelines,
both NEPA and rolapitant are
recommended as effective in
prevention of delayed nausea. 7
Other agents
Other agents in this class, such as
vestipitant, are currently under
investigation.
Glucocorticosteroids
Although not approved as
antiemetics, glucocorticosteroids
(dexamethasone and
methylprednisolone) are very
beneficial in combination with
other antiemetic agents (for
example, 5-HT 3 RAs) 1,3,54 and
have become an integral part of
antiemetic guidelines.
In a study by Ito et al, the non-
inferiority of dexamethasone on
day 1, with sparing on days 2 and
3, combined with an NK 1 RA and
palonosetron compared with the
three-day use of dexamethasone
in HEC was studied and found
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