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Netupitant

AKYNZEO

What it isNK1 receptor antagonist, co-formulated with palonosetron; chemotherapy-induced nausea.

Why this oneOne capsule covers both the acute and delayed phases, replacing two separate agents.

What limits itIt inhibits CYP3A4, so dexamethasone must be reduced. Headache and constipation.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Prevention of nausea/vomiting with emetogenic chemotherapyadult1 capsule PO 1 h before chemotherapy (Day 1)1 capsule per chemotherapy cycle1 capsule per cycle

Renal Avoid in severe renal impairment or ESRD; no adjustment for mild–moderate

Hepatic Avoid in severe hepatic impairment (Child-Pugh >9); no adjustment for mild–moderate

Instructions

Cautions

Adverse reactions

Pregnancy May cause fetal harm based on animal data; human data insufficient

Lactation Undefined

NO BOXED WARNINGS

Principal riskIt inhibits CYP3A4, so dexamethasone must be reduced

Classes and tags

Clinical profile

Direct muscarinic antagonism0 / 4

Mechanism of action: Netupitant ballicule

Netupitant ballicule: receptor binding, kinetics and half-life diagram

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