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
- chemotherapy-induced nausea and vomiting with palonosetron (2014)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Prevention of nausea/vomiting with emetogenic chemotherapy | adult | 1 capsule PO 1 h before chemotherapy (Day 1) | 1 capsule per chemotherapy cycle | 1 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
- Give with dexamethasone per the emetogenicity regimen
- Capsule with or without food, 1 hour before chemotherapy
Available strengths
- inj 235/0.25 mg
Cautions
- Hypersensitivity, including anaphylaxis (palonosetron component)
- MAOIs due to risk of serotonin syndrome
Adverse reactions
- Headache
- Asthenia
- Dyspepsia
- Fatigue
- Constipation
- Erythema
Pregnancy May cause fetal harm based on animal data; human data insufficient
Lactation Undefined
Cost
| Strength | #/mo | generic $/unit | CostPlus | |
|---|---|---|---|---|
| 235/0.25 mg | inj | per unit | not offered |
NO BOXED WARNINGS
Principal riskIt inhibits CYP3A4, so dexamethasone must be reduced
Classes and tags
Clinical profile
Defining liabilityProlonged CYP3A interactions and hypersensitivity