Binding Affinity
ALOXI®
STRONG BINDING, LONG HALF-LIFE
As a 5-HT3 receptor antagonists, ALOXI blocks serotonin
from binding to the receptors so the vomiting reflex is not triggered.1
The correlation between this pharmacological data and clinical efficacy has
not been established.
ALOXI Molecular Properties
- Allosteric binding—ALOXI is thought to bind
to the serotonin receptor site and an additional allosteric* site2
- Positive cooperativity—when ALOXI binds to
the serotonin and allosteric binding sites, a conformational change occurs, increasing
overall receptor affinity for ALOXI2
- Receptor internalization—ALOXI triggers 5-HT3
receptor internalization and induces prolonged inhibition of serotonin binding to
cell surface receptors3
- Long plasma half-life—approximately 40 hours4
*A second site in which binding is influenced due to binding at the first
site.
Indication
ALOXI® (palonosetron HCl) injection 0.25 mg is indicated for the
prevention of acute and delayed nausea and vomiting associated with initial and
repeat courses of moderately emetogenic chemotherapy, and acute nausea and vomiting
associated with initial and repeat courses of highly emetogenic chemotherapy.
Important Safety Information
- Aloxi is contraindicated in patients known to have hypersensitivity to the drug
of any of its components
- Most commonly reported adverse reactions in chemotherapy-induced nausea and vomiting
include headache (9%) and constipation (5%)
ALOXI is available by prescription only.
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