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APF530 + dexamethasone
- Development stage
- Unknown
- Lead developer
- Heron Therapeutics
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Subcutaneous, Oral, Intravenous
01
Overview
APF530 + dexamethasone is a **combination drug regimen** intended primarily for the prevention of chemotherapy-induced nausea and vomiting (CINV). APF530 is an extended-release, subcutaneous formulation of granisetron, a first-generation serotonin 5-HT3 receptor antagonist, designed for sustained-release over five or more days. Dexamethasone is a synthetic glucocorticoid with antiemetic and anti-inflammatory properties. This combination is often used as part of guideline-recommended antiemetic regimens in patients receiving moderate to highly emetogenic chemotherapy, including regimens containing anthracyclines, cyclophosphamide, or cisplatin. APF530’s mechanism allows prolonged 5-HT3 blockade to prevent both acute and delayed CINV, while dexamethasone enhances antiemetic efficacy through glucocorticoid-mediated mechanisms. APF530 (granisetron extended-release injection) is developed and manufactured by Heron Therapeutics.
- Brand names
- SUSTOL
- Other names
- APF530 + dexamethasone
02
Targets
GR (Glucocorticoid receptor)HTR3A (5-hydroxytryptamine receptor 3A)
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