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granisetron (Heron Therapeutics, Inc.)
- Development stage
- Unknown
- Lead developer
- Heron Therapeutics
- Modality
- Small Molecules
- Administration
- Subcutaneous
01
Overview
Granisetron is a potent and highly selective serotonin 5-HT3 receptor antagonist used for the prevention of chemotherapy-induced nausea and vomiting (CINV). The specific formulation associated with Heron Therapeutics is Sustol (APF530), an extended-release subcutaneous injection that utilizes the proprietary Biochronomer polymer-based delivery platform. This technology enables the sustained release of granisetron over a period of at least five days, addressing both the acute (0–24 hours) and delayed (24–120 hours) phases of nausea and vomiting. Sustol was evaluated in the pivotal Phase 3 MAGIC trial, where it was compared to intravenous ondansetron as part of a three-drug regimen including a neurokinin-1 (NK1) receptor antagonist and dexamethasone in patients receiving highly emetogenic chemotherapy (HEC). Although the trial demonstrated the efficacy of the Sustol-based regimen in the HEC setting, the drug is currently FDA-approved for use in moderately emetogenic chemotherapy (MEC) and anthracycline/cyclophosphamide (AC) regimens.
- Brand names
- Sustol
- Other names
- granisetron extended-release
02
Targets
HTR3A (5-hydroxytryptamine receptor 3A)
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