Palonosetron
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| ID | DRUG-PALONOSETRON |
|---|---|
| Тип | Препарат |
| Синоніми | AloxiOnicitПалоносетрон |
| Статус | переглянуто 2026-04-27 | очікує клінічного підпису |
| Хвороби | Не вказано |
| Джерела | SRC-ESMO-DLBCL-2024 SRC-NCCN-BCELL-2025 |
Дані про препарат
| Клас | Long-acting second-generation 5-HT3 receptor antagonist (antiemetic) |
|---|---|
| Механізм дії | Selective competitive antagonist at the 5-hydroxytryptamine type 3 (5-HT3) serotonin receptor located peripherally on vagal afferent terminals in the GI tract and centrally in the chemoreceptor trigger zone (area postrema). Distinguishing features vs first-generation 5-HT3 antagonists (ondansetron, granisetron): ~30× higher receptor binding affinity, ~7× longer plasma half-life (~40 h vs ~4-6 h), and demonstrated allosteric receptor cross-talk with NK1 receptors that contributes to superior delayed-phase CINV control. A single IV or oral dose covers both acute (0-24 h) and delayed (24-120 h) phases of CINV. Approved by FDA July 2003 and EMA March 2005. |
| Типове дозування | 0.25 mg IV bolus over 30 seconds, 30 minutes before chemotherapy on day 1 only (single dose covers ≥120 h). Oral 0.5 mg PO 1 hour before chemotherapy is alternative. For multi-day chemotherapy (e.g., ICE, cisplatin × 5), repeat on alternate days (e.g., d1 and d3) is common off-label practice; dosing every 7 days has supportive evidence in metronomic regimens. No dose adjustment for renal or hepatic impairment. Pediatric (1 month-17 years): 20 µg/kg IV (max 1.5 mg). No dose cap with concomitant strong CYP enzyme modulators (minimal CYP-mediated metabolism). NK1 antagonist + dexamethasone added to palonosetron for HEC = standard triple-antiemetic regimen. |
| Зареєстровано в Україні | True |
| Відшкодовується НСЗУ | True |
| Остання перевірка для України | 2026-04-27 |
Нотатки
Preferred 5-HT3 antagonist for HEC and for multi-day chemotherapy regimens because of long half-life and demonstrated superiority in delayed-phase CINV control vs ondansetron in head-to-head trials (Saito 2009, Aapro 2014). Triple antiemetic regimen for HEC: NK1 antagonist (aprepitant or fosaprepitant) + palonosetron 0.25 mg IV + dexamethasone 12 mg IV day 1, with dex tapered through delayed phase. Akynzeo (netupitant 300 mg + palonosetron 0.5 mg) fixed-dose oral capsule simplifies triple therapy to two pills (Akynzeo + dex) on day 1. Lowest QT signal in 5-HT3 class — preferred when ondansetron contraindicated due to QT concerns or cardiac comorbidity. Minimal CYP-mediated metabolism makes it the safer 5-HT3 choice in polypharmacy patients (e.g., patients on CYP3A4 inhibitors).
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