Generic Name and Formulations:
Netupitant, palonosetron (as HCl); 300mg/0.5mg; hard gel caps.
Helsinn Therapeutics, Inc.
Indications for AKYNZEO:
Prevention of acute and delayed nausea and vomiting due to initial and repeat courses of chemotherapy, including highly emetogenic chemotherapy.
≥18yrs: Highly emetogenic chemotherapy (including cisplatin-based): 1 cap approx. 1hr prior to chemotherapy with oral dexamethasone 12mg given 30mins before chemotherapy on Day 1, then 8mg orally once daily on Days 2–4. Anthracyclines and cyclophosphamide-based chemotherapy, or non-highly emetogenic chemotherapy: 1 cap approx. 1hr prior to chemotherapy with oral dexamethasone 12mg given 30mins prior to chemotherapy on Day 1.
<18yrs: not established.
Monitor for symptoms of serotonin syndrome; discontinue and treat if occurs. Severe hepatic or renal impairment, ESRD: avoid. Elderly. Pregnancy. Nursing mothers.
Increased risk of serotonin syndrome with concomitant other serotonergic drugs (eg, SSRIs, SNRIs, MAOIs, mirtazapine, fentanyl, lithium, tramadol, IV methylene blue). May potentiate CYP3A4 substrates (eg, dexamethasone [use reduced dose], midazolam, alprazolam, triazolam, docetaxel, paclitaxel, etoposide, irinotecan, cyclophosphamide, ifosfamide, imatinib, vinorelbine, vinblastine, vincristine); caution and monitor. Avoid concomitant strong CYP3A4 inducers (eg, rifampin). Potentiated by strong CYP3A4 inhibitors (eg, ketoconazole). Concomitant warfarin: monitor INR and adjust dose as needed. Inj: incompatible with divalent cation-containing solutions, Lactated Ringer's Injection, Hartmann's Solution.
Substance P/NK1 receptor antagonist + 5-HT3 receptor antagonist.
Headache, asthenia, dyspepsia, fatigue, constipation, erythema; hypersensitivity reactions.
Blister—1, 4; Single-dose vial—1