NAVELBINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for NAVELBINE (NAVELBINE).
Semisynthetic vinca alkaloid that inhibits microtubule assembly by binding to tubulin, causing mitotic arrest in metaphase.
| Metabolism | Hepatic metabolism primarily via CYP3A4; also metabolized by CYP2D6. 4-O-deacetylvinorelbine is the active metabolite. |
| Excretion | Primarily hepatic metabolism with biliary excretion; ~50% excreted in feces as metabolites, <20% excreted unchanged in urine |
| Half-life | Terminal elimination half-life approximately 27–43 hours (mean 27.5 h); clinical context: supports weekly dosing schedule |
| Protein binding | 79–91% bound, primarily to alpha-1-acid glycoprotein and albumin |
| Volume of Distribution | Extensive distribution with Vd 27–40 L/kg (range 18–75); indicates widespread tissue binding |
| Bioavailability | Oral: approximately 27–38% (absolute bioavailability; highly variable) |
| Onset of Action | Intravenous: rapid, within 5–10 minutes; Oral: onset within 1–2 hours |
| Duration of Action | Intravenous: clinical effects persist for 24–48 hours; Oral: duration similar to IV; myelosuppression may last longer |
| Action Class | Antimicrotubule agents- Vinka alkaloid |
| Brand Substitutes | Neoben 50mg Injection, Relbovin 50 Injection, Zorelbin 50mg Injection, Vinelbine 50mg Injection, Vinbicel 50 Injection, Neoben 10mg Injection, Relbovin 10mg Injection, Cevin 10mg Injection, Zorelbin 10mg Injection, Vinotec 10mg Injection |
25 to 30 mg/m² intravenously over 6-10 minutes on days 1 and 8 of a 21-day cycle.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment recommended; use with caution in severe renal impairment (CrCl <30 mL/min). |
| Liver impairment | Child-Pugh A: 20 mg/m². Child-Pugh B: 15 mg/m². Child-Pugh C: not recommended. |
| Pediatric use | Not established; safety and efficacy in pediatric patients have not been determined. |
| Geriatric use | No specific dose adjustment; monitor for increased toxicity, especially myelosuppression and neurotoxicity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for NAVELBINE (NAVELBINE).
| Breastfeeding | Excretion into human milk is unknown; however, other vinca alkaloids are excreted. M/P ratio not established. Due to potential for serious adverse reactions in breastfeeding infants, a decision should be made to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. |
| Teratogenic Risk | Pregnancy Category D. Vinorelbine is embryotoxic and teratogenic in animal studies. First trimester: high risk of congenital malformations, including skeletal and visceral anomalies. Second and third trimesters: risk of intrauterine growth restriction, spontaneous abortion, and fetal toxicity. Contraindicated in pregnancy unless benefit outweighs risk. |
■ FDA Black Box Warning
NAVELBINE is for intravenous administration only. Intrathecal administration of other vinca alkaloids has resulted in death. Severe granulocytopenia and severe peripheral neuropathy may occur. Monitor complete blood counts prior to each dose and adjust dosage accordingly.
| Serious Effects |
Severe granulocytopenia (absolute neutrophil count <1000 cells/mm³), current or recent severe infection, severe hepatic impairment, pregnancy.
| Precautions | Bone marrow suppression (especially granulocytopenia), severe peripheral neuropathy, respiratory failure, bronchospasm, interstitial pneumonitis, syndrome of inappropriate antidiuretic hormone secretion (SIADH), hepatic impairment, and GI toxicity (constipation, paralytic ileus, intestinal obstruction). Monitor liver function and blood counts. |
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| Fetal Monitoring | Monitor complete blood count, hepatic and renal function regularly. During pregnancy, perform fetal ultrasound for growth and anatomy, and consider serial growth scans. Monitor for maternal myelosuppression, infection, and neuropathy. |
| Fertility Effects | Vinorelbine can cause amenorrhea and may impair fertility in females. In males, may cause temporary or permanent infertility due to testicular damage. Effects may be irreversible. |