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 |
| Molecular Weight | 778.93 |
| 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 | Avoid due to teratogenicity (FDA Pregnancy Category D). Vinorelbine is embryotoxic and fetotoxic in animal studies. |
| 2nd trimester | Avoid unless potential benefit outweighs risk. May cause fetal harm; use only if clearly needed. |
| 3rd trimester | Avoid near term due to risk of neonatal myelosuppression and other adverse effects. |
Clinical note
Comprehensive clinical and safety monograph for NAVELBINE (NAVELBINE).
| Placental transfer | Placental transfer is expected; vinorelbine has low molecular weight and crosses the placenta in animal models. |
| Breastfeeding | It is not known whether vinorelbine is excreted in human milk. Due to potential for serious adverse reactions in nursing infants, breastfeeding is not recommended during treatment and for at least 2 weeks after the last dose. |
■ 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 |
Hypersensitivity to vinorelbine or other vinca alkaloidsSevere neutropenia (absolute neutrophil count < 1000/mm3)
| 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. |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they may inhibit CYP3A4 and increase vinorelbine toxicity. No other specific food interactions; maintain adequate hydration. |
Loading safety data…
| Lactation Rating |
| L5 - Contraindicated |
| 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. |
| 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. |
| Clinical Pearls | Navelbine (vinorelbine) is a vinca alkaloid that inhibits microtubule assembly. It is associated with significant myelosuppression (neutropenia) and is a moderate vesicant; avoid extravasation with a central line preferred. Administer over 6-10 minutes IV push or short infusion. Monitor for acute infusion reactions and paralytic ileus. Dose adjustment needed for hepatic impairment (bilirubin >2 mg/dL). |
| Patient Advice | Report any pain, redness, or swelling at injection site immediately. · Notify your doctor if you develop fever, chills, or signs of infection. · Avoid grapefruit and grapefruit juice during treatment. · Use effective contraception during and for at least 3 months after therapy. · Report persistent constipation, abdominal pain, or nausea. · Avoid live vaccines and close contact with recently vaccinated individuals. |