Vinca alkaloid, microtubule assembly inhibitor
Brand names: Oncovin, Vincasar, Marqibo (liposomal)
Updated · Methodology
First line
Vincristine is a first-line chemotherapy component in acute lymphoblastic leukaemia in children and adults, non-Hodgkin lymphoma and neuroblastoma. ESMO and SEHH include vincristine in CHOP, COP, ABVD regimens and ALL induction. Strictly IV administration (intrathecal route is FATAL). Dose capped at 2 mg to avoid neurotoxicity.
Sources
ICD-10: C95.0 · ICD-11: 2B33.0
Binds tubulin and blocks mitotic spindle microtubule assembly – cells arrest at metaphase and undergo apoptosis. Selective for rapidly dividing tumour cells but also affects neurons (neurotoxicity is the main dose-limiting adverse effect). Metabolised by CYP3A4, excreted via P-glycoprotein. Combination with CYP3A4 inhibitors causes fatal neurotoxicity.
Contraindicated in first trimester. In second and third trimesters use only by multidisciplinary decision for pregnancy-associated cancer.
Breastfeeding contraindicated.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
3 pairs found. Sorted from critical to minor.
Mechanism
Itraconazole inhibits CYP3A4 and P-gp. Vincristine rises 5+ fold – fatal neurotoxicity with motor deficit and autonomic neuropathy.
Symptoms
Severe peripheral neuropathy, paralytic ileus, autonomic disorders.
Management
Combination contraindicated. Alternative antifungal – micafungin or caspofungin.
Mechanism
Same CYP3A4 + P-gp pharmacodynamics. Fatal neurotoxicity.
Symptoms
Severe neuropathy.
Management
Combination contraindicated.
Sources
Mechanism
Strong CYP3A4 inhibitor. Fatal neurotoxicity.
Symptoms
Severe neuropathy.
Management
Combination contraindicated.
Sources
Verbatim lines from the interaction sections, in the language of the label
«Drug Interactions: Vincristine sulfate is a substrate for cytochrome P450 3A isozymes (CYP3A). Concurrent administration of vincristine sulfate with itraconazole or fluconazole (known inhibitors of…»FDA, section 7 · Open on DailyMed
«Drug Interactions: Vincristine sulfate is a substrate for cytochrome P450 3A isozymes (CYP3A). Concurrent administration of vincristine sulfate with itraconazole or fluconazole (known inhibitors of…»FDA, section 7 · Open on DailyMed
«Drug Interactions: Vincristine sulfate is a substrate for cytochrome P450 3A isozymes (CYP3A). Concurrent administration of vincristine sulfate with itraconazole or fluconazole (known inhibitors of…»FDA, section 7 · Open on DailyMed
«Drug Interactions: Concurrent use of strong CYP3A inducers (e.g., St. John's Wort) with vincristine sulfate should be avoided.»FDA, section 7 · Open on DailyMed
«Drug Interactions: The simultaneous oral or intravenous administration of phenytoin and antineoplastic chemotherapy combinations that included vincristine sulfate has been reported to reduce blood…»FDA, section 7 · Open on DailyMed
«Alcaloides de la vinca: Muchos de los alcaloides de la vinca (por ejemplo vincristina y vinblastina) son sustratos del CYP3A4. La administración concomitante de antifúngicos azólicos, incluyendo…»AEMPS, section 4.5 · Open on CIMA
«Established and Other Potentially Significant Drug Interactions: Anticancer Agents: abemaciclib, apalutamide, dasatinib, encorafenib, ibrutinib, ivosidenib, neratinib, nilotinib, venetoclax…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Interactions: dasatinib nilotinib vinblastine vincristine ↑ anticancer agents A decrease in the dosage or an adjustment of the dosing interval of…»FDA, section 7 · Open on DailyMed
«ANTINEOPLÁSICOS: Dasatinib Nilotinib Vinblastina Vincristina Everolimus Irinotecan»AEMPS, section 4.5 · Open on CIMA
«Established and Other Potentially Significant Drug Interactions: Antineoplastics: dasatinib, nilotinib vinblastine, vincristine antineoplastics A decrease in the dosage or an adjustment of the…»FDA, section 7 · Open on DailyMed
«Fármacos antineoplásicos: Alcaloides de la vinca (que incluyen, entre otros: vincristina y vinblastina) [sustratos del CYP3A4]»AEMPS, section 4.5 · Open on CIMA
«Alcaloides de la vinca: Aunque no se ha estudiado, fluconazol puede aumentar los niveles plasmáticos de los alcaloides de la vinca (por ejemplo, vincristina y vinblastina) y producir neurotoxicidad…»AEMPS, section 4.5 · Open on CIMA
«Effects of Posaconazole on Other Drugs: Vinca alkaloids (e.g., vincristine, vinblastine) Reserve concomitant use for patients with no alternative antifungal treatment options [see Warnings and…»FDA, section 7 · Open on DailyMed
«Agentes anticancerígenos e inhibidores de la quinasa: Dasatinib, nilotinib, vincristina, vinblastina»AEMPS, section 4.5 · Open on CIMA
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Vincristine is evaluated for the following indications with varying evidence strength: Acute leukemia (evidence tier A). See the full indication matrix with dosing and citations above on this page.
Common side effects of Vincristine (≥ 1 in 100): Peripheral neuropathy, Constipation (may be severe), Alopecia, Myalgia. See the Safety section for uncommon and serious reactions.
Contraindicated in first trimester. In second and third trimesters use only by multidisciplinary decision for pregnancy-associated cancer.
Breastfeeding contraindicated.
Vincristine is contraindicated in: Intrathecal administration (FATAL); Itraconazole, posaconazole, voriconazole, ritonavir, cobicistat (fatal neurotoxicity); Demyelinating Charcot-Marie-Tooth syndrome; Pregnancy (first trimester). Full list in the Safety section.
Direct links to regulator labels. Open in a new tab.
Capecitabine, Everolimus, Fluorouracil, Methotrexate, Nintedanib, Sunitinib