# Vinblastine

**Canonical URL:** https://ingredients.hermeticasuperfoods.com/ingredients/vinblastine
**Data Source:** Hermetica Superfoods Ingredient Encyclopedia
**Updated:** 2026-04-05
**Evidence Score:** 2 / 10
**Category:** Compound
**Also Known As:** VLB, Vincaleukoblastine, Velban, Vinblastine sulfate, 29060-10-2, Vinca alkaloid, Madagascar periwinkle alkaloid, Catharanthus alkaloid, Dimeric indole alkaloid

## Overview

Vinblastine is a vinca alkaloid derived from Catharanthus roseus (periwinkle plant) that functions as a mitotic inhibitor by binding to tubulin dimers. It prevents microtubule polymerization, arresting cell division at metaphase and triggering apoptosis in rapidly dividing cancer cells.

## Health Benefits

• Treatment of Hodgkin lymphoma with 72.7% complete remission rate in phase 2 trial (CALGB 50203) with 99 patients • Management of high-risk anaplastic large-cell lymphoma in pediatric populations, as demonstrated in the ALCL99-vinblastine trial with 217 patients • Treatment option for urothelial cancer in cisplatin-ineligible patients, though with modest survival benefit (median 8.1 months) in phase II/III trial • Therapeutic activity in doxorubicin-refractory metastatic breast cancer when administered as continuous infusion • Component of neoadjuvant therapy for muscle-invasive bladder cancer in the BA06 30894 international phase III trial with 976 patients

## Mechanism of Action

Vinblastine binds with high affinity to beta-tubulin at the vinca domain, preventing tubulin heterodimer polymerization into functional mitotic spindles and inducing tubulin spiral aggregation. This disruption arrests the cell cycle at the G2/M phase metaphase checkpoint, activating the spindle assembly checkpoint via Mad2 and BubR1 kinase signaling. Prolonged mitotic arrest triggers caspase-dependent apoptosis, particularly affecting rapidly proliferating cells with high mitotic indices such as lymphoma and carcinoma cells.

## Clinical Summary

A Phase 2 CALGB 50203 trial in 99 patients with Hodgkin lymphoma demonstrated a 72.7% complete remission rate when vinblastine was incorporated into ABVD-based regimens, providing strong prospective evidence for its role in first-line therapy. The ALCL99-vinblastine randomized trial in 217 pediatric patients with high-risk anaplastic large-cell lymphoma showed that vinblastine maintenance improved event-free survival compared to standard chemotherapy alone. Vinblastine also serves as a treatment option for urothelial carcinoma, typically in platinum-ineligible or relapsed settings, though evidence here derives largely from smaller cohort studies and retrospective analyses. Overall, the strongest evidence base exists for lymphoma indications, while its role in solid tumors requires further large-scale randomized validation.

## Nutritional Profile

Vinblastine is a purified alkaloid compound derived from Catharanthus roseus (Madagascar periwinkle), not a nutritional substance. It has no macronutrient, micronutrient, fiber, or caloric value. Chemically, it is a dimeric indole-dihydroindole alkaloid with molecular formula C46H58N4O9 and molecular weight of 810.98 g/mol. It is composed primarily of two alkaloid units: vindoline and catharanthine linked via a carbon-carbon bond. Clinical formulations (Velban) are typically supplied as lyophilized powder at 10 mg per vial with mannitol as excipient. Bioavailability via oral route is negligible due to extensive first-pass [metabolism](/ingredients/condition/weight-management) and poor GI absorption; it is administered exclusively via intravenous injection. Plasma protein binding is approximately 75%. It undergoes hepatic metabolism via CYP3A4 to its active metabolite desacetylvinblastine. Half-life is triphasic: initial 3.7 minutes, intermediate 1.6 hours, terminal 24.8 hours. No dietary vitamins, minerals, or fiber content are applicable. As a vinca alkaloid, its bioactive mechanism involves tubulin binding (Kd approximately 1-2 µM), inhibiting microtubule polymerization rather than providing nutritional function.

## Dosage & Preparation

Clinically studied dosages include 6 mg/m² per chemotherapy course for high-risk ALCL, 1.7 mg/m²/day by continuous infusion for metastatic breast cancer, and varying doses when combined with other agents in AVG and M-CAVI regimens. Vinblastine is administered intravenously as a pharmaceutical preparation with dosing calculated based on body surface area. Consult a healthcare provider before starting any new supplement.

## Safety & Drug Interactions

Vinblastine carries significant neurotoxicity risk, including peripheral neuropathy, paresthesia, and autonomic dysfunction such as constipation, ileus, and urinary retention due to axonal tubulin disruption. Severe myelosuppression—particularly leukopenia with nadir around days 5–10—is dose-limiting, requiring CBC monitoring and dose adjustments in hepatic impairment since the drug is primarily CYP3A4-metabolized and biliary-excreted. Concurrent use of strong CYP3A4 inhibitors (e.g., itraconazole, erythromycin) can markedly elevate plasma vinblastine levels, increasing toxicity risk, while P-glycoprotein inducers such as rifampin may reduce efficacy. Vinblastine is classified FDA Category D in pregnancy, with documented teratogenicity and fetotoxicity in animal models, and is contraindicated in breastfeeding.

## Scientific Research

Multiple randomized controlled trials have evaluated vinblastine across various cancers, including the CALGB 50203 trial in Hodgkin lymphoma (99 patients), the ALCL99-vinblastine trial in pediatric lymphoma (217 patients), and a phase II/III trial in urothelial cancer (238 patients). The BA06 30894 international phase III trial assessed neoadjuvant CMV chemotherapy in 976 patients with muscle-invasive bladder cancer over 8 years of follow-up.

## Historical & Cultural Context

Vinblastine is not a traditional medicine compound but rather a modern pharmaceutical alkaloid isolated from the Madagascar periwinkle in the 20th century. While the periwinkle plant has been used in traditional medicine systems, vinblastine itself represents a transition from ethnobotanical observation to modern oncology development.

## Synergistic Combinations

Doxorubicin, gemcitabine, methotrexate, carboplatin, cisplatin

## Frequently Asked Questions

### What is vinblastine used to treat?

Vinblastine is used primarily to treat Hodgkin lymphoma, anaplastic large-cell lymphoma (ALCL) in pediatric patients, and urothelial carcinoma, among other malignancies. The CALGB 50203 trial confirmed a 72.7% complete remission rate in Hodgkin lymphoma, and the ALCL99 trial validated its benefit in pediatric high-risk ALCL over 217 patients.

### How does vinblastine work at the molecular level?

Vinblastine binds to the vinca domain on beta-tubulin subunits, preventing their assembly into the mitotic spindle microtubules required for chromosome segregation during cell division. This arrests cells at the G2/M metaphase checkpoint via spindle assembly checkpoint proteins Mad2 and BubR1, ultimately triggering caspase-mediated apoptosis in dividing cancer cells.

### What are the most common side effects of vinblastine?

The most common dose-limiting side effect is myelosuppression, especially leukopenia, which typically reaches nadir at days 5–10 post-administration and necessitates regular complete blood count monitoring. Neurotoxicity is also prominent, manifesting as peripheral neuropathy, paresthesia, and autonomic effects including constipation and urinary retention due to disruption of neuronal tubulin function.

### Does vinblastine interact with other medications?

Yes, vinblastine is metabolized primarily by the CYP3A4 enzyme and is a P-glycoprotein substrate, making it vulnerable to multiple drug interactions. Strong CYP3A4 inhibitors such as itraconazole, ketoconazole, and erythromycin can significantly increase vinblastine plasma concentrations and toxicity, while CYP3A4 inducers like rifampin or phenytoin can reduce its therapeutic efficacy.

### Is vinblastine safe during pregnancy or breastfeeding?

Vinblastine is classified as FDA Pregnancy Category D, meaning there is positive evidence of human fetal risk, and it is contraindicated in breastfeeding due to its cytotoxic properties and potential for serious harm to the nursing infant. Animal studies have demonstrated teratogenic and fetotoxic effects, and its use during pregnancy is reserved only for situations where the benefit clearly outweighs the substantial risk to the fetus.

### What clinical evidence supports vinblastine's effectiveness in treating Hodgkin lymphoma?

The CALGB 50203 phase 2 trial demonstrated a 72.7% complete remission rate in 99 patients with Hodgkin lymphoma receiving vinblastine-based therapy, providing robust clinical evidence for its efficacy in this indication. This data supports vinblastine's role as a standard component in combination chemotherapy regimens for Hodgkin lymphoma management. The high remission rates reflect decades of clinical experience with this agent in lymphoid malignancies.

### Which patient populations are most appropriate candidates for vinblastine treatment?

Vinblastine is most appropriate for patients with Hodgkin lymphoma, high-risk anaplastic large-cell lymphoma (particularly in pediatric populations as shown in the ALCL99 trial with 217 patients), and cisplatin-ineligible urothelial cancer patients. Pediatric patients with ALCL represent a specific population where vinblastine demonstrates significant benefit as part of combination therapy. Elderly patients and those with significant comorbidities require careful evaluation due to vinblastine's toxicity profile.

### How does vinblastine's efficacy in urothelial cancer compare to its use in lymphoid malignancies?

Vinblastine shows substantially better outcomes in lymphoid malignancies like Hodgkin lymphoma (72.7% complete remission) compared to urothelial cancer, where it provides only modest survival benefit with a median of 8.1 months in cisplatin-ineligible patients. This difference reflects vinblastine's greater sensitivity in hematologic malignancies versus solid tumors. The modest efficacy in urothelial cancer positions it as a second-line option rather than a primary treatment choice.

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*Source: Hermetica Superfoods Ingredient Encyclopedia — https://ingredients.hermeticasuperfoods.com*
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