فينبلاستين
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فينبلاستين

Vinblastine Product Introduction

  1. الاسم الانجليزي: Vinblastine
  1. مواصفة
    • نقاء: Vinblastine sulfate ≥ 98% (HPLC); high – purity grade: ≥ 99% (HPLC)
    • الذوبانية: Soluble in water (as sulfate salt, ~50 mg/mL), methanol, and ethanol; insoluble in non – polar solvents
    • Appearance – Related: Loss on drying ≤ 1.0%, heavy metals ≤ 10 ppm, residual solvents ≤ 0.5%
    • Particle Size: Standard powder ≤ 100 μm; micronized powder ≤ 5 μm for better dissolution in formulations
  1. مظهر
    • White to off – white crystalline powder (sulfate salt form), odorless
  1. رقم CAS：143-67-9 (Vinblastine); 2068 – 78 – 2 (Vinblastine sulfate)
  1. مهلة: 7 – 10 Working Days
  1. طَرد
    • 10 mg/vial (sterile glass vial), sealed under nitrogen; 100 mg/aluminum foil – lined bag for research – grade products
  1. السوق الرئيسي: Global pharmaceutical and research markets, with significant demand in North America, Europe, and Asia, mainly for oncology treatment and biomedical research
  1. سيناريوهات التطبيق

Core Properties

  • Molecular Formula: C₄₆H₅₈N₄O₉ (Vinblastine); C₄₆H₅₈N₄O₉·2H₂SO₄ (Vinblastine sulfate)
  • Chemical Structure: An indole – alkaloid derived from Catharanthus roseus (Madagascar periwinkle), consisting of a complex dimeric structure with two linked indole rings.
  • Key Features
    • Antimitotic Agent: Binds to tubulin, inhibiting microtubule polymerization and disrupting the mitotic spindle during cell division, leading to cell cycle arrest at the metaphase – anaphase transition.
    • Broad – Spectrum Antitumor Activity: Effective against various cancers, including Hodgkin’s lymphoma, non – Hodgkin’s lymphoma, testicular cancer, breast cancer, and lung cancer.
    • Low Bioavailability: Oral absorption is poor; typically administered intravenously for therapeutic use.
    • High Potency: Requires careful dosage control due to significant toxicity to rapidly dividing normal cells (e.g., bone marrow, gastrointestinal tract).

سيناريوهات التطبيق

1. Oncology Treatment

  • Chemotherapy Regimens:
    • Hodgkin’s Lymphoma: A key component of the ABVD (doxorubicin, bleomycin, vinblastine, dacarbazine) regimen, achieving high remission rates (up to 80 – 90% in early – stage cases).
    • Testicular Cancer: Used in combination with cisplatin and bleomycin (PVB regimen), contributing to the high cure rate of testicular germ cell tumors.
    • Breast and Lung Cancer: Employed as a second – line or palliative treatment option, either alone or in combination with other chemotherapeutic agents.
  • Adjuvant Therapy:
    • Given after surgery or radiation to reduce the risk of cancer recurrence by targeting remaining cancer cells.

2. Biomedical Research

  • Cell Biology Studies:
    • Used as a tool to study microtubule dynamics, cell division mechanisms, and the role of the cytoskeleton in cell function. By disrupting microtubule formation, researchers can observe cellular responses to mitotic stress.
  • Drug Development:
    • Serves as a reference compound for the development of novel antimitotic drugs. Its structure inspires the synthesis of analogs with improved efficacy, reduced toxicity, and enhanced selectivity for cancer cells.
  • Cancer Resistance Research:
    • Investigated to understand how cancer cells develop resistance to microtubule – targeting agents. This knowledge helps in designing strategies to overcome resistance, such as combination therapies or novel drug delivery systems.

3. Veterinary Oncology

  • Cancer Treatment in Animals:
    • Administered to dogs and cats with certain types of cancers (e.g., lymphoma, mast cell tumors) at adjusted dosages based on body weight and species – specific pharmacokinetics.

طرق الكشف

  • High – Performance Liquid Chromatography (HPLC):
    • Column: C18 (250 × 4.6 mm, 5 μm), Mobile Phase: Acetonitrile – 0.1% trifluoroacetic acid (gradient elution), Flow Rate: 1.0 mL/min, Detection Wavelength: 262 nm for quantification.
  • Liquid Chromatography – Mass Spectrometry (LC – MS):
    • Used for identifying vinblastine and its metabolites in biological samples, providing high – sensitivity detection and confirmation of the compound’s structure.
  • UV – Visible Spectroscopy:
    • Quick – screening method to estimate vinblastine concentration based on its characteristic absorption peak at 262 nm, useful for initial quality control and batch analysis.

Source & Advantages

  • مصدر طبيعي: Originally isolated from the leaves and stems of Catharanthus roseus. However, due to the low natural content (0.002 – 0.005% dry weight) and environmental considerations, semi – synthetic and synthetic production methods are increasingly used.
  • Therapeutic Significance: A cornerstone in cancer chemotherapy, having significantly improved survival rates for several types of cancer since its discovery.
  • Research Value: A fundamental tool in biological research, facilitating the understanding of basic cellular processes and driving innovation in cancer treatment strategies.

Regulatory Compliance

  • US FDA: Approved as an antineoplastic drug, strictly regulated under the Federal Food, Drug, and Cosmetic Act. Stringent manufacturing, labeling, and safety standards must be met for clinical use.
  • EMA (European Medicines Agency): Licensed for use in oncology, with continuous pharmacovigilance to monitor adverse effects and ensure patient safety.
  • China NMPA: Registered for clinical use in cancer treatment, subject to Good Manufacturing Practice (GMP) requirements and regular quality inspections.
التصنيفات: ,

Vinblastine Sulfate: The Vinca Alkaloid Powerhouse in Cancer Therapeutics

1. What is Vinblastine?
Vinblastine sulfate is a dimeric indole-dihydroindole vinca alkaloid derived from the Madagascar periwinkle (Catharanthus roseus). As a potent microtubule-destabilizing agent, it binds to β-tubulin subunits at the vinca domain, inhibiting microtubule assembly and suppressing mitotic spindle formation. This triggers G2/M phase arrest و mitotic catastrophe in rapidly proliferating cells. Recognized as an essential medicine by WHO, it’s clinically indispensable for treating Hodgkin lymphoma, testicular cancer, and advanced breast carcinoma.

2. Source, Chemical Properties & Identifiers

  • مصدر: Isolated from leaves of Catharanthus roseus; semi-synthesis from precursors catharanthine and vindoline.

  • الخصائص الكيميائية:

    • Chemical Name: Methyl (3aR,4R,5S,5aR,10bR,13aR)-4-acetoxy-3a-ethyl-9-((5S,7R,9S)-5-ethyl-5-hydroxy-9-(methoxycarbonyl)-1,4,5,6,7,8,9,10-octahydro-2H-3,7-methanoazacycloundecino(5,4-b)indol-9-yl)-6-formyl-5-hydroxy-8-methoxy-3a,4,5,5a,6,11,12,13a-octahydro-1H-indolizino(8,1-cd)carbazole-5-carboxylate sulfate

    • Molecular Formula: C₄₆H₅₈N₄O₉ · H₂SO₄

    • Molecular Weight: 909.06 g/mol

    • مظهر: White to off-white hygroscopic crystalline powder

    • الذوبان: Freely soluble in water, methanol; insoluble in ether

    • Stability: Light-sensitive; oxidizes under alkaline conditions

  • Key Identifiers:

    • CAS: 143-67-9 (vinblastine sulfate)

    • EC Number (EINECS): 205-620-3

    • MF: C₄₆H₆₀N₄O₁₃S

    • MW: 909.06

3. Pharmaceutical-Grade Quality & Clinical Profile

  • Optimal Product: Requires >99.5% HPLC purity, <0.1% vincristine (toxic isomer), and undetectable endotoxins (<0.25 EU/mg). Shaanxi Zhonghong guarantees this via countercurrent chromatography و crystallization controls.

  • Therapeutic Applications:

    • Oncology: First-line for Hodgkin’s lymphoma (ABVD regimen), NSGCT, choriocarcinoma, Kaposi sarcoma.

    • الآلية: Binds tubulin → depolymerizes microtubules → blocks metaphase → apoptosis.

    • (Note: Nattokinase exhibits anticoagulant properties; no robust evidence supports kidney-specific benefits)

  • Dosage:

    • Medical Use Only: Administered IV (0.1-0.5 mg/kg weekly). No oral supplement form exists.

  • Critical Safety Profile:

    • Hematologic: Severe neutropenia (nadir Day 7-10), thrombocytopenia.

    • Neurotoxicity: Peripheral neuropathy (less severe than vincristine).

    • GI Effects: Nausea, constipation, ileus.

    • Extravasation Hazard: Causes tissue necrosis; requires central line administration.

    • موانع الاستعمال: Active infections, bone marrow suppression, pregnancy (FDA Category D).

4. Shaanxi Zhonghong: Pioneering Vinca Alkaloid Production
With 28+ years in plant-derived oncology APIs, we deliver cGMP vinblastine sulfate meeting USP/EP monographs. Core strengths:

  • Scientific Infrastructure:

    • 5 Academic Joint Labs (Isolation chemistry, analytical development)

    • Patented Extraction Tech (CN202310XXXXXX: high-yield vindoline purification)

  • Analytical Superiority:

    • HPLC-ELSD/MS (purity)

    • UPLC-PDA (isomeric impurity control)

    • Superconducting 600MHz NMR (structural confirmation)

    • LAL Endotoxin Testing (<0.25 EU/mg)

  • Global Supply: APIs shipped to 80+ countries under cold-chain protocols.

5. Rigorous Quality Specifications

فئة المعلمة مواصفة Method
المبيدات الحشرية ديكلوروفوس ≤0.01 mg/kg GC-MS/MS (EU 2021/601)
Malathion ≤0.05 mg/kg كروماتوغرافيا الغاز-مطياف الكتلة/مطياف الكتلة
المعادن الثقيلة Pb ≤1 ppm ICP-MS (USP <232>)
As ≤0.5 ppm ICP-MS
علم الأحياء الدقيقة TAMC ≤10² CFU/g جامعة ساو باولو <61>
Bile-tolerant GNR Absent/10g جامعة ساو باولو <62>
Critical Attributes Vinblastine Sulfate ≥99.5% HPLC-ELSD (USP <621>)
فينكريستين ≤0.1% UPLC-PDA
Water Content ≤5.0% Karl Fischer
Endotoxins <0.25 EU/mg LAL (USP <85>)

6. cGMP Manufacturing Process

  1. Biomass Cultivation: C. roseus grown under GACP-controlled conditions.

  2. Alkaloid Extraction: pH-modulated solvent extraction (EtOAc/H₂O).

  3. Chromatographic Separation: Flash chromatography → HPLC purification (vindoline/catharanthine).

  4. Dimerization: Fe³⁺-catalyzed coupling of vindoline and catharanthine.

  5. Sulfation: Reaction with sulfur trioxide complex.

  6. بلورة: Controlled anti-solvent addition for crystal polymorphism management.

  7. التجميد بالتجميد: Freeze-drying under argon atmosphere.

7. Clinical & Research Applications

  • Oncology: Core component of:

    • ABVD (Doxorubicin, Bleomycin, Vinblastine, Dacarbazine)

    • VEBEP (Vinblastine, Etoposide, Bleomycin, Cisplatin)

  • Drug Delivery Innovations:

    • Liposomal encapsulation (reduced neurotoxicity)

    • Antibody-drug conjugates (anti-CD30-VLA complexes)

  • Cell Biology: Tool compound for mitotic inhibition studies.

8. cGMP Quality Control Protocol
Our 360° QC strategy includes:

  • Identity: ¹H/¹³C NMR spectral match (δ 0.98 ppm, 3H, t; δ 3.70 ppm, 3H, s).

  • Purity: RP-HPLC-ELSD (Luna C18, 0.1% TFA/MeCN gradient) quantifies vinblastine (≥99.5%), vincristine (≤0.1%).

  • Potency: Cell-based mitotic arrest assay (HeLa cells, EC₅₀ ≤2 nM).

  • Safety: Bacterial endotoxins (LAL kinetic chromogenic), sterility (membrane filtration USP <71>), residual solvents (GC-HS).

  • Stability: 36-month shelf-life at 2-8°C (validated per ICH Q1A(R2)).

9. Cold-Chain Logistics

  • Primary Pack: Type I glass vials (nitrogen headspace) with fluoropolymer-coated stoppers.

  • Secondary Pack: Vacuum-sealed Alu-bags in UN-certified shippers with temperature loggers.

  • تخزين: 2-8°C protected from light; desiccant included.

  • Shipping: Global cold-chain transport (2-8°C) via DHL LifeConEx.

10. Mechanism & Innovation

  • Molecular Action: Binds β-tubulin vinca site → tubulin dissociation constant (Kd=6.8 μM) → suppressed GTP hydrolysis → microtubule fragmentation.

  • Zhonghong Innovations:

    • PAT-enabled crystallization (Patent CN202210XXXXXX)

    • Enzymatic dimerization (yield ↑40%)

  • Research Frontiers:

    • Oral formulations (P-glycoprotein inhibitors)

    • Tubulin isotype-selective analogs (βIII-tubulin targeting)

  • التحديات: Myelosuppression, neuropathy, chemoresistance (ABCB1 overexpression).

11. FAQ

Q1: Can vinblastine be used as a dietary supplement?
A: Absolutely not. Vinblastine is a cytotoxic chemotherapy agent requiring medical supervision. Self-administration is life-threatening.

Q2: How does nattokinase compare for kidney health?
A: Nattokinase lacks clinical evidence for nephroprotection. Vinblastine may cause nephrotoxicity at high doses. Neither compound is indicated for renal conditions.

Q3: Why is vincristine impurity control critical?
*A: Vincristine causes severe neurotoxicity at microgram doses. Our UPLC-PDA method detects ≤0.01% impurity.*

Q4: What distinguishes Zhonghong’s vinblastine?
*A: cGMP manufacturing, 99.5%+ HPLC purity, endotoxin control (<0.25 EU/mg), and patented crystallization technology ensuring polymorph stability.*

Q5: Do you supply vinblastine for ADC development?
A: Yes. GMP-grade linker-conjugated vinblastine (maleimide-PEG₃-vinblastine) available for antibody-drug conjugates.

12. Global Sourcing
Procure cGMP vinblastine sulfate:
✉️ بريد إلكتروني: liaodaohai@gmail.com
🌐 Web: www.aiherba.com
Request: COA, DMF, CEP, and custom synthesis quotations.

13. Conclusion
Vinblastine sulfate remains a cornerstone antineoplastic agent with irreplaceable clinical value. Its efficacy hinges on ultra-high purity (>99.5%), stringent impurity control (vincristine ≤0.1%)، و temperature-controlled handling. Shaanxi Zhonghong combines 28 years of vinca alkaloid expertise, patented purification technology، و cGMP compliance to deliver oncology APIs that meet global pharmacopeial standards. Partner with us for uncompromising quality in cancer therapeutics.

14. References

  1. Noble RL, et al. (1958). J Am Chem Soc. 80:3487. [DOI:10.1021/ja01546a092]

  2. Jordan MA, et al. (2002). Mol Cancer Ther. 1:935–943. [PMID:12481413]

  3. WHO Model List of Essential Medicines (2023). Vinblastine sulfate injection.

  4. USP Monograph: Vinblastine Sulfate. USP44-NF39.

  5. EMA Guideline: Specifications for cytotoxic APIs (CPMP/QWP/1850/04)

  6. Dumontet C, et al. (2020). Nat Rev Drug Discov. 19:585–608. [DOI:10.1038/s41573-020-0072-8]

  7. Zhonghong Patent: CN202310XXXXXX (Vinblastine crystallization control)

  8. ICH Q3D (R2): Elemental Impurities (2022)

  9. FDA Guidance: Vinblastine Label (NSC-49842)

  10. Gidding CEM, et al. (1999). Cancer Chemother Pharmacol. 44:266–272. [DOI:10.1007/s002800050976]

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