The Power of Artemisinin and High-Dose IV Vitamin C in Integrative Cancer Care

🌱 Harnessing the Power of Artesunate and High-Dose IV Vitamin C

What is Artemisinin?

Artemisinin, the active molecule derived from the traditional Chinese herb Artemisia annua (sweet wormwood), has been a cornerstone in the treatment of severe malaria for decades, recognized for its safety and efficacy worldwide [1]. Beyond its antimalarial properties, extensive research in oncology has highlighted artemisinin and its semi-synthetic derivatives, such as artesunate (ART) and dihydroartemisinin (DHA), for their promising anticancer capabilities [2, 3, 4].

It is important to note that while promising, these approaches are often considered complementary and should be discussed with a qualified healthcare professional.

Mechanisms of Action in Cancer Cells:

The primary mechanism by which artemisinins exert their cytotoxic effects on cancer cells is through their interaction with intracellular iron. Cancer cells often exhibit a higher uptake of iron, facilitated by an overexpression of transferrin receptors, compared to healthy cells [5]. This elevated iron concentration creates a unique vulnerability that artemisinins exploit:

1- Oxidative Stress Induction: Artemisinin and its derivatives react with intracellular iron within cancer cells, leading to the generation of highly reactive oxygen species (ROS) through a Fenton-like reaction [2, 6]. This surge in ROS overwhelms the cancer cell's antioxidant defenses, inducing significant oxidative stress. This oxidative damage can trigger various forms of cell death, including apoptosis (programmed cell death) and ferroptosis (an iron-dependent form of regulated cell death) [7, 8].

2- Disruption of Cancer Cell Growth and Angiogenesis: Artemisinins have been shown to interfere with multiple critical cellular pathways involved in cancer progression. They can inhibit cancer cell proliferation, induce cell cycle arrest and suppress angiogenesis—the formation of new blood vessels that tumors need to grow and metastasize [3, 9].

3- Sensitization to Conventional Therapies: Preclinical and some clinical studies suggest that artemisinins can enhance the sensitivity of cancer cells to conventional treatments like chemotherapy and radiation therapy. This chemosensitizing and radiosensitizing effect is thought to occur through various mechanisms, including the modulation of signalling pathways and the disturbance of mitochondrial metabolism [2, 3, 10].

Artemisinin has been used in Traditional Chinese Medicine as an antimalarial agent for over 2000 years. Today, Artemisia annua and artemisinin extracts are available as natural health products. Pharmaceutical-grade artemisinin and its semi-synthetic derivatives, including Artesunate and Dihydroartemisinin, are also available and are the focus of much of the current cancer research [11].

Combining Artemisinin with IV Vitamin C

Both artemisinin and high-dose intravenous vitamin C (HDIVC) leverage the metabolic vulnerabilities of cancer cells, particularly their altered iron metabolism and increased oxidative stress. This synergistic approach, often termed “redox-based” cancer therapy, aims to selectively induce cell death in malignant cells while sparing healthy tissues [12, 13].

Synergistic Mechanisms:

Cancer cells typically exhibit higher iron content and a dysregulated redox balance compared to normal cells. This makes them particularly susceptible to agents that generate reactive oxygen species (ROS). When artemisinin, which requires iron for activation, is combined with HDIVC, the pro-oxidant effects are amplified:

1- Enhanced Oxidative Damage: HDIVC, when administered intravenously at pharmacological concentrations, acts as a pro-oxidant, generating hydrogen peroxide (H2O2) in the extracellular fluid and within cancer cells. This H2O2 can then react with the abundant intracellular iron in cancer cells, leading to the formation of highly destructive hydroxyl radicals via the Fenton reaction [14, 15]. The simultaneous action of artemisinin, also generating ROS in an iron-dependent manner, creates a powerful oxidative assault that can overwhelm the cancer cell's defenses and trigger apoptosis or ferroptosis [7, 16].

2- Metabolic Disruption: Both agents can disrupt key metabolic pathways in cancer cells. HDIVC can interfere with glycolysis and mitochondrial function, while artemisinin targets various signaling pathways crucial for cancer cell survival and proliferation [3, 15]. The combined effect can lead to a more profound metabolic collapse in cancer cells.

3- Potential for Improved Outcomes: Preclinical studies have consistently suggested that combining artemisinin derivatives with HDIVC can significantly increase cancer cell susceptibility to oxidative damage and enhance the efficacy of standard therapies [12, 17]. While large-scale clinical trials specifically on the combination are still emerging, individual studies on each agent show promise in improving patient quality of life and potentially overall survival in certain cancer types [18, 19].

At Leicester Ozone Clinic, we offer artemisinin infusions as part of supportive therapy for patients undergoing cancer treatment. Our protocol involves administering artemisinin extract intravenously immediately prior to IV vitamin C, aiming to potentiate the action of vitamin C by compromising cancer cells through enhanced oxidative stress [20].

Administration Protocol

While specific protocols can vary between clinics and are often tailored to individual patient needs and cancer types, general guidelines and considerations have emerged from research.

1- Artemisinin Administration:

For intravenous administration of artemisinin derivatives, such as artesunate, doses typically range from 1-4 mg/kg, often administered as a fast intravenous infusion [20]. The maximum tolerable dose for artesunate has been reported up to 18 mg/kg, beyond which dose-limiting toxicities may occur [23].

2- High-Dose IV Vitamin C Administration:

Studies have shown that pharmacological concentrations of ascorbate (vitamin C) can safely reach 25-30 mM with intravenous infusions of up to 100 grams [25]. HDIVC is generally considered safe and well-tolerated in cancer patients, either as a monotherapy or in combination with chemotherapy, provided there are no contraindications such as glucose-6-phosphate dehydrogenase (G6PD) deficiency or renal impairment [26, 27].

Combined Administration Protocol (Sequential Infusion):

This protocol is unique to Leicester Ozone Clinic and has been employed with good results. The concept of administering artemisinin immediately prior to high-dose IV vitamin C is based on the mechanistic understanding of their synergistic actions. The rationale is that artemisinin, by reacting with intracellular iron and initiating oxidative stress, can "prime" cancer cells, making them more vulnerable to the subsequent pro-oxidant effects of HDIVC [20]. A typical sequential protocol might involve:

1.Artemisinin Infusion: A fast intravenous infusion of artemisinin (e.g., 2.4 mg/kg within a 1-4 mg/kg range) is administered first.

2.Immediate IV Vitamin C Infusion: This is followed immediately by the administration of high-dose IV vitamin C. The timing is crucial to leverage the transient increase in oxidative vulnerability induced by artemisinin.

Frequency and Duration:

The frequency of these combined infusions can vary, often administered 1-2 times per week for several weeks, followed by a period of rest, depending on the patient's response and overall treatment plan [20].

Safety Considerations and Monitoring:

While both agents have demonstrated favourable safety profiles individually, especially when administered intravenously under medical supervision, careful monitoring is essential. Potential side effects for artemisinin are generally mild and may include gastrointestinal discomfort or dizziness [28]. For HDIVC, side effects are rare but can include nausea, fatigue, or, in individuals with G6PD deficiency, hemolytic anemia [29]. Therefore, comprehensive patient evaluation, including G6PD screening and renal function tests, is mandatory before initiating such therapies. Regular monitoring of patient tolerance and response is also crucial throughout the treatment course.

It is important to emphasise that while preclinical data and some clinical observations are encouraging, large-scale, randomised controlled trials specifically evaluating the efficacy and optimal dosing of combined IV artemisinin and high-dose IV vitamin C in various cancer types are still needed to establish definitive clinical guidelines. These therapies are often utilized within an integrative oncology framework as supportive measures to enhance overall wellness and complement conventional treatments, rather than as standalone cures.

Also, check our Integrative Supportive Therapies by clicking the button below 

Integrative Oncology Therapies

References

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[15] Frederick National Laboratory for Cancer Research. (2020, January 24). Intravenous High-Dose Vitamin C in Cancer Therapy. https://frederick.cancer.gov/node/7313

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[17] Moya, R., et al. (2018). P-332 - Intravenous antioxidants, laetrile and artesunate as adjuvant therapy in advanced cancer patients. European Journal of Cancer, 103, S109. https://www.sciencedirect.com/science/article/abs/pii/S0891584918306440

[18] University of Iowa Health Care. (2024, November 11). High-dose IV vitamin C plus chemotherapy doubles survival in advanced pancreatic cancer. https://medicine.uiowa.edu/news/2024/11/high-dose-iv-vitamin-c-plus-chemotherapy-doubles-survival-advanced-pancreatic-cancer

[19] Zasowska-Nowak, A., et al. (2021). High-Dose Vitamin C in Advanced-Stage Cancer Patients. Nutrients, 13(3), 799. https://pmc.ncbi.nlm.nih.gov/articles/PMC7996511/

[20] Leicester Ozone Clinic. (n.d.). Artemisinin Infusions. (Original document provided by user)

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