Artesunate and Artemisinin-based Drugs

Safety and precautions

At doses used to treat malaria, artemisia-derived drugs are generally safe and well tolerated, but no phase I clinical trials have tested the safety of higher doses that are likely required for treating cancer. Doses used in animal cancer studies have been much higher than those used to treat malaria.

Side effects

The maximum tolerable dose was set at 18 mg/kg due to dose-limiting toxicities observed in dose titration involving people with any type of solid tumor in a phase 1 study.¹Deeken JF, Wang H et al. A phase I study of intravenous artesunate in patients with advanced solid tumor malignancies. Cancer Chemotherapy and Pharmacology. 2018 Mar;81(3):587-596.

Use is generally associated with mild side effects

• Long-term use (up to 37 months) of oral artesunate among metastatic breast cancer patients did not result in any major safety concerns.²von Hagens C, Walter-Sack I et al. Long-term add-on therapy (compassionate use) with oral artesunate in patients with metastatic breast cancer after participating in a phase I study (ARTIC M33/2). Phytomedicine. 2018 Sep 17;54:140-148.
• Multiple grade 1 or 2 adverse events, but no severe adverse events and no patients dropped out of the study or stopped treatment due to adverse events, among people with cervical intraepithelial neoplasia treated with artesunate intravaginally in an uncontrolled studya study in which a therapy is used, but without a comparison group against which to judge outcomes; an uncontrolled trial is considered a weak study design.³Trimble CL, Levinson K et al. A first-in-human proof-of-concept trial of intravaginal artesunate to treat cervical intraepithelial neoplasia 2/3 (CIN2/3). Gynecologic Oncology. 2020 Apr;157(1):188-194. 

In their book, Parmar and Kazcor state that use may cause dose-dependent low white counts.⁴Parmar G, Kaczor T. Textbook of Naturopathic Oncology: A Desktop Guide of Integrative Cancer Care. 1st edition. Medicatrix Holdings Ltd. 2020.

Interactions with other therapies

Liver toxicity has been reported among people using artemisinin-based drugs when combined with oxidative chemotherapies or radiation.⁵Efferth T. Cancer combination therapies with artemisinin-type drugs. Biochemical Pharmacology. 2017 Sep 1;139:56-70.

Artemisinin-based therapies have shown pharmacokinetic and pharmacodynamic drug interactions with HIV antiviral treatment and treatment failure in some studies with cardiovascular, antibiotic, and antiparasitic drugs.⁶Hernandez Maldonado J, Grundmann O. Drug-drug interactions of artemisinin-based combination therapies in malaria treatment: a narrative review of the literature. Journal of Clinical Pharmacology. 2022 Oct;62(10):1197-1205.

Do not use (contraindications)

Artemisinin during pregnancy may cause harm to the fetus.⁷Alschuler LN, Gazella KA. The Definitive Guide to Cancer, 3rd Edition: An Integrative Approach to Prevention, Treatment, and Healing. Berkeley, California: Celestial Arts. 2010. p. 162.

Consult your pharmacist for interactions, and discuss using artemisinin-based drugs with your doctor. We suggest that patients who use artemisinin derivatives for cancer seek guidance for usage, dose, and formulation from an integrative cancer care clinician or traditional Chinese medicine practitioner with experience working with people with cancer.

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