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Artemisinin
Natural API
Artemisinin.jpg
Artemisia annua.jpg

Artemisinin

Artemisinin (CAS: 63968-64-9) is a sesquiterpene lactone compound extracted from the Asteraceae plant Artemisia annua. As a revolutionary antimalarial drug, its unique peroxide bridge structure confers potent antimalarial activity, saving millions of lives. Chinese scientist Tu Youyou was awarded the 2015 Nobel Prize in Physiology or Medicine for its discovery. WHO lists it as a first-line treatment for Plasmodium falciparum malaria and includes it in the Essential Medicines List..

Product Name: Artemisinin

IUPAC Name: (3R,5aS,6R,8aS,9R,12S,12aR)-Octahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin-10(3H)-one

CAS No.​: 63968-64-9

Molecular Formula: C₁₅H₂₂O₅

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    Artemisinin

    Basic information

    Product Name: Artemisinin

    IUPAC Name: (3R,5aS,6R,8aS,9R,12S,12aR)-Octahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin-10(3H)-one

    CAS No.​: 63968-64-9

    Molecular Formula: C₁₅H₂₂O₅

    Physicochemical Properties:

    Parameter

    Value/Description

    ​Appearance​

    Colorless needle crystals

    ​Melting Point​

    156-158°C

    ​Solubility​

    Water solubility 0.05 mg/mL, soluble in chloroform/acetone (50 mg/mL)

    ​logP​

    2.8 (moderate lipophilicity)

    ​Optical Rotation​

    [α]²⁵D = +66° (c=1, chloroform)

    Quality Standard: CP2020,JP,Customer Made

    Specification

    Test Items

    Standard

    Artemisinin (CAS: 63968-64-9)

    98% by HPLC

    Loss on drying

    ≤0.5%

    Total impurities

    ≤1%

    Key Features

    index_10-7

    Natural Source

     Artemisia annua leaves (content 0.1-1.2%, up to 2% in optimized strains).
    index_10-7

    Structural Uniqueness

    Contains a 1,2,4-trioxane (peroxide bridge), essential for activity.
    index_10-7

    Clinical Impact

    Effective against chloroquine-resistant malaria, with onset speed 3× faster than traditional drugs.

    Pharmacological Mechanisms

    1.Molecular Mechanism

    Molecular Mechanism

    2.Pharmacokinetics

    Absorption

    Oral bioavailability 30% (↑to 60% with fatty meals).

    Distribution

    100× higher in RBCs vs. plasma; 5% CSF penetration.

    Metabolism

    Hepatic CYP3A4/2B6 hydroxylation (forms dihydroartemisinin).

    Excretion

    Primarily biliary (t₁/₂=1-2h)

    Clinical Applications​

    Indications & Protocols​

    Condition​

    ​Regimen​

    ​Efficacy​

    ​Falciparum Malaria​

    Artesunate + Amodiaquine

    95% cure rate*

    ​Cancer Adjuvant​

    Artemisinin + Cisplatin (Phase II)

    ↑3mo PFS in HCC

    ​Lupus Erythematosus​

    Low-dose long-term oral

    ↓40% disease activity

    *WHO multicenter study (n=10,000)

    Special Populations​

    Pregnancy: Safe in 2nd/3rd trimesters (limited 1st-trimester data).

    Pediatrics: Weight-based dosing (≥5kg).

    Dosage and Administration

    Formulations​

    Oral: 50 mg tablets (artemether-lumefantrine).

    Injection: 60 mg artesunate powder (reconstituted).

    Suppository: 40 mg (pediatric emergency).

    Dosing Guidelines​

    Use​

    ​Dose​

    ​Duration​

    Malaria Treatment

    4 mg/kg load, then 2 mg/kg qd×3d

    7d combo therapy

    Cancer Trials

    200 mg/day

    4 weeks

    Safety Evaluation

    Adverse Reactions​

    ​System​

    ​Incidence​

    ​Manifestations​

    Hematologic

    0.1%

    Reticulocytopenia

    Neurologic

    1%

    Mild dizziness

    Hypersensitivity

    Rare

    Rash

     Contraindications & Interactions​

    Absolute CI:
    Artemisinin allergy.
    Severe liver failure (Child-Pugh C).

    Cautions:Strong CYP3A4 inducers (e.g., rifampin): ↓80% AUC.

    Research Progress Green max

    Novel Formulations​

    Nanoliposomes: Tumor-targeted delivery (preclinical).

    Sustained-release Microspheres: Single injection for 3-month malaria prophylaxis.

    New Indications​

    COVID-19: Inhibits viral replication (IC₅₀=2.5 μM).

    Alzheimer’s: Reduces Tau phosphorylation (animal models).

    Artemisia annua

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