Skip to main content

Table 1 Characteristics of artemisinin and its derivatives

From: Anti-malarial drug: the emerging role of artemisinin and its derivatives in liver disease treatment

Derivatives Molecular formulas Chemical structures Structural modifications Physical properties Formulations Route of administration Pharmacokinetics Pharmacological activities Ref
Artemisinin C15H22O5 - Poorly soluble in water and oil;
Melting point 156–157℃;
Molecular weight 282.35
Powder;
Micronized powder;
Tablet;
Capsule;
Suppository
Oral
Intramuscular injection
Rectal
Tmax 1–3 h
Volume of distribution 1420–1560L
Clearance 445–479L/h
T1/2 2.27–2.29 h
Tmax 3.4 h
Tmax 5.6 h
Antimalaria; Antivirus;
Antihelminth;
Anticancer;
Antiinflammation;
[24,25,26, 31, 32]
DHA C15H24O5 Modifying carbonyl groups into
hydroxyl groups;
The active metabolite of all artemisinins
Molecular weight 284.4 Powder;
Tablet;
Oral
Intramuscular injection
Rectal
Tmax 0.9–1.6 h

Tmax 4 h
Antimalaria;
Anticancer;
[24, 26, 28, 29, 32]
ART C19H28O8 Hemisuccinate derivative of DHA Water-soluble;
Molecular weight
384.4
Powder
Suppository
Tablet
Injection
Oral
Intramuscular injection
Rectal
Intravenous administration
Bioavailability 61%-88%
Tmax 15–39 min
Volume of distribution 14.8L/kg
Clearance 20.6L/kg/hr
T1/2 0.36–1.2 h
Bioavailability 86.4–88%
Tmax 7.2–12 min
T1/2 25.2–48.2 h
Clearance 2.4–3.48L/kg/hr
Volume of distribution 1.09–3.98L/kg
Bioavailability 54.9%
Tmax 0.58–1.43 h
T1/2 0.9–0.95 h
Clearance 2–3L/kg/hr
Volume of distribution 0.1–0.3L/kg
Antimalaria;
Antiparasite;
Antitumor;
Antivirus;
Antiinflammation;
Antibacterial
[24, 27, 30,31,32]
ARM C16H26O5 Production methyl ether from DHA Oil-soluble;
Molecular weight
298.4
Powder
Injection
Capsule
Oral
Intramuscular injection
Rectal
Tmax 1.7–6 h
Tmax 1.3–8.7 h
Tmax 3.1 h
Antimalaria [24, 31, 32]
ARE C17H28O5 Production β-ethyl ether from DHA Oil-soluble;
Practically insoluble in water;
Molecular weight
312.4
Powder
Injection
Oral
Intramuscular injection
Rectal

Tmax 4.8–7 h
Antimalaria [24, 31, 32]
  1. Tmax Time to maximal concentration, T1/2 Elimination half-life