Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H28O8 |
Molecular Weight | 384.4208 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC[C@@H](C)[C@]3([H])CC[C@@]4(C)OO[C@@]13[C@]([H])(O[C@@H](OC(=O)CCC(O)=O)[C@@H]2C)O4
InChI
InChIKey=FIHJKUPKCHIPAT-AHIGJZGOSA-N
InChI=1S/C19H28O8/c1-10-4-5-13-11(2)16(23-15(22)7-6-14(20)21)24-17-19(13)12(10)8-9-18(3,25-17)26-27-19/h10-13,16-17H,4-9H2,1-3H3,(H,20,21)/t10-,11-,12+,13+,16-,17-,18-,19-/m1/s1
Molecular Formula | C19H28O8 |
Molecular Weight | 384.4208 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.cdc.gov/malaria/diagnosis_treatment/artesunate.htmlhttp://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/001199/WC500118113.pdfhttps://www.ncbi.nlm.nih.gov/pubmed/11231359 | https://www.ncbi.nlm.nih.gov/pubmed/9241384 | https://www.ncbi.nlm.nih.gov/pubmed/1966574Curator's Comment: Description was created based on several sources, including
http://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/human/medicines/001199/human_med_001450.jsp&mid=WC0b01ac058001d124 | https://www.hpra.ie/docs/default-source/3rd-party-documents/educational-materials/eurartesim_hcp-guide.pdf?sfvrsn=4 | https://www.ncbi.nlm.nih.gov/pubmed/20649950
Sources: https://www.cdc.gov/malaria/diagnosis_treatment/artesunate.htmlhttp://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/001199/WC500118113.pdfhttps://www.ncbi.nlm.nih.gov/pubmed/11231359 | https://www.ncbi.nlm.nih.gov/pubmed/9241384 | https://www.ncbi.nlm.nih.gov/pubmed/1966574
Curator's Comment: Description was created based on several sources, including
http://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/human/medicines/001199/human_med_001450.jsp&mid=WC0b01ac058001d124 | https://www.hpra.ie/docs/default-source/3rd-party-documents/educational-materials/eurartesim_hcp-guide.pdf?sfvrsn=4 | https://www.ncbi.nlm.nih.gov/pubmed/20649950
Sodium artesunate, an artemisinin derivative, is used in malaria treatment. Artesunate, has been licensed in Thailand for the
treatment of falciparum malaria since 1990. It is a potent antimalarial drug that can reduce parasitaemia by 90% within 24 h of administration. Sodium artesunate was first isolated in China, it is a water soluble antimalaria used clinically in China.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC148951/https://www.ncbi.nlm.nih.gov/pubmed/12499215
Curator's Comment: Active metabolite of artesunate was detected in CSF after intravenous administration of artesunate.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/8891104http://adisinsight.springer.com/drugs/800023198Journal of traditional Chinese medicine = Chung i tsa chih ying wen pan (1982), 2, (2), 99-103.
Curator's Comment: Indicated originators are originators of Dihydroartemisinin/piperaquine formulation. Originator of Dihydroartemisinin is unknown.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL613064 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11802960 |
|||
Target ID: P06685 Gene ID: 24211.0 Gene Symbol: Atp1a1 Target Organism: Rattus norvegicus (Rat) |
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Target ID: CHEMBL364 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1394893 |
4.1 nM [IC50] | ||
Target ID: CHEMBL612889 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1307277 |
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Target ID: CHEMBL612653 Sources: https://www.ncbi.nlm.nih.gov/pubmed/3009719 |
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Target ID: CHEMBL364 |
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Target ID: CHEMBL2311221 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25348537 |
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Target ID: CHEMBL2366043 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25348537 |
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Target ID: CHEMBL364 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8891104 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Sodium artesunate Approved UsePlasmodium falciparum malaria |
|||
Curative | Eurartesim Approved UseEurartesim tablets (piperaquine tetraphosphate in combination with dihydroartemisinin) are indicated for the treatment of uncomplicated Plasmodium falciparum malaria in adults, children and infants aged ≥6 months and weighing ≥5kg. Launch Date2011 |
|||
Curative | Unknown Approved UseAlthough not FDA-approved for use in the United States, artesunate is used as the treatment of choice for severe malaria by the World Health Organization (WHO) over quinidine. |
|||
Curative | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.1 μg/mL |
2.4 mg/kg multiple, intravenous dose: 2.4 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
ARTENIMOL unknown | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
3.3 μg/mL |
2.4 mg/kg multiple, intravenous dose: 2.4 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
ARTESUNATE unknown | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.5 μg × h/mL |
2.4 mg/kg multiple, intravenous dose: 2.4 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
ARTENIMOL unknown | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
0.7 μg × h/mL |
2.4 mg/kg multiple, intravenous dose: 2.4 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
ARTESUNATE unknown | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.3 h |
2.4 mg/kg multiple, intravenous dose: 2.4 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
ARTENIMOL unknown | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
0.3 h |
2.4 mg/kg multiple, intravenous dose: 2.4 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
ARTESUNATE unknown | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
7% |
2.4 mg/kg multiple, intravenous dose: 2.4 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
ARTENIMOL unknown | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
7% |
2.4 mg/kg multiple, intravenous dose: 2.4 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
ARTESUNATE unknown | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
2.4 mg/kg 1 times / day multiple, intravenous (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 1-72 years n = 92 Health Status: unhealthy Condition: malaria Age Group: 1-72 years Sex: M+F Population Size: 92 Sources: |
Other AEs: Anemia, Transaminases increased... Other AEs: Anemia (65%) Sources: Transaminases increased (27%) Thrombocytopenia (18%) Hyperbilirubinemia (14%) Acute renal failure (10%) Leukocytosis (10%) Acute respiratory distress syndrome (8%) Lymphopenia (7%) Neutropenia (5%) Disseminated intravascular coagulation (3%) Creatinine increased (3%) Pneumonia (3%) Pulmonary edema (3%) Diarrhea (3%) |
100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, 15-35 years n = 31 Health Status: unhealthy Condition: Uncomplicated Malaria Age Group: 15-35 years Sex: M Population Size: 31 Sources: |
Other AEs: Nausea, Dizziness... Other AEs: Nausea (grade 1, 45%) Sources: Dizziness (grade 1, 52%) Vomiting (grade 1, 26%) Convulsions (grade 1, 3%) Bradycardia (grade 1, 23%) |
2.4 mg/kg 1 times / day multiple, intravenous|oral (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous|oral Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 2-87 years n = 730 Health Status: unhealthy Condition: malaria Age Group: 2-87 years Sex: M+F Population Size: 730 Sources: |
Other AEs: Acute renal failure, Hemoglobinuria... Other AEs: Acute renal failure (8.9%) Sources: Hemoglobinuria (6.7%) Jaundice (2.3%) |
25 mg/kg 2 times / 3 weeks multiple, intravenous Highest studied dose Dose: 25 mg/kg, 2 times / 3 weeks Route: intravenous Route: multiple Dose: 25 mg/kg, 2 times / 3 weeks Sources: |
unhealthy, 58 years n = 2 Health Status: unhealthy Condition: advanced solid tumor malignancies Age Group: 58 years Sex: M+F Population Size: 2 Sources: |
DLT: Nausea, Vomiting... Dose limiting toxicities: Nausea (grade 3, 1 patient) Sources: Vomiting (grade 3, 1 patient) ALT increased (grade 3-4, 1 patient) Neutropenic infection (grade 3-4, 1 patient) |
18 mg/kg 2 times / 3 weeks multiple, intravenous MTD Dose: 18 mg/kg, 2 times / 3 weeks Route: intravenous Route: multiple Dose: 18 mg/kg, 2 times / 3 weeks Sources: |
unhealthy, 58 years n = 6 Health Status: unhealthy Condition: advanced solid tumor malignancies Age Group: 58 years Sex: M+F Population Size: 6 Sources: |
DLT: Hypersensitivity reaction... Dose limiting toxicities: Hypersensitivity reaction (grade 3, 1 patient) Sources: |
12 mg/kg 2 times / 3 weeks multiple, intravenous Studied dose Dose: 12 mg/kg, 2 times / 3 weeks Route: intravenous Route: multiple Dose: 12 mg/kg, 2 times / 3 weeks Sources: |
unhealthy, 58 years n = 6 Health Status: unhealthy Condition: advanced solid tumor malignancies Age Group: 58 years Sex: M+F Population Size: 6 Sources: |
DLT: Neutropenic fever... Dose limiting toxicities: Neutropenic fever (grade 3, 1 patient) Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Acute renal failure | 10% | 2.4 mg/kg 1 times / day multiple, intravenous (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 1-72 years n = 92 Health Status: unhealthy Condition: malaria Age Group: 1-72 years Sex: M+F Population Size: 92 Sources: |
Leukocytosis | 10% | 2.4 mg/kg 1 times / day multiple, intravenous (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 1-72 years n = 92 Health Status: unhealthy Condition: malaria Age Group: 1-72 years Sex: M+F Population Size: 92 Sources: |
Hyperbilirubinemia | 14% | 2.4 mg/kg 1 times / day multiple, intravenous (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 1-72 years n = 92 Health Status: unhealthy Condition: malaria Age Group: 1-72 years Sex: M+F Population Size: 92 Sources: |
Thrombocytopenia | 18% | 2.4 mg/kg 1 times / day multiple, intravenous (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 1-72 years n = 92 Health Status: unhealthy Condition: malaria Age Group: 1-72 years Sex: M+F Population Size: 92 Sources: |
Transaminases increased | 27% | 2.4 mg/kg 1 times / day multiple, intravenous (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 1-72 years n = 92 Health Status: unhealthy Condition: malaria Age Group: 1-72 years Sex: M+F Population Size: 92 Sources: |
Creatinine increased | 3% | 2.4 mg/kg 1 times / day multiple, intravenous (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 1-72 years n = 92 Health Status: unhealthy Condition: malaria Age Group: 1-72 years Sex: M+F Population Size: 92 Sources: |
Diarrhea | 3% | 2.4 mg/kg 1 times / day multiple, intravenous (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 1-72 years n = 92 Health Status: unhealthy Condition: malaria Age Group: 1-72 years Sex: M+F Population Size: 92 Sources: |
Disseminated intravascular coagulation | 3% | 2.4 mg/kg 1 times / day multiple, intravenous (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 1-72 years n = 92 Health Status: unhealthy Condition: malaria Age Group: 1-72 years Sex: M+F Population Size: 92 Sources: |
Pneumonia | 3% | 2.4 mg/kg 1 times / day multiple, intravenous (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 1-72 years n = 92 Health Status: unhealthy Condition: malaria Age Group: 1-72 years Sex: M+F Population Size: 92 Sources: |
Pulmonary edema | 3% | 2.4 mg/kg 1 times / day multiple, intravenous (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 1-72 years n = 92 Health Status: unhealthy Condition: malaria Age Group: 1-72 years Sex: M+F Population Size: 92 Sources: |
Neutropenia | 5% | 2.4 mg/kg 1 times / day multiple, intravenous (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 1-72 years n = 92 Health Status: unhealthy Condition: malaria Age Group: 1-72 years Sex: M+F Population Size: 92 Sources: |
Anemia | 65% | 2.4 mg/kg 1 times / day multiple, intravenous (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 1-72 years n = 92 Health Status: unhealthy Condition: malaria Age Group: 1-72 years Sex: M+F Population Size: 92 Sources: |
Lymphopenia | 7% | 2.4 mg/kg 1 times / day multiple, intravenous (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 1-72 years n = 92 Health Status: unhealthy Condition: malaria Age Group: 1-72 years Sex: M+F Population Size: 92 Sources: |
Acute respiratory distress syndrome | 8% | 2.4 mg/kg 1 times / day multiple, intravenous (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 1-72 years n = 92 Health Status: unhealthy Condition: malaria Age Group: 1-72 years Sex: M+F Population Size: 92 Sources: |
Bradycardia | grade 1, 23% | 100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, 15-35 years n = 31 Health Status: unhealthy Condition: Uncomplicated Malaria Age Group: 15-35 years Sex: M Population Size: 31 Sources: |
Vomiting | grade 1, 26% | 100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, 15-35 years n = 31 Health Status: unhealthy Condition: Uncomplicated Malaria Age Group: 15-35 years Sex: M Population Size: 31 Sources: |
Convulsions | grade 1, 3% | 100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, 15-35 years n = 31 Health Status: unhealthy Condition: Uncomplicated Malaria Age Group: 15-35 years Sex: M Population Size: 31 Sources: |
Nausea | grade 1, 45% | 100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, 15-35 years n = 31 Health Status: unhealthy Condition: Uncomplicated Malaria Age Group: 15-35 years Sex: M Population Size: 31 Sources: |
Dizziness | grade 1, 52% | 100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy, 15-35 years n = 31 Health Status: unhealthy Condition: Uncomplicated Malaria Age Group: 15-35 years Sex: M Population Size: 31 Sources: |
Jaundice | 2.3% | 2.4 mg/kg 1 times / day multiple, intravenous|oral (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous|oral Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 2-87 years n = 730 Health Status: unhealthy Condition: malaria Age Group: 2-87 years Sex: M+F Population Size: 730 Sources: |
Hemoglobinuria | 6.7% | 2.4 mg/kg 1 times / day multiple, intravenous|oral (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous|oral Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 2-87 years n = 730 Health Status: unhealthy Condition: malaria Age Group: 2-87 years Sex: M+F Population Size: 730 Sources: |
Acute renal failure | 8.9% | 2.4 mg/kg 1 times / day multiple, intravenous|oral (complex) Recommended Dose: 2.4 mg/kg, 1 times / day Route: intravenous|oral Route: multiple Dose: 2.4 mg/kg, 1 times / day Sources: |
unhealthy, 2-87 years n = 730 Health Status: unhealthy Condition: malaria Age Group: 2-87 years Sex: M+F Population Size: 730 Sources: |
Nausea | grade 3, 1 patient DLT |
25 mg/kg 2 times / 3 weeks multiple, intravenous Highest studied dose Dose: 25 mg/kg, 2 times / 3 weeks Route: intravenous Route: multiple Dose: 25 mg/kg, 2 times / 3 weeks Sources: |
unhealthy, 58 years n = 2 Health Status: unhealthy Condition: advanced solid tumor malignancies Age Group: 58 years Sex: M+F Population Size: 2 Sources: |
Vomiting | grade 3, 1 patient DLT |
25 mg/kg 2 times / 3 weeks multiple, intravenous Highest studied dose Dose: 25 mg/kg, 2 times / 3 weeks Route: intravenous Route: multiple Dose: 25 mg/kg, 2 times / 3 weeks Sources: |
unhealthy, 58 years n = 2 Health Status: unhealthy Condition: advanced solid tumor malignancies Age Group: 58 years Sex: M+F Population Size: 2 Sources: |
ALT increased | grade 3-4, 1 patient DLT |
25 mg/kg 2 times / 3 weeks multiple, intravenous Highest studied dose Dose: 25 mg/kg, 2 times / 3 weeks Route: intravenous Route: multiple Dose: 25 mg/kg, 2 times / 3 weeks Sources: |
unhealthy, 58 years n = 2 Health Status: unhealthy Condition: advanced solid tumor malignancies Age Group: 58 years Sex: M+F Population Size: 2 Sources: |
Neutropenic infection | grade 3-4, 1 patient DLT |
25 mg/kg 2 times / 3 weeks multiple, intravenous Highest studied dose Dose: 25 mg/kg, 2 times / 3 weeks Route: intravenous Route: multiple Dose: 25 mg/kg, 2 times / 3 weeks Sources: |
unhealthy, 58 years n = 2 Health Status: unhealthy Condition: advanced solid tumor malignancies Age Group: 58 years Sex: M+F Population Size: 2 Sources: |
Hypersensitivity reaction | grade 3, 1 patient DLT |
18 mg/kg 2 times / 3 weeks multiple, intravenous MTD Dose: 18 mg/kg, 2 times / 3 weeks Route: intravenous Route: multiple Dose: 18 mg/kg, 2 times / 3 weeks Sources: |
unhealthy, 58 years n = 6 Health Status: unhealthy Condition: advanced solid tumor malignancies Age Group: 58 years Sex: M+F Population Size: 6 Sources: |
Neutropenic fever | grade 3, 1 patient DLT |
12 mg/kg 2 times / 3 weeks multiple, intravenous Studied dose Dose: 12 mg/kg, 2 times / 3 weeks Route: intravenous Route: multiple Dose: 12 mg/kg, 2 times / 3 weeks Sources: |
unhealthy, 58 years n = 6 Health Status: unhealthy Condition: advanced solid tumor malignancies Age Group: 58 years Sex: M+F Population Size: 6 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no [IC50 >100 uM] | ||||
no [IC50 >100 uM] | ||||
no [IC50 >100 uM] | ||||
no [IC50 >100 uM] | ||||
no [IC50 >100 uM] | ||||
no [IC50 >100 uM] | ||||
no [IC50 >100 uM] | ||||
no [IC50 >100 uM] | ||||
no [IC50 >100 uM] | ||||
no [IC50 >100 uM] | ||||
weak [IC50 32.3 uM] | ||||
weak [IC50 75.4 uM] | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213036Orig1s000MultidisciplineR.pdf#page=258 Page: 258.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213036Orig1s000MultidisciplineR.pdf#page=258 Page: 258.0 |
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
yes | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
[Effects of sodium artesunate on electrical properties and Na+,K(+)-ATPase activities of mouse small intestine]. | 1990 Jul |
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Monotherapy with sodium artesunate for uncomplicated falciparum malaria in Thailand: a comparison of 5- and 7-day regimens. | 1997 Sep 30 |
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Effects of sodium artesunate, a new antimalarial drug, on renal function. | 2001 Mar |
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Penetration of dihydroartemisinin into cerebrospinal fluid after administration of intravenous artesunate in severe falciparum malaria. | 2003 Jan |
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Adding artesunate to sulphadoxine-pyrimethamine greatly improves the treatment efficacy in children with uncomplicated falciparum malaria on the coast of Benin, West Africa. | 2007 Dec 21 |
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Artesunate-mefloquine combination therapy in acute Plasmodium falciparum malaria in young children: a field study regarding neurological and neuropsychiatric safety. | 2010 Oct 21 |
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Artesunate induces apoptosis through caspase-dependent and -independent mitochondrial pathways in human myelodysplastic syndrome SKM-1 cells. | 2014 Aug 5 |
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Delayed anemia after treatment with injectable artesunate in the Democratic Republic of the Congo: a manageable issue. | 2014 Oct |
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Utilization of human nuclear receptors as an early counter screen for off-target activity: a case study with a compendium of 615 known drugs. | 2015 Jun |
|
Untargeted Proteomics and Systems-Based Mechanistic Investigation of Artesunate in Human Bronchial Epithelial Cells. | 2015 Oct 19 |
Sample Use Guides
In Vivo Use Guide
Curator's Comment: Oral route is possible: One group of 45 patients received 400 mg of Sodium artesunate on the first day of treatment and then 200 mg daily for 4 days for a total of 1200 mg (group I: 5-day treatment). A second group of 46 patients received 400 mg of Sodium artesunate on the first day of treatment and then 200 mg daily for 6 days for a total of 1600 mg (group II: 7-day treatment). 5- or 7-day regimens of sodium artesunate with a total dose of 1200-1600 mg are effective and safe in treating falciparum malaria acquired in Thailand.
https://www.ncbi.nlm.nih.gov/pubmed/9241384
Artesunate can be used orally, by intravenous or intramuscular injection or as a suppository. As an injection, artesunate 2.4mg/kg bw i.v or i.m. given on admission (time =0), then at 12hr and 24hr, then once a day.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/8891104
An artemisinin concentration of 100-300 nM in vitro caused swelling of the endoplasmic reticulum and mitochondria, as well as injuries both to the limiting and to the nuclear membranes of chloroquine-resistant P. falciparum (ItG2 strain) within 2 h.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:38:51 GMT 2023
by
admin
on
Fri Dec 15 15:38:51 GMT 2023
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Record UNII |
60W3249T9M
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Record Status |
Validated (UNII)
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Record Version |
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FDA ORPHAN DRUG |
651218
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FDA ORPHAN DRUG |
221206
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FDA ORPHAN DRUG |
598517
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WHO-ATC |
P01BE03
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admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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WHO-ESSENTIAL MEDICINES LIST |
6.5.3.1 (ART/AMO)
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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WHO-ATC |
P01BF03
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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WHO-ATC |
P01BF02
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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WHO-ESSENTIAL MEDICINES LIST |
6.5.3.1
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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WHO-ATC |
P01BF04
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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WHO-ATC |
P01BF06
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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EU-Orphan Drug |
EU/3/15/1521
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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FDA ORPHAN DRUG |
693719
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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FDA ORPHAN DRUG |
125599
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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NCI_THESAURUS |
C277
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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Code System | Code | Type | Description | ||
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247
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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Artesunate
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admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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PRIMARY | |||
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88495-63-0
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CHEMBL361497
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6459
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PRIMARY | |||
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18346
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admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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PRIMARY | RxNorm | ||
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100000086605
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PRIMARY | |||
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DTXSID3042681
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PRIMARY | |||
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DB09274
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PRIMARY | |||
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m2078
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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PRIMARY | Merck Index | ||
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60W3249T9M
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63918
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6917864
Created by
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PRIMARY | |||
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C73005
Created by
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7458
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PRIMARY | |||
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712571
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PRIMARY | |||
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PP-05
Created by
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ARTESUNATE
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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PRIMARY | Description: A fine, white crystalline powder. Solubility: Very slightly soluble in water; very soluble in dichloromethane R; freely soluble in ethanol (~750 g/l) TS and acetone R. Category: Antimalarial. Storage: Artesunate should be kept in a well-closed container or, if sterile, in a hermetically closed container. It should be protected from light. Labelling: The label states where applicable:? that the substance is free from bacterial endotoxins;? that the substance is sterile. Definition: Artesunate contains not less than 96.0% and not more than 102.0% of artesunate (C19H28O8) using Assay method A, and not less than 98.0% and not more than 102.0% of artesunate (C19H28O8) using Assay method B, both calculated with reference to the anhydrous substance. | ||
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C039726
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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PRIMARY | |||
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1042850
Created by
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PRIMARY | |||
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SUB05576MIG
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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ARTESUNATE
Created by
admin on Fri Dec 15 15:38:51 GMT 2023 , Edited by admin on Fri Dec 15 15:38:51 GMT 2023
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PRIMARY |
Related Record | Type | Details | ||
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TRANSPORTER -> INHIBITOR |
WEAK
IC50
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TARGET ORGANISM->INHIBITOR |
IC50
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TRANSPORTER -> SUBSTRATE |
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SALT/SOLVATE -> PARENT |
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TRANSPORTER -> SUBSTRATE |
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BINDER->LIGAND |
BINDING
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TRANSPORTER -> INHIBITOR |
WEAK
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Related Record | Type | Details | ||
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METABOLITE ACTIVE -> PARENT |
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METABOLITE ACTIVE -> PRODRUG |
ratio of alpha to beta DIHYDROARTEMISININ is 3.5
PLASMA
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Related Record | Type | Details | ||
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IMPURITY -> PARENT |
In the chromatogram obtained with solution (1): the area of any peak corresponding to impurity B (artemisinin) is not greater than 0.5 times the area of the principal peak obtained with solution (4) (0.5%).
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IMPURITY -> PARENT |
In the chromatogram obtained with solution (1): the area of any peak corresponding to impurity C, when multiplied by a correction factor of 0.07, is not greater than 0.2 times the area of the principal peak obtained with solution (4) (0.2%)
the sum of the corrected area of any peak corresponding to impurity C and the areas of all other peaks, other than the principal peak, is not greater than twice the area of the principal peak obtained with solution (4) (2.0%).
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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INTRAVENOUS ADMINISTRATION |
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Biological Half-life | PHARMACOKINETIC |
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IN PATIENTS WITH SEVERE MALARIA |
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