Drug Information

Drug (ID: DG00645) and It's Reported Resistant Information

• Name: Artesunate
• Synonyms: Artesunate; Artesunic acid; Arsumax; 88495-63-0; Dihydroqinghasu hemsuccinate; Artesunatum; Plasmotrin; Qinghaozhi; Saphnate; Arinate; Artesunato; Zysunate; Asumax; Gsunate Forte; Plasmotrim; UNII-60W3249T9M; CHEBI:63918; Succinyl dihydroartemisinin; 60W3249T9M; Arsuamoon; WR-256283; Butanedioic acid, 1-[(3R,5aS,6R,8aS,9R,10S,12R,12aR)-decahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin-10-yl] ester; cosunate; Artesunata; SM 804; Cosinate; 4-oxo-4-(((3R,5aS,6R,8aS,9R,10S,12R,12aR)-3,6,9-trimethyldecahydro-3H-3,12-epoxy[1,2]dioxepino[4,3-i]isochromen-10-yl)oxy)butanoic acid; 4-oxo-4-{[(3R,5aS,6R,8aS,9R,10S,12R,12aR)-3,6,9-trimethyldecahydro-3,12-epoxypyrano[4,3-j][1,2]benzodioxepin-10-yl]oxy}butanoic acid; Armax 200; Artesunatum [INN-Latin]; Artesunato [INN-Spanish]; Artsuna; Nuartez; Artesunate [USAN:INN:BAN]; HSDB 7458; NSC-712571; Quinghaosu reduced succinate ester; D95; Dihydroartemisinine-12alpha-succinate; .alpha.-artesunic acid; WR 256283; Dihydroqinghaosu hemisuccinate; MLS006011590; CHEMBL361497; GTPL9956; SCHEMBL14552891; LJPC-0118; (3R,5aS,6R,8aS,9R,10S,12R,12aR)-Decahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano(4,3-j)-1,2-benzodioxepin-10-ol, hydrogen succinate; ACT02643; HY-N0193; STR09744; BDBM50248021; ZINC14096305; AKOS037515734; CS-8151; DB09274; NCGC00164600-10; NCGC00164600-15; SMR002499399; Q707939; BRD-K54634444-001-05-9; WR-256283;ART;Armax 200;SM-804;HSDB-7458; 4-Oxo-4-(((3R,5aS,6R,8aS,9R,10S,12R,12aR)-3,6,9-trimethyldecahydro-3,12-epoxypyrano(4,3-j)-1,2-benzodioxepin-10-yl hydrogen butanedioate; 4-oxo-4-[[(1R,4S,5R,8S,9R,10S,12R,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-yl]oxy]butanoic acid; 4-oxo-4-{[(1R,4S,5R,8S,9R,10S,12R,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.0 ,(1)(3).0 ,(1)(3)]hexadecan-10-yl]oxy}butanoic acid; Butanedioic acid, mono((3R,5aS,6R,8aS,9R,10S,12R,12aR)-decahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano(4,3-j)-1,2-benzodioxepin-10-yl) ester
• Indication:
  In total 2 Indication(s)
  Malaria [ICD-11: 1F45]; Approved; [1]
  Malaria [ICD-11: 1F45]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
  Falciparum malaria [ICD-11: 1F40]; [1]
• Target: Sarcoplasmic/endoplasmic reticulum calcium ATPase (ATP2A); NOUNIPROTAC; [1]
• Formula: C19H28O8
• IsoSMILES: C[C@@H]1CC[C@H]2[C@H]([C@@H](O[C@H]3[C@@]24[C@H]1CC[C@](O3)(OO4)C)OC(=O)CCC(=O)O)C
• 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
• InChIKey: FIHJKUPKCHIPAT-AHIGJZGOSA-N
• PubChem CID: 6917864
• ChEBI ID: CHEBI:63918
• TTD Drug ID: D0D4JO
• DrugBank ID: DB09274

Type(s) of Resistant Mechanism of This Drug

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-01: Infectious/parasitic diseases

Falciparum malaria [ICD-11: 1F40]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Cysteine desulfurase (K13) [1]

• Molecule Alteration: Missense mutation; p.C580Y
• Resistant Disease: Plasmodium falciparum malaria [ICD-11: 1F40.1]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Red blood cells; Blood; Homo sapiens (Human); N.A.
• Experiment for Molecule Alteration: Whole genome sequencing assay
• Experiment for Drug Resistance: Giemsa stain assay
• Mechanism Description: All 63 isolates had the K13(C580Y) marker for artemisinin resistance; 79.4% (50/63) had Pfpm2 amplification. K13 mutations confer artemisinin resistance by dampening hemoglobin endocytosis.

References

• Ref 1: Clinical and In Vitro Resistance of Plasmodium falciparum to Artesunate-Amodiaquine in Cambodia .Clin Infect Dis. 2021 Aug 2;73(3):406-413. doi: 10.1093/cid/ciaa628. 10.1093/cid/ciaa628