Drug Information

Drug (ID: DG00100) and It's Reported Resistant Information

• Name: Sulphadoxine
• Synonyms: 2447-57-6; Sulforthomidine; Fanasil; Sulphormethoxine; 4-amino-N-(5,6-dimethoxypyrimidin-4-yl)benzenesulfonamide; Sulfadoxinum; Sulfadoxina; Sulfadoxin; Fanzil; Solfadossina; Ro 4-4393; Solfadossina [DCIT]; Sulfadoxinum [INN-Latin]; Sulfadoxina [INN-Spanish]; 4-Sulfanilamido-5,6-dimethoxypyrimidine; 4-Amino-N-(5,6-dimethoxy-4-pyrimidinyl)benzenesulfonamide; Benzenesulfonamide, 4-amino-N-(5,6-dimethoxy-4-pyrimidinyl)-; WR 4873; N'-(5,6-Dimethoxy-4-pyrimidyl)sulfanilamide; UNII-88463U4SM5; Orthosulfin; Sulformethoxine; Sulformetoxine; Sulphormetoxin; Sulphorthodimethoxine; WR 4073; Ro-4-4393; Sanasil: Sulfadoxine: Sulformetoxin; Sulfadoxine (JAN/USP/INN); Sulfadoxine [USAN:INN:BAN:JAN]; N1-(5,6-Dimethoxy-4-pyrimidinyl)sulfanilamide; N(sup 1)-(5,6-Dimethoxy-4-pyrimidinyl)sulfanilamide; 4-amino-N-[5,6-bis(methyloxy)pyrimidin-4-yl]benzenesulfonamide; 6-(4-Aminobenzenesulfonamido)-4,5-dimethoxypyrimidine; RS-1653
• Indication:
  In total 1 Indication(s)
  Malaria [ICD-11: 1F45]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Validated by in-vivo Model for This Drug (1 diseases)
  Astrocytoma [ICD-11: 2F36]; [1]
• Target: Bacterial Dihydropteroate synthetase (Bact folP); DHPS_ECOLI; [1]
• Target: Monoamine oxidase type B (MAO-B); AOFB_HUMAN; [1]
• Formula: C12H14N4O4S
• IsoSMILES: COC1=C(N=CN=C1OC)NS(=O)(=O)C2=CC=C(C=C2)N
• InChI: 1S/C12H14N4O4S/c1-19-10-11(14-7-15-12(10)20-2)16-21(17,18)9-5-3-8(13)4-6-9/h3-7H,13H2,1-2H3,(H,14,15,16)
• InChIKey: PJSFRIWCGOHTNF-UHFFFAOYSA-N
• PubChem CID: 17134
• ChEBI ID: CHEBI:9329
• TTD Drug ID: D07PAO
• DrugBank ID: DB01299

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Astrocytoma [ICD-11: 2F36]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Dihydrofolate reductase (DHFR) [1]

• Molecule Alteration: Missense mutation; p.N51I+p.C59R+p.S108N
• Resistant Disease: Malaria [ICD-11: 1F45.0]
• Experimental Note: Discovered Using In-vivo Testing Model
• In Vitro Model: Plasmodium falciparum strains; 5833
• Experiment for Molecule Alteration: PCR
• Mechanism Description: The high prevalence of the pfdhfr 108N (99%) and 51I + 108N/59R + 108N (92%) in our study indicate that decreased susceptibility to sulphadoxine-pyrimethamine is widespread in Pakistan. However, only seven patients had infections with the triple pfdhfr resistance associated haplotype and only one patient was infected with P. falciparum that had the quintuple pfdhfr + pfdhps haplotype associated with high grade sulphadoxine-pyrimethamine resistance. These results indicate that high grade resistance to sulphadoxine-pyrimethamine is not wide.

Key Molecule: Dihydrofolate reductase (DHFR) [1]

• Molecule Alteration: Missense mutation; p.G437A+p.E540K
• Resistant Disease: Malaria [ICD-11: 1F45.0]
• Experimental Note: Discovered Using In-vivo Testing Model
• In Vitro Model: Plasmodium falciparum strains; 5833
• Experiment for Molecule Alteration: PCR
• Mechanism Description: The high prevalence of the pfdhfr 108N (99%) and 51I + 108N/59R + 108N (92%) in our study indicate that decreased susceptibility to sulphadoxine-pyrimethamine is widespread in Pakistan. However, only seven patients had infections with the triple pfdhfr resistance associated haplotype and only one patient was infected with P. falciparum that had the quintuple pfdhfr + pfdhps haplotype associated with high grade sulphadoxine-pyrimethamine resistance. These results indicate that high grade resistance to sulphadoxine-pyrimethamine is not wide.

Key Molecule: Dihydrofolate reductase (DHFR) [1]

• Molecule Alteration: Missense mutation; p.N51I+p.C59R+p.S108N
• Resistant Disease: Malaria [ICD-11: 1F45.0]
• Experimental Note: Discovered Using In-vivo Testing Model
• In Vitro Model: Plasmodium falciparum strains; 5833
• Experiment for Molecule Alteration: PCR
• Mechanism Description: The high prevalence of the pfdhfr 108N (99%) and 51I + 108N/59R + 108N (92%) in our study indicate that decreased susceptibility to sulphadoxine-pyrimethamine is widespread in Pakistan. However, only seven patients had infections with the triple pfdhfr resistance associated haplotype and only one patient was infected with P. falciparum that had the quintuple pfdhfr + pfdhps haplotype associated with high grade sulphadoxine-pyrimethamine resistance. These results indicate that high grade resistance to sulphadoxine-pyrimethamine is not wide.

References

• Ref 1: Prevalence of resistance associated polymorphisms in Plasmodium falciparum field isolates from southern Pakistan. Malar J. 2011 Jan 28;10:18. doi: 10.1186/1475-2875-10-18.