Drug Information

Drug (ID: DG00263) and It's Reported Resistant Information

• Name: Clofazimine
• Synonyms: Clofazimine; 2030-63-9; Lamprene; Lampren; Chlofazimine; Clofazimina; Clofaziminum; Clofaziminum [INN-Latin]; B 663 (Pharmaceutical); Clofazimina [INN-Spanish]; B-663; NSC-141046; G 30320; UNII-D959AE5USF; B 663 (VAN); C27H22Cl2N4; 3-(p-Chloranilino)-10-(p-chlorphenyl)-2,10-dihydro-2-(isopropylimino)-phenazin; B 663; 3-(p-Chloroanilino)-10-(p-chlorophenyl)-2,10-dihydro-2-(isopropylimino)phenazine; 3-(p-Chloranilino)-10-(p-chlorophenyl)-2,10-dihydro-2-(isopropylimino)-phenazine; EINECS 217-980-2; CFZ; SMP2_000339; B 663, pharmaceutical; G-30320; Lamprene (TN); Liposome-encapsulated clofazimine; Clofazimine [USAN:INN:BAN]; G-30,320; Clofazimine (JAN/USP/INN); N,5-bis(4-chlorophenyl)-3-propan-2-yliminophenazin-2-amine; N,5-Bis(4-chlorophenyl)-3,5-dihydro-3-(isopropylimino)phenazin-2-amine; N,5-Bis(4-chlorophenyl)-3,5-dihydro-3-(1-methylethyl)imino)-2-phenazinamine; N,5-Bis(4-chlorophenyl)-3,5-dihydro-3-[(1-methylethyl)imino]-2-phenazinamine; N,5-bis(4-chlorophenyl)-3-(propan-2-ylimino)-3,5-dihydrophenazin-2-amine; (3Z)-N,5-bis(4-chlorophenyl)-3-[(1-methylethyl)imino]-3,5-dihydrophenazin-2-amine; 3-(p-Chloranilino)-10-(p-chlorophenyl)-2,10-dihydro-2-(isopropylimino)phenazine; 3-(p-Chloranilino)-10-(p-chlorphenyl)-2,10-dihydro-2-(isopropylimino)-phenazin [German]; Riminophenazine
• Indication:
  In total 2 Indication(s)
  Crohn disease [ICD-11: DD70]; Approved; [1]
  Mycobacterium infection [ICD-11: 1B10-1B21]; Investigative; [1]
• Drug Resistance Disease(s):
  Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
  Leprosy [ICD-11: 1B20]; [1]
• Target: Bacterial Deoxyribonucleic acid (Bact DNA); NOUNIPROTAC; [1]
• Formula: C27H22Cl2N4
• IsoSMILES: CC(C)N=C1C=C2C(=NC3=CC=CC=C3N2C4=CC=C(C=C4)Cl)C=C1NC5=CC=C(C=C5)Cl
• InChI: 1S/C27H22Cl2N4/c1-17(2)30-24-16-27-25(15-23(24)31-20-11-7-18(28)8-12-20)32-22-5-3-4-6-26(22)33(27)21-13-9-19(29)10-14-21/h3-17,31H,1-2H3
• InChIKey: WDQPAMHFFCXSNU-UHFFFAOYSA-N
• PubChem CID: 2794
• ChEBI ID: CHEBI:3749
• TTD Drug ID: D0S5UH
• VARIDT ID: DR00669
• INTEDE ID: DR0346
• DrugBank ID: DB00845

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-01: Infectious/parasitic diseases

Leprosy [ICD-11: 1B20]

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.T53A
• Resistant Disease: Leprosy [ICD-11: 1B20.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Mycobacterium leprae isolates; 1769
• In Vivo Model: Footpad granuloma from M. leprae-infected nude mice model; Mus musculus
• Experiment for Molecule Alteration: PCR and single-stranded conformational polymorphism (SSCP) assay
• Experiment for Drug Resistance: Mouse footpad assay
• Mechanism Description: The mutations genes reported in this study have been demonstrated to be responsible for drug resistance by mouse footpad assay.

Key Molecule: Dihydrofolate reductase (DHFR) [1]

• Molecule Alteration: Missense mutation; p.P55R
• Resistant Disease: Leprosy [ICD-11: 1B20.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Mycobacterium leprae isolates; 1769
• In Vivo Model: Footpad granuloma from M. leprae-infected nude mice model; Mus musculus
• Experiment for Molecule Alteration: PCR and single-stranded conformational polymorphism (SSCP) assay
• Experiment for Drug Resistance: Mouse footpad assay
• Mechanism Description: The mutations genes reported in this study have been demonstrated to be responsible for drug resistance by mouse footpad assay.

Key Molecule: Dihydrofolate reductase/DNA-directed RNA polymerase subunit beta (DHFR/RPOB) [1]

• Molecule Alteration: Missense mutation; folP p.P55L+poB p.S531L
• Resistant Disease: Leprosy [ICD-11: 1B20.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Mycobacterium leprae isolates; 1769
• In Vivo Model: Footpad granuloma from M. leprae-infected nude mice model; Mus musculus
• Experiment for Molecule Alteration: PCR and single-stranded conformational polymorphism (SSCP) assay
• Experiment for Drug Resistance: Mouse footpad assay
• Mechanism Description: The mutations genes reported in this study have been demonstrated to be responsible for drug resistance by mouse footpad assay.

Key Molecule: Dihydrofolate reductase/DNA-directed RNA polymerase subunit beta (DHFR/RPOB) [1]

• Molecule Alteration: Missense mutation; folP p.P55S+rpoB p.S531L+rpoB p.V547I
• Resistant Disease: Leprosy [ICD-11: 1B20.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Mycobacterium leprae isolates; 1769
• In Vivo Model: Footpad granuloma from M. leprae-infected nude mice model; Mus musculus
• Experiment for Molecule Alteration: PCR and single-stranded conformational polymorphism (SSCP) assay
• Experiment for Drug Resistance: Mouse footpad assay
• Mechanism Description: The mutations genes reported in this study have been demonstrated to be responsible for drug resistance by mouse footpad assay.

Key Molecule: Dihydrofolate reductase/DNA gyrase subunit A/DNA gyrase subunit B (DHFR/GYRA/GYRB) [1]

• Molecule Alteration: Missense mutation; folP p.P55L+gyrA p.A91V+gyrB p.A91V
• Resistant Disease: Leprosy [ICD-11: 1B20.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Mycobacterium leprae isolates; 1769
• In Vivo Model: Footpad granuloma from M. leprae-infected nude mice model; Mus musculus
• Experiment for Molecule Alteration: PCR and single-stranded conformational polymorphism (SSCP) assay
• Experiment for Drug Resistance: Mouse footpad assay
• Mechanism Description: The mutations genes reported in this study have been demonstrated to be responsible for drug resistance by mouse footpad assay.

Key Molecule: Dihydrofolate reductase/DNA gyrase subunit A/DNA gyrase subunit B (DHFR/GYRA/GYRB) [1]

• Molecule Alteration: Missense mutation; folP p.P55L+gyrA p.D205N+gyrB p.D205N
• Resistant Disease: Leprosy [ICD-11: 1B20.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Mycobacterium leprae isolates; 1769
• In Vivo Model: Footpad granuloma from M. leprae-infected nude mice model; Mus musculus
• Experiment for Molecule Alteration: PCR and single-stranded conformational polymorphism (SSCP) assay
• Experiment for Drug Resistance: Mouse footpad assay
• Mechanism Description: The mutations genes reported in this study have been demonstrated to be responsible for drug resistance by mouse footpad assay.

References

• Ref 1: Mutations in genes related to drug resistance in Mycobacterium leprae isolates from leprosy patients in Korea. J Infect. 2005 Jan;50(1):6-11. doi: 10.1016/j.jinf.2004.03.012.