Drug Information

Drug (ID: DG00013) and It's Reported Resistant Information

• Name: Terbinafine
• Synonyms: Bramazil; Lamasil; TerbiFoam; Terbina; Lamisil AT; Lamisil Tablet; Ternbinafine HCl; Lamasil (TN); Lamisil (TN); SF 86-327; Terbisil (TN); Zabel (TN); SF-86-327; Terbinafine (USAN/INN); Terbinafine [USAN:BAN:INN]; Lamisil, Terbinex, Corbinal, Zabel, Terbinafine; Terbinafine, SF-86-327, Lamisil, TBNF; (2E)-N,6,6-trimethyl-N-(1-naphthylmethyl)-2-hepten-4-yn-1-amine; (2E)-N,6,6-trimethyl-N-(naphthalen-1-ylmethyl)hept-2-en-4-yn-1-amine; (E)-N,6,6-trimethyl-N-(naphthalen-1-ylmethyl)hept-2-en-4-yn-1-amine; (E)-N-(6,6-Dimethyl-2-hepten-4-ynyl)-N-methyl-1-naphthalene methanamine; (E)-N-(6,6-Dimethyl-2-hepten-4-ynyl)-N-methyl-1-naphthalenemethylamine; (E)-N-(6,6-dimethyl-2-heptenynyl)-N-methyl-1-naphthalenementhamin hydrochloride
• Indication:
  In total 2 Indication(s)
  Fungal infection [ICD-11: 1F29-1F2F]; Approved; [1]
  Nail/perionychium infection [ICD-11: EE12]; Phase 2; [1]
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases)
  Dermatophytosis [ICD-11: 1F28]; [2]
• Target: Candida Squalene epoxidase (Candi ERG1); ERG1_CANAL; [1]
• Formula: C21H25N
• IsoSMILES: CC(C)(C)C#C/C=C/CN(C)CC1=CC=CC2=CC=CC=C21
• InChI: 1S/C21H25N/c1-21(2,3)15-8-5-9-16-22(4)17-19-13-10-12-18-11-6-7-14-20(18)19/h5-7,9-14H,16-17H2,1-4H3/b9-5+
• InChIKey: DOMXUEMWDBAQBQ-WEVVVXLNSA-N
• PubChem CID: 1549008
• ChEBI ID: CHEBI:9448
• TTD Drug ID: D01AYJ
• DrugBank ID: DB00857

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

  IDUE: Irregularity in Drug Uptake and Drug Efflux

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-01: Infectious/parasitic diseases

Candidosis [ICD-11: 1F23]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Key Molecule: Pleiotropic ABC efflux transporter of multiple drugs CDR1 (CDR1) [1]

• Sensitive Disease: Recurrent oropharyngeal candidiasis [ICD-11: 1F23.6]
• Molecule Alteration: Deletion mutation; Deleteion
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Candida albicans strain DSY448; 5476
• Experiment for Molecule Alteration: PCR; Southern blotting analysis; Northern blottling analysis
• Experiment for Drug Resistance: Growth differences between the different C. albicans strains assay
• Mechanism Description: The delta cdr1 mutant was also hypersusceptible to other antifungal agents (terbinafine and amorolfine) and to different metabolic inhibitors (cycloheximide, brefeldin A, and fluphenazine).

Dermatophytosis [ICD-11: 1F28]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Squalene epoxidase (SQLE) [2]

• Resistant Disease: t. indotineae infection [ICD-11: 1F28]
• Molecule Alteration: Missense mutation; L38HL
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: T. indotineae; 5475
• Experiment for Molecule Alteration: PCR; PCR-ELISA assay; GeneSeq assay
• Experiment for Drug Resistance: In vitro drug susceptibility testing; Resistance testing
• Mechanism Description: Mutations L393S, L393F, F397L, and F397I of the SQLE gene were associated with terbinafine resistance. Resistance to itraconazole could not be explained by mutations in the ERG11B gene.

References

• Ref 1: Susceptibilities of Candida albicans multidrug transporter mutants to various antifungal agents and other metabolic inhibitors. Antimicrob Agents Chemother. 1996 Oct;40(10):2300-5. doi: 10.1128/AAC.40.10.2300.
• Ref 2: Trichophyton mentagrophytes ITS Genotype VIII/Trichophyton indotineae Infection and Antifungal Resistance in Bangladesh. J Fungi (Basel). 2024 Nov 5;10(11):768.