Drug Information

Drug (ID: DG00438) and It's Reported Resistant Information

• Name: Toremifene
• Synonyms: Acapodene; Estrimex; Farestone; Toremifeno; Toremifenum; Toremifene Base; Toremifeno [Spanish]; Toremifenum [Latin]; GTx 006; Acapodene (TN); FC-1157a; Fareston (TN); GTx-006; Toremifene (INN); Toremifene [INN:BAN]; Z-Toremifene; GTX-006 (Acapodene); Toremifene Citrate (1:1); {2-[4-(4-Chloro-1,2-diphenyl-but-1-enyl)-phenoxy]-ethyl}-dimethyl-amine; (Z)-2-(4-(4-Chloro-1,2-diphenyl-1-butenyl)phenoxy)-N,N-dimethylethanamine; 2-(p-[(Z)-4-chloro-1,2-diphenyl-1-butenyl]-phenoxy)-N,N-dimethyl-ethylamine citrate(1:1); 2-(para-((Z)-4-Chloro-1,2-diphenyl-1-butenyl)phenoxy)-N,N-dimethylethylamine (IUPAC); 2-({4-[(1Z)-4-chloro-1,2-diphenylbut-1-en-1-yl]phenyl}oxy)-N,N-dimethylethanamine; 2-[4-[(Z)-4-chloro-1,2-diphenylbut-1-enyl]phenoxy]-N,N-dimethylethanamine; 2-{4-[(1Z)-4-chloro-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine
• Indication:
  In total 1 Indication(s)
  Breast cancer [ICD-11: 2C60]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
  Breast cancer [ICD-11: 2C60]; [1]
• Target: Estrogen receptor (ESR); ESR1_HUMAN; [1]
• Formula: C26H28ClNO
• IsoSMILES: CN(C)CCOC1=CC=C(C=C1)/C(=C(/CCCl)\\C2=CC=CC=C2)/C3=CC=CC=C3
• InChI: 1S/C26H28ClNO/c1-28(2)19-20-29-24-15-13-23(14-16-24)26(22-11-7-4-8-12-22)25(17-18-27)21-9-5-3-6-10-21/h3-16H,17-20H2,1-2H3/b26-25-
• InChIKey: XFCLJVABOIYOMF-QPLCGJKRSA-N
• PubChem CID: 3005573
• ChEBI ID: CHEBI:9635
• TTD Drug ID: D04VFJ
• VARIDT ID: DR01170
• DrugBank ID: DB00539

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

Breast cancer [ICD-11: 2C60]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Estrogen receptor alpha (ESR1) [1]

• Molecule Alteration: Missense mutation; p.Y537C
• Resistant Disease: Breast cancer [ICD-11: 2C60.3]
• Experimental Note: Identified from the Human Clinical Data
• In Vivo Model: A retrospective survey in conducting clinical studies; Homo sapiens
• Experiment for Molecule Alteration: Droplet digital polymerase chain reaction assay
• Experiment for Drug Resistance: Chest x-ray assay; Computed tomography assay; Magnetic resonance imaging assay; Positron emission tomography assay
• Mechanism Description: We have developed a ddPCR-based method for the sensitive detection and quantification of 4 representative ESR1 mutations, Y537S, Y537N, Y537C, and D538G, in 325 breast cancer specimens, in which 270 primary breast cancer and 55 MBC specimens.

References

• Ref 1: Droplet digital polymerase chain reaction assay for screening of ESR1 mutations in 325 breast cancer specimens. Transl Res. 2015 Dec;166(6):540-553.e2. doi: 10.1016/j.trsl.2015.09.003. Epub 2015 Sep 14.