Drug Information

Drug (ID: DG00422) and It's Reported Resistant Information

• Name: Exemestane
• Synonyms: Aromasil; Aromasin; Aromasine; EXE; Exemestance; Exemestano; Exemestanum; Nikidess; Pfizer brand of exemestane; Curator_000009; Fce 24304; Aromasin (TN); Aromasin, Exemestane; Exemestano [INN-Spanish]; Exemestanum [INN-Latin]; FCE-24304; PNU-155971; Exemestane [USAN:INN:BAN]; Exemestane (JAN/USP/INN); (8R,9S,10R,13S,14S)-10,13-dimethyl-6-methylidene-7,8,9,11,12,14,15,16-octahydrocyclopenta[a]phenanthrene-3,17-dione; 6-Methylenandrosta-1,4-diene-3,17-dione; 6-Methyleneandrosta-1,4-diene-3,17-dione; 6-methylideneandrosta-1,4-diene-3,17-dione
• Indication:
  In total 1 Indication(s)
  Breast cancer [ICD-11: 2C60]; Approved; [1], [2]
• Drug Resistance Disease(s):
  Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
  Breast cancer [ICD-11: 2C60]; [1], [2]
• Target: Aromatase (CYP19A1); CP19A_HUMAN; [2]
• Formula: C20H24O2
• IsoSMILES: C[C@]12CC[C@H]3[C@H]([C@@H]1CCC2=O)CC(=C)C4=CC(=O)C=C[C@]34C
• InChI: 1S/C20H24O2/c1-12-10-14-15-4-5-18(22)20(15,3)9-7-16(14)19(2)8-6-13(21)11-17(12)19/h6,8,11,14-16H,1,4-5,7,9-10H2,2-3H3/t14-,15-,16-,19+,20-/m0/s1
• InChIKey: BFYIZQONLCFLEV-DAELLWKTSA-N
• PubChem CID: 60198
• ChEBI ID: CHEBI:4953
• TTD Drug ID: D0D2VS
• INTEDE ID: DR0675
• DrugBank ID: DB00990

Type(s) of Resistant Mechanism of This Drug

  UAPP: Unusual Activation of Pro-survival Pathway

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

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Estrogen receptor alpha (ESR1) [1], [2]

• Molecule Alteration: Missense mutation; p.Y537S
• 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.

Key Molecule: Estrogen receptor alpha (ESR1) [2]

• Molecule Alteration: Missense mutation; p.Y537N
• 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.

Key Molecule: Estrogen receptor alpha (ESR1) [2]

• 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.

Key Molecule: Estrogen receptor alpha (ESR1) [2], [3]

• Molecule Alteration: Missense mutation; p.D538G
• 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: Activating ESR1 mutations in hormone-resistant metastatic breast cancer. Nat Genet. 2013 Dec;45(12):1446-51. doi: 10.1038/ng.2823. Epub 2013 Nov 3.
• Ref 2: 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.
• Ref 3: D538G mutation in estrogen receptor-Alpha: A novel mechanism for acquired endocrine resistance in breast cancer. Cancer Res. 2013 Dec 1;73(23):6856-64. doi: 10.1158/0008-5472.CAN-13-1197. Epub 2013 Nov 11.