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Description: Letrozole (INN, trade name Femara®) is an oral non-steroidal aromatase inhibitor that has been introduced for the adjuvant treatment of hormonally-responsive breast cancer
Drug Type: Small Molecule; Approved; Investigational
Pharmacology: Letrozole is an aromatase inhibitor used in the treatment of breast cancer. Aromatase inhibitors work by inhibiting the action of the enzyme aromatase, which converts androgens into estrogens by a process called aromatization. As breast tissue is stimulated by estrogens, decreasing their production is a way of suppressing recurrence of the breast tumor tissue.
Mechanism of Action: Letrozole is a nonsteroidal competitive inhibitor of the aromatase enzyme system; it inhibits the conversion of androgens to estrogens. In adult nontumor- and tumorbearing female animals, letrozole is as effective as ovariectomy in reducing uterine weight, elevating serum Leuteinizing hormone (LH), and causing the regression of estrogen-dependent tumors. In contrast to ovariectomy, treatment with letrozole does not lead to an increase in serum (folicile stimulating hormone (FSH). Letrozole selectively inhibits gonadal steroidogenesis but has no significant effect on adrenal mineralocorticoid or glucocorticoid synthesis.
Indication: For the extended adjuvant treatment of early breast cancer in postmenopausal women who have received 5 years of adjuvant tamoxifen therapy. Also for first-line treatment of postmenopausal women with hormone receptor positive or hormone receptor unknown locally advanced or metastatic breast cancer. Also indicated for the treatment of advanced breast cancer in postmenopausal women with disease progression following antiestrogen therapy.
Half Life: 2 days
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Data Correlations | 6 studies

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Genes category icon Genes
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CYP19A1 100 100
PUM2 95 95
RGN 88 88
ASCL1 88 88
ALB 88 88
CYP2B6 87 87
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Biogroups category icon Biogroups
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Cytochrome P450, E-class, group I 100 100
ECM Receptor Interaction 99 99
Cell Communication 99 99
T-helper 1/T-helper 2 Differentiati… 99 99
Hematopoietic Cell Lineage 99 99
Peptidase M14, carboxypeptidase A 99 99
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Individual Studies

  • Letrozole (Femara) early response to treatment

    Homo sapiens Homo sapiens | RNA Expression   RNA Expression

    In the present investigation, we have exploited the opportunity provided by neoadjuvant treatment of a group of postmenopausal women with large operable or locally advanced breast cancer (in which therapy is given with the primary tumour remaining within the breast) to take sequential biopsies of th…

    Authors: Miller R William, Larionov Alexey, Renshaw Lorna et al.

    Organization: Genomics Institute of the Novartis Resea…
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Associated Researchers

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Thought leaders and organizations working on research involving Femara.

View All Author iconAuthors
  • Luciana Macedo
  • Angela M H Brodie
  • Angela Brodie
  • Gauri Sabnis
  • Olga G Goloubeva
View All Clinical trial sponsors icon Clinical Trials Sponsors
  • Novartis
  • M.D. Anderson Cancer Center
  • Dana-Farber Cancer Institute
  • Novartis Pharmaceuticals
  • NCIC Clinical Trials Group
View All Affiliations icon Organizations
  • University of Maryland
  • University of Maryland School of Medicine
  • University of Toronto
  • Washington University
  • Western General Hospital

Clinical Trials | 186 trials

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News | 22 stories

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