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Journal ArticleDOI

Fulvestrant ('Faslodex')--a new treatment option for patients progressing on prior endocrine therapy.

C Morris, +1 more
- 01 Dec 2002 - 
- Vol. 9, Iss: 4, pp 267-276
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TLDR
Fulvestrant has recently gained US Food and Drug Administration approval for the treatment of hormone receptor-positive metastatic breast cancer in postmenopausal women with disease progression following antiestrogen therapy and these new hormonal treatments expand the choice of endocrine therapy for women with advanced breast cancer.
Abstract
Since its introduction more than 30 years ago, tamoxifen has been the most widely used endocrine therapy for the treatment of women with advanced breast cancer. More recently, a number of alternative endocrine treatments have been developed, including several selective estrogen receptor modulators (SERMs), aromatase inhibitors (AIs) and, most recently, fulvestrant ('Faslodex'). Fulvestrant is an estrogen receptor (ER) antagonist, which, unlike the SERMs, has no known agonist (estrogenic) effect and downregulates the ER protein. Tamoxifen is effective and well tolerated, although the non-steroidal AIs, anastrozole and letrozole, are more effective treatments for advanced disease than tamoxifen. Fulvestrant has recently gained US Food and Drug Administration approval for the treatment of hormone receptor-positive metastatic breast cancer in postmenopausal women with disease progression following antiestrogen therapy. In two global phase III clinical trials fulvestrant was at least as effective and as equally well tolerated as anastrozole for the treatment of postmenopausal women with advanced and metastatic breast cancer. In a retrospective analysis of the combined data from these trials, mean duration of response was significantly greater for fulvestrant compared with anastrozole. These new hormonal treatments expand the choice of endocrine therapy for women with advanced breast cancer and offer new options for sequencing and combining treatments.

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Journal ArticleDOI

A novel UPLC-PDA isocratic method for the quantification fulvestrant in oil-based pre-filled syringe injection matrix formulations

TL;DR: In this article, the chromatographic separation of fulvestrant was carried out by using ACQUITY UPLC and a BEH Shield RP18, 50mm × 2.1mm, i.d 1.7-μm column with a prepared mobile phase consisting of water, acetonitrile, and methanol in the ratio of 300:400:300 v/v/v, respectively.
Journal ArticleDOI

An alternative synthesis of the breast cancer drug fulvestrant (Faslodex®): catalyst control over C–C bond formation

TL;DR: Fulvestrant (Faslodex®) was synthesized in four steps (35% overall yield) from 6-dehydronandrolone acetate using Catalyst controlled, room temperature, diastereoselective 1,6-addition of the zirconocene derived from commercially available 9-bromonon-1-ene as the key C-C bond forming step.
Journal ArticleDOI

Preclinical profile and phase I clinical trial of a novel androgen receptor antagonist GT0918 in castration-resistant prostate cancer

TL;DR: GT0918, a full AR antagonist without agonist effect, has high binding affinity to AR with AR protein down-regulation activity and exhibits promising antitumour activity in CRPC.
Journal ArticleDOI

Identification of a Novel Compound That Suppresses Breast Cancer Invasiveness by Inhibiting Transforming Growth Factor-β Signaling via Estrogen Receptor α

TL;DR: N-23 may be a candidate compound that is effective in inhibiting breast cancer progression and it is shown that N-23 suppressed the migration and invasion of breast cancer cells to the same extent as by estrogen.
Journal ArticleDOI

Mechanisms of androgen receptor repression in prostate cancer

TL;DR: Using a cellular model, it is found different anti-androgens have diverse effects on subcellular localization of AR, revealing that they work via different mechanisms and suggesting that an informed sequential treatment regime may benefit patients.
References
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Journal ArticleDOI

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TL;DR: The FACT-G meets or exceeds all requirements for use in oncology clinical trials, including ease of administration, brevity, reliability, validity, and responsiveness to clinical change.
Journal ArticleDOI

Anastrozole alone or in combination with tamoxifen versus tamoxifen alone for adjuvant treatment of postmenopausal women with early breast cancer: first results of the ATAC randomised trial.

TL;DR: Anastrozole is an effective and well tolerated endocrine option for the treatment of postmenopausal patients with hormone-sensitive early breast cancer and longer follow-up is required before a final benefit:risk assessment can be made.
Journal Article

A potent specific pure antiestrogen with clinical potential.

TL;DR: The properties of ICI 182,780 identify this pure antiestrogen as a prime candidate with which to evaluate the potential therapeutic benefits of complete estrogen withdrawal in endocrine-responsive human breast cancer.
Journal ArticleDOI

Endometrial Cancer in Tamoxifen-Treated Breast Cancer Patients: Findings From the National Surgical Adjuvant Breast and Bowel Project (NSABP) B-14

TL;DR: Risk of endometrial cancer increases following tamoxifen therapy for invasive breast cancer; however, net benefit greatly outweighs risk, and tamoxIFen treatment for breast cancer should continue.
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