Activity of Formestane in de novo Tamoxifen–Resistant Patients with Metastatic Breast Cancer

Noberasco, Cristina; Bajetta, Emilio; Zilembo, Nicoletta; Leo, Angelo Di; Cappuzzo, Federico; Bartoli, Cesare; Bono, Aldo; Bichisao, E.

doi:10.1159/000227510

Cited by 6 publications

(1 citation statement)

References 10 publications

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“…[57] Homoharringtonine Binds to the 80S ribosome in eukaryotic cells and inhibits protein synthesis by interfering with chain elongation. [58] Idarubicin Antileukemia agent with higher DNA binding capacity and greater cytotoxicity than daunorubicin [59] Formestane Aromatase inhibitor [76] Fostriecin Interferes with the reversible phosphorylation of proteins that are critical for progression through the cell cycle. [77] Hispidin Potent inhibitor of protein kinase Cβ.…”

Section: Daunorubicinmentioning

confidence: 99%

Drug Targets for Cancer Treatment: An Overview

Kumar¹,

Ahmad²,

Waseem³

et al. 2015

Med chem

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Cancer is one of the major cause of death worldwide. Malignant cells display metabolic changes, when compared to normal cells, because of both genetic and epigenetic alterations. Number of drugs being used for the cancer treatment follows different mechanisms of action. Therapeutic strategies include targeting of drugs at specific genes or proteins/enzymes found in cancer cells or the internal tissue environment which contributes to growth and survival of these cells. Targeted therapy is often used along with chemotherapy and other treatments to restrict the growth and spread of cancer cells. During the past few decades, targeted therapy has emerged as a promising approach for the development of selective anticancer agents. There is a class of targeted therapy drugs called angiogenesis inhibitors which focus on blocking the development of new blood vessels in tumor tissues. In addition, anticancer drugs also include DNA intercalators, DNA synthesis inhibitors, transcription regulators, enzyme inhibitors etc. This review focuses on major classes of anticancer drug targets and their therapeutic importance.

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Section: Daunorubicinmentioning

confidence: 99%

Drug Targets for Cancer Treatment: An Overview

Kumar¹,

Ahmad²,

Waseem³

et al. 2015

Med chem

View full text Add to dashboard Cite

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New aromatase inhibitors for the treatment of advanced breast cancer in postmenopausal women

Jong

Blijham²

1999

The Netherlands Journal of Medicine

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Formestane is feasible and effective in elderly breast cancer patients with comorbidity and disability

Venturino¹,

Comandini²,

Granetto³

et al. 2000

Breast Cancer Res Treat

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Age is a major risk factor for solid tumors, including breast cancer. The majority of elderly breast cancer patients have oestrogen-dependent tumors, thus, tamoxifen is widely administered. However, it has been noted that tamoxifen-related thrombotic events are not exceptional. Due to the increasing prevalence of comorbidity, including vascular diseases, with age, such events are more frequently observed in the aged patients. Formestane, a selective steroidal aromatase inhibitor, may represent a therapeutic option after failure with tamoxifen, or in the presence of vascular diseases contraindicating its administration. The present report provides a new clinical experience on a consecutive series of 45 elderly breast cancer women affected by moderate to severe degree of comorbidity and disability measured by a Comprehensive Geriatric Assessment (CGA) scale validated on oncological patients. Formestane was given intramuscularly at the dose of 250 mg every 2 weeks. The study included 31 patients who had metastatic disease, and 14 who received formestane as an adjuvant treatment. Median age was 74 years (range 65-93), with nine patients > 80 years. Median ECOG Performance Status (PS) was one. The more frequent comorbidities observed in our series were arthrosis-arthritis (64.4% of patients), hypertension (44.4%), vascular diseases (35.5%), CNS diseases (28.8%). Twenty percent of patients presented at least one dependency in Activities of Daily Living (ADL) and 51.2% in Instrumental Activities of Daily Living (IADL). The treatment was well tolerated - only two patients interrupted formestane because of minor adverse reaction at the injection site and generalised itching. In particular Formestane was not responsible for any worsening of pre-treatment comorbidities, especially hypertension and vascular diseases. Objective responses (OR) were observed in 11.1% of advanced patients, while the disease was stabilised in 51.8% subjects. Median duration of OR was 12 months; median overall survival was 11 months. Among patients receiving formestane as adjuvant treatment, three relapsed, with a time to failure (TTF) of 12 months. Formestane is effective and minimally toxic in an elderly breast cancer population with comorbidities and disabilities measured by CGA.

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Activity of Formestane in de novo Tamoxifen–Resistant Patients with Metastatic Breast Cancer

Cited by 6 publications

References 10 publications

Drug Targets for Cancer Treatment: An Overview

Drug Targets for Cancer Treatment: An Overview

New aromatase inhibitors for the treatment of advanced breast cancer in postmenopausal women

Formestane is feasible and effective in elderly breast cancer patients with comorbidity and disability

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