Liarozole fumarate (R85246): a novel imidazole in the treatment of receptor positive postmenopausal metastatic breast cancer
| Autor: | L. M. Tye, Michael Crump, Nancy Wadden, Paul E. Goss, Caroline Reid, Amit M. Oza, Roland De Coster, Rakesh Goel, Jean-Marc Nabholtz, J. Bruynseels |
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| Rok vydání: | 2000 |
| Předmět: |
Cancer Research
medicine.medical_specialty Antineoplastic Agents Hormonal medicine.drug_class Phases of clinical research Breast Neoplasms Liarozole Fumarate Antiandrogen Gastroenterology Skin Diseases chemistry.chemical_compound Breast cancer Internal medicine medicine Humans Liarozole Aged Aged 80 and over business.industry Imidazoles Cancer Estrogens Middle Aged medicine.disease Metastatic breast cancer Postmenopause Endocrinology Oncology chemistry Tolerability Receptors Estrogen Disease Progression Quality of Life Female business |
| Zdroj: | Breast cancer research and treatment. 59(1) |
| ISSN: | 0167-6806 |
| Popis: | This phase II study of liarozole fumarate (R85246, liarozole), a novel imidazole with retinomimetic and aromatase inhibitory effects, was designed to determine the efficacy and tolerability in postmenopausal women with advanced breast cancer in progression, to correlate these effects with hormonal levels, and to evaluate quality of life. Twenty-nine women with ER-positive or unknown metastatic disease who receivedor = 2 prior hormonal therapies were treated with 150-300 mg liarozole twice daily until disease progression. All patients were evaluable for toxicity and 25 for response. Four patients (16.0%, 95% CI 5.3-37.4%) had partial remission (PR) of their disease for a median of 7.4 months (range 1.2-12.9) and 7 (28%) had disease stabilization for a median of 4.8 months (1.6-16.0). Estradiol decreased from pre-treatment levels of 9.2-52 pM (mean 17.1) to below detection (9.2 pM, p = 0.0005) after 1 month. Similarly estrone levels fell from 14-307 pM (mean 92.7) to below detection (9.2 pM, p = 0.0001). The most common toxicity was dermatological (96.6%) with features compatible with hypervitaminosis A syndrome such as rash, pruritus, dry skin, and brittle nails. The majority of these were mild to moderate in severity. No significant improvement in quality of life scores (FLI-C) were noted. Liarozole is an active new treatment for breast cancer in patients heavily pre-treated with hormone therapies. Further studies are needed to confirm its relative efficacy in both receptor positive and negative postmenopausal breast cancer. |
| Databáze: | OpenAIRE |
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