Hormonal Therapy Agents
Abarelix (Plenaxis)
Sarma A.V., Schottenfeld D. Prostate cancer incidence, mortality, and survival trends in the United States 1981-2001. Seminars in Urologic Oncology. 2002;20:3–9.
Schellhammer, P. F. (2000). Therapy of advanced cancer of the prostate. Report to the 95th Annual Meeting of the American Urological Association, April 29–May 4, 2000, Atlanta, GA.
Aminoglutethimide (Cytadren)
SPECIAL CONSIDERATIONS
• Adjuvant corticosteroids should be administered.
• Most side effects will decrease in severity and incidence after the first 2 to 6 weeks of therapy.
• Adrenal hypofunction may develop with stressful situations such as acute illness, surgery, or trauma. Additional steroids may be required to ensure normal response to stress.
• Approximately 50% of patients will require mineralocorticoid replacement with fludrocortisone.
PATIENT EDUCATION
• Emphasize importance of not stopping the hydrocortisone abruptly.
• Warn patient of possible transient drowsiness.
• Avoid hazardous activities that require alertness until sedative effects subside.
• Stand up slowly to avoid dizziness.
• Take this medication with 8 ounces of water.
• Do not take on an empty stomach.
• If a skin rash develops when starting therapy and the rash persists more than 5 days, therapy should be temporarily discontinued.
• May restart therapy after rash resolves.
• Elderly may be more sensitive to central nervous system adverse events.
Honig S.F. Treatment of metastic disease: hormonal therapy and chemotherapy. In: Harris J.R., Lippman M.E., Morrow M. Disease of the breast. Philadelphia: Lippincott-Raven; 1996:669–734.
Stege R., Grande M., Carlstrom K., et al. Prognostic significance of tissue prostate-specific antigen in endocrine-treated prostate carcinoma. Clinical Cancer Research. 2000;6:160–165.
Anastrozole (Arimidex)
USE
• First-line treatment in postmenopausal women with advanced or locally advanced breast cancer that is hormone receptor positive or unknown receptor status.
• Advanced breast cancer in postmenopausal women with progression of disease after tamoxifen therapy.
• Adjuvant treatment of postmenopausal early breast cancer that is hormone receptor positive.
PHARMACOKINETICS
• Binds reversibly to the aromatase enzyme
• Resulting in inhibition, the conversion of androgens to estrogens
• Decreased biosynthesis of estrogen in all tissue
• Has no effect on adrenal corticosteroids or aldosterone formation
• Well absorbed from the gastrointestinal tract
• Food does not affect absorption.
Bicalutamide (Casodex)
PHARMACOKINETICS
Boccardo F., Rubagotti A., Barichello M., et al. Bicalutamide monotherapy versus flutamide plus goserelin in prostrate cancer patients: results of an Italian Prostate Cancer Project Study. Journal of Clinical Oncology. 1999;17:2027–2038.
Trachienberg, J., Gittelman, M., Steidle, C., et al. (2000). Abarelix—depot (A-D) versus leuprolide acetate (L) plus bicalutamide (casodex©), for prostate cancer: results of a multi-institutional, randomized phase III study in 255 patients. In Proceedings and Abstracts of the American Society of Clinical Oncology, Abstract 1307.
Buserelin (Suprefact)
Exemestane (Aromasin)
USE
• Treatment of advanced breast cancer in postmenopausal women, after disease progression after tamoxifen treatment
• Adjuvant treatment of postmenopausal women with estrogen receptor–positive early breast cancer who have had 2-3 years of tamoxifen. Then stay on exemestane for a completion of a 5-year regimen.
PHARMACOKINETICS
• Orally active and selective type 1 aromatase inhibitor
• A derivative of androstenedione
• Binds to the steroid-binding site of aromatase
• Converted by the normal catalytic mechanism of the enzyme
• The binding of the substrate results in inactivation of the aromatase.
• Enzymatic activity is blocked and no estrogen can be produced until a new enzyme is synthesized.
• Metabolites are excreted from the kidneys and from the liver.
• Clinical relevance of the irreversible binding properties is not yet clear.
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