No

Androgen

Palliative treatment of advanced disseminated breast carcinoma

C-III

C

In men for the treatment of breast cancer; known hypersensitivity to testolactone

The U.S. Food and Drug Administration (FDA) currently recommends that procedures for proper handling and disposal of antineoplastic agents be considered. Use with caution in hepatic, renal, or cardiac disease; prolonged use may cause drug-induced hepatic disease; history of porphyria.

1% to 10%:

Dermatologic: Maculopapular rash

Endocrine & metabolic: Hypercalcemia

Gastrointestinal: Anorexia, diarrhea, nausea, edema of the tongue

Neuromuscular & skeletal: Paresthesias, peripheral neuropathies

Increased toxicity: Increased effects of oral anticoagulants

No data reported

Testolactone is a synthetic testosterone derivative without significant androgen activity. The drug inhibits steroid aromatase activity, thereby blocking the production of estradiol and estrone from androgen precursors such as testosterone and androstenedione. Unfortunately, the enzymatic block provided by testolactone is transient and is usually limited to a period of 3 months.

Absorption: Oral: Absorbed well

Metabolism: In the liver

Elimination: In urine

Adults: Female: Oral: 250 mg 4 times/day for at least 3 months; desired response may take as long as 3 months

Plasma calcium levels

Plasma estradiol concentrations by RIA

None reported

None reported

No information available to require special precautions

No effects or complications reported

Take as directed; do not discontinue without consulting prescriber. Effectiveness of therapy may take several months. Maintain adequate fluid intake (2-3 L/day of fluids unless instructed to restrict fluid intake) and diet and exercise program recommended by prescriber. You may experience nausea or vomiting (small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help). Report fluid retention (swelling of ankles, feet, or hands; difficulty breathing or sudden weight gain); numbness, tingling, or swelling of fingers, toes, or face; skin rash, redness, or irritation; or other adverse reactions. Pregnancy/breast-feeding precautions: Consult prescriber about pregnancy and breast-feeding.

Monitor plasma calcium levels

Tablet: 50 mg

Jeffrey LP, Chairman, National Study Commission on Cytotoxic Exposure. Position Statement. "The Handling of Cytotoxic Agents by Women Who Are Pregnant, Attempting to Conceive, or Breast-Feeding," January 12, 1987.