Action and Spectrum

Actions and Spectrum: 

some of the actions and spectrum of testolactone: 

• Treatment of breast cancer: testolactone is primarily used in the treatment of hormone receptor-positive breast cancer in postmenopausal women. By reducing the levels of estrogen in the body, it can help to slow or stop the growth of breast cancer cells. 
• Gynecomastia: testolactone may also be used in the treatment of gynecomastia, a condition in which men develop breast tissue due to imbalances in hormone levels. By reducing estrogen levels, testolactone can help to reduce the size of breast tissue in men. 
• Cushing’s syndrome: testolactone may be used in the treatment of Cushing’s syndrome, a condition in which there is excess production of cortisol by the adrenal glands. testolactone can help to reduce the levels of cortisol in the body, which can improve symptoms associated with Cushing’s syndrome. 
• Precocious puberty: testolactone may also be used in the treatment of precocious puberty, a condition in which children begin to develop sexual characteristics at an early age. By reducing the levels of estrogen in the body, testolactone can help to slow the progression of puberty. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Edema 

Acne 

Priapism 

Menstrual irregularities 

Virilization 

Breast soreness 

Frequency not defined 

Gynecomastia 

Anaphylaxis 

Cholestatic jaundice syndrome 

Neoplasm of liver 

Anaphylaxis 

Black Box Warning

Contraindication / Caution

Contraindication/Caution: 

• Hypersensitivity: testolactone should not be used in patients who are allergic or hypersensitive to testolactone or any of its components. 
• Pregnancy and breastfeeding: testolactone should not be used in pregnant or breastfeeding women, as it may harm the developing fetus or infant. 
• Liver disease: testolactone may cause liver damage, especially in patients with pre-existing liver disease. Liver function tests should be monitored regularly while using testolactone. 
• Cardiovascular disease: testolactone may increase the risk of cardiovascular events such as heart attack and stroke. It should be used with caution in patients with a history of cardiovascular disease. 
• Diabetes: testolactone may affect blood sugar levels and should be used with caution in patients with diabetes. 
• Interactions: testolactone may interact with other medications, including other hormonal therapies, and should be used with caution in patients taking other medications. 
• Children: testolactone should not be used in children unless specifically directed by a healthcare provider. 

Pregnancy / Lactation

Pregnancy consideration:  

Category X 

Breastfeeding warnings:  

testolactone is excreted in breastmilk; hence contraindicated in breastfeeding females 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women. 
• Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

testolactone is an aromatase inhibitor, which means it works by inhibiting the action of the enzyme aromatase. Aromatase is responsible for the conversion of androgens (such as testosterone) into estrogens (such as estradiol). By inhibiting aromatase, testolactone reduces the production of estrogen in the body.  

Pharmacodynamics: 

The pharmacodynamics of testolactone involves its action as an aromatase inhibitor, leading to a reduction in the production of estrogen in the body.

testolactone competitively inhibits the aromatase enzyme, which is responsible for the conversion of androgens (such as testosterone) to estrogens (such as estradiol) in various tissues, including the ovaries, adrenal glands, and adipose tissue.

By inhibiting aromatase, testolactone decreases the levels of circulating and tissue estrogen, which may help to slow or stop the growth of hormone receptor-positive breast cancer cells. 

In addition to its anti-estrogenic effects, testolactone also has weak androgenic and progestogenic properties, which may contribute to its therapeutic effects in certain conditions. testolactone may also inhibit the production of adrenal androgens, such as dehydroepiandrosterone (DHEA) and androstenedione, which can contribute to the growth of hormone receptor-positive breast cancer cells. 

Pharmacokinetics: 

Absorption 

testolactone is rapidly and almost completely absorbed from the gastrointestinal tract after oral administration. 

Distribution 

testolactone is extensively protein-bound and is distributed mainly to the liver and the kidneys. 

Metabolism 

testolactone is extensively metabolized in the liver by oxidation, reduction, and conjugation reactions. The major metabolites of testolactone are 2-hydroxytestolactone, 3-hydroxytestolactone, and their corresponding glucuronide and sulfate conjugates. 

Elimination and Excretion 

The elimination half-life of testolactone is approximately 2-3 hours. It is primarily excreted in the urine, with only a small fraction excreted in the feces. 

Adminstartion

Administration: 

testolactone is available in the form of oral tablets and should be taken orally with water. The exact dosage and duration of treatment may vary depending on the condition being treated, the patient’s age, weight, and overall health, and other factors. It is important to follow the dosing instructions provided by the healthcare provider or pharmacist. 

For the treatment of breast cancer in postmenopausal women, the usual adult dose of testolactone is 250 mg to 500 mg four times daily. The dose may be adjusted based on the patient’s response and tolerance. The treatment is usually continued until the cancer progresses or until the desired therapeutic effect is achieved. 

For the treatment of gynecomastia in men, the usual adult dose of testolactone is 125 mg to 250 mg four times daily. The duration of treatment may vary depending on the severity of the condition and the patient’s response. testolactone should be taken at regular intervals to maintain a consistent level of the drug in the blood. Missing a dose may decrease the effectiveness of the treatment. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: testolactone 

Pronounced: tes-toe-lak-tone 

Why do we use testolactone? 

testolactone is used for the treatment of hormone receptor-positive breast cancer in postmenopausal women.

It is an aromatase inhibitor, which means that it works by inhibiting the activity of the aromatase enzyme that is responsible for converting androgens (such as testosterone) to estrogens (such as estradiol) in various tissues, including the ovaries, adrenal glands, and adipose tissue.

By inhibiting aromatase, testolactone decreases the levels of circulating and tissue estrogen, which may help to slow or stop the growth of hormone receptor-positive breast cancer cells. 

testolactone may also be used for the treatment of gynecomastia (enlargement of breast tissue) in men. It may also be used in the treatment of precocious puberty and Cushing’s syndrome.