Testolactone
- Atc Codes:G03B
- CAS Codes:968-93-4
- PHARMGKB ID:968-93-4
Table of contents
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Drug combinations
Chemistry
Testolactone: C~19~H~24~O~3~. Mw: 300.39. (1) D-Homo-17a-oxaandrosta-1,4-diene-3,17-dione; (2) 13-Hydroxy-3-oxo-13,17-secoandrosta-1,4-dien-17-oic acid δ-lactone. CAS-968-93-4 (1964).
Pharmacologic Category
Antineoplastic Agents; Endocrine Therapy. Hormones and Synthetic Substitutes; Androgens. (ATC-Code: G03B).
Mechanism of action
Inhibits steroid aromatase activity, thereby blocking production of estradiol and estrone from androgen precursors such as testosterone and androstenedione. The enzymatic block provided by testolactone is usually limited to a period of 3 months.
Therapeutic use
Palliative treatment of advanced or disseminated breast carcinoma.
Pregnancy and lactiation implications
Testolactone should only be used in postmenopausal women. Use during pregnancy not recommended. Not recommended in nursing women (excretion in breast milk unknown).
Unlabeled use
Contraindications
Hypersensitivity to testolactone or any component of the formulation. Treatment of breast cancer in men.
Warnings and precautions
Use with caution in cardiovascular disease, in diabetes mellitus, in hepatic and renal impairment, and in history of porphyria. Exclusively for use in postmenopausal women or in premenopausal women without ovarian function.