Fludestrin
Fludestrin - General Information
An antineoplastic agent that is a derivative of progesterone and used to treat advanced breast cancer. [PubChem]
Pharmacology of Fludestrin
Fludestrin is a synthetic anti-neoplastic agent that is structurally distinct from the androgen steroid nucleus in possessing a six-membered lactone ring in place of the usual five-membered carbocyclic D-ring. Despite some similarity to testosterone, testolactone has no in vivo androgenic effect. No other hormonal effects have been reported in clinical studies in patients receiving testolactone.
Fludestrin for patients
The physician should be consulted regarding missed doses. Notify the physician if adverse reactions occur or become more pronounced.
Fludestrin Interactions
When administered concurrently, testolactone may increase the effects of oral anticoagulants; monitor and adjust anticoagulant dosage accordingly.
Drug/Laboratory Test Interactions: Physiologic effects of testolactone may result in decreased estradiol concentrations with radioimmunoassays for estradiol, increased plasma calcium concentrations, and increased 24-hour urinary excretion of creatine and 17-ketosteroids.
Fludestrin Contraindications
Testolactone is contraindicated in the treatment of breast cancer in men and in patients with a history of hypersensitivity to the drug.
Additional information about Fludestrin
Fludestrin Indication: For palliative treatment of advanced breast cancer in postmenopausal women.
Mechanism Of Action: Although the precise mechanism by which testolactone produces its clinical antineoplastic effects has not been established, its principal action is reported to be inhibition of steroid aromatase activity and consequent reduction in estrone synthesis from adrenal androstenedione, the major source of estrogen in postmenopausal women. Based on in vitro studies, the aromatase inhibition may be noncompetitive and irreversible. This phenomenon may account for the persistence of testolactone's effect on estrogen synthesis after drug withdrawal.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Testolactone
Synonyms: Testolactona [Inn-Spanish]; Testolactonum [Inn-Latin]; Testolattone [Dcit]
Drug Category: Antineoplastic Agents, Hormonal
Drug Type: Small Molecule; Approved
Other Brand Names containing Testolactone: Fludestrin; Teolit; Teslac; Teslak; Testolacton;
Absorption: Testolactone is well absorbed from the gastrointestinal tract.
Toxicity (Overdose): Oral LD50s in mouse and dog are 1630 mg/kg and 593-926 mg/kg, respectively.
Protein Binding: ~85%
Biotransformation: Hepatic. Metabolized to several derivatives in the liver, all of which preserve the lactone D-ring.
Half Life: Not Available
Dosage Forms of Fludestrin: Tablet Oral
Chemical IUPAC Name: (4aS,4bR,10aR,10bS,12aS)-10a,12a-dimethyl-4,4a,4b,5,6,10b,11,12-octahydro-3H-naphtho[6,5-f]chromene-2,8-dione
Chemical Formula: C19H24O3
Testolactone on Wikipedia: Not Available
Organisms Affected: Humans and other mammals
