1-dehydrotestololactone
1-dehydrotestololactone Uses, Dosage, Side Effects, Food Interaction and all others data.
An antineoplastic agent that is a derivative of progesterone and used to treat advanced breast cancer.
1-dehydrotestololactone 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.
| Trade Name | 1-dehydrotestololactone |
| Availability | Discontinued |
| Generic | Testolactone |
| Testolactone Other Names | 1-dehydrotestololactone, delta(1)-testololactone, Testolactona, Testolactone, Testolactonum, Testolattone |
| Related Drugs | estradiol, tamoxifen, Premarin, testosterone, megestrol, Soltamox |
| Type | |
| Formula | C19H24O3 |
| Weight | Average: 300.3921 Monoisotopic: 300.172544634 |
| Protein binding | ~85% |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
1-dehydrotestololactone is a medication used to treat advanced breast cancer.
For palliative treatment of advanced breast cancer in postmenopausal women.
How 1-dehydrotestololactone works
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.
Toxicity
Oral LD50s in mouse and dog are 1630 mg/kg and 593-926 mg/kg, respectively.
1-dehydrotestololactone Drug Interaction
Unknown: amphetamine / dextroamphetamine, amphetamine / dextroamphetamine, multivitamin with minerals, mirabegron, fesoterodine, cholecalciferol
Elimination Route
1-dehydrotestololactone is well absorbed from the gastrointestinal tract.
Elimination Route
No clinical effects in humans of testolactone on adrenal function have been reported; however, one study noted an increase in urinary excretion of 17-ketosteroids in most of the patients treated with 150 mg/day orally. It is metabolized to several derivatives in the liver, all of which preserve the lactone D-ring. These metabolites, as well as some unmetabolized drug, are excreted in the urine.
Innovators Monograph
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