Bookmark
Forward
QuickView for Testolactone (compound)
PubChem
| Name: | Testolactone |
|---|---|
| PubChem Compound ID: | 13769 |
| Description: | An antineoplastic agent that is a derivative of progesterone and used to treat advanced breast cancer. |
| Molecular formula: | C19H24O3 |
| Molecular weight: | 300.392 g/mol |
| Synonyms: |
Testolactona [INN-Spanish]; NCI60_001908; 13,17-Secoandrosta-1,4-dien-17-oic acid, 13-hydroxy-3-oxo-, .delta.-lactone; CHEBI:9460; .DELTA.1-Dehydrotestololactone; NSC 12173; 1,2-Didehydrotestololactone; D00153; 3-oxo-13,17-secoandrosta-1,4-dieno-17,13alpha-lactone; 13-Hydroxy-3-oxo-13,17-secoandrosta-1, 4-dien-17-oic acid .delta.-lactone.
show more » |
DrugBank
Identification
| Name: | Testolactone |
|---|---|
| Name (isomeric): | DB00894 |
| Drug Type: | small molecule |
| Description: | An antineoplastic agent that is a derivative of progesterone and used to treat advanced breast cancer. |
| Synonyms: |
Testolactona [INN-Spanish]; Testolattone [Dcit]; Testolactonum [INN-Latin]
|
| Brand: | Teslac, Testolacton, Fludestrin, Teslak, Teolit |
| Category: | Antineoplastic Agents, Hormonal |
| CAS number: | 968-93-4 |
Pharmacology
| Indication: | For palliative treatment of advanced breast cancer in postmenopausal women. |
|---|---|
| Pharmacology: |
Testolactone 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 cl...
show more » |
| 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 vitr...
show more » |
| Absorption: | Testolactone is well absorbed from the gastrointestinal tract. |
| Protein binding: | ~85% |
| Biotransformation: | Hepatic. Metabolized to several derivatives in the liver, all of which preserve the lactone D-ring. |
| Route of elimination: | 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. |
| Toxicity: | Oral LD50s in mouse and dog are 1630 mg/kg and 593-926 mg/kg, respectively. |
| Affected organisms: | Humans and other mammals |
Interactions
| Drug interaction: |
|
|---|
Targets
