Testolactone

CAS No:
968-93-4 Category:
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  • #LGM Pharma offers this active ingredient but not the finished dosage forms.

Product Details:

  • CAS No: 968-93-4
  • AHFC code:
  • Synonyms: Testolactona [INN-Spanish] Testolactonum [INN-Latin] Testolattone [Dcit]
  • ATC Code:
  • Chemical Formula: C13H10N2O4
  • Molecular Weight: 300.3921
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB00894 (APRD00640)
  • SMILES: C[C,]12CC[C,H]3[C,,H](CCC4=CC(=O)C=C[C,]34C)[C,,H]1CCC(=O)O2
  • InChl: BPEWUONYVDABNZ-DZBHQSCQSA-N
  • PubChem: 13769
  • IUPAC: (1R,2S,7S,10S,11R)-7,11-dimethyl-6-oxatetracyclo[8.8.0.0^{2,7}.0^{11,16}]octadeca-12,15-diene-5,14-dione

Additional Details

Indication:
For palliative treatment of advanced breast cancer in postmenopausal women.
Pharmacodynamics:
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 clinical studies in patients receiving testolactone.
Mode 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.
Metabolism:
Hepatic. Metabolized to several derivatives in the liver, all of which preserve the lactone D-ring.
Toxicity:
Oral LD50s in mouse and dog are 1630 mg/kg and 593-926 mg/kg, respectively.
General Reference:
Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

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