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Testolactone

Catalog No. DB00894 Name DrugBank
CAS Number 968-93-4 Website http://www.ualberta.ca/
M. F. C19H24O3 Telephone (780) 492-3111
M. W. 300.39206 Fax (780) 492-1071
Purity Email david.wishart@ualberta.ca
Storage Chembase ID: 770

SYNONYMS

IUPAC name
(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
IUPAC Traditional name
testolactone
Brand Name
Teslac
Testolacton
Fludestrin
Teolit
Teslak
Synonyms
Testolactona [INN-Spanish]
Testolactonum [INN-Latin]
Testolattone [Dcit]

DATABASE IDS

PubChem CID 13769
PubChem SID 46508076
CAS Number 968-93-4

PROPERTIES

Hydrophobicity(logP) 3.7
Solubility Slightly soluble (27.4 mg/L)

DETAILS

Description (English)
Item Information
Drug Groups approved
Description An antineoplastic agent that is a derivative of progesterone and used to treat advanced breast cancer. [PubChem]
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 clinical studies in patients receiving testolactone.
Toxicity Oral LD50s in mouse and dog are 1630 mg/kg and 593-926 mg/kg, respectively.
Affected Organisms
Humans and other mammals
Biotransformation Hepatic. Metabolized to several derivatives in the liver, all of which preserve the lactone D-ring.
Absorption Testolactone is well absorbed from the gastrointestinal tract.
Protein Binding ~85%
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.
External Links
RxList
Drugs.com

REFERENCES