Testolactonum

Testolactonum 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.

Testolactonum 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 Testolactonum
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
Testolactonum
Testolactonum

Uses

Testolactonum is a medication used to treat advanced breast cancer.

For palliative treatment of advanced breast cancer in postmenopausal women.

How Testolactonum 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.

Elimination Route

Testolactonum 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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https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:9460
http://www.genome.jp/dbget-bin/www_bget?cpd:C02197
http://www.lipidmaps.org/data/LMSDRecord.php?LMID=LMST02020084
http://www.hmdb.ca/metabolites/HMDB0015031
http://www.genome.jp/dbget-bin/www_bget?drug:D00153
http://www.genome.jp/dbget-bin/www_bget?cpd:C02197
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=13769
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508076
https://www.chemspider.com/Chemical-Structure.13172.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50367848
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=10378
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=9460
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1571
https://zinc.docking.org/substances/ZINC000004081771
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000624
http://www.pharmgkb.org/drug/PA164743056
http://www.rxlist.com/cgi/generic2/testolactone.htm
https://www.drugs.com/cdi/testolactone.html
https://en.wikipedia.org/wiki/Testolactone
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