Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H24O3 |
Molecular Weight | 300.3921 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 5 / 5 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CCC3=CC(=O)C=C[C@]3(C)[C@@]1([H])CC[C@]4(C)OC(=O)CC[C@@]24[H]
InChI
InChIKey=BPEWUONYVDABNZ-DZBHQSCQSA-N
InChI=1S/C19H24O3/c1-18-9-7-13(20)11-12(18)3-4-14-15(18)8-10-19(2)16(14)5-6-17(21)22-19/h7,9,11,14-16H,3-6,8,10H2,1-2H3/t14-,15+,16+,18+,19+/m1/s1
Molecular Formula | C19H24O3 |
Molecular Weight | 300.3921 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 5 / 5 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Testolactone (Teslac brand name) is an anti-cancer agent, which was used as adjunctive therapy in the palliative treatment of advanced or disseminated breast cancer. The mechanism of testolactone action is reported to be related to the inhibition of aromatase enzymatic activity. Testolactone is no longer available in the USA.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P11511 Gene ID: 1588.0 Gene Symbol: CYP19A1 Target Organism: Homo sapiens (Human) |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Palliative | TESLAC Approved UseTESLAC (testolactone tablets, USP) is recommended as adjunctive therapy in the palliative treatment of advanced or disseminated breast cancer in postmenopausal women when hormonal therapy is indicated. It may also be used in women who were diagnosed as having had disseminated breast carcinoma when premenopausal, in whom ovarian function has been subsequently terminated. Launch Date1.26144E10 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/6643639/ |
500 mg 4 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TESTOLACTONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.5 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/6643639/ |
500 mg 4 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TESTOLACTONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/6643639/ |
500 mg 4 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TESTOLACTONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://go.drugbank.com/drugs/DB00894 |
yes |
PubMed
Title | Date | PubMed |
---|---|---|
A new hypothesis based on suicide substrate inhibitor studies for the mechanism of action of aromatase. | 1982 Aug |
|
Evidence of a treatable endocrinopathy in infertile men. | 2001 Mar |
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Effective aromatase inhibition by anastrozole in a patient with gonadotropin-independent precocious puberty in McCune-Albright syndrome. | 2002 |
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McCune-Albright syndrome--the German experience. | 2002 |
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Feminizing Sertoli cell tumor associated with Peutz-Jeghers syndrome. | 2002 Apr |
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Aromatase inhibitors for male infertility. | 2002 Feb |
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[Androgen replacement therapy]. | 2002 Jun |
|
Cyclic AMP and the reverse transformation reaction. | 2002 Jun |
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Reversal of the hypogonadotropic hypogonadism of obese men by administration of the aromatase inhibitor testolactone. | 2003 Sep |
|
Paediatric management of endocrine complications in McCune-Albright syndrome. | 2005 Jan |
|
Adult height after ketoconazole treatment in patients with familial male-limited precocious puberty. | 2005 Jan |
|
Dominant transmission of prepubertal gynecomastia due to serum estrone excess: hormonal, biochemical, and genetic analysis in a large kindred. | 2005 Jan |
|
Fate of novel Quasi reverse steroidal substrates by Aspergillus tamarii KITA: bypass of lactonisation and an exclusive role for the minor hydroxylation pathway. | 2005 May 15 |
|
Structure-activity relationships of new A,D-ring modified steroids as aromatase inhibitors: design, synthesis, and biological activity evaluation. | 2005 Oct 6 |
|
Heritability of testosterone levels in 12-year-old twins and its relation to pubertal development. | 2006 Aug |
|
Tamoxifen improved final height prediction in a girl with McCune-Albright syndrome: patient report and literature review. | 2006 Jan |
|
Use of aromatase inhibitors to increase final height. | 2006 Jul 25 |
|
[Testotoxicosis]. | 2006 Jun 28 |
|
Synthesis of steroidal lactone by penicillium citreo-viride. | 2006 Nov |
|
Distinct metabolic handling of 3beta-hydroxy-17a-oxa-D-homo-5alpha-androstan-17-one by the filamentous fungus Aspergillus tamarii KITA: Evidence in support of steroid/hydroxylase binding hypothesis. | 2007 Sep |
|
Baeyer-Villiger oxidation of DHEA, pregnenolone, and androstenedione by Penicillium lilacinum AM111. | 2008 Dec 22 |
|
Statistics and the prostate gland. | 2008 Jun |
|
Desmoid tumor of the supraclavicular region: a case report. | 2009 Jun 22 |
|
Enhanced ERbeta immunoexpression and apoptosis in the germ cells of cimetidine-treated rats. | 2009 Nov 18 |
|
Alternative strategies for the treatment of classical congenital adrenal hyperplasia: pitfalls and promises. | 2010 |
|
Management of the adult with congenital adrenal hyperplasia. | 2010 |
|
An Evidence-Based Model of Multidisciplinary Care for Patients and Families Affected by Classical Congenital Adrenal Hyperplasia due to 21-Hydroxylase Deficiency. | 2010 |
|
3β,11α-Dihy-droxy-17a-oxa-d-homoandrost-5-en-17-one. | 2010 Jul 14 |
Patents
Substance Class |
Chemical
Created
by
admin
on
Edited
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by
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on
Fri Dec 15 15:09:05 UTC 2023
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Record UNII |
6J9BLA949Q
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Record Status |
Validated (UNII)
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Record Version |
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NDF-RT |
N0000175563
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NDF-RT |
N0000175080
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DEA NO. |
4000
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LIVERTOX |
943
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NCI_THESAURUS |
C2017
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SUB10936MIG
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9460
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100000082735
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C2301
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6J9BLA949Q
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2606
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CHEMBL1571
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968-93-4
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TESTOLACTONE
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DB00894
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1839
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7303
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13769
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23759
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m10593
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3255
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DTXSID2023644
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1645006
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213-534-6
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10378
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ACTIVE MOIETY |