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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
Structure of TESTOLACTONE

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

HIDE SMILES / InChI

Description

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.

Originator

Approval Year

1969
24
Targets

Targets

Primary TargetPharmacologyConditionPotency
Aromatase
8
Target ID: P11511
Gene ID: 1588.0
Gene Symbol: CYP19A1
Target Organism: Homo sapiens (Human)
Inhibitor
8297
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Approved
8429
TESLAC

Approved Use

TESLAC (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 Date

1970
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
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

AUC

ValueDoseCo-administeredAnalytePopulation
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

T1/2

ValueDoseCo-administeredAnalytePopulation
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

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP19A1
60
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP19A1
60
 yes
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:9460
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:9460
ChemicalBook
CB4371689
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB4371689
ZINC
ZINC000004081771
http://zinc15.docking.org/substances/ZINC000004081771
eMolecules
30151977
https://www.emolecules.com/cgi-bin/more?vid=30151977
PubMed

PubMed

TitleDatePubMed
Evidence of a treatable endocrinopathy in infertile men.
2001 Mar
Effective aromatase inhibition by anastrozole in a patient with gonadotropin-independent precocious puberty in McCune-Albright syndrome.
2002
Reversal of the hypogonadotropic hypogonadism of obese men by administration of the aromatase inhibitor testolactone.
2003 Sep
Aromatase inhibitors in precocious puberty: rationale and experience to date.
2004
Use of aromatase inhibitors to increase final height.
2006 Jul 25
A boy with McCune-Albright syndrome associated with GH secreting pituitary microadenoma. Clinical findings and response to treatment.
2006 Jul-Sep
[Testotoxicosis].
2006 Jun 28
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
Statistics and the prostate gland.
2008 Jun
An Evidence-Based Model of Multidisciplinary Care for Patients and Families Affected by Classical Congenital Adrenal Hyperplasia due to 21-Hydroxylase Deficiency.
2010
Patents

Patents

JP2011525180A
180
JP4701159B2
70

Sample Use Guides

In Vivo Use Guide
The recommended oral dose is 250 mg qid.
Route of Administration: Oral
In Vitro Use Guide
Unknown
Name Type Language
TESTOLACTONE
HSDB   INN   MART.   MI   ORANGE BOOK   USAN   USP   VANDF   WHO-DD  
INN   USAN  
Official Name English
TESTOLACTONE [HSDB]
Common Name English
TESTOLACTONE [VANDF]
Common Name English
NSC-23759
Code English
TEOLIT
Brand Name English
TESTOLACTONE [USAN]
Common Name English
TESTOLACTONE [MI]
Common Name English
TESTOLACTONE CIII
USP-RS  
Common Name English
TESTOLACTONE CIII [USP-RS]
Common Name English
testolactone [INN]
Common Name English
TESLAC
Brand Name English
TESTOLACTONE [ORANGE BOOK]
Common Name English
Testolactone [WHO-DD]
Common Name English
TESTOLACTONE [USP IMPURITY]
Common Name English
TESTOLACTONE [USP-RS]
Common Name English
SQ-9538
Code English
SQ 9538
Code English
Classification Tree Code System Code
NDF-RT N0000175563
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
NDF-RT N0000175080
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
DEA NO. 4000
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
LIVERTOX 943
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
NCI_THESAURUS C2017
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
Code System Code Type Description
EVMPD
SUB10936MIG
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
CHEBI
9460
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
SMS_ID
100000082735
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
NCI_THESAURUS
C2301
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
FDA UNII
6J9BLA949Q
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
DRUG CENTRAL
2606
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
ChEMBL
CHEMBL1571
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
CAS
968-93-4
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
WIKIPEDIA
TESTOLACTONE
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
DRUG BANK
DB00894
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
INN
1839
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
IUPHAR
7303
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
PUBCHEM
13769
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
NSC
23759
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
MERCK INDEX
m10593
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY Merck Index
HSDB
3255
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
EPA CompTox
DTXSID2023644
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
RS_ITEM_NUM
1645006
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
ECHA (EC/EINECS)
213-534-6
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY
RXCUI
10378
Created by admin on Fri Dec 15 15:09:05 GMT 2023 , Edited by admin on Fri Dec 15 15:09:05 GMT 2023
PRIMARY RxNorm
ACTIVE MOIETY
Structure of TESTOLACTONE
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
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