U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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
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

Targets

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

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
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

1.26144E10
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1 μg/mL
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
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
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

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
yes
PubMed

PubMed

TitleDatePubMed
A new hypothesis based on suicide substrate inhibitor studies for the mechanism of action of aromatase.
1982 Aug
Evaluation of the male pubertal onset assay to detect testosterone and steroid biosynthesis inhibitors in CD rats.
2001 Apr
Effective aromatase inhibition by anastrozole in a patient with gonadotropin-independent precocious puberty in McCune-Albright syndrome.
2002
Aromatase inhibitors for male infertility.
2002 Feb
Cyclic AMP and the reverse transformation reaction.
2002 Jun
Dominant transmission of prepubertal gynecomastia due to serum estrone excess: hormonal, biochemical, and genetic analysis in a large kindred.
2005 Jan
Heritability of testosterone levels in 12-year-old twins and its relation to pubertal development.
2006 Aug
[Testotoxicosis].
2006 Jun 28
Synthesis of steroidal lactone by penicillium citreo-viride.
2006 Nov
Enhanced ERbeta immunoexpression and apoptosis in the germ cells of cimetidine-treated rats.
2009 Nov 18
Growth and reproductive outcomes in congenital adrenal hyperplasia.
2010
Patents

Sample Use Guides

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 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
NDF-RT N0000175080
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
DEA NO. 4000
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
LIVERTOX 943
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
NCI_THESAURUS C2017
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
Code System Code Type Description
EVMPD
SUB10936MIG
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
CHEBI
9460
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
NCI_THESAURUS
C2301
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
FDA UNII
6J9BLA949Q
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
DRUG CENTRAL
2606
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
ChEMBL
CHEMBL1571
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
CAS
968-93-4
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
WIKIPEDIA
TESTOLACTONE
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
DRUG BANK
DB00894
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
INN
1839
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
IUPHAR
7303
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
PUBCHEM
13769
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
NSC
23759
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
MERCK INDEX
M10593
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY Merck Index
HSDB
3255
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
EPA CompTox
DTXSID2023644
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
RS_ITEM_NUM
1645006
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
ECHA (EC/EINECS)
213-534-6
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY
RXCUI
10378
Created by admin on Fri Dec 16 16:19:39 UTC 2022 , Edited by admin on Fri Dec 16 16:19:39 UTC 2022
PRIMARY RxNorm