TESTOLACTONE

US Previously Marketed

First approved in 1969

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 Search

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
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/16118slr023_teslac_lbl.pdf

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

Targets

Primary Target	Pharmacology	Condition	Potency
Aromatase 8 Target ID: P11511 Gene ID: 1588.0 Gene Symbol: CYP19A1 Target Organism: Homo sapiens (Human) Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/16118slr023_teslac_lbl.pdf	Inhibitor 8297

Conditions

Condition	Modality	Targets	Highest Phase	Product
Breast cancer 434 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/16118slr023_teslac_lbl.pdf	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

C_max

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

T_1/2

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
CYP19A1 60

Drug as perpetrator

Target	Modality	Activity	Metabolite	Clinical evidence
CYP19A1 60	inhibitor 3277 Sources: https://go.drugbank.com/drugs/DB00894	yes

Sourcing

Vendor/Aggregator	ID	URL
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

Title	Date	PubMed
A new hypothesis based on suicide substrate inhibitor studies for the mechanism of action of aromatase.	1982 Aug	7083195
Evaluation of the male pubertal onset assay to detect testosterone and steroid biosynthesis inhibitors in CD rats.	2001 Apr	11248141
Evidence of a treatable endocrinopathy in infertile men.	2001 Mar	11176482
Male LH-independent sexual precocity in a 3.5-year-old boy caused by a somatic activating mutation of the LH receptor in a Leydig cell tumor.	2002 Mar	11889161
Testotoxicosis: current viewpoint.	2005 Dec	16361981
Success of testicular sperm extraction [corrected] and intracytoplasmic sperm injection in men with Klinefelter syndrome.	2005 Nov	16131585
Heritability of testosterone levels in 12-year-old twins and its relation to pubertal development.	2006 Aug	16899163
Nonsurgical treatment of male infertility: specific and empiric therapy.	2007 Sep	19707335
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	17692565
Baeyer-Villiger oxidation of DHEA, pregnenolone, and androstenedione by Penicillium lilacinum AM111.	2008 Dec 22	18755205
Statistics and the prostate gland.	2008 Jun	18317483
Desmoid tumor of the supraclavicular region: a case report.	2009 Jun 22	19829936
Alternative strategies for the treatment of classical congenital adrenal hyperplasia: pitfalls and promises.	2010	20652035
Management of the adult with congenital adrenal hyperplasia.	2010	20613954
3β,11α-Dihy-droxy-17a-oxa-d-homoandrost-5-en-17-one.	2010 Jul 14	21588317

Patents

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

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

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