TESTOLACTONE

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

C[C@]12CC[C@H]3[C@@H](CCC4=CC(=O)C=C[C@]34C)[C@@H]1CCC(=O)O2

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

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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

Targets

Primary Target	Pharmacology	Condition	Potency
Aromatase 8	Inhibitor 8,504

Conditions

Condition	Modality	Targets	Highest Phase	Product
Breast cancer 432	Palliative		Approved 8,583	TESLAC

C_max

Value	Dose	Co-administered	Analyte	Population
1 μg/mL	500 mg 4 times / day steady-state, oral		TESTOLACTONE plasma	Homo sapiens

AUC

Value	Dose	Co-administered	Analyte	Population
3.5 μg × h/mL	500 mg 4 times / day steady-state, oral		TESTOLACTONE plasma	Homo sapiens

T_1/2

Value	Dose	Co-administered	Analyte	Population
1.7 h	500 mg 4 times / day steady-state, oral		TESTOLACTONE plasma	Homo sapiens

Overview

CYP3A4	CYP2C9	CYP2D6	hERG

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP19A1 429

Drug as perpetrator

Show entries

Target	Modality	Activity	Metabolite	Clinical evidence
CYP19A1 430	inhibitor 4,027	yes

Showing 1 to 1 of 1 entries

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Sourcing

Sourcing

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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
eMolecules	30151977	https://www.emolecules.com/cgi-bin/more?vid=30151977
ZINC	ZINC000004081771	http://zinc15.docking.org/substances/ZINC000004081771

Showing 1 to 4 of 4 entries

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PubMed

Show entries

Title	Date	PubMed
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
Feminizing Sertoli cell tumor associated with Peutz-Jeghers syndrome.	2002 Apr	12008693
Aromatase inhibitors for male infertility.	2002 Feb	11792932
Flutamide decreases cortisol clearance in patients with congenital adrenal hyperplasia.	2002 Jul	12107224

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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

Show entries

Name

Type

Language

TESLAC

Preferred Name

English

TESTOLACTONE

Official Name

English

TESTOLACTONE [HSDB]

Common Name

English

TESTOLACTONE [VANDF]

Common Name

English

NSC-23759

Code

English

Showing 1 to 5 of 17 entries

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Classification Tree

Code System

Code

Established Pharmacologic Class

NDF-RT

N0000175563

Estrogen Synthesis Inhibitors

NDF-RT

N0000175080

Sec. 1308.11 Schedule III.

DEA NO.

4000

Breast Cancer

LIVERTOX

943

Aromatase Inhibitor

NCI_THESAURUS

C2017

Showing 1 to 5 of 5 entries

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Code System

Code

Type

Description

EVMPD

SUB10936MIG

PRIMARY

CHEBI

9460

PRIMARY

SMS_ID

100000082735

PRIMARY

NCI_THESAURUS

C2301

PRIMARY

FDA UNII

6J9BLA949Q

PRIMARY

Showing 1 to 5 of 20 entries

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ACTIVE MOIETY


					6J9BLA949Q

TESTOLACTONE

SMILES

InChI

Originator

Approval Year

Targets

Conditions

Cmax

AUC

T1/2

Overview

OverviewOther

Drug as perpetrator​

Sourcing

PubMed

Patents

Sample Use Guides

C_max

T_1/2

Drug as perpetrator