Page last updated: 2024-12-05

testolactone

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Testolactone is a synthetic anabolic steroid. It is a derivative of testosterone, with an added lactone ring. Testolactone is a potent androgen, and it has been used in the treatment of hypogonadism and other conditions. Testolactone is also studied for its potential therapeutic effects in conditions such as osteoporosis and anemia. Testolactone is generally well-tolerated, but it can cause side effects, such as acne, hair loss, and mood swings. It is important to note that testosterone and its derivatives are controlled substances, and their use should be under the guidance of a qualified healthcare professional.'

Testolactone: An antineoplastic agent that is a derivative of progesterone and used to treat advanced breast cancer. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID13769
CHEMBL ID1571
CHEBI ID9460
SCHEMBL ID4053
MeSH IDM0021194

Synonyms (102)

Synonym
AKOS015840139
d-homo-17a-oxaandrosta-1,4-diene-3,17-dione
1,2-dehydrotestololactone
fludestrin
nsc 12173
17a-oxa-d-homoandrosta-1,17-dione
13,4-dien-17-oic acid, 13.alpha.-hydroxy-3-oxo-, .delta.-lactone
sq 9538
delta-1-testololactone
1-dehydrotestololactone
teslak
.delta.1-testololactone
d-homo-17a-oxaandrosta-1,17-dione
13-hydroxy-3-oxo-13,4-dien-17-oic acid .delta.-lactone
.delta.1-dehydrotestolactone
testololactone,2-didehydro-
13,4-dien-17-oic acid, 13-hydroxy-3-oxo-, lactone
2h-phenanthro[2,8(4bh)-dione, 3,4,4a,5,6,10a,10b,11,12,12a-decahydro-10a,12a-dimethyl-, lactone
teslac
.delta.1-dehydrotestololactone
teolit
1,2-didehydrotestololactone
testolacton
testololactone, 1-dehydro-
nsc-23759
nsc23759
13,4-dien-17-oic acid, 13-hydroxy-3-oxo-, .delta.-lactone
NCI60_001908
testolactone (usp/inn)
teslac (tn)
D00153
17alpha-oxo-d-homo-1,4-androstadiene-3,17-dione
testolactonum [inn-latin]
testololactone, 1,2-didehydro-
13,17-secoandrosta-1,4-dien-17-oic acid, 13-hydroxy-3-oxo-, delta-lactone
einecs 213-534-6
1,2,3,4,4a,4b,7,9,10,10a-decahydro-2-hydroxy-2,4b-dimethyl-7-oxo-1-phenanthrenepropionic acid delta-lactone
delta(1)-testolactone
nsc 23759
testolattone [dcit]
hsdb 3255
testolactona [inn-spanish]
delta(1)-dehydrotestolactone
delta(1)-testololactone
13-hydroxy-3-oxo-13,17-secoandrosta-1,4-dien-17-oic acid delta-lactone
CHEBI:9460 ,
3-oxo-13,17-secoandrosta-1,4-dieno-17,13alpha-lactone
(4as,4br,10ar,10bs,12as)-10a,12a-dimethyl-3,4,4a,5,6,10a,10b,11,12,12a-decahydro-2h-naphtho[2,1-f]chromene-2,8(4bh)-dione
testolactone
968-93-4
C02197
DB00894
NCGC00159329-02
delta1-testololactone
1-dehydrotestolactone
1 dehydrotestolactone
(4as,4br,10ar,10bs,12as)-10a,12a-dimethyl-4,4a,4b,5,6,10b,11,12-octahydro-3h-naphtho[2,1-f]chromene-2,8-dione
sq-9538
CHEMBL1571
testolactone ciii
LMST02020084
13-hydroxy-3-oxo-13,17-secoandrosta-1,4-dien-17-oic acid lactone
testolattone
unii-6j9bla949q
6j9bla949q ,
testolactona
testolactone [usan:usp:inn]
testolactonum
dtxsid2023644 ,
dtxcid303644
cas-968-93-4
tox21_111576
bdbm50367848
testolactone ciii [usp-rs]
testolactone [usp-rs]
testolactone [hsdb]
testolactone [mi]
testolactone [inn]
testolactone [usan]
testolactone [usp impurity]
testolactone [who-dd]
testolactone [vandf]
testolactone [orange book]
gtpl7303
SCHEMBL4053
HY-13763
CS-5268
W-100129
(4as,4br,10ar,10bs,12as)-10a,12a-dimethyl-4,4a,4b,5,6,10a,10b,11,12,12a-decahydro-2h-naphtho[2,1-f]chromene-2,8(3h)-dione
Q3985253
BCP10926
HMS3750O07
therapeutic testolactone
testolactona (inn-spanish)
testolactone (usan:usp:inn)
testolactone (usp-rs)
(4as,4br,10ar,10bs,12as)-10a,12a-dimethyl-3,4,4a,5,6,10a,10b,11,12,12a-decahydro-2h-naphtho(2,1-f)chromene-2,8(4bh)-dione
13-hydroxy-3-0x0-13,17-secoandrosta-1,4-dien-17-oic acid delta-lactone
delta(1)-dehydrotestololactone
testolactone ciii (usp-rs)
testolactonum (inn-latin)
testolactone (usp impurity)

Research Excerpts

Overview

Testolactone is a potent steroid aromatase (CYP19A1) inhibitor. Its main effect is a reduction in estradiol and estrone and an increase in testosterone and androstenedione levels.

ExcerptReferenceRelevance
"Testolactone is a potent steroid aromatase (CYP19A1) inhibitor, and its main effect is a reduction in estradiol and estrone and an increase in testosterone and androstenedione levels. "( Comprehensive Zebrafish Water Tank Experiment for Metabolic Studies of Testolactone.
Anselmo, CS; de Aquino Neto, FR; de Carvalho, AR; Lisboa, RR; Matias, BF; Nunes, IKC; Padilha, MC; Pereira, HMG; Sardela, PDO; Sardela, VF, 2020
)
2.23

Treatment

ExcerptReferenceRelevance
"Men treated with testolactone had an increase in testosterone-to-estradiol ratios during therapy (mean plus or minus standard error of the mean 5.3 +/- 0.2 versus 12.4 +/- 1.1, p <0.001). "( Aromatase inhibitors for male infertility.
Raman, JD; Schlegel, PN, 2002
)
0.65

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" If correct, two clinically available aromatase inhibitors, aminoglutethimide (AG) and testololactone (TL) could potentially be given together at lower than usual dosage with reduction of patient side effects and preservation of aromatase inhibition."( Additive effects of aminoglutethimide, testololactone, and 4-hydroxyandrostenedione as inhibitors of aromatase.
Osawa, Y; Rosen, H; Santen, RJ; Santner, SJ, 1984
)
0.27
" Long-term therapy (up to 6 months) with the 250-mg dosage showed continual suppression of estrone with no escape being observed."( In vivo effects of delta 1-testololactone on peripheral aromatization.
Barone, RM; Gambone, JC; Judd, HL; Lasley, BL; Laufer, LR; Monfort, SL, 1982
)
0.26
" Six families acknowledged difficulty in adhering to the daily dosing schedule."( Long-term testolactone therapy for precocious puberty in girls with the McCune-Albright syndrome.
Cutler, GB; Feuillan, PP; Jones, J, 1993
)
0.69
" In two similar experiments, weanling female rats were dosed for 20 days by gavage with vehicle (0."( Evaluation of the EDSTAC female pubertal assay in CD rats using 17beta-estradiol, steroid biosynthesis inhibitors, and a thyroid inhibitor.
Carney, EW; Crissman, JW; Marty, MS, 1999
)
0.3
" Testolactone had no important adverse effects in any group of patients, although the need for a four-times-daily dosing schedule made compliance difficult for many families."( Use of aromatase inhibitors in precocious puberty.
Cutler, GB; Feuillan, P; Leschek, EW; Merke, D, 1999
)
1.21
" Recently, this assay was evaluated by several laboratories using a variety of dosing schemes."( Evaluation of the male pubertal onset assay to detect testosterone and steroid biosynthesis inhibitors in CD rats.
Carney, EW; Crissman, JW; Marty, MS, 2001
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
seco-androstane
3-oxo-Delta(1),Delta(4)-steroidA 3-oxo-Delta(1) steroid containing an additional double bond between positions 4 and 5.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AR proteinHomo sapiens (human)Potency13.33320.000221.22318,912.5098AID743040
estrogen nuclear receptor alphaHomo sapiens (human)Potency15.62460.000229.305416,493.5996AID743069; AID743075; AID743077; AID743079
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency39.81070.01789.637444.6684AID588834
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AromataseHomo sapiens (human)Ki35.00000.00000.60469.5010AID53875
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (15)

Processvia Protein(s)Taxonomy
negative regulation of chronic inflammatory responseAromataseHomo sapiens (human)
steroid biosynthetic processAromataseHomo sapiens (human)
estrogen biosynthetic processAromataseHomo sapiens (human)
androgen catabolic processAromataseHomo sapiens (human)
syncytium formationAromataseHomo sapiens (human)
negative regulation of macrophage chemotaxisAromataseHomo sapiens (human)
sterol metabolic processAromataseHomo sapiens (human)
female genitalia developmentAromataseHomo sapiens (human)
mammary gland developmentAromataseHomo sapiens (human)
uterus developmentAromataseHomo sapiens (human)
prostate gland growthAromataseHomo sapiens (human)
testosterone biosynthetic processAromataseHomo sapiens (human)
positive regulation of estradiol secretionAromataseHomo sapiens (human)
female gonad developmentAromataseHomo sapiens (human)
response to estradiolAromataseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
iron ion bindingAromataseHomo sapiens (human)
steroid hydroxylase activityAromataseHomo sapiens (human)
electron transfer activityAromataseHomo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenAromataseHomo sapiens (human)
oxygen bindingAromataseHomo sapiens (human)
heme bindingAromataseHomo sapiens (human)
aromatase activityAromataseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
endoplasmic reticulumAromataseHomo sapiens (human)
endoplasmic reticulum membraneAromataseHomo sapiens (human)
membraneAromataseHomo sapiens (human)
endoplasmic reticulumAromataseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID54051In vitro inactivation of human placental Cytochrome P450 19A11989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Is there a case for P-450 inhibitors in cancer treatment?
AID53875In vitro inhibition of Cytochrome P450 19A11989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Is there a case for P-450 inhibitors in cancer treatment?
AID54197Percent inhibition of human placental Cytochrome P450 19A1 at 3:1 inhibitor: androstenedione (0.7 uM) ratio1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
Aromatase inhibitors. Synthesis and biological activity of androstenedione derivatives.
AID54198Percent inhibition of human placental Cytochrome P450 19A1 at 6:1 inhibitor: androstenedione (0.7 uM) ratio1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
Aromatase inhibitors. Synthesis and biological activity of androstenedione derivatives.
AID409956Inhibition of mouse brain MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1345280Human CYP19A1 (CYP11, CYP17, CYP19, CYP20 and CYP21 families)1982Cancer research, Aug, Volume: 42, Issue:8 Suppl
A new hypothesis based on suicide substrate inhibitor studies for the mechanism of action of aromatase.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (177)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990112 (63.28)18.7374
1990's35 (19.77)18.2507
2000's19 (10.73)29.6817
2010's7 (3.95)24.3611
2020's4 (2.26)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 39.32

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index39.32 (24.57)
Research Supply Index5.38 (2.92)
Research Growth Index4.19 (4.65)
Search Engine Demand Index57.69 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (39.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials24 (12.57%)5.53%
Reviews21 (10.99%)6.00%
Case Studies12 (6.28%)4.05%
Observational0 (0.00%)0.25%
Other134 (70.16%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
The Influence of Sex Steroid Hormones on Serotonin Transporter Binding in the Human Brain Investigated by Positron Emission Tomography [NCT01065220]Phase 432 participants (Actual)Interventional2010-02-28Completed
Testolactone Treatment of Girls With LHRH Analog-Resistant Precocious Puberty Due to Autonomous, Non-Neoplastic Ovarian Estrogen Secretion [NCT00001181]Phase 2100 participants Interventional1982-10-31Completed
Spironolactone and Testolactone Treatment of Boys With Familial Isosexual Precocious Puberty [NCT00001202]Phase 280 participants Interventional1985-01-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]