Testolactone

Summary

Testolactone (CHEMBL1571) is an approved small molecule targeting CYP19A1; indicated across 1 condition including precocious puberty.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Targets: 1 (CYP19A1)
• Indications: 1 condition
• Clinical trials: 4
• Chemistry: 300.4 Da · C19H24O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1571
Name	Testolactone
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	13769
ChEBI	CHEBI:9460
Molecular formula	C19H24O3
Molecular weight	300.4
InChIKey	BPEWUONYVDABNZ-DZBHQSCQSA-N

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

IUPAC name: (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

Also known as: Fludestrin, NSC-23759, SQ 9538, SQ-9538, Teolit, Teslac, Testolactona, Testolactone, Testolactone ciii, TESTOLACTONE, SID85554, SID144205129

Patent coverage: 13,090 distinct patent families (57,527 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
CYP19A1	CYP19A1	Inhibition	4.46	0%	P11511

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Aromatase.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): CYP19A1.

Top Reactome pathways

3 total, by targets touching each:

Pathway	Targets	Genes
Estrogen biosynthesis	1	CYP19A1
Endogenous sterols	1	CYP19A1
Defective CYP19A1 causes AEXS	1	CYP19A1

Dominant GO biological processes

GO term	Targets
negative regulation of chronic inflammatory response	1
steroid biosynthetic process	1
estrogen biosynthetic process	1
androgen catabolic process	1
obsolete syncytium formation	1
female gonad development	1
negative regulation of macrophage chemotaxis	1
sterol metabolic process	1
female genitalia development	1
mammary gland development	1
response to estradiol	1
uterus development	1
prostate gland growth	1
testosterone biosynthetic process	1
positive regulation of estradiol secretion	1

Indications & clinical

Indications

1 disease in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
precocious puberty	2	MONDO:0000088	MONDO:0000088

Clinical trials

Total trials: 4.

Phase distribution

Phase	Trials
PHASE2	2
PHASE4	1
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01065220	PHASE4	COMPLETED	Sex Steroids and the Serotonin Transporter
NCT00001521	PHASE3	COMPLETED	Three Drug Combination Therapy Versus Conventional Treatment of Children With Congenital Adrenal Hyperplasia
NCT00001181	PHASE2	COMPLETED	Testolactone for the Treatment of Girls With LHRH Resistant Precocious Puberty
NCT00001202	PHASE2	COMPLETED	Treatment of Boys With Precocious Puberty

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

40 molecules share ≥1 primary target. Top 40 by shared-target count:

Molecule	Source	Status	Shared targets
AMINOGLUTETHIMIDE	ChEMBL	Phase 4 (approved)	CYP19A1
ANASTROZOLE	ChEMBL	Phase 4 (approved)	CYP19A1
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	CYP19A1
ESTRONE	ChEMBL	Phase 4 (approved)	CYP19A1
EXEMESTANE	ChEMBL	Phase 4 (approved)	CYP19A1
FLUCONAZOLE	ChEMBL	Phase 4 (approved)	CYP19A1
FLUOROURACIL	ChEMBL	Phase 4 (approved)	CYP19A1
KETOCONAZOLE	ChEMBL	Phase 4 (approved)	CYP19A1
LETROZOLE	ChEMBL	Phase 4 (approved)	CYP19A1
MICONAZOLE	ChEMBL	Phase 4 (approved)	CYP19A1
NIMESULIDE	ChEMBL	Phase 4 (approved)	CYP19A1
OSILODROSTAT	ChEMBL	Phase 4 (approved)	CYP19A1
POSACONAZOLE	ChEMBL	Phase 4 (approved)	CYP19A1
TESTOSTERONE	ChEMBL	Phase 4 (approved)	CYP19A1
DOCONEXENT	ChEMBL	Phase 3	CYP19A1
ENDOXIFEN	ChEMBL	Phase 3	CYP19A1
ICOSAPENT	ChEMBL	Phase 3	CYP19A1
QUERCETIN	ChEMBL	Phase 3	CYP19A1
RESVERATROL	ChEMBL	Phase 3	CYP19A1
2-METHOXYESTRADIOL	ChEMBL	Phase 2	CYP19A1
AZALANSTAT	ChEMBL	Phase 2	CYP19A1
DAIDZEIN	ChEMBL	Phase 2	CYP19A1
DEXFADROSTAT	ChEMBL	Phase 2	CYP19A1
DOCOSAPENTAENOIC ACID	ChEMBL	Phase 2	CYP19A1
FADROZOLE	ChEMBL	Phase 2	CYP19A1
FLAVONE	ChEMBL	Phase 2	CYP19A1
FORMESTANE	ChEMBL	Phase 2	CYP19A1
GENISTEIN	ChEMBL	Phase 2	CYP19A1
IROSUSTAT	ChEMBL	Phase 2	CYP19A1
LIAROZOLE	ChEMBL	Phase 2	CYP19A1
LINOLEIC ACID	ChEMBL	Phase 2	CYP19A1
LUTEOLIN	ChEMBL	Phase 2	CYP19A1
OLEIC ACID	ChEMBL	Phase 2	CYP19A1
PINOCEMBRIN	ChEMBL	Phase 2	CYP19A1
PLOMESTANE	ChEMBL	Phase 2	CYP19A1
ROGLETIMIDE	ChEMBL	Phase 2	CYP19A1
STANOLONE	ChEMBL	Phase 2	CYP19A1
URSOLIC ACID	ChEMBL	Phase 2	CYP19A1
VOROZOLE	ChEMBL	Phase 2	CYP19A1
Fulvestrant	PubChem	Approved	CYP19A1