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Atlas / Drug / Levonorgestrel

Levonorgestrel

drug
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Also known as Athentia nextEmerresEmerres unaEzinelleFallback soloHer styleIsterandaJadelleJaydessKyleenaLevonelleLevonelle one stepLevonelle-2Levonorgestrel component of afirmelleLevonorgestrel component of alesseLevonorgestrel component of altaveraLevonorgestrel component of avianeLevonorgestrel component of balcoltraLevonorgestrel component of climara pro

Summary

Levonorgestrel (CHEMBL1389) is an approved small-molecule female contraceptive drug (ATC G03AD01) targeting PGR; indicated across 21 conditions including endometriosis and migraine disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: G03AD01 (+1 more)
  • Targets: 1 (PGR)
  • Indications: 21 conditions
  • Clinical trials: 106
  • Chemistry: 312.4 Da · C21H28O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1389
NameLevonorgestrel
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID13109
ChEBICHEBI:6443
ATCG03AD01, G03AC03
Molecular formulaC21H28O2
Molecular weight312.4
InChIKeyWWYNJERNGUHSAO-XUDSTZEESA-N

SMILES: CC[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@]2(C#C)O)CCC4=CC(=O)CC[C@H]34

IUPAC name: (8R,9S,10R,13S,14S,17R)-13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one

ChEBI definition: The (−)-enantiomer of norgestrel.

Pharmacological roles (ChEBI): progestin, synthetic oral contraceptive, female contraceptive drug.

Also known as: Athentia next, Emerres, Emerres una, Ezinelle, Fallback solo, Her style, Isteranda, Jadelle, Jaydess, Kyleena, Levonelle, Levonelle one step

Patent coverage: 7,708 distinct patent families (23,643 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).

GeneTargetActionpAffinityCancer dependencyUniProt
PGRProgesterone receptorAgonist0.1%P06401

Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Androgen receptor, Estrogen receptor, Progesterone receptor, Sodium-dependent serotonin transporter, Gamma-aminobutyric acid receptor subunit alpha-1, Bile salt export pump.

Bioactivity

ChEMBL activities: 6 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
PGR9EC501nMCHEMBL_ACT_24858585
PGR9EC501nMCHEMBL_ACT_24858586
PGR8.52AC503nMCHEMBL_ACT_25204362
AR8.04AC509.2nMCHEMBL_ACT_25203429
P628135.46AC503440nMCHEMBL_ACT_25207932
ESR15.06AC508647nMCHEMBL_ACT_25138929

Target pathways

Aggregated over 1 target gene(s): PGR.

Top Reactome pathways

7 total, by targets touching each:

PathwayTargetsGenes
Nuclear signaling by ERBB41PGR
HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand1PGR
Nuclear Receptor transcription pathway1PGR
SUMOylation of intracellular receptors1PGR
Estrogen-dependent gene expression1PGR
Developmental Lineage of Mammary Gland Luminal Epithelial Cells1PGR
Developmental Lineage of Mammary Gland Alveolar Cells1PGR

Dominant GO biological processes

GO termTargets
ovulation from ovarian follicle1
glandular epithelial cell maturation1
regulation of DNA-templated transcription1
regulation of transcription by RNA polymerase II1
signal transduction1
cell-cell signaling1
positive regulation of gene expression1
negative regulation of gene expression1
nuclear receptor-mediated steroid hormone signaling pathway1
paracrine signaling1
positive regulation of transcription by RNA polymerase II1
lung alveolus development1
regulation of epithelial cell proliferation1
progesterone receptor signaling pathway1
maintenance of protein location in nucleus1

Indications & clinical

Indications

21 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
endometriosis3MONDO:0005133EFO:0001065
migraine disorder3MONDO:0005277MONDO:0005277
anorexia nervosa3MONDO:0005351MONDO:0005351
HIV infectious disease2MONDO:0005109EFO:0000764
ovarian carcinoma2MONDO:0005140EFO:0001075
adenomyosis2MONDO:0010888EFO:1001757
endometrial carcinoma2MONDO:0002447EFO:1001512
B-cell chronic lymphocytic leukemia1MONDO:0004948EFO:0000095
chronic hepatitis C virus infection1MONDO:0005354EFO:0004220
chronic hepatitis B virus infection1MONDO:0005366EFO:0004239
metabolic dysfunction-associated steatohepatitis1MONDO:0007027EFO:1001249
type 2 diabetes mellitus1MONDO:0005148MONDO:0005148
neoplasm1MONDO:0005070MONDO:0004992
diabetes mellitus1MONDO:0005015EFO:0000400

7 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 106.

Phase distribution

PhaseTrials
PHASE130
Not specified22
PHASE219
PHASE416
PHASE314
PHASE2/PHASE34
PHASE1/PHASE21

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05058872PHASE4RECRUITINGContraceptive Hormone and Reward Measurement (CHARM Study)
NCT00131885PHASE4COMPLETEDEffects of St. John’s Wort on the Oral Contraceptive Hormone Levonorgestrel
NCT00204451PHASE4COMPLETEDHuman Ovarian Follicular Dynamics and Emergency Contraception
NCT00498784PHASE4COMPLETEDHR-QoL and Sexuality in Mirena Inserted Contraception Users
NCT00570440PHASE4COMPLETEDContinuous Use of COCs
NCT00662454PHASE4COMPLETEDOral Contraceptive Efficacy and Body Weight
NCT00696202PHASE4COMPLETEDMirena Efficiency and Tolerability During the First Year of Use
NCT01074892PHASE4COMPLETEDA Study Comparing Mirena and Systemic Progestin for Endometrial Hyperplasia
NCT01501448PHASE4COMPLETEDOral Estradiol Valerate Versus Oral Contraceptive Pill in Invitro Fertilization Patients
NCT01569113PHASE4COMPLETEDAssessment of Effects on Ovarian Activity of a Combined Oral Contraceptive Pill When Preceded by the Intake of ellaOne® or Placebo.
NCT02480647PHASE4COMPLETEDClinical Trial the Use of Levonorgestrel-releasing Intrauterine System Versus Etonogestrel Implant in Endometriosis
NCT02531321PHASE4TERMINATEDProtease Inhibitors and Combined Oral Contraceptive Pharmacokinetics and Pharmacodynamics
NCT02706509PHASE4UNKNOWNPain Management Associated With the Insertion of Jaydess® in Nulliparous Women
NCT02957292PHASE4COMPLETEDA Study to Compare the Menstrual Bleeding Profile Among Jaydess® and Copper Intrauterine Device (IUD) Users. COLIBRI STUDY (Copper and Levonorgestrel IUD Barcelona Research Initiative).
NCT03537768PHASE4TERMINATEDStudy Comparing Emergency Contraception Effectiveness in Women Who Weight ≥ 80 kg
NCT04910711PHASE4UNKNOWNInvestigating the Interaction Between Two Long-acting Reversible Methods of Contraception and Dolutegravir, a Treatment for HIV
NCT06492889PHASE2/PHASE3NOT_YET_RECRUITINGAssessing the Efficacy and Acceptability of Two Missed Period Pills Regimens
NCT06727734PHASE3RECRUITINGLevonorgestrel-piroxicam Versus Ulipristal Acetate for Emergency Contraception
NCT00128934PHASE3COMPLETEDStudy Evaluating Combination of Levonorgestrel (LNG) and Ethinyl Estradiol (EE) in Premenstrual Dysphoric Disorder
NCT00161681PHASE3COMPLETEDStudy Evaluating Levonorgestrel/Ethinyl Estradiol (LNG/EE) in PMS
NCT00195559PHASE3COMPLETEDStudy Evaluating Combination of Levonorgestrel and Ethinyl Estradiol in Pre-Menstrual Dysphoric Disorder
NCT00245921PHASE3COMPLETEDStudy Evaluating Levonorgestrel and Ethinyl Estradiol for Oral Contraception
NCT00271583PHASE2/PHASE3COMPLETEDEfficacy Trial of CDB 2914 for Emergency Contraception
NCT00511355PHASE3COMPLETEDEffects on Hemostasis, Lipids, Carbohydrate Metabolism, Adrenal & Thyroid Function of the Combined Oral Contraceptive NOMAC-E2 Compared to a COC Containing LNG-EE (292004)(COMPLETED)(P05764)
NCT00551616PHASE3COMPLETEDSafety and Efficacy of CDB-2914 in Comparison to Levonorgestrel for Emergency Contraception
NCT00922233PHASE3COMPLETEDPericoital Oral Contraception With Levonorgestrel
NCT00995150PHASE3TERMINATEDA Study of a Levonorgestrel-Releasing Intrauterine System for Long-Term, Reversible Contraception
NCT01695902PHASE3COMPLETEDTherapeutic Equivalence Trial of Two Hormonal-IUDs in Patients With Heavy Menstrual Bleeding
NCT02021097PHASE3UNKNOWNStudy Evaluating Levonorgestrel and Ethinyl Estradiol for Oral Contraception
NCT02403401PHASE3COMPLETEDSafety and Contraceptive Efficacy of an Intravaginal Ring With LNG (Levonorgestrel) Over One Year in Healthy Women
NCT02599077PHASE2/PHASE3SUSPENDEDImpact vs. Dienogest: A Combined Oral Contraceptive in the Size of Endometriomas
NCT03359057PHASE3COMPLETEDTrial Evaluating Folic Acid Supplementation by Concomitant Administration of Ethinyl Estradiol + Levonorgestrel
NCT03614494PHASE2/PHASE3COMPLETEDPiroxicam and Levonorgestrel Co-treatment for Emergency Contraception
NCT04007874PHASE3UNKNOWNOral Contraceptive Pill Compared With Vitamin E in Women With Migraine
NCT01686126PHASE2ACTIVE_NOT_RECRUITINGImproving the Treatment for Women With Early Stage Cancer of the Uterus
NCT05695352PHASE2RECRUITINGOral Levonorgestrel Plus Meloxicam, IG-002 Delays Ovulation in Normal Menstruating Women by Seven Days
NCT06073184PHASE2NOT_YET_RECRUITINGWeight-loss Drug for Fertility-Sparing Treatment of Atypical Hyperplasia and Low-grade Cancer of the Endometrium
NCT06306131PHASE2RECRUITINGPhase II Study of Ovulation in Obese Women
NCT07222228PHASE2NOT_YET_RECRUITINGA Study to Evaluate the Efficacy and Safety of Subcutaneous Levonorgestrel Butanoate for Female Contraception
NCT00033358PHASE2COMPLETEDHormone Therapy in Preventing Endometrial Cancer in Patients With a Genetic Risk For Hereditary Nonpolyposis Colon Cancer

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 9 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

290 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
FIDAXOMICINChEMBL + PubChemPhase 4 (approved)PGR
FULVESTRANTChEMBL + PubChemPhase 4 (approved)PGR
GENTIAN VIOLETChEMBL + PubChemPhase 4 (approved)PGR
ABIRATERONEChEMBLPhase 4 (approved)PGR
ACETYLCHOLINEChEMBLPhase 4 (approved)PGR
ADAPALENEChEMBLPhase 4 (approved)PGR
ALCLOMETASONE DIPROPIONATEChEMBLPhase 4 (approved)PGR
ALECTINIBChEMBLPhase 4 (approved)PGR
AMCINONIDEChEMBLPhase 4 (approved)PGR
APOMORPHINEChEMBLPhase 4 (approved)PGR
ARFORMOTEROLChEMBLPhase 4 (approved)PGR
ARIPIPRAZOLEChEMBLPhase 4 (approved)PGR
AZATHIOPRINEChEMBLPhase 4 (approved)PGR
BECLOMETHASONE DIPROPIONATEChEMBLPhase 4 (approved)PGR
BENPERIDOLChEMBLPhase 4 (approved)PGR
BENZBROMARONEChEMBLPhase 4 (approved)PGR
BENZIODARONEChEMBLPhase 4 (approved)PGR
BETAMETHASONEChEMBLPhase 4 (approved)PGR
BETAMETHASONE DIPROPIONATEChEMBLPhase 4 (approved)PGR
BETAMETHASONE VALERATEChEMBLPhase 4 (approved)PGR
BEXAROTENEChEMBLPhase 4 (approved)PGR
BICALUTAMIDEChEMBLPhase 4 (approved)PGR
BIFONAZOLEChEMBLPhase 4 (approved)PGR
BITHIONOLChEMBLPhase 4 (approved)PGR
BOSUTINIBChEMBLPhase 4 (approved)PGR
BUDESONIDEChEMBLPhase 4 (approved)PGR
BUTOCONAZOLEChEMBLPhase 4 (approved)PGR
CABOZANTINIBChEMBLPhase 4 (approved)PGR
CALCIPOTRIENEChEMBLPhase 4 (approved)PGR
CALCITRIOLChEMBLPhase 4 (approved)PGR
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)PGR
CANRENONEChEMBLPhase 4 (approved)PGR
CARBARILChEMBLPhase 4 (approved)PGR
CASPOFUNGINChEMBLPhase 4 (approved)PGR
CEFAMANDOLEChEMBLPhase 4 (approved)PGR
CEFMENOXIMEChEMBLPhase 4 (approved)PGR
CEFTAZIDIMEChEMBLPhase 4 (approved)PGR
CEFTIZOXIMEChEMBLPhase 4 (approved)PGR
CEFTRIAXONEChEMBLPhase 4 (approved)PGR
CEFUROXIMEChEMBLPhase 4 (approved)PGR
CEPHRADINEChEMBLPhase 4 (approved)PGR
CHLORHEXIDINEChEMBLPhase 4 (approved)PGR
CHLORMADINONEChEMBLPhase 4 (approved)PGR
CHOLECALCIFEROLChEMBLPhase 4 (approved)PGR
CICLESONIDEChEMBLPhase 4 (approved)PGR
CLOBETASOL PROPIONATEChEMBLPhase 4 (approved)PGR
CLOCORTOLONE PIVALATEChEMBLPhase 4 (approved)PGR
CLOMIPHENEChEMBLPhase 4 (approved)PGR
CYCLOFENILChEMBLPhase 4 (approved)PGR
DANAZOLChEMBLPhase 4 (approved)PGR
DAUNORUBICINChEMBLPhase 4 (approved)PGR
DEFLAZACORTChEMBLPhase 4 (approved)PGR
DEQUALINIUMChEMBLPhase 4 (approved)PGR
DESOGESTRELChEMBLPhase 4 (approved)PGR
DESONIDEChEMBLPhase 4 (approved)PGR
DESOXIMETASONEChEMBLPhase 4 (approved)PGR
DESOXYCORTICOSTERONE PIVALATEChEMBLPhase 4 (approved)PGR
DEXAMETHASONEChEMBLPhase 4 (approved)PGR
DIETHYLPROPIONChEMBLPhase 4 (approved)PGR
DIETHYLSTILBESTROLChEMBLPhase 4 (approved)PGR

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot