Asoprisnil
drugOn this page
Also known as AsoprisniloJ-867J867Asoprinsil
Summary
Asoprisnil (CHEMBL267431) is a phase-3 clinical-stage small molecule targeting PGR; indicated across 6 conditions including uterine corpus leiomyoma and leiomyoma.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 1 (PGR)
- Indications: 6 conditions
- Clinical trials: 15
- Chemistry: 449.6 Da · C28H35NO4
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL267431 |
| Name | Asoprisnil |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 9577221 |
| Molecular formula | C28H35NO4 |
| Molecular weight | 449.6 |
| InChIKey | GJMNAFGEUJBOCE-MEQIQULJSA-N |
SMILES: C[C@]12C[C@@H](C3=C4CCC(=O)C=C4CC[C@H]3[C@@H]1CC[C@]2(COC)OC)C5=CC=C(C=C5)/C=N/O
IUPAC name: (8S,11R,13S,14S,17S)-11-[4-[(E)-hydroxyiminomethyl]phenyl]-17-methoxy-17-(methoxymethyl)-13-methyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one
Also known as: Asoprisnil, Asoprisnilo, J-867, J867, asoprisnil, Asoprinsil, ASOPRISNIL
Patent coverage: 488 distinct patent families (1,789 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 |
|---|---|---|---|---|---|
| PGR | Progesterone receptor | Antagonist | 9 | 0.1% | P06401 |
Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: Androgen receptor, Mineralocorticoid receptor, Glucocorticoid receptor, Estrogen receptor, Progesterone receptor.
Bioactivity
ChEMBL activities: 11 potent at pChembl ≥ 5 of 11 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| PGR | 9.7 | IC50 | 0.2 | nM | CHEMBL_ACT_2141342 |
| PGR | 9.52 | IC50 | 0.3 | nM | CHEMBL_ACT_12187253 |
| PGR | 9.52 | IC50 | 0.3 | nM | CHEMBL_ACT_12187298 |
| AR | 8.21 | IC50 | 6.1 | nM | CHEMBL_ACT_2120088 |
| AR | 8.05 | IC50 | 9 | nM | CHEMBL_ACT_12187251 |
| NR3C1 | 7.07 | IC50 | 85 | nM | CHEMBL_ACT_2120094 |
| NR3C1 | 6.92 | IC50 | 120 | nM | CHEMBL_ACT_12187249 |
| NR3C2 | 5.8 | IC50 | 1600 | nM | CHEMBL_ACT_12187248 |
| NR3C2 | 5.8 | IC50 | 1600 | nM | CHEMBL_ACT_2120101 |
| ESR1 | 5.72 | IC50 | 1900 | nM | CHEMBL_ACT_2120106 |
| ESR1 | 5.7 | IC50 | 2000 | nM | CHEMBL_ACT_12187247 |
Target pathways
Aggregated over 1 target gene(s): PGR.
Top Reactome pathways
7 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Nuclear signaling by ERBB4 | 1 | PGR |
| HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand | 1 | PGR |
| Nuclear Receptor transcription pathway | 1 | PGR |
| SUMOylation of intracellular receptors | 1 | PGR |
| Estrogen-dependent gene expression | 1 | PGR |
| Developmental Lineage of Mammary Gland Luminal Epithelial Cells | 1 | PGR |
| Developmental Lineage of Mammary Gland Alveolar Cells | 1 | PGR |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| ovulation from ovarian follicle | 1 |
| glandular epithelial cell maturation | 1 |
| regulation of DNA-templated transcription | 1 |
| regulation of transcription by RNA polymerase II | 1 |
| signal transduction | 1 |
| cell-cell signaling | 1 |
| positive regulation of gene expression | 1 |
| negative regulation of gene expression | 1 |
| nuclear receptor-mediated steroid hormone signaling pathway | 1 |
| paracrine signaling | 1 |
| positive regulation of transcription by RNA polymerase II | 1 |
| lung alveolus development | 1 |
| regulation of epithelial cell proliferation | 1 |
| progesterone receptor signaling pathway | 1 |
| maintenance of protein location in nucleus | 1 |
Indications & clinical
Indications
6 indications (0 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).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| uterine corpus leiomyoma | 3 | MONDO:0007886 | EFO:0000731 |
| leiomyoma | 3 | MONDO:0001572 | MONDO:0001572 |
| endometriosis | 2 | MONDO:0005133 | EFO:0001065 |
3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 15.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 9 |
| PHASE3 | 6 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00152256 | PHASE3 | COMPLETED | A Study to Evaluate of the Safety and Effectiveness of Asoprisnil in Treating Women With Uterine Fibroids |
| NCT00152269 | PHASE3 | COMPLETED | Treatment of Uterine Fibroids With Asoprisnil(J867) |
| NCT00156156 | PHASE3 | COMPLETED | Study of Asoprisnil in the Treatment of Uterine Fibroids. |
| NCT00156195 | PHASE3 | COMPLETED | Study to Evaluate the Safety of Asoprisnil in the Treatment of Uterine Fibroids |
| NCT00156208 | PHASE3 | COMPLETED | Safety of Treatment of Uterine Fibroids With Asoprisnil |
| NCT00160381 | PHASE3 | COMPLETED | A Study to Evaluate the Safety and Effectiveness of Asoprisnil in the Treatment of Uterine Fibroids |
| NCT00150644 | PHASE2 | COMPLETED | A Study to Evaluate the Effects of Asoprisnil(J867) in Women With Uterine Fibroids Who Are Scheduled for a Hysterectomy |
| NCT00152282 | PHASE2 | COMPLETED | A Study to Evaluate the Safety and Effectiveness of Asoprisnil and Estrogen Administration to Postmenopausal Women |
| NCT00152295 | PHASE2 | COMPLETED | A Long-Term Study to Evaluate the Safety of Asoprisnil and Estrogen Administration to Postmenopausal Women |
| NCT00156182 | PHASE2 | COMPLETED | A Long-Term Safety Study of Asoprisnil in the Treatment of Uterine Fibroids. |
| NCT00160420 | PHASE2 | COMPLETED | A Long-Term Study to Evaluate the Safety of Asoprisnil in the Treatment of Women With Endometriosis From Study M01-398 |
| NCT00160433 | PHASE2 | COMPLETED | A Study to Evaluate the Safety and Effectiveness of Asoprisnil in the Treatment of Women With Endometriosis. |
| NCT00160446 | PHASE2 | COMPLETED | A Study to Evaluate the Safety and Effectiveness of Three Asoprisnil Doses in the Treatment of Women With Endometriosis |
| NCT00160459 | PHASE2 | COMPLETED | A Study to Evaluate the Safety and Effectiveness of Asoprisnil in the Treatment of Uterine Fibroids |
| NCT00288691 | PHASE2 | COMPLETED | Menorrhagia Study in Women With Treatment-resistant Menorrhagia |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
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.
290 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| FIDAXOMICIN | ChEMBL + PubChem | Phase 4 (approved) | PGR |
| FULVESTRANT | ChEMBL + PubChem | Phase 4 (approved) | PGR |
| GENTIAN VIOLET | ChEMBL + PubChem | Phase 4 (approved) | PGR |
| ABIRATERONE | ChEMBL | Phase 4 (approved) | PGR |
| ACETYLCHOLINE | ChEMBL | Phase 4 (approved) | PGR |
| ADAPALENE | ChEMBL | Phase 4 (approved) | PGR |
| ALCLOMETASONE DIPROPIONATE | ChEMBL | Phase 4 (approved) | PGR |
| ALECTINIB | ChEMBL | Phase 4 (approved) | PGR |
| AMCINONIDE | ChEMBL | Phase 4 (approved) | PGR |
| APOMORPHINE | ChEMBL | Phase 4 (approved) | PGR |
| ARFORMOTEROL | ChEMBL | Phase 4 (approved) | PGR |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | PGR |
| AZATHIOPRINE | ChEMBL | Phase 4 (approved) | PGR |
| BECLOMETHASONE DIPROPIONATE | ChEMBL | Phase 4 (approved) | PGR |
| BENPERIDOL | ChEMBL | Phase 4 (approved) | PGR |
| BENZBROMARONE | ChEMBL | Phase 4 (approved) | PGR |
| BENZIODARONE | ChEMBL | Phase 4 (approved) | PGR |
| BETAMETHASONE | ChEMBL | Phase 4 (approved) | PGR |
| BETAMETHASONE DIPROPIONATE | ChEMBL | Phase 4 (approved) | PGR |
| BETAMETHASONE VALERATE | ChEMBL | Phase 4 (approved) | PGR |
| BEXAROTENE | ChEMBL | Phase 4 (approved) | PGR |
| BICALUTAMIDE | ChEMBL | Phase 4 (approved) | PGR |
| BIFONAZOLE | ChEMBL | Phase 4 (approved) | PGR |
| BITHIONOL | ChEMBL | Phase 4 (approved) | PGR |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | PGR |
| BUDESONIDE | ChEMBL | Phase 4 (approved) | PGR |
| BUTOCONAZOLE | ChEMBL | Phase 4 (approved) | PGR |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | PGR |
| CALCIPOTRIENE | ChEMBL | Phase 4 (approved) | PGR |
| CALCITRIOL | ChEMBL | Phase 4 (approved) | PGR |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | PGR |
| CANRENONE | ChEMBL | Phase 4 (approved) | PGR |
| CARBARIL | ChEMBL | Phase 4 (approved) | PGR |
| CASPOFUNGIN | ChEMBL | Phase 4 (approved) | PGR |
| CEFAMANDOLE | ChEMBL | Phase 4 (approved) | PGR |
| CEFMENOXIME | ChEMBL | Phase 4 (approved) | PGR |
| CEFTAZIDIME | ChEMBL | Phase 4 (approved) | PGR |
| CEFTIZOXIME | ChEMBL | Phase 4 (approved) | PGR |
| CEFTRIAXONE | ChEMBL | Phase 4 (approved) | PGR |
| CEFUROXIME | ChEMBL | Phase 4 (approved) | PGR |
| CEPHRADINE | ChEMBL | Phase 4 (approved) | PGR |
| CHLORHEXIDINE | ChEMBL | Phase 4 (approved) | PGR |
| CHLORMADINONE | ChEMBL | Phase 4 (approved) | PGR |
| CHOLECALCIFEROL | ChEMBL | Phase 4 (approved) | PGR |
| CICLESONIDE | ChEMBL | Phase 4 (approved) | PGR |
| CLOBETASOL PROPIONATE | ChEMBL | Phase 4 (approved) | PGR |
| CLOCORTOLONE PIVALATE | ChEMBL | Phase 4 (approved) | PGR |
| CLOMIPHENE | ChEMBL | Phase 4 (approved) | PGR |
| CYCLOFENIL | ChEMBL | Phase 4 (approved) | PGR |
| DANAZOL | ChEMBL | Phase 4 (approved) | PGR |
| DAUNORUBICIN | ChEMBL | Phase 4 (approved) | PGR |
| DEFLAZACORT | ChEMBL | Phase 4 (approved) | PGR |
| DEQUALINIUM | ChEMBL | Phase 4 (approved) | PGR |
| DESOGESTREL | ChEMBL | Phase 4 (approved) | PGR |
| DESONIDE | ChEMBL | Phase 4 (approved) | PGR |
| DESOXIMETASONE | ChEMBL | Phase 4 (approved) | PGR |
| DESOXYCORTICOSTERONE PIVALATE | ChEMBL | Phase 4 (approved) | PGR |
| DEXAMETHASONE | ChEMBL | Phase 4 (approved) | PGR |
| DIETHYLPROPION | ChEMBL | Phase 4 (approved) | PGR |
| DIETHYLSTILBESTROL | ChEMBL | Phase 4 (approved) | PGR |
Related Atlas pages
- Genes: PGR
- Diseases: uterine corpus leiomyoma, leiomyoma
- Drugs: Fidaxomicin, Fulvestrant, Abiraterone, Acetylcholine, Adapalene, Alclometasone Dipropionate, Alectinib, Amcinonide, Apomorphine, Arformoterol, Aripiprazole, Azathioprine, Beclomethasone Dipropionate, Benperidol, Benzbromarone, Benziodarone, Betamethasone, Betamethasone Dipropionate, Betamethasone Valerate, Bexarotene, Bicalutamide, Bifonazole, Bithionol, Bosutinib, Budesonide, Butoconazole, Cabozantinib, Calcipotriene, Calcitriol, Candesartan Cilexetil, Canrenone, Carbaril, Caspofungin, Cefamandole, Cefmenoxime, Ceftazidime, Ceftizoxime, Ceftriaxone, Cefuroxime, Cephradine, Chlorhexidine, Chlormadinone, Cholecalciferol, Ciclesonide, Clobetasol Propionate, Clocortolone Pivalate, Clomiphene, Cyclofenil, Danazol, Daunorubicin, Deflazacort, Dequalinium, Desogestrel, Desonide, Desoximetasone, Desoxycorticosterone Pivalate, Dexamethasone, Diethylpropion, Diethylstilbestrol