Pruxelutamide
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Also known as Gt-0918Gt0918Proxalutamide
Summary
Pruxelutamide (CHEMBL4594417) is a phase-3 clinical-stage small molecule targeting AR; indicated across 4 conditions including severe acute respiratory syndrome and breast neoplasm.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 1 (AR)
- Indications: 4 conditions
- Clinical trials: 11
- Chemistry: 517.5 Da · C24H19F4N5O2S
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL4594417 |
| Name | Pruxelutamide |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 60194102 |
| Molecular formula | C24H19F4N5O2S |
| Molecular weight | 517.5 |
| InChIKey | KCBJGVDOSBKVKP-UHFFFAOYSA-N |
SMILES: CC1(C(=O)N(C(=S)N1C2=CN=C(C=C2)CCCC3=NC=CO3)C4=C(C(=C(C=C4)C#N)C(F)(F)F)F)C
IUPAC name: 4-[4,4-dimethyl-3-[6-[3-(1,3-oxazol-2-yl)propyl]-3-pyridinyl]-5-oxo-2-sulfanylideneimidazolidin-1-yl]-3-fluoro-2-(trifluoromethyl)benzonitrile
Also known as: Gt-0918, Gt0918, Proxalutamide, Pruxelutamide, PRUXELUTAMIDE
Patent coverage: 60 distinct patent families (185 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 163 (88%) of the total. 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 |
|---|---|---|---|---|---|
| AR | Androgen receptor | Antagonist | 7.49 | P10275 |
Bioactivity
No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).
Target pathways
Aggregated over 1 target gene(s): AR.
Top Reactome pathways
23 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 1 | AR |
| Signaling by Rho GTPases | 1 | AR |
| RHO GTPase Effectors | 1 | AR |
| Generic Transcription Pathway | 1 | AR |
| Cellular responses to stress | 1 | AR |
| SUMOylation | 1 | AR |
| SUMO E3 ligases SUMOylate target proteins | 1 | AR |
| HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand | 1 | AR |
| Nuclear Receptor transcription pathway | 1 | AR |
| Metabolism of proteins | 1 | AR |
| SUMOylation of intracellular receptors | 1 | AR |
| RHO GTPases activate PKNs | 1 | AR |
| Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3 | 1 | AR |
| Deubiquitination | 1 | AR |
| Ub-specific processing proteases | 1 | AR |
| Post-translational protein modification | 1 | AR |
| RNA Polymerase II Transcription | 1 | AR |
| Gene expression (Transcription) | 1 | AR |
| Transcriptional regulation by RUNX2 | 1 | AR |
| RUNX2 regulates osteoblast differentiation | 1 | AR |
| RUNX2 regulates bone development | 1 | AR |
| Cellular responses to stimuli | 1 | AR |
| Signaling by Rho GTPases, Miro GTPases and RHOBTB3 | 1 | AR |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| negative regulation of transcription by RNA polymerase II | 1 |
| MAPK cascade | 1 |
| in utero embryonic development | 1 |
| regulation of systemic arterial blood pressure | 1 |
| epithelial cell morphogenesis | 1 |
| transcription by RNA polymerase II | 1 |
| signal transduction | 1 |
| cell-cell signaling | 1 |
| spermatogenesis | 1 |
| single fertilization | 1 |
| positive regulation of cell population proliferation | 1 |
| negative regulation of cell population proliferation | 1 |
| male gonad development | 1 |
| positive regulation of gene expression | 1 |
| male somatic sex determination | 1 |
Indications & clinical
Indications
4 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 |
|---|---|---|---|
| severe acute respiratory syndrome | 3 | MONDO:0005091 | MONDO:0100096 |
| breast neoplasm | 1 | MONDO:0021100 | MONDO:0007254 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 11.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 6 |
| PHASE2 | 2 |
| PHASE1 | 2 |
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT04728802 | PHASE3 | COMPLETED | Proxalutamide Treatment for Hospitalized COVID-19 Patients |
| NCT04853134 | PHASE3 | WITHDRAWN | Proxalutamide Treatment for COVID-19 Female Outpatients |
| NCT04853927 | PHASE3 | WITHDRAWN | Proxalutamide Treatment for COVID-19 Patients in Intensive Care Unit |
| NCT04870606 | PHASE3 | COMPLETED | Proxalutamide (GT0918) Treatment for Outpatients With Mild or Moderate COVID-19 Illness |
| NCT05009732 | PHASE3 | TERMINATED | A Study to Evaluate the Efficacy and Safety of Proxalutamide (GT0918) in Hospitalized COVID-19 Subjects |
| NCT05126628 | PHASE3 | COMPLETED | The South Proxa-Rescue AndroCoV Trial Against COVID-19 |
| NCT03899467 | PHASE2 | COMPLETED | The Safety and Tolerability of GT0918 in Subjects With mHSPC and mCRPC |
| NCT05076851 | PHASE2 | UNKNOWN | Neoadjuvant Therapy With Proxalutamide Combined With Androgen Deprivation Therapy（ADT）for High Risk Prostate Cancer |
| NCT02826772 | PHASE1 | COMPLETED | Safety, Tolerability, and PK of GT0918 (Proxalutamide) in Subjects With Metastatic Castrate Prostate Cancer |
| NCT04103853 | PHASE1 | COMPLETED | Safety, Tolerability, and Pharmacokinetics of Proxalutamide Therapy in Women With Metastatic Breast Cancer |
| NCT04446429 | Not specified | COMPLETED | Anti-Androgen Treatment for COVID-19 |
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.
130 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| MEGESTROL | ChEMBL + PubChem | Phase 4 (approved) | AR |
| ABIRATERONE | ChEMBL | Phase 4 (approved) | AR |
| APALUTAMIDE | ChEMBL | Phase 4 (approved) | AR |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | AR |
| BECLOMETHASONE DIPROPIONATE | ChEMBL | Phase 4 (approved) | AR |
| BETAMETHASONE | ChEMBL | Phase 4 (approved) | AR |
| BICALUTAMIDE | ChEMBL | Phase 4 (approved) | AR |
| BITHIONOL | ChEMBL | Phase 4 (approved) | AR |
| BROMHEXINE | ChEMBL | Phase 4 (approved) | AR |
| BUDESONIDE | ChEMBL | Phase 4 (approved) | AR |
| CHLORMADINONE | ChEMBL | Phase 4 (approved) | AR |
| CLARITHROMYCIN | ChEMBL | Phase 4 (approved) | AR |
| CLASCOTERONE | ChEMBL | Phase 4 (approved) | AR |
| CLOCORTOLONE PIVALATE | ChEMBL | Phase 4 (approved) | AR |
| CLOMIPHENE | ChEMBL | Phase 4 (approved) | AR |
| CORTISONE | ChEMBL | Phase 4 (approved) | AR |
| CYCLOFENIL | ChEMBL | Phase 4 (approved) | AR |
| DAROLUTAMIDE | ChEMBL | Phase 4 (approved) | AR |
| DESOGESTREL | ChEMBL | Phase 4 (approved) | AR |
| DESOXIMETASONE | ChEMBL | Phase 4 (approved) | AR |
| DEXAMETHASONE | ChEMBL | Phase 4 (approved) | AR |
| DIETHYLSTILBESTROL | ChEMBL | Phase 4 (approved) | AR |
| DIFLORASONE DIACETATE | ChEMBL | Phase 4 (approved) | AR |
| DORZOLAMIDE | ChEMBL | Phase 4 (approved) | AR |
| DROSPIRENONE | ChEMBL | Phase 4 (approved) | AR |
| DYDROGESTERONE | ChEMBL | Phase 4 (approved) | AR |
| ENZALUTAMIDE | ChEMBL | Phase 4 (approved) | AR |
| EPLERENONE | ChEMBL | Phase 4 (approved) | AR |
| ESTRADIOL | ChEMBL | Phase 4 (approved) | AR |
| ESTRADIOL CYPIONATE | ChEMBL | Phase 4 (approved) | AR |
| ESTRADIOL VALERATE | ChEMBL | Phase 4 (approved) | AR |
| ESTRIOL | ChEMBL | Phase 4 (approved) | AR |
| ESTRONE | ChEMBL | Phase 4 (approved) | AR |
| ETHINYL ESTRADIOL | ChEMBL | Phase 4 (approved) | AR |
| ETHYNODIOL DIACETATE | ChEMBL | Phase 4 (approved) | AR |
| ETONOGESTREL | ChEMBL | Phase 4 (approved) | AR |
| FLUMETHASONE PIVALATE | ChEMBL | Phase 4 (approved) | AR |
| FLUOCINOLONE ACETONIDE | ChEMBL | Phase 4 (approved) | AR |
| FLUOCINONIDE | ChEMBL | Phase 4 (approved) | AR |
| FLUOXYMESTERONE | ChEMBL | Phase 4 (approved) | AR |
| FLURANDRENOLIDE | ChEMBL | Phase 4 (approved) | AR |
| FLUTAMIDE | ChEMBL | Phase 4 (approved) | AR |
| FLUTICASONE FUROATE | ChEMBL | Phase 4 (approved) | AR |
| FLUTICASONE PROPIONATE | ChEMBL | Phase 4 (approved) | AR |
| HALCINONIDE | ChEMBL | Phase 4 (approved) | AR |
| HALOBETASOL PROPIONATE | ChEMBL | Phase 4 (approved) | AR |
| HEXACHLOROPHENE | ChEMBL | Phase 4 (approved) | AR |
| HEXESTROL | ChEMBL | Phase 4 (approved) | AR |
| HYDROCORTISONE | ChEMBL | Phase 4 (approved) | AR |
| INDOMETHACIN | ChEMBL | Phase 4 (approved) | AR |
| LEVONORGESTREL | ChEMBL | Phase 4 (approved) | AR |
| MEDROXYPROGESTERONE | ChEMBL | Phase 4 (approved) | AR |
| METHYLPREDNISOLONE | ChEMBL | Phase 4 (approved) | AR |
| MIFEPRISTONE | ChEMBL | Phase 4 (approved) | AR |
| MOMETASONE FUROATE | ChEMBL | Phase 4 (approved) | AR |
| NILUTAMIDE | ChEMBL | Phase 4 (approved) | AR |
| NOMEGESTROL | ChEMBL | Phase 4 (approved) | AR |
| NORETHINDRONE | ChEMBL | Phase 4 (approved) | AR |
| NORETHYNODREL | ChEMBL | Phase 4 (approved) | AR |
| OXANDROLONE | ChEMBL | Phase 4 (approved) | AR |
Related Atlas pages
- Genes: AR
- Diseases: severe acute respiratory syndrome
- Drugs: Megestrol, Abiraterone, Apalutamide, Aripiprazole, Beclomethasone Dipropionate, Betamethasone, Bicalutamide, Bithionol, Bromhexine, Budesonide, Chlormadinone, Clarithromycin, Clascoterone, Clocortolone Pivalate, Clomiphene, Cortisone, Cyclofenil, Darolutamide, Desogestrel, Desoximetasone, Dexamethasone, Diethylstilbestrol, Diflorasone Diacetate, Dorzolamide, Drospirenone, Dydrogesterone, Enzalutamide, Eplerenone, Estradiol, Estradiol Cypionate, Estradiol Valerate, Estriol, Estrone, Ethinyl Estradiol, Ethynodiol Diacetate, Etonogestrel, Flumethasone Pivalate, Fluocinolone Acetonide, Fluocinonide, Fluoxymesterone, Flurandrenolide, Flutamide, Fluticasone Furoate, Fluticasone Propionate, Halcinonide, Halobetasol Propionate, Hexachlorophene, Hexestrol, Hydrocortisone, Indomethacin, Levonorgestrel, Medroxyprogesterone, Methylprednisolone, Mifepristone, Mometasone Furoate, Nilutamide, Norethindrone, Norethynodrel, Oxandrolone