Methyltestosterone
drugOn this page
Also known as AndroidAndroid 10Android 25Android 5CDB-110L 589.372L-589.372L-589372MetandrenMethyltestosterone ciiiMetiltestosteronaMethitestNSC-139965NSC-9701OretonOreton methylOxandrolone impuritymethyltestosterone-Perandren
Summary
Methyltestosterone (CHEMBL1395) is an approved small-molecule antineoplastic agent (ATC G03BA02) targeting AR; indicated across 4 conditions including orchitis and hypogonadism.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: G03BA02 (+1 more)
- Targets: 1 (AR)
- Indications: 4 conditions
- Clinical trials: 3
- Chemistry: 302.5 Da · C20H30O2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1395 |
| Name | Methyltestosterone |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 6010 |
| ChEBI | CHEBI:27436 |
| ATC | G03BA02, G03EK01 |
| Molecular formula | C20H30O2 |
| Molecular weight | 302.5 |
| InChIKey | GCKMFJBGXUYNAG-HLXURNFRSA-N |
SMILES: C[C@]12CCC(=O)C=C1CC[C@@H]3[C@@H]2CC[C@]4([C@H]3CC[C@]4(C)O)C
IUPAC name: (8R,9S,10R,13S,14S,17S)-17-hydroxy-10,13,17-trimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-one
ChEBI definition: A 17β-hydroxy steroid that is testosterone bearing a methyl group at the 17α position.
Pharmacological roles (ChEBI): antineoplastic agent, anabolic agent, androgen.
Also known as: Android, Android 10, Android 25, Android 5, CDB-110, L 589.372, L-589.372, L-589372, Metandren, Methyltestosterone, Methyltestosterone ciii, Metiltestosterona
Patent coverage: 244,503 distinct patent families (486,600 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 |
|---|---|---|---|---|---|
| AR | Androgen receptor | Full agonist | 9.66 | P10275 |
Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Glucocorticoid receptor, Progesterone receptor, Alpha-1A adrenergic receptor, Androgen receptor, Sex hormone-binding globulin, Aldehyde dehydrogenase 1A1.
Bioactivity
ChEMBL activities: 9 potent at pChembl ≥ 5 of 12 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| SHBG | 8.43 | Kd | 3.71 | nM | CHEMBL_ACT_2155720 |
| P15207 | 8.37 | Ki | 4.27 | nM | CHEMBL_ACT_7638289 |
| P15207 | 8.21 | AC50 | 6.1 | nM | CHEMBL_ACT_25233053 |
| P15207 | 8.19 | IC50 | 6.4 | nM | CHEMBL_ACT_7638288 |
| P15207 | 7.8 | IC50 | 15.85 | nM | CHEMBL_ACT_1606528 |
| PGR | 6.7 | AC50 | 200 | nM | CHEMBL_ACT_25223316 |
| NR3C1 | 6.36 | AC50 | 440 | nM | CHEMBL_ACT_25176177 |
| NR3C1 | 6.08 | Ki | 838 | nM | CHEMBL_ACT_7636812 |
| NR3C1 | 5.73 | IC50 | 1843 | nM | CHEMBL_ACT_7636811 |
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 (3 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 |
|---|---|---|---|
| orchitis | 4 | MONDO:0006882 | EFO:1001078 |
| hypogonadism | 4 | MONDO:0002146 | MONDO:0002146 |
| breast neoplasm | 4 | MONDO:0021100 | MONDO:0007254 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 3.
Phase distribution
| Phase | Trials |
|---|---|
| Not specified | 2 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT04327934 | EARLY_PHASE1 | TERMINATED | Mechanisms of Hypertension in Women With Polycystic Ovary Syndrome |
| NCT01928108 | Not specified | COMPLETED | Fluid Intake Application to Reduce Kidney Stone Risks |
| NCT05728723 | Not specified | COMPLETED | The Effectiveness of the Android Application as a Pharmaceutical Education Tool in Hypertensive Patients |
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: orchitis, hypogonadism, breast neoplasm
- 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