Linrodostat
drugOn this page
Also known as BMS 986205Bms-986205F 001287F-001287F001287ONO 7701ONO-7701ONO7701
Summary
Linrodostat (CHEMBL4297598) is a phase-3 clinical-stage small molecule targeting IDO1; indicated across 13 conditions including melanoma and non-small cell lung carcinoma.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 1 (IDO1)
- Indications: 13 conditions
- Clinical trials: 18
- Chemistry: 410.9 Da · C24H24ClFN2O
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL4297598 |
| Name | Linrodostat |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 121328278 |
| Molecular formula | C24H24ClFN2O |
| Molecular weight | 410.9 |
| InChIKey | KRTIYQIPSAGSBP-KLAILNCOSA-N |
SMILES: C[C@H](C1CCC(CC1)C2=C3C=C(C=CC3=NC=C2)F)C(=O)NC4=CC=C(C=C4)Cl
IUPAC name: (2R)-N-(4-chlorophenyl)-2-[4-(6-fluoroquinolin-4-yl)cyclohexyl]propanamide
Also known as: BMS 986205, Bms-986205, BMS-986205, F 001287, F-001287, F001287, Linrodostat, ONO 7701, ONO-7701, ONO7701, LINRODOSTAT
Parent form; salt/anhydrous children: CHEMBL4298147
Patent coverage: 539 distinct patent families (1,679 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,643 (98%) 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 |
|---|---|---|---|---|---|
| IDO1 | indoleamine 2,3-dioxygenase 1 | Inhibition | 0% | P14902 |
Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Indoleamine 2,3-dioxygenase 1.
Bioactivity
ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| IDO1 | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_24711536 |
| IDO1 | 8.77 | IC50 | 1.7 | nM | CHEMBL_ACT_24518920 |
Target pathways
Aggregated over 1 target gene(s): IDO1.
Top Reactome pathways
1 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Tryptophan catabolism | 1 | IDO1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| positive regulation of T cell tolerance induction | 1 |
| positive regulation of chronic inflammatory response | 1 |
| positive regulation of type 2 immune response | 1 |
| L-tryptophan catabolic process | 1 |
| inflammatory response | 1 |
| female pregnancy | 1 |
| obsolete L-tryptophan catabolic process to L-kynurenine | 1 |
| quinolinate biosynthetic process | 1 |
| response to lipopolysaccharide | 1 |
| negative regulation of interleukin-10 production | 1 |
| positive regulation of interleukin-12 production | 1 |
| multicellular organismal response to stress | 1 |
| kynurenic acid biosynthetic process | 1 |
| ‘de novo’ NAD+ biosynthetic process from L-tryptophan | 1 |
| swimming behavior | 1 |
Indications & clinical
Indications
13 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 |
|---|---|---|---|
| melanoma | 3 | MONDO:0005105 | EFO:0000756 |
| non-small cell lung carcinoma | 3 | MONDO:0005233 | EFO:0003060 |
| head and neck cancer | 3 | MONDO:0005627 | EFO:0006859 |
| skin neoplasm | 3 | MONDO:0002531 | MONDO:0002898 |
| lung neoplasm | 3 | MONDO:0021117 | MONDO:0008903 |
| gastric neoplasm | 2 | MONDO:0021085 | MONDO:0001056 |
| oral cavity squamous cell carcinoma | 2 | MONDO:0004958 | EFO:0000199 |
| urinary bladder neoplasm | 2 | MONDO:0004987 | EFO:0000294 |
| neoplasm | 2 | MONDO:0005070 | EFO:0000616 |
| hepatocellular carcinoma | 1 | MONDO:0007256 | EFO:0000182 |
| glioblastoma | 1 | MONDO:0018177 | EFO:0000519 |
| hematopoietic and lymphoid system neoplasm | 1 | MONDO:0002334 | MONDO:0002334 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 18.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1 | 7 |
| PHASE2 | 5 |
| PHASE3 | 3 |
| PHASE1/PHASE2 | 3 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03329846 | PHASE3 | COMPLETED | An Investigational Immuno-therapy Study of BMS-986205 Combined With Nivolumab, Compared to Nivolumab by Itself, in Patients With Advanced Melanoma |
| NCT03386838 | PHASE3 | WITHDRAWN | An Immuno-therapy Study of Nivolumab in Combination With Experimental Medication BMS-986205 Compared to Standard of Care EXTREME Regimen in First-line Recurrent/Metastatic Squamous Cell Carcinoma of Head and Neck |
| NCT03417037 | PHASE3 | WITHDRAWN | An Immuno-Therapy Study of Experimental Medication BMS-986205 Given With Nivolumab With or Without Chemotherapy Compared to Chemotherapy in Participants With Previously Untreated Stage IV or Recurrent Non-Small Cell Lung Cancer |
| NCT02658890 | PHASE1/PHASE2 | COMPLETED | An Investigational Immuno-therapy Study of BMS-986205 Given in Combination With Nivolumab and in Combination With Both Nivolumab and Ipilimumab in Cancers That Are Advanced or Have Spread |
| NCT02750514 | PHASE2 | TERMINATED | An Investigational Immuno-therapy Study to Test Combination Treatments in Patients With Advanced Non-Small Cell Lung Cancer |
| NCT02935634 | PHASE2 | COMPLETED | A Study to Test Combination Treatments in Participants With Advanced Gastric Cancer |
| NCT02996110 | PHASE2 | COMPLETED | A Study to Test Combination Treatments in People With Advanced Renal Cell Carcinoma |
| NCT03459222 | PHASE1/PHASE2 | COMPLETED | An Investigational Study of Immunotherapy Combinations in Participants With Solid Cancers That Are Advanced or Have Spread |
| NCT03519256 | PHASE2 | TERMINATED | A Study of Nivolumab or Nivolumab Plus Experimental Medication BMS-986205 With or Without Bacillus Calumette-Guerin (BCG) in BCG Unresponsive Bladder Cancer That Has Not Invaded Into the Muscle Wall of the Bladder |
| NCT03792750 | PHASE1/PHASE2 | COMPLETED | A Study of BMS-986205 Alone and in Combination With Nivolumab in Chinese Patients With Advanced Malignant Solid Tumors |
| NCT04007588 | PHASE2 | WITHDRAWN | A Phase II Trial of Neoadjuvant Treatment With PD-1 Inhibition (Nivolumab) With or Without IDO Inhibition (BMS-986205) and With or Without CTLA-4 Inhibition (Ipilimumab) in Resectable Stage III or IV Melanoma |
| NCT03192943 | PHASE1 | COMPLETED | A Study of BMS-986205 Given in Combination With Nivolumab in Patients With Advanced Tumors |
| NCT03247283 | PHASE1 | COMPLETED | Pharmacokinetics and Metabolism Study in Healthy Male Participants |
| NCT03312426 | PHASE1 | COMPLETED | An Investigational Study to Assess the Effect of a Light Meal and a High-Fat Meal on the Absorption of BMS-986205 in Healthy Participants |
| NCT03346837 | PHASE1 | COMPLETED | A Study to Evaluate the Effect of 2 Drugs on the Pharmacokinetics of BMS-986205 in Healthy Subjects |
| NCT03362411 | PHASE1 | COMPLETED | A Study to Assess the Absorption of a Single Dose of BMS-986205 in Healthy Volunteers When Administered as a Crushed Tablet Orally or Crushed Tablet Suspension Via Nasogastric Tube, as Compared to a Tablet |
| NCT03374228 | PHASE1 | COMPLETED | A Study to Evaluate the Bioavailability of BMS-986205 |
| NCT03936374 | PHASE1 | COMPLETED | A Study to Evaluate the Effect of Omeprazole on the Pharmacokinetics of BMS-986205 in Healthy Participants |
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.
20 molecules share ≥1 primary target. Top 20 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| BERBERINE | ChEMBL | Phase 4 (approved) | IDO1 |
| BIFONAZOLE | ChEMBL | Phase 4 (approved) | IDO1 |
| ECONAZOLE | ChEMBL | Phase 4 (approved) | IDO1 |
| ISOCONAZOLE | ChEMBL | Phase 4 (approved) | IDO1 |
| KETOCONAZOLE | ChEMBL | Phase 4 (approved) | IDO1 |
| MENADIONE | ChEMBL | Phase 4 (approved) | IDO1 |
| MICONAZOLE | ChEMBL | Phase 4 (approved) | IDO1 |
| MITOMYCIN | ChEMBL | Phase 4 (approved) | IDO1 |
| OXICONAZOLE | ChEMBL | Phase 4 (approved) | IDO1 |
| PHENELZINE | ChEMBL | Phase 4 (approved) | IDO1 |
| SERTACONAZOLE | ChEMBL | Phase 4 (approved) | IDO1 |
| SULCONAZOLE | ChEMBL | Phase 4 (approved) | IDO1 |
| EBSELEN | ChEMBL | Phase 3 | IDO1 |
| EPACADOSTAT | ChEMBL | Phase 3 | IDO1 |
| DICHLOROPHEN | ChEMBL | Phase 2 | IDO1 |
| ENILCONAZOLE | ChEMBL | Phase 2 | IDO1 |
| INDOXIMOD | ChEMBL | Phase 2 | IDO1 |
| LAPACHONE | ChEMBL | Phase 2 | IDO1 |
| NAVOXIMOD | ChEMBL | Phase 2 | IDO1 |
| Berberine Chloride | PubChem | Approved | IDO1 |
Related Atlas pages
- Genes: IDO1
- Diseases: melanoma, non-small cell lung carcinoma, head and neck cancer, skin neoplasm, lung neoplasm
- Drugs: Berberine, Bifonazole, Econazole, Isoconazole, Ketoconazole, Menadione, Mitomycin, Oxiconazole, Phenelzine, Sertaconazole, Sulconazole, Ebselen, Epacadostat