Lenabasum
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Also known as Ajulemic acidCPL-7075CPL7075CT-3HU-239IP-751JBT-101Resunab
Summary
Lenabasum (CHEMBL456341) is a phase-3 clinical-stage small molecule targeting CNR1 and CNR2; indicated across 4 conditions including dermatomyositis and diffuse scleroderma.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 2 (CNR1, CNR2)
- Indications: 4 conditions
- Clinical trials: 7
- Chemistry: 400.5 Da · C25H36O4
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL456341 |
| Name | Lenabasum |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 3083542 |
| Molecular formula | C25H36O4 |
| Molecular weight | 400.5 |
| InChIKey | YCHYFHOSGQABSW-RTBURBONSA-N |
SMILES: CCCCCCC(C)(C)C1=CC(=C2[C@@H]3CC(=CC[C@H]3C(OC2=C1)(C)C)C(=O)O)O
IUPAC name: (6aR,10aR)-1-hydroxy-6,6-dimethyl-3-(2-methyloctan-2-yl)-6a,7,10,10a-tetrahydrobenzo[c]chromene-9-carboxylic acid
Also known as: Ajulemic acid, CPL-7075, CPL7075, CT-3, HU-239, IP-751, JBT-101, Lenabasum, Resunab, LENABASUM, AJULEMIC ACID
Patent coverage: 776 distinct patent families (1,313 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,168 (89%) 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 |
|---|---|---|---|---|---|
| CNR1 | CB1 receptor | Agonist | 7.49 | 0% | P21554 |
| CNR2 | CB2 receptor | Agonist | 6.77 | P34972 |
Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Cannabinoid receptor 1, Cannabinoid receptor 2.
Bioactivity
ChEMBL activities: 4 potent at pChembl ≥ 5 of 4 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| CNR1 | 8.24 | Ki | 5.7 | nM | CHEMBL_ACT_14655724 |
| CNR1 | 7.49 | Ki | 32.3 | nM | CHEMBL_ACT_14574041 |
| CNR2 | 6.77 | Ki | 170.5 | nM | CHEMBL_ACT_14574075 |
| CNR1 | 6.03 | EC50 | 927 | nM | CHEMBL_ACT_14574112 |
Target pathways
Aggregated over 2 target gene(s): CNR1, CNR2.
Top Reactome pathways
2 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Class A/1 (Rhodopsin-like receptors) | 2 | CNR1, CNR2 |
| G alpha (i) signalling events | 2 | CNR1, CNR2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | 2 |
| adenylate cyclase-activating G protein-coupled receptor signaling pathway | 2 |
| cannabinoid signaling pathway | 2 |
| signal transduction | 2 |
| G protein-coupled receptor signaling pathway | 2 |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | 1 |
| axonal fasciculation | 1 |
| glucose homeostasis | 1 |
| retrograde trans-synaptic signaling by endocannabinoid | 1 |
| regulation of presynaptic cytosolic calcium ion concentration | 1 |
| response to amphetamine | 1 |
| inflammatory response | 1 |
| immune response | 1 |
| leukocyte chemotaxis | 1 |
| negative regulation of synaptic transmission, GABAergic | 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 |
|---|---|---|---|
| dermatomyositis | 3 | MONDO:0016367 | EFO:0000398 |
| diffuse scleroderma | 3 | MONDO:0005019 | EFO:0000404 |
| cystic fibrosis | 2 | MONDO:0009061 | MONDO:0009061 |
| systemic lupus erythematosus | 2 | MONDO:0007915 | MONDO:0007915 |
Clinical trials
Total trials: 7.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 5 |
| PHASE3 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03398837 | PHASE3 | TERMINATED | Trial to Evaluate Efficacy and Safety of Lenabasum in Diffuse Cutaneous Systemic Sclerosis |
| NCT03813160 | PHASE3 | COMPLETED | Trial to Evaluate Efficacy and Safety of Lenabasum in Dermatomyositis |
| NCT02465437 | PHASE2 | TERMINATED | Safety, Tolerability, Efficacy, and Pharmacokinetics of JBT-101 in Systemic Sclerosis |
| NCT02465450 | PHASE2 | COMPLETED | Safety, Tolerability, Pharmacokinetics, and Efficacy of JBT-101 (Lenabasum) in Cystic Fibrosis |
| NCT02466243 | PHASE2 | TERMINATED | Safety, Tolerability, and Efficacy of JBT-101 in Subjects With Dermatomyositis |
| NCT03093402 | PHASE2 | COMPLETED | JBT-101 in Systemic Lupus Erythematosus (SLE) |
| NCT03451045 | PHASE2 | COMPLETED | Trial to Evaluate Efficacy and Safety of Lenabasum in Cystic Fibrosis |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
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.
128 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CANNABIDIOL | ChEMBL | Phase 4 (approved) | CNR1, CNR2 |
| DRONABINOL | ChEMBL | Phase 4 (approved) | CNR1, CNR2 |
| NABILONE | ChEMBL | Phase 4 (approved) | CNR1, CNR2 |
| RIMONABANT | ChEMBL | Phase 4 (approved) | CNR1, CNR2 |
| CANNABINOL | ChEMBL | Phase 3 | CNR1, CNR2 |
| DEXANABINOL | ChEMBL | Phase 3 | CNR1, CNR2 |
| EPIGALOCATECHIN GALLATE | ChEMBL | Phase 3 | CNR1, CNR2 |
| OTENABANT | ChEMBL | Phase 3 | CNR1, CNR2 |
| TARANABANT | ChEMBL | Phase 3 | CNR1, CNR2 |
| CANNABIDIVARIN | ChEMBL | Phase 2 | CNR1, CNR2 |
| CANNABIGEROL | ChEMBL | Phase 2 | CNR1, CNR2 |
| DELTA-8-TETRAHYDROCANNABINOL | ChEMBL | Phase 2 | CNR1, CNR2 |
| IBIPINABANT | ChEMBL | Phase 2 | CNR1, CNR2 |
| PRS-211375 | ChEMBL | Phase 2 | CNR1, CNR2 |
| REDAFAMDASTAT | ChEMBL | Phase 2 | CNR1, CNR2 |
| S-777469 | ChEMBL | Phase 2 | CNR1, CNR2 |
| SURINABANT | ChEMBL | Phase 2 | CNR1, CNR2 |
| TEDALINAB | ChEMBL | Phase 2 | CNR1, CNR2 |
| TETRAHYDROCANNABIVARIN | ChEMBL | Phase 2 | CNR1, CNR2 |
| TAFAMIDIS | ChEMBL + PubChem | Phase 4 (approved) | CNR1 |
| ACARBOSE | ChEMBL | Phase 4 (approved) | CNR1 |
| ALCLOMETASONE DIPROPIONATE | ChEMBL | Phase 4 (approved) | CNR1 |
| ALPRAZOLAM | ChEMBL | Phase 4 (approved) | CNR1 |
| AMCINONIDE | ChEMBL | Phase 4 (approved) | CNR1 |
| AMPRENAVIR | ChEMBL | Phase 4 (approved) | CNR1 |
| ATENOLOL | ChEMBL | Phase 4 (approved) | CNR1 |
| BECLOMETHASONE DIPROPIONATE | ChEMBL | Phase 4 (approved) | CNR1 |
| BEPRIDIL | ChEMBL | Phase 4 (approved) | CNR1 |
| BIFONAZOLE | ChEMBL | Phase 4 (approved) | CNR1 |
| BUCLIZINE | ChEMBL | Phase 4 (approved) | CNR1 |
| BUSPIRONE | ChEMBL | Phase 4 (approved) | CNR1 |
| CAFFEINE | ChEMBL | Phase 4 (approved) | CNR1 |
| CALCITRIOL | ChEMBL | Phase 4 (approved) | CNR1 |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | CNR1 |
| CARBENOXOLONE | ChEMBL | Phase 4 (approved) | CNR1 |
| CEFDINIR | ChEMBL | Phase 4 (approved) | CNR1 |
| CHLORHEXIDINE | ChEMBL | Phase 4 (approved) | CNR1 |
| CICLESONIDE | ChEMBL | Phase 4 (approved) | CNR1 |
| DEXAMETHASONE | ChEMBL | Phase 4 (approved) | CNR1 |
| ECONAZOLE | ChEMBL | Phase 4 (approved) | CNR1 |
| EFAVIRENZ | ChEMBL | Phase 4 (approved) | CNR1 |
| ENZALUTAMIDE | ChEMBL | Phase 4 (approved) | CNR1 |
| ERYTHROMYCIN | ChEMBL | Phase 4 (approved) | CNR1 |
| ETHAMBUTOL | ChEMBL | Phase 4 (approved) | CNR1 |
| FELODIPINE | ChEMBL | Phase 4 (approved) | CNR1 |
| FENOFIBRATE | ChEMBL | Phase 4 (approved) | CNR1 |
| FENTICONAZOLE | ChEMBL | Phase 4 (approved) | CNR1 |
| FEXOFENADINE | ChEMBL | Phase 4 (approved) | CNR1 |
| FLUOXETINE | ChEMBL | Phase 4 (approved) | CNR1 |
| FLUSPIRILENE | ChEMBL | Phase 4 (approved) | CNR1 |
| FLUTICASONE FUROATE | ChEMBL | Phase 4 (approved) | CNR1 |
| GLIPIZIDE | ChEMBL | Phase 4 (approved) | CNR1 |
| IMIPRAMINE | ChEMBL | Phase 4 (approved) | CNR1 |
| INDOCYANINE GREEN ACID FORM | ChEMBL | Phase 4 (approved) | CNR1 |
| KETOTIFEN | ChEMBL | Phase 4 (approved) | CNR1 |
| LOFEPRAMINE | ChEMBL | Phase 4 (approved) | CNR1 |
| LORCASERIN | ChEMBL | Phase 4 (approved) | CNR1 |
| LOSARTAN | ChEMBL | Phase 4 (approved) | CNR1 |
| MASOPROCOL | ChEMBL | Phase 4 (approved) | CNR1 |
| MECLIZINE | ChEMBL | Phase 4 (approved) | CNR1 |
Related Atlas pages
- Genes: CNR1, CNR2
- Diseases: dermatomyositis, diffuse scleroderma
- Drugs: Cannabidiol, Dronabinol, Nabilone, Rimonabant, Cannabinol, Dexanabinol, Epigalocatechin Gallate, Otenabant, Taranabant, Tafamidis, Acarbose, Alclometasone Dipropionate, Alprazolam, Amcinonide, Amprenavir, Atenolol, Beclomethasone Dipropionate, Bepridil, Bifonazole, Buclizine, Buspirone, Caffeine, Calcitriol, Candesartan Cilexetil, Carbenoxolone, Cefdinir, Chlorhexidine, Ciclesonide, Dexamethasone, Econazole, Efavirenz, Enzalutamide, Erythromycin, Ethambutol, Felodipine, Fenofibrate, Fenticonazole, Fexofenadine, Fluoxetine, Fluspirilene, Fluticasone Furoate, Glipizide, Imipramine, Indocyanine Green Acid Form, Ketotifen, Lofepramine, Lorcaserin, Losartan, Masoprocol, Meclizine