Nabiximols

Summary

Nabiximols (CHEMBL3833333) is a phase-3 clinical-stage small molecule (ATC N02BG10) targeting GPR55, TRPA1, and TRPM8; indicated across 13 conditions including tourette syndrome and neuralgia.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: N02BG10
• Targets: 15 (GPR55, TRPA1, TRPM8…)
• Indications: 13 conditions
• Clinical trials: 42
• Chemistry: 628.9 Da · C42H60O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3833333
Name	Nabiximols
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	9852188
ATC	N02BG10
Molecular formula	C42H60O4
Molecular weight	628.9
InChIKey	SSNHGLKFJISNTR-DYSNNVSPSA-N

SMILES: CCCCCC1=CC(=C(C(=C1)O)[C@@H]2C=C(CC[C@H]2C(=C)C)C)O.CCCCCC1=CC(=C2[C@@H]3C=C(CC[C@H]3C(OC2=C1)(C)C)C)O

IUPAC name: (6aR,10aR)-6,6,9-trimethyl-3-pentyl-6a,7,8,10a-tetrahydrobenzo[c]chromen-1-ol;2-[(1R,6R)-3-methyl-6-prop-1-en-2-ylcyclohex-2-en-1-yl]-5-pentylbenzene-1,3-diol

Also known as: Cannabinoids, GW 1000, GW-1000, Nabidiolex, Nabiximols, SAB 378, SAB-378, Sativex, Tetranabinex, NABIXIMOLS

Patent coverage: 296 distinct patent families (758 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
GPR55	GPR55	Antagonist	6.46	0%	Q9Y2T6
TRPA1	TRPA1	Agonist	6.32	0.1%	O75762
TRPM8	TRPM8	Antagonist	5.55	0.5%	Q7Z2W7
TRPV2	TRPV2	Activation	4.5	1.4%	Q9Y5S1
TRPV3	TRPV3	Activation	5.43	0%	Q8NET8
CNR1	CB1 receptor	Negative		0%	P21554
SCN1A	Nav1.1		4.9	0%	P35498
SCN2A	Nav1.2		5.54	0.1%	Q99250
SCN3A	Nav1.3		5.48	0.1%	Q9NY46
SCN4A	Nav1.4		5	0%	P35499
SCN5A	Nav1.5		5.42	0.2%	Q14524
SCN8A	Nav1.6		5.52	0.7%	Q9UQD0
SCN9A	Nav1.7		6.7	0%	Q15858
SCN10A	Nav1.8		5.7	0.1%	Q9Y5Y9
GPR18	GPR18	Partial agonist	4.29	0.2%	Q14330

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 15 target gene(s): GPR55, TRPA1, TRPM8, TRPV2, TRPV3, CNR1, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A, SCN10A, GPR18.

Top Reactome pathways

14 total, by targets touching each:

Pathway	Targets	Genes
Developmental Biology	8	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
L1CAM interactions	8	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
Muscle contraction	8	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
Axon guidance	8	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
Interaction between L1 and Ankyrins	8	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
Cardiac conduction	8	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
Phase 0 - rapid depolarisation	8	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
Nervous system development	8	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
TRP channels	4	TRPA1, TRPM8, TRPV2, TRPV3
Class A/1 (Rhodopsin-like receptors)	3	CNR1, GPR18, GPR55
G alpha (i) signalling events	3	CNR1, GPR18, GPR55
Sensory Perception	3	SCN2A, SCN3A, SCN9A
Sensory perception of taste	3	SCN2A, SCN3A, SCN9A
Sensory perception of sweet, bitter, and umami (glutamate) taste	3	SCN2A, SCN3A, SCN9A

Dominant GO biological processes

GO term	Targets
monoatomic ion transport	12
monoatomic ion transmembrane transport	12
transmembrane transport	12
sodium ion transmembrane transport	9
sodium ion transport	8
cardiac muscle cell action potential involved in contraction	8
monoatomic cation transmembrane transport	7
action potential	6
regulation of heart rate	6
calcium ion transmembrane transport	4
calcium ion transport	4
membrane depolarization during action potential	4
cardiac muscle cell action potential	4
regulation of muscle system process	4
G protein-coupled receptor signaling pathway	3

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
Tourette syndrome	3	MONDO:0007661	EFO:0004895
neuralgia	3	MONDO:0021667	EFO:0005762
cerebral palsy	3	MONDO:0006497	EFO:1000632
multiple sclerosis	3	MONDO:0005301	MONDO:0005301
autism	2	MONDO:0005260	EFO:0003758
peripheral neuropathy	2	MONDO:0005244	EFO:0003100
cannabis dependence	2	MONDO:0005689	EFO:0007191
post-traumatic stress disorder	2	MONDO:0005146	EFO:0001358
head and neck squamous cell carcinoma	1	MONDO:0010150	EFO:0000181
liver disorder	1	MONDO:0005154	EFO:0001421
neoplasm	1	MONDO:0005070	MONDO:0004992

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 42.

Phase distribution

Phase	Trials
PHASE3	18
PHASE1	11
PHASE2	6
Not specified	3
PHASE1/PHASE2	2
PHASE4	1
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01964547	PHASE4	COMPLETED	A Randomized Study of Sativex on Cognitive Function and Mood: Multiple Sclerosis Patients
NCT00391079	PHASE3	COMPLETED	Sativex Versus Placebo When Added to Existing Treatment for Central Neuropathic Pain in MS
NCT00675948	PHASE3	COMPLETED	Study to Compare the Safety and Tolerability of Sativex® in Patients With Cancer Related Pain
NCT00702468	PHASE3	COMPLETED	Evaluate the Maintenance of Effect After Long-term Treatment With Sativex® in Subjects With Symptoms of Spasticity Due to Multiple Sclerosis
NCT00710424	PHASE3	COMPLETED	A Study of Sativex® for Pain Relief Due to Diabetic Neuropathy
NCT00710554	PHASE3	COMPLETED	A Study of Sativex® for Pain Relief of Peripheral Neuropathic Pain, Associated With Allodynia
NCT00872144	PHASE3	COMPLETED	Sativex for Treatment of Chemotherapy Induced Neuropathic Pain
NCT01262651	PHASE3	COMPLETED	Sativex® for Relieving Persistent Pain in Participants With Advanced Cancer
NCT01337089	PHASE3	COMPLETED	Long Term Safety of Sativex Oromucosal Spray (Sativex®; Nabiximols) as Adjunctive Therapy in Patients With Uncontrolled Persistent Chronic Cancer Related Pain
NCT01361607	PHASE3	COMPLETED	Sativex® for Relieving Persistent Pain in Patients With Advanced Cancer
NCT01424566	PHASE3	COMPLETED	A Two-Part Study of Sativex® Oromucosal Spray for Relieving Uncontrolled Persistent Pain in Patients With Advanced Cancer
NCT01599234	PHASE3	COMPLETED	A Study to Evaluate the Efficacy of Sativex in Relieving Symptoms of Spasticity Due to Multiple Sclerosis
NCT01604265	PHASE3	COMPLETED	A Study of Sativex in the Treatment of Central Neuropathic Pain Due to Multiple Sclerosis
NCT01868048	PHASE3	WITHDRAWN	Phase 3, 28-week, Randomized, Double-blind, Placebo-controlled Safety and Efficacy Study of Nabiximols as an add-on Therapy in Subjects With Spasticity Due to Multiple Sclerosis.
NCT01898520	PHASE3	COMPLETED	A Safety, Efficacy and Tolerability Study of Sativex for the Treatment of Spasticity in Children Aged 8 to 18 Years
NCT03087201	PHASE3	COMPLETED	CANNAbinoids in the Treatment of TICS (CANNA-TICS)
NCT04203498	PHASE3	TERMINATED	Safety and Effectiveness of Nabiximols Oromucosal Spray as Add-on Therapy in Participants With Spasticity Due to Multiple Sclerosis
NCT04592159	PHASE2/PHASE3	WITHDRAWN	Study of the Safety and Efficacy of Nabiximols Oromucosal Spray Versus Placebo in Patients With Post-traumatic Stress Disorder
NCT04657666	PHASE3	COMPLETED	Trial to Evaluate the Effect of Nabiximols Oromucosal Spray on Clinical Measures of Spasticity in Participants With Multiple Sclerosis
NCT04984278	PHASE3	TERMINATED	Evaluation of the Effect of Nabiximols Oromucosal Spray on Clinical Measures of Spasticity in Participants With Multiple Sclerosis
NCT05629702	PHASE2	RECRUITING	ARISTOCRAT: Blinded Trial of Temozolomide +/- Cannabinoids
NCT07393672	PHASE2	RECRUITING	Effects of Hemp-Derived Cannabinoids on Menopause Symptoms
NCT00202423	PHASE2	UNKNOWN	Use of Cannabinoids in Patients With Multiple Sclerosis
NCT01747850	PHASE2	COMPLETED	Sativex and Behavioral-relapse Prevention Strategy in Cannabis Dependence
NCT01812603	PHASE1/PHASE2	COMPLETED	A Safety Study of Sativex in Combination With Dose-intense Temozolomide in Patients With Recurrent Glioblastoma
NCT01812616	PHASE1/PHASE2	COMPLETED	A Safety Study of Sativex Compared With Placebo (Both With Dose-intense Temozolomide) in Recurrent Glioblastoma Patients
NCT03782402	PHASE2	TERMINATED	Cannabinoids for Taxane Induced Peripheral Neuropathy
NCT05974293	PHASE2	WITHDRAWN	A Phase IIb Study of Nabiximols for Spasticity Due to Neuromyelitis Optica Spectrum Disorders
NCT01322464	PHASE1	COMPLETED	Study to Assess Food Effect on Sativex Bioavailability
NCT01323465	PHASE1	COMPLETED	Study to Evaluate the Effect of Rifampicin, Ketoconazole, and Omeprazole on the Pharmacokinetics of Sativex
NCT01323569	PHASE1	COMPLETED	Abuse Potential of Sativex
NCT01887301	PHASE1	COMPLETED	Assessment of the Single Dose Pharmacokinetics and Tolerability of Sativex in Patients With Impaired Hepatic Function and Healthy Patients
NCT01975688	PHASE1	TERMINATED	A Pharmacokinetic Study of Single Doses of Sativex in Treatment-induced Mucositis
NCT02240160	PHASE1	TERMINATED	A Randomised, Open-label, Three-way Crossover Study to Assess the Pharmacokinetics and Safety of Single Doses of Four Sprays of Sativex® in a Range of Oral pH Environments in Healthy Subjects
NCT02325024	PHASE1	WITHDRAWN	A Study to Evaluate the Pharmacokinetics Of Sativex® in Subjects With Severe Renal Impairment or End Stage Renal Disease, Compared to Matched Subjects With Normal Renal Function.
NCT02432612	PHASE1	WITHDRAWN	A Study to Assess the Pharmacokinetic (PK) Properties of Sativex® in Patients With Advanced Cancer
NCT03201835	PHASE1	COMPLETED	5-Way Crossover Study to Compare the Safety, Tolerability and Pharmacokinetics of New Oral Cannabinoid Formulations Administered as Single Doses, With Buccal Sativex®, in Healthy Volunteers
NCT03936907	PHASE1	COMPLETED	Comparison of Safety, Tolerability and Pharmacokinetics of Medical Grade Cannabis (MGC) Orally Disintegrating Tablets With Buccal Sativex®, in Healthy Adult Volunteers
NCT05503147	PHASE1	UNKNOWN	Sativex® and Gentamicin for Optimized Pharmagological Treatment in Older Patients (CanPan)
NCT01748799	Not specified	COMPLETED	Fixed or Self-Titrated Dosages of Sativex on Cannabis Users

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.

350 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
IMIPRAMINE	ChEMBL + PubChem	Phase 4 (approved)	CNR1, SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
SERTINDOLE	ChEMBL	Phase 4 (approved)	CNR1, SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
NITRENDIPINE	ChEMBL	Phase 3	CNR1, SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
AMIODARONE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
AMITRIPTYLINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
CHLORPROMAZINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
DILTIAZEM	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
HALOPERIDOL	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
Lamotrigine	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
MEXILETINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
NIFEDIPINE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
PIMOZIDE	ChEMBL + PubChem	Phase 4 (approved)	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
MIBEFRADIL	ChEMBL	Phase 4 (approved)	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
AJMALINE	ChEMBL	Phase 3	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
ELECLAZINE	ChEMBL	Phase 3	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
TEDISAMIL	ChEMBL	Phase 3	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
VIXOTRIGINE	ChEMBL	Phase 3	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
CIFENLINE	ChEMBL	Phase 2	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
TETRACAINE	ChEMBL + PubChem	Phase 4 (approved)	CNR1, SCN1A, SCN2A, SCN3A, SCN5A, SCN8A, SCN9A
TETRODOTOXIN	ChEMBL	Phase 3	SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
PF-05089771	ChEMBL	Phase 2	SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN8A, SCN9A
CANNABIDIOL	ChEMBL + PubChem	Phase 4 (approved)	CNR1, GPR18, GPR55, SCN9A, TRPM8, TRPV2
Carbamazepine	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN9A
Lidocaine	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A, SCN4A, SCN5A, SCN9A
CANNABIDIVARIN	ChEMBL	Phase 2	CNR1, GPR55, TRPA1, TRPM8, TRPV2, TRPV3
TETRAHYDROCANNABIVARIN	ChEMBL	Phase 2	CNR1, GPR55, TRPA1, TRPM8, TRPV2, TRPV3
Dofetilide	PubChem	Approved	SCN10A, SCN1A, SCN2A, SCN3A, SCN4A, SCN8A
Caffeine	ChEMBL + PubChem	Phase 4 (approved)	CNR1, SCN1A, SCN2A, SCN3A, TRPA1
DRONABINOL	ChEMBL + PubChem	Phase 4 (approved)	CNR1, GPR18, GPR55, TRPA1, TRPM8
FELODIPINE	ChEMBL + PubChem	Phase 4 (approved)	CNR1, SCN1A, SCN2A, SCN3A, SCN5A
NISOLDIPINE	ChEMBL + PubChem	Phase 4 (approved)	CNR1, SCN1A, SCN2A, SCN3A, SCN5A
PHENYTOIN	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A, SCN4A, SCN5A
BEPRIDIL	ChEMBL	Phase 4 (approved)	CNR1, SCN1A, SCN2A, SCN3A, SCN5A
PRENYLAMINE	ChEMBL	Phase 4 (approved)	CNR1, SCN1A, SCN2A, SCN3A, SCN5A
CANNABIGEROL	ChEMBL	Phase 2	CNR1, TRPA1, TRPM8, TRPV2, TRPV3
FUNAPIDE	ChEMBL	Phase 2	SCN10A, SCN2A, SCN5A, SCN8A, SCN9A
BUSPIRONE	ChEMBL + PubChem	Phase 4 (approved)	CNR1, SCN1A, SCN2A, SCN3A
DESIPRAMINE	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A, SCN5A
DIBUCAINE	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A, SCN5A
DIPHENHYDRAMINE	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A, SCN5A
DROPERIDOL	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A, SCN5A
FLUPHENAZINE	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A, SCN5A
LOPERAMIDE	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A, SCN5A
QUINIDINE	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A, SCN5A
RILUZOLE	ChEMBL + PubChem	Phase 4 (approved)	SCN2A, SCN4A, SCN5A, SCN9A
THIORIDAZINE	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A, SCN5A
VERAPAMIL	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A, SCN5A
ETIDOCAINE	ChEMBL	Phase 4 (approved)	SCN1A, SCN2A, SCN3A, SCN5A
MIANSERIN	ChEMBL	Phase 4 (approved)	CNR1, SCN1A, SCN2A, SCN3A
CANNABINOL	ChEMBL	Phase 3	CNR1, TRPA1, TRPV2, TRPV3
DS-1971	ChEMBL	Phase 2	SCN2A, SCN5A, SCN8A, SCN9A
FLUNARIZINE	ChEMBL	Phase 2	CNR1, SCN1A, SCN2A, SCN3A
MEPRYLCAINE	ChEMBL	Phase 2	SCN1A, SCN2A, SCN3A, SCN5A
PF-04531083	ChEMBL	Phase 2	SCN10A, SCN1A, SCN5A, SCN9A
BROMPHENIRAMINE	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A
CHLORPHENIRAMINE	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A
COCAINE	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A
CYPROHEPTADINE	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A
DICYCLOMINE	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A
LEVORPHANOL	ChEMBL + PubChem	Phase 4 (approved)	SCN1A, SCN2A, SCN3A