Cevimeline

Summary

Cevimeline (CHEMBL168815) is an approved small molecule (ATC N07AX03) targeting CHRM1, CHRM2, and CHRM3; indicated across 1 condition.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N07AX03
• Targets: 4 (CHRM1, CHRM2, CHRM3…)
• Indications: 1 condition
• Clinical trials: 4
• Chemistry: 199.32 Da · C10H17NOS

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL168815
Name	Cevimeline
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	2684
ATC	N07AX03
Molecular formula	C10H17NOS
Molecular weight	199.32
InChIKey	WUTYZMFRCNBCHQ-UHFFFAOYSA-N

SMILES: CC1OC2(CN3CCC2CC3)CS1

IUPAC name: 2-methylspiro[1,3-oxathiolane-5,3’-1-azabicyclo[2.2.2]octane]

Also known as: Cevimelina, Cevimeline, CEVIMELINE, cevimeline

Parent form; salt/anhydrous children: CHEMBL2218917

Patent coverage: 43 distinct patent families (87 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
CHRM1	M1 receptor	Agonist	5.31	0.2%	P11229
CHRM2	M2 receptor	Agonist	6.07	0%	P08172
CHRM3	M3 receptor	Agonist	5.59	0%	P20309
CHRM4	M4 receptor	Agonist	5.99	1.6%	P08173

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Muscarinic acetylcholine receptor M4, Muscarinic acetylcholine receptor M2, Muscarinic acetylcholine receptor M1, Muscarinic acetylcholine receptor M3.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 6 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CHRM2	6.07	Ki	851.1	nM	CHEMBL_ACT_15028297
CHRM4	5.99	Ki	1023	nM	CHEMBL_ACT_15028295
CHRM3	5.59	Ki	2570	nM	CHEMBL_ACT_15028283
CHRM2	5.52	AC50	3031	nM	CHEMBL_ACT_25214804
CHRM1	5.31	Ki	4898	nM	CHEMBL_ACT_15028277

Target pathways

Aggregated over 4 target gene(s): CHRM1, CHRM2, CHRM3, CHRM4.

Top Reactome pathways

17 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	4	CHRM1, CHRM2, CHRM3, CHRM4
Signaling by GPCR	4	CHRM1, CHRM2, CHRM3, CHRM4
Class A/1 (Rhodopsin-like receptors)	4	CHRM1, CHRM2, CHRM3, CHRM4
Amine ligand-binding receptors	4	CHRM1, CHRM2, CHRM3, CHRM4
GPCR downstream signalling	4	CHRM1, CHRM2, CHRM3, CHRM4
Muscarinic acetylcholine receptors	4	CHRM1, CHRM2, CHRM3, CHRM4
GPCR ligand binding	4	CHRM1, CHRM2, CHRM3, CHRM4
G alpha (q) signalling events	2	CHRM1, CHRM3
G alpha (i) signalling events	2	CHRM2, CHRM4
Metabolism	1	CHRM3
Integration of energy metabolism	1	CHRM3
Membrane Trafficking	1	CHRM2
Acetylcholine regulates insulin secretion	1	CHRM3
Regulation of insulin secretion	1	CHRM3
Vesicle-mediated transport	1	CHRM2
Cargo recognition for clathrin-mediated endocytosis	1	CHRM2
Clathrin-mediated endocytosis	1	CHRM2

Dominant GO biological processes

GO term	Targets
signal transduction	4
G protein-coupled receptor signaling pathway	4
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	4
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	4
G protein-coupled acetylcholine receptor signaling pathway	4
chemical synaptic transmission	4
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathway	3
nervous system development	3
regulation of locomotion	2
saliva secretion	2
acetylcholine receptor signaling pathway	2
regulation of smooth muscle contraction	2
phospholipase C-activating G protein-coupled receptor signaling pathway	1
neuromuscular synaptic transmission	1
positive regulation of monoatomic ion transport	1

Indications & clinical

Indications

1 indication (0 at ChEMBL trial phase 4).

The 1 indication record carries no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 4.

Phase distribution

Phase	Trials
EARLY_PHASE1	2
PHASE4	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00466388	PHASE4	COMPLETED	Study of the Effectiveness of Cevimeline on Oral Health in Patients With Radiation Induced Xerostomia
NCT01903109	EARLY_PHASE1	COMPLETED	Crossover Bioequivalence Study of Cevimeline 30 mg Capsules Under Fed Conditions
NCT01903122	EARLY_PHASE1	COMPLETED	Crossover Bioequivalence Study of Cevimeline 30 mg Capsules Under Fasted Conditions
NCT01690052	Not specified	COMPLETED	Efficacy of Cevimeline Versus Pilocarpine in the Secretion of Saliva

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.

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

Molecule	Source	Status	Shared targets
ACLIDINIUM BROMIDE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
GENTIAN VIOLET	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
Mavorixafor	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
ACETYLCHOLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
AMIODARONE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
AMOXAPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
ATROPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
BENZTROPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
BETHANECHOL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
BIPERIDEN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
CARBACHOL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
CARBAMOYLCHOLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
CHLOROQUINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
CINNARIZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
CLEMASTINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
CLIDINIUM	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
CLOZAPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
CYCLIZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
DARIFENACIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
DESLORATADINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
DEXCHLORPHENIRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
DICYCLOMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
DIMENHYDRINATE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
DIPHENHYDRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
DIPHENIDOL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
DOXEPIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
EBASTINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
ECONAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
GLYCOPYRRONIUM BROMIDE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
HALOPERIDOL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
HOMATROPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
HYDROXYCHLOROQUINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
IMIPRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
IPRATROPIUM	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
KETOTIFEN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
LOXAPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
MAPROTILINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
MEPAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
METHSCOPOLAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
METHSCOPOLAMINE BROMIDE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
MIANSERIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
MICONAZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
NORTRIPTYLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
OLANZAPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
ORPHENADRINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
OXYBUTYNIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
PAROXETINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
PERHEXILINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
PILOCARPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
PIRENZEPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
PROMAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4
PROMETHAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4