Cenerimod

Summary

Cenerimod (CHEMBL4297505) is a phase-3 clinical-stage small molecule targeting S1PR1; indicated across 3 conditions including systemic lupus erythematosus and liver disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (S1PR1)
• Indications: 3 conditions
• Clinical trials: 13
• Chemistry: 453.5 Da · C25H31N3O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4297505
Name	Cenerimod
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	49871973
Molecular formula	C25H31N3O5
Molecular weight	453.5
InChIKey	KJKKMMMRWISKRF-FQEVSTJZSA-N

SMILES: CCC1=C(C(=CC(=C1)C2=NOC(=N2)C3=CC(=NC(=C3)OC)C4CCCC4)C)OC[C@H](CO)O

IUPAC name: (2S)-3-[4-[5-(2-cyclopentyl-6-methoxy-4-pyridinyl)-1,2,4-oxadiazol-3-yl]-2-ethyl-6-methylphenoxy]propane-1,2-diol

Also known as: Act-334441, ACT-334441, ACT334441, Cenerimod, CENERIMOD

Patent coverage: 93 distinct patent families (244 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 195 (80%) 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
S1PR1	S1P1 receptor	Agonist	9	0.2%	P21453

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Sphingosine 1-phosphate receptor 1.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
S1PR1	9	EC50	1	nM	CHEMBL_ACT_25708621

Target pathways

Aggregated over 1 target gene(s): S1PR1.

Top Reactome pathways

14 total, by targets touching each:

Pathway	Targets	Genes
Cytokine Signaling in Immune system	1	S1PR1
Signal Transduction	1	S1PR1
Disease	1	S1PR1
Immune System	1	S1PR1
Signaling by GPCR	1	S1PR1
Class A/1 (Rhodopsin-like receptors)	1	S1PR1
Lysosphingolipid and LPA receptors	1	S1PR1
Signaling by Interleukins	1	S1PR1
GPCR ligand binding	1	S1PR1
Infectious disease	1	S1PR1
Interleukin-4 and Interleukin-13 signaling	1	S1PR1
Potential therapeutics for SARS	1	S1PR1
SARS-CoV Infections	1	S1PR1
Viral Infection Pathways	1	S1PR1

Dominant GO biological processes

GO term	Targets
angiogenesis	1
blood vessel maturation	1
cardiac muscle tissue growth involved in heart morphogenesis	1
sphingosine-1-phosphate receptor signaling pathway	1
chemotaxis	1
cell adhesion	1
G protein-coupled receptor signaling pathway	1
adenylate cyclase-activating G protein-coupled receptor signaling pathway	1
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1
brain development	1
cell population proliferation	1
cell migration	1
transmission of nerve impulse	1
lamellipodium assembly	1

Indications & clinical

Indications

3 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
systemic lupus erythematosus	3	MONDO:0007915	MONDO:0007915
liver disorder	1	MONDO:0005154	EFO:0001421
kidney disorder	1	MONDO:0005240	EFO:0003086

Clinical trials

Total trials: 13.

Phase distribution

Phase	Trials
PHASE1	6
PHASE3	4
PHASE2	2
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05648500	PHASE3	ACTIVE_NOT_RECRUITING	A Research Study to Evaluate the Effects of a New Oral Medicine Called Cenerimod in Adults With Systemic Lupus Erythematosus
NCT05672576	PHASE3	ACTIVE_NOT_RECRUITING	A Research Study to Evaluate the Efficacy and Safety of Cenerimod in Subjects Suffering From Systemic Lupus Erythematosus
NCT06475742	PHASE3	ENROLLING_BY_INVITATION	Long-term Safety and Tolerability of Cenerimod in Adults With Systemic Lupus Erythematosus
NCT07201129	PHASE3	RECRUITING	A Research Trial to Assess if Cenerimod is Efficacious and Safe to Treat Active Lupus Nephritis on Top of Regular Treatment
NCT07266090	PHASE2	ACTIVE_NOT_RECRUITING	A Study to Evaluate the Safety,Tolerability,Pharmacokinetics and Pharmacodynamics of Cenerimod in Adult Chinese Participants With Moderate-to-severe Systemic Lupus Erythematosus (SLE)
NCT02472795	PHASE1/PHASE2	COMPLETED	Clinical Study to Investigate the Biological Activity, Safety, Tolerability, and Pharmacokinetics of ACT-334441 in Subjects With Systemic Lupus Erythematosus
NCT03742037	PHASE2	COMPLETED	Efficacy and Safety of Four Doses of Cenerimod Compared to Placebo in Adult Subjects With Active Systemic Lupus Erythematosus
NCT02479204	PHASE1	TERMINATED	Clinical Study to Investigate Safety and Effects on Heart Rate, Blood Pressure, and Pharmacokinetic Interactions of ACT-334441
NCT02914223	PHASE1	COMPLETED	A Study to Evaluate Cenerimod in Healthy Male Subjects
NCT04052360	PHASE1	COMPLETED	Single Oral Dose of 4 mg Cenerimod in Healthy Japanese and Caucasian Subjects
NCT04255277	PHASE1	COMPLETED	To Study the Effect of Cenerimod on the Electrical Activity of the Heart, in Men and Women. To Study the Effect of Cenerimod on the Use of Oral Contraceptives in Women. To Study the Effect That Charcoal Has on the Elimination of Cenerimod From the Body, in Women and Men.
NCT04819464	PHASE1	COMPLETED	A Study to Investigate the Effect of Hepatic Impairment on the Pharmacokinetics of a Single Dose of Cenerimod
NCT05004311	PHASE1	COMPLETED	The Effect of Severe Kidney Impairment on Cenerimod Pharmacokinetics

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.

9 molecules share ≥1 primary target. Top 9 by shared-target count:

Molecule	Source	Status	Shared targets
FINGOLIMOD	ChEMBL + PubChem	Phase 4 (approved)	S1PR1
ETRASIMOD	ChEMBL	Phase 4 (approved)	S1PR1
OZANIMOD	ChEMBL	Phase 4 (approved)	S1PR1
PONESIMOD	ChEMBL	Phase 4 (approved)	S1PR1
SIPONIMOD	ChEMBL	Phase 4 (approved)	S1PR1
AMISELIMOD	ChEMBL	Phase 2	S1PR1
ICANBELIMOD	ChEMBL	Phase 2	S1PR1
NIGULDIPINE	ChEMBL	Phase 2	S1PR1
PINAFIDE	ChEMBL	Phase 2	S1PR1