Siponimod

Sphingosine 1-phosphate Receptor Modulator — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Siponimod is an onp drug in the Sphingosine 1-phosphate Receptor Modulator class catalogued in DrugCentral. It was first approved by the FDA in 2019. Its mechanism of action is classified as Sphingosine 1-Phosphate Receptor Modulators. DrugCentral lists 5 molecular targets, including S1PR1, S1PR5 and S1PR4. Recorded indications include Relapsing remitting multiple sclerosis and Secondary progressive multiple sclerosis.

• Approval status: onp (first approved 2019 by the FDA).
• Drug class: Sphingosine 1-phosphate Receptor Modulator.
• Mechanism of action: Sphingosine 1-Phosphate Receptor Modulators.
• Molecular targets: S1PR1, S1PR5, S1PR4 and S1PR2 (5 listed in DrugCentral).
• Indications: Relapsing remitting multiple sclerosis and Secondary progressive multiple sclerosis.
• ATC code: L04AE03 (Sphingosine-1-phosphate (S1P) receptor modulators).
• Molecular formula: C29H35F3N2O3; molecular weight 516.61 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Relapsing remitting multiple sclerosis
• Secondary progressive multiple sclerosis

Contraindications (2)

• Atrioventricular block
• Sick sinus syndrome

Mechanism & targets

• Mechanism of action (MoA): Sphingosine 1-Phosphate Receptor Modulators
• Established pharmacologic class: Sphingosine 1-phosphate Receptor Modulator

Molecular targets (5)

Target	Gene	Action	Activity
Sphingosine 1-phosphate receptor 1	S1PR1	modulator	EC50 9.41
Sphingosine 1-phosphate receptor 5	S1PR5	modulator	EC50 9.01
Sphingosine 1-phosphate receptor 4	S1PR4	modulator	EC50 6.12
Sphingosine 1-phosphate receptor 2	S1PR2	modulator	EC50 4.00
Sphingosine 1-phosphate receptor 3	S1PR3	modulator	EC50 3.00

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2020-06-29	PMDA	—	Novartis Pharma K.K.
2020-01-13	EMA	—	Novartis Europharm Limited
2019-03-26	FDA	—	NOVARTIS PHARMS CORP

ATC classification

ATC code	Therapeutic hierarchy
L04AE03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › IMMUNOSUPPRESSANTS › IMMUNOSUPPRESSANTS › Sphingosine-1-phosphate (S1P) receptor modulators

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: CYP2C9 · Testing Required
• FDA label: CYP2C9 · Testing Required
• HCSC label: CYP2C9 · Testing Required

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Lymphocyte count decreased	665.2
Multiple sclerosis relapse	622.1
Lymphopenia	550.4
Expanded disability status scale score increased	294.6
Multiple sclerosis	239.6
Gait disturbance	203.5
Basal cell carcinoma	168.5
Gait spastic	157.7
Balance disorder	156.7
Central nervous system lesion	134.7
Urinary tract infection	129.3
Relapsing-remitting multiple sclerosis	126.5

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Siponimod is on its molecule page.

• Molecular formula: C₂₉H₃₅F₃N₂O₃
• Molecular weight: 516.61 g/mol
• CAS number: 1230487-00-9
• InChIKey: KIHYPELVXPAIDH-HNSNBQBZSA-N
• PubChem CID: 44599207

CCC1=CC(=CC=C1CN1CC(C1)C(O)=O)C(\C)=N\OCC1=CC=C(C2CCCCC2)C(=C1)C(F)(F)F

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Siponimod used for?

DrugCentral lists the following indications for Siponimod: Relapsing remitting multiple sclerosis and Secondary progressive multiple sclerosis.

How does Siponimod work?

Siponimod is classified as Sphingosine 1-Phosphate Receptor Modulators; its molecular targets in DrugCentral include S1PR1 (modulator), S1PR5 (modulator), S1PR4 (modulator) and S1PR2 (modulator).

When was Siponimod first approved?

Siponimod was first approved by the FDA in 2019.

What drug class does Siponimod belong to?

Siponimod is in the Sphingosine 1-phosphate Receptor Modulator class.

What is the chemical formula of Siponimod?

Siponimod has the molecular formula C29H35F3N2O3 and a molecular weight of 516.61 g/mol.

Sources

• DrugCentral drug card 5326 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2336071 — compound record and bioactivity
• PubChem CID 44599207 — chemical identifiers
• DrugBank DB12371 — drug record
• FDA UNII RR6P8L282I — substance identity
• DailyMed: FDA labels for Siponimod — current prescribing information (label search)
• UniProt P21453 (S1PR1) — target protein
• UniProt Q9H228 (S1PR5) — target protein
• UniProt O95977 (S1PR4) — target protein
• UniProt O95136 (S1PR2) — target protein
• UniProt Q99500 (S1PR3) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.