Fingolimod

Sphingosine 1-phosphate Receptor Modulator — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Fingolimod is an ofp drug in the Sphingosine 1-phosphate Receptor Modulator class catalogued in DrugCentral. It was first approved by the FDA in 2010. Its mechanism of action is classified as Sphingosine 1-Phosphate Receptor Modulators. DrugCentral lists 8 molecular targets, including S1PR5, S1PR4 and S1PR1. Recorded indications include Relapsing remitting multiple sclerosis.

• Approval status: ofp (first approved 2010 by the FDA).
• Drug class: Sphingosine 1-phosphate Receptor Modulator.
• Mechanism of action: Sphingosine 1-Phosphate Receptor Modulators.
• Molecular targets: S1PR5, S1PR4, S1PR1 and S1PR3 (8 listed in DrugCentral).
• Indications: Relapsing remitting multiple sclerosis.
• ATC code: L04AE01 (Sphingosine-1-phosphate (S1P) receptor modulators).
• Molecular formula: C19H33NO2; molecular weight 307.48 g/mol.

Indications & contraindications

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

Indications (1)

• Relapsing remitting multiple sclerosis

Contraindications (17)

• Acute infectious disease
• Bradycardia
• Breastfeeding (mother)
• Chronic infectious disease
• Complete atrioventricular block
• Diabetes mellitus
• Disorder of lung
• Hepatic failure
• Kidney disease
• Leukopenia
• Liver function tests abnormal
• Macular retinal edema
• Pregnancy, function
• Second degree atrioventricular block
• Sick sinus syndrome
• Syncope
• Uveitis

Mechanism & targets

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

Molecular targets (8)

Target	Gene	Action	Activity
Sphingosine 1-phosphate receptor 5	S1PR5	agonist	EC50 9.52
Sphingosine 1-phosphate receptor 4	S1PR4	agonist	EC50 9.52
Sphingosine 1-phosphate receptor 1	S1PR1	agonist	EC50 9.52
Sphingosine 1-phosphate receptor 3	S1PR3	agonist	EC50 8.52
Transient receptor potential cation channel subfamily M member 7	Trpm7	blocker	IC50 6.14
Troponin C, slow skeletal and cardiac muscles	TNNC1	unknown	Kd 5.30
Sphingosine-1-phosphate lyase 1	SGPL1	unknown	IC50 4.77
Sphingosine-1-phosphate lyase 1, S1PL, SP-lyase 1, SPL 1, mSPL, EC 4.1.2.27	Sgpl1	unknown	IC50 4.28

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2021-08-18	EMA	—	MYLAN IRELAND LIMITED
2010-09-21	FDA	—	NOVARTIS

ATC classification

ATC code	Therapeutic hierarchy
L04AE01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › IMMUNOSUPPRESSANTS › IMMUNOSUPPRESSANTS › Sphingosine-1-phosphate (S1P) receptor modulators

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
Multiple sclerosis relapse	9418.3
Lymphocyte count decreased	6706.8
Central nervous system lesion	3957.7
Lymphopenia	3420.3
Expanded disability status scale score increased	2210.0
White blood cell count decreased	1892.2
Macular oedema	1690.7
JC polyomavirus test positive	960.4
Heart rate decreased	911.5
Visual impairment	902.1
Off label use	897.5
Vision blurred	877.1

Chemical structure

• Molecular formula: C₁₉H₃₃NO₂
• Molecular weight: 307.48 g/mol
• CAS number: 162359-55-9
• InChIKey: KKGQTZUTZRNORY-UHFFFAOYSA-N
• PubChem CID: 107970

CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1

Frequently asked questions

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

What is Fingolimod used for?

DrugCentral lists the following indications for Fingolimod: Relapsing remitting multiple sclerosis.

How does Fingolimod work?

Fingolimod is classified as Sphingosine 1-Phosphate Receptor Modulators; its molecular targets in DrugCentral include S1PR5 (agonist), S1PR4 (agonist), S1PR1 (agonist) and S1PR3 (agonist).

When was Fingolimod first approved?

Fingolimod was first approved by the FDA in 2010.

What drug class does Fingolimod belong to?

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

What is the chemical formula of Fingolimod?

Fingolimod has the molecular formula C19H33NO2 and a molecular weight of 307.48 g/mol.

Sources

• DrugCentral drug card 4167 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL314854 — compound record and bioactivity
• PubChem CID 107970 — chemical identifiers
• DrugBank DB08868 — drug record
• FDA UNII 3QN8BYN5QF — substance identity
• DailyMed: FDA labels for Fingolimod — current prescribing information (label search)
• UniProt Q9H228 (S1PR5) — target protein
• UniProt O95977 (S1PR4) — target protein
• UniProt P21453 (S1PR1) — target protein
• UniProt Q99500 (S1PR3) — target protein
• UniProt P63316 (TNNC1) — target protein
• UniProt O95470 (SGPL1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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