Details of the Drug

General Information of Drug (ID: DM5JVAN)

Drug Name

Fingolimod

Synonyms

2-Amino-2-(4-octylphenethyl)propane-1,3-diol

Indication

Disease Entry	ICD 11	Status	REF
Multiple sclerosis	8A40	Approved	[1]
Primary progressive multiple sclerosis	8A40.1	Approved	[2]
Coronavirus Disease 2019 (COVID-19)	1D6Y	Phase 2	[3]
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Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 1

Molecular Weight (mw)

307.5

Logarithm of the Partition Coefficient (xlogp)

4.2

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Clearance: The drug present in the plasma can be removed from the body at the rate of 1.53 mL/min/kg [4]
Half-life: The concentration or amount of drug in body reduced by one-half in 144 hours [4]
Unbound Fraction: The unbound fraction of drug in plasma is 0.002% [4]
Vd: Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 17.3 L/kg [4]

Chemical Identifiers

Formula: C19H33NO2
IUPAC Name: 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol
Canonical SMILES: CCCCCCCCC1=CC=C(C=C1)CCC(CO)(CO)N
InChI: InChI=1S/C19H33NO2/c1-2-3-4-5-6-7-8-17-9-11-18(12-10-17)13-14-19(20,15-21)16-22/h9-12,21-22H,2-8,13-16,20H2,1H3
InChIKey: KKGQTZUTZRNORY-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 107970
ChEBI ID: CHEBI:63115
CAS Number: 162359-55-9
DrugBank ID: DB08868
TTD ID: D07UHS
INTEDE ID: DR0696
ACDINA ID: D00276

Combinatorial Drugs (CBD)

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Repurposed Drugs (RPD)

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Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Sphingosine-1-phosphate receptor 1 (S1PR1)	TT9JZCK	S1PR1_HUMAN	Modulator	[5]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 4F12 (CYP4F12)	DED26GV	CP4FC_HUMAN	Substrate	[6]
Cytochrome P450 4F2 (CYP4F2)	DE3GT9C	CP4F2_HUMAN	Substrate	[6]

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Molecular Interaction Atlas (MIA)

MIA Detail

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Molecular Expression Atlas of This Drug

ICD Disease Classification

08 Nervous system disease

Disease Class

ICD-11: 8A40 Multiple sclerosis

The Studied Tissue

Plasmacytoid dendritic cells

The Studied Disease

Multiple sclerosis [ICD-11:8A40]

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Cytochrome P450 4F12 (CYP4F12)	DME	CYP4F12	4.68E-01	-5.96E-03	-2.58E-02
Cytochrome P450 4F2 (CYP4F2)	DME	CYP4F2	2.36E-01	-6.45E-02	-1.81E-01

Molecular Expression Atlas (MEA)

MEA Detail

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Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Fingolimod

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Tecfidera	DM2OVDT	Major	Additive immunosuppressive effects by the combination of Fingolimod and Tecfidera.	Multiple sclerosis [8A40]	[7]
Ocrelizumab	DMEZ2KH	Major	Additive immunosuppressive effects by the combination of Fingolimod and Ocrelizumab.	Multiple sclerosis [8A40]	[7]
Ozanimod	DMT6AM2	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Ozanimod.	Multiple sclerosis [8A40]	[7]
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Coadministration of a Drug Treating the Disease Different from Fingolimod (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Remdesivir	DMBFZ6L	Moderate	Increased risk of hepatotoxicity by the combination of Fingolimod and Remdesivir.	1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019]	[8]
Ivosidenib	DM8S6T7	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Ivosidenib.	Acute myeloid leukaemia [2A60]	[9]
Arn-509	DMT81LZ	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Arn-509.	Acute myeloid leukaemia [2A60]	[9]
Oliceridine	DM6MDCF	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Oliceridine.	Acute pain [MG31]	[9]
Siltuximab	DMGEATB	Major	Additive immunosuppressive effects by the combination of Fingolimod and Siltuximab.	Anemia [3A00-3A9Z]	[7]
Ivabradine	DM0L594	Moderate	Increased risk of bradycardia by the combination of Fingolimod and Ivabradine.	Angina pectoris [BA40]	[7]
Bedaquiline	DM3906J	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Bedaquiline.	Antimicrobial drug resistance [MG50-MG52]	[9]
Levalbuterol	DM5YBO1	Moderate	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Levalbuterol.	Asthma [CA23]	[10]
Dupilumab	DMOAD2Y	Major	Additive immunosuppressive effects by the combination of Fingolimod and Dupilumab.	Atopic eczema [EA80]	[7]
Eribulin	DM1DX4Q	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Eribulin.	Breast cancer [2C60-2C6Y]	[7]
Talazoparib	DM1KS78	Major	Additive immunosuppressive effects by the combination of Fingolimod and Talazoparib.	Breast cancer [2C60-2C6Y]	[7]
LY2835219	DM93VBZ	Major	Additive immunosuppressive effects by the combination of Fingolimod and LY2835219.	Breast cancer [2C60-2C6Y]	[7]
Palbociclib	DMD7L94	Major	Additive immunosuppressive effects by the combination of Fingolimod and Palbociclib.	Breast cancer [2C60-2C6Y]	[7]
PF-04449913	DMSB068	Major	Additive immunosuppressive effects by the combination of Fingolimod and PF-04449913.	Chronic myelomonocytic leukaemia [2A40]	[7]
Olodaterol	DM62B78	Moderate	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Olodaterol.	Chronic obstructive pulmonary disease [CA22]	[11]
Vilanterol	DMF5EK1	Moderate	Increased risk of prolong QT interval by the combination of Fingolimod and Vilanterol.	Chronic obstructive pulmonary disease [CA22]	[10]
Aflibercept	DMT3D5I	Major	Additive immunosuppressive effects by the combination of Fingolimod and Aflibercept.	Colorectal cancer [2B91]	[7]
Osilodrostat	DMIJC9X	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Osilodrostat.	Cushing syndrome [5A70]	[9]
Polatuzumab vedotin	DMF6Y0L	Major	Additive immunosuppressive effects by the combination of Fingolimod and Polatuzumab vedotin.	Diffuse large B-cell lymphoma [2A81]	[7]
Lisocabtagene maraleucel	DMP45ME	Major	Additive immunosuppressive effects by the combination of Fingolimod and Lisocabtagene maraleucel.	Diffuse large B-cell lymphoma [2A81]	[7]
Axicabtagene ciloleucel	DMYHN59	Major	Additive immunosuppressive effects by the combination of Fingolimod and Axicabtagene ciloleucel.	Diffuse large B-cell lymphoma [2A81]	[7]
Deutetrabenazine	DMUPFLI	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Deutetrabenazine.	Dystonic disorder [8A02]	[9]
Ingrezza	DMVPLNC	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Ingrezza.	Dystonic disorder [8A02]	[9]
Cannabidiol	DM0659E	Moderate	Increased risk of hepatotoxicity by the combination of Fingolimod and Cannabidiol.	Epileptic encephalopathy [8A62]	[12]
Bay 80-6946	DMLOS5R	Major	Additive immunosuppressive effects by the combination of Fingolimod and Bay 80-6946.	Follicular lymphoma [2A80]	[7]
Avapritinib	DMK2GZX	Major	Additive immunosuppressive effects by the combination of Fingolimod and Avapritinib.	Gastrointestinal stromal tumour [2B5B]	[7]
Levobetaxolol	DMSREPX	Moderate	Increased risk of atrioventricular block by the combination of Fingolimod and Levobetaxolol.	Glaucoma [9C61]	[7]
177Lu-DOTATATE	DMT8GVU	Major	Additive immunosuppressive effects by the combination of Fingolimod and 177Lu-DOTATATE.	Hepatitis virus infection [1E50-1E51]	[7]
Brentuximab vedotin	DMWLC57	Major	Additive immunosuppressive effects by the combination of Fingolimod and Brentuximab vedotin.	Hodgkin lymphoma [2B30]	[7]
Fostemsavir	DM50ILT	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Fostemsavir.	Human immunodeficiency virus disease [1C60-1C62]	[9]
Teriflunomide	DMQ2FKJ	Major	Additive immunosuppressive effects by the combination of Fingolimod and Teriflunomide.	Hyper-lipoproteinaemia [5C80]	[13]
Levamlodipine	DM92S6N	Moderate	Increased risk of atrioventricular block by the combination of Fingolimod and Levamlodipine.	Hypertension [BA00-BA04]	[7]
Brigatinib	DM7W94S	Major	Additive immunosuppressive effects by the combination of Fingolimod and Brigatinib.	Lung cancer [2C25]	[7]
Ceritinib	DMB920Z	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Ceritinib.	Lung cancer [2C25]	[9]
Lurbinectedin	DMEFRTZ	Major	Additive immunosuppressive effects by the combination of Fingolimod and Lurbinectedin.	Lung cancer [2C25]	[7]
Alectinib	DMP1I6Y	Moderate	Increased risk of atrioventricular block by the combination of Fingolimod and Alectinib.	Lung cancer [2C25]	[7]
Osimertinib	DMRJLAT	Major	Additive immunosuppressive effects by the combination of Fingolimod and Osimertinib.	Lung cancer [2C25]	[7]
Selpercatinib	DMZR15V	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Selpercatinib.	Lung cancer [2C25]	[9]
Belimumab	DM3OBQF	Major	Additive immunosuppressive effects by the combination of Fingolimod and Belimumab.	Lupus erythematosus [4A40]	[7]
Obinutuzumab	DM3BVAE	Major	Additive immunosuppressive effects by the combination of Fingolimod and Obinutuzumab.	Mature B-cell leukaemia [2A82]	[7]
Idelalisib	DM602WT	Major	Additive immunosuppressive effects by the combination of Fingolimod and Idelalisib.	Mature B-cell leukaemia [2A82]	[7]
GDC-0199	DMH0QKA	Major	Additive immunosuppressive effects by the combination of Fingolimod and GDC-0199.	Mature B-cell leukaemia [2A82]	[7]
IPI-145	DMWA24P	Major	Additive immunosuppressive effects by the combination of Fingolimod and IPI-145.	Mature B-cell leukaemia [2A82]	[7]
Acalabrutinib	DM7GCVW	Major	Additive immunosuppressive effects by the combination of Fingolimod and Acalabrutinib.	Mature B-cell lymphoma [2A85]	[7]
Blinatumomab	DMGECIJ	Major	Additive immunosuppressive effects by the combination of Fingolimod and Blinatumomab.	Mature B-cell lymphoma [2A85]	[7]
Ibrutinib	DMHZCPO	Major	Additive immunosuppressive effects by the combination of Fingolimod and Ibrutinib.	Mature B-cell lymphoma [2A85]	[7]
Tisagenlecleucel	DMM9BJD	Major	Additive immunosuppressive effects by the combination of Fingolimod and Tisagenlecleucel.	Mature B-cell lymphoma [2A85]	[7]
Ponatinib	DMYGJQO	Major	Additive immunosuppressive effects by the combination of Fingolimod and Ponatinib.	Mature B-cell lymphoma [2A85]	[7]
Vemurafenib	DM62UG5	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Vemurafenib.	Melanoma [2C30]	[9]
LGX818	DMNQXV8	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and LGX818.	Melanoma [2C30]	[9]
Carfilzomib	DM48K0X	Major	Additive immunosuppressive effects by the combination of Fingolimod and Carfilzomib.	Multiple myeloma [2A83]	[7]
Selinexor	DMBD4K3	Major	Additive immunosuppressive effects by the combination of Fingolimod and Selinexor.	Multiple myeloma [2A83]	[7]
Belantamab mafodotin	DMBT3AI	Major	Additive immunosuppressive effects by the combination of Fingolimod and Belantamab mafodotin.	Multiple myeloma [2A83]	[7]
Daratumumab	DMKCIUZ	Major	Additive immunosuppressive effects by the combination of Fingolimod and Daratumumab.	Multiple myeloma [2A83]	[7]
Deflazacort	DMV0RNS	Major	Additive immunosuppressive effects by the combination of Fingolimod and Deflazacort.	Muscular dystrophy [8C70]	[7]
Ruxolitinib	DM7Q98D	Major	Additive immunosuppressive effects by the combination of Fingolimod and Ruxolitinib.	Myeloproliferative neoplasm [2A20]	[7]
Inebilizumab	DMI0RHA	Major	Additive immunosuppressive effects by the combination of Fingolimod and Inebilizumab.	Nervous system paraneoplastic/autoimmune disorder [8E4A]	[7]
Atezolizumab	DMMF8U0	Major	Additive immunosuppressive effects by the combination of Fingolimod and Atezolizumab.	Non-small cell lung cancer [2C25]	[7]
Entrectinib	DMMPTLH	Major	Additive immunosuppressive effects by the combination of Fingolimod and Entrectinib.	Non-small cell lung cancer [2C25]	[7]
Olaparib	DM8QB1D	Major	Additive immunosuppressive effects by the combination of Fingolimod and Olaparib.	Ovarian cancer [2C73]	[7]
Rucaparib	DM9PVX8	Major	Additive immunosuppressive effects by the combination of Fingolimod and Rucaparib.	Ovarian cancer [2C73]	[7]
MK-4827	DMLYGH4	Major	Additive immunosuppressive effects by the combination of Fingolimod and MK-4827.	Ovarian cancer [2C73]	[7]
Triclabendazole	DMPWGBR	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Triclabendazole.	Parasitic worm infestation [1F90]	[9]
Macimorelin	DMQYJIR	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Macimorelin.	Pituitary gland disorder [5A60-5A61]	[9]
Lefamulin	DME6G97	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Lefamulin.	Pneumonia [CA40]	[9]
Enzalutamide	DMGL19D	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Enzalutamide.	Prostate cancer [2C82]	[9]
Relugolix	DMK7IWL	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Relugolix.	Prostate cancer [2C82]	[9]
Brodalumab	DMASDQ6	Major	Additive immunosuppressive effects by the combination of Fingolimod and Brodalumab.	Psoriasis [EA90]	[7]
Tildrakizumab	DMLW9HG	Major	Additive immunosuppressive effects by the combination of Fingolimod and Tildrakizumab.	Psoriasis [EA90]	[7]
Risankizumab	DMM32GT	Major	Additive immunosuppressive effects by the combination of Fingolimod and Risankizumab.	Psoriasis [EA90]	[7]
Ixekizumab	DMXW92T	Major	Additive immunosuppressive effects by the combination of Fingolimod and Ixekizumab.	Psoriasis [EA90]	[7]
Upadacitinib	DM32B5U	Major	Additive immunosuppressive effects by the combination of Fingolimod and Upadacitinib.	Rheumatoid arthritis [FA20]	[7]
Baricitinib	DM4ONW5	Major	Additive immunosuppressive effects by the combination of Fingolimod and Baricitinib.	Rheumatoid arthritis [FA20]	[7]
Tofacitinib	DMBS370	Major	Additive immunosuppressive effects by the combination of Fingolimod and Tofacitinib.	Rheumatoid arthritis [FA20]	[7]
Sarilumab	DMOGNXY	Major	Additive immunosuppressive effects by the combination of Fingolimod and Sarilumab.	Rheumatoid arthritis [FA20]	[7]
Mogamulizumab	DMISH0Z	Major	Additive immunosuppressive effects by the combination of Fingolimod and Mogamulizumab.	Sezary syndrome [2B02]	[7]
LEE011	DMMX75K	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and LEE011.	Solid tumour/cancer [2A00-2F9Z]	[7]
Pitolisant	DM8RFNJ	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Pitolisant.	Somnolence [MG42]	[9]
Pomalidomide	DMTGBAX	Major	Additive immunosuppressive effects by the combination of Fingolimod and Pomalidomide.	Systemic sclerosis [4A42]	[7]
Lenvatinib	DMB1IU4	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Lenvatinib.	Thyroid cancer [2D10]	[9]
Cabozantinib	DMIYDT4	Major	Increased risk of ventricular arrhythmias by the combination of Fingolimod and Cabozantinib.	Thyroid cancer [2D10]	[9]
Durvalumab	DM4PVDY	Major	Additive immunosuppressive effects by the combination of Fingolimod and Durvalumab.	Ureteral cancer [2C92]	[7]
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Mannitol	E00103	6251	Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Magnesium stearate	E00208	11177	lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
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Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Fingolimod 0.5 mg capsule	0.5 mg	Oral Capsule	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2407).
3	ClinicalTrials.gov (NCT04280588) Fingolimod in COVID-19
4	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
5	Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
6	CYP4F enzymes are responsible for the elimination of fingolimod (FTY720), a novel treatment of relapsing multiple sclerosis. Drug Metab Dispos. 2011 Feb;39(2):191-8.
7	Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
8	Cerner Multum, Inc. "Australian Product Information.".
9	Canadian Pharmacists Association.
10	Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
11	Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176]
12	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
13	Product Information. Arava (leflunomide). Hoechst Marion-Roussel Inc, Kansas City, MO.