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fingolimod 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
immunomodulators, both stimulant/suppressive and stimulant	4167	162359-55-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: FTY-720 fingolimod fingolimod hydrochloride gilenya fingolimod HCl	A sphingosine-derivative and IMMUNOSUPPRESSIVE AGENT that blocks the migration and homing of LYMPHOCYTES to the CENTRAL NERVOUS SYSTEM through its action on SPHINGOSINE 1-PHOSPHATE RECEPTORS. It is used in the treatment of MULTIPLE SCLEROSIS. Molecular weight: 307.48 Formula: C19H33NO2 CLOGP: 5.06 LIPINSKI: 1 HAC: 3 HDO: 3 TPSA: 66.48 ALOGS: -4.65 ROTB: 12 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

FTY-720
fingolimod
fingolimod hydrochloride
gilenya
fingolimod HCl

A sphingosine-derivative and IMMUNOSUPPRESSIVE AGENT that blocks the migration and homing of LYMPHOCYTES to the CENTRAL NERVOUS SYSTEM through its action on SPHINGOSINE 1-PHOSPHATE RECEPTORS. It is used in the treatment of MULTIPLE SCLEROSIS.

Molecular weight: 307.48
Formula: C19H33NO2
CLOGP: 5.06
LIPINSKI: 1
HAC: 3
HDO: 3
TPSA: 66.48
ALOGS: -4.65
ROTB: 12

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.50	mg	O

ADMET properties:

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Property	Value	Reference
Vd (Volume of distribution)	17.30 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	144 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	1.53 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	0.93 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
fu (Fraction unbound in plasma)	0.00 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Aug. 18, 2021	EMA	MYLAN IRELAND LIMITED
Sept. 21, 2010	FDA	NOVARTIS

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Multiple sclerosis relapse	5098.35	13.23	2055	84450	46423	63356094
Lymphocyte count decreased	4456.86	13.23	1640	84865	28617	63373900
Central nervous system lesion	2515.72	13.23	822	85683	9813	63392704
Lymphopenia	1998.50	13.23	799	85706	17528	63384989
White blood cell count decreased	1380.59	13.23	1290	85215	137814	63264703
Expanded disability status scale score increased	1258.44	13.23	263	86242	333	63402184
Macular oedema	995.01	13.23	319	86186	3558	63398959
Heart rate decreased	711.12	13.23	549	85956	45011	63357506
Visual impairment	695.53	13.23	708	85797	83738	63318779
Melanocytic naevus	642.50	13.23	239	86266	4269	63398248

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Multiple sclerosis relapse	1965.13	16.68	605	23043	12528	34920755
Lymphocyte count decreased	1114.70	16.68	457	23191	22165	34911118
Central nervous system lesion	816.17	16.68	262	23386	6201	34927082
Expanded disability status scale score increased	588.76	16.68	113	23535	224	34933059
Lymphopenia	480.26	16.68	230	23418	16105	34917178
Macular oedema	350.79	16.68	114	23534	2800	34930483
Alanine aminotransferase increased	332.29	16.68	337	23311	80478	34852805
Gamma-glutamyltransferase increased	264.84	16.68	192	23456	29039	34904244
Gait disturbance	262.29	16.68	305	23343	84835	34848448
White blood cell count decreased	243.78	16.68	311	23337	95134	34838149

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Multiple sclerosis relapse	4586.28	13.47	1742	80221	44791	79617634
Lymphocyte count decreased	4244.48	13.47	1654	80309	45635	79616790
Central nervous system lesion	2048.49	13.47	695	81268	12673	79649752
Lymphopenia	1737.88	13.47	773	81190	29784	79632641
Expanded disability status scale score increased	1359.05	13.47	272	81691	389	79662036
White blood cell count decreased	1272.85	13.47	1245	80718	187043	79475382
Macular oedema	879.20	13.47	295	81668	5179	79657246
Melanocytic naevus	835.38	13.47	274	81689	4467	79657958
Heart rate decreased	718.52	13.47	588	81375	69728	79592697
Vision blurred	652.94	13.47	667	81296	105231	79557194

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L04AA27	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Selective immunosuppressants
CHEBI has role	CHEBI:35705	immunosuppressive agents
CHEBI has role	CHEBI:50266	Prodrugs
CHEBI has role	CHEBI:63114	SIP agonist
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:73416	CB1 receptor antagonists
FDA EPC	N0000181816	Sphingosine 1-phosphate Receptor Modulator
FDA MoA	N0000181815	Sphingosine 1-Phosphate Receptor Modulators
MeSH PA	D007155	Immunologic Factors
MeSH PA	D007166	Immunosuppressive Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Relapsing remitting multiple sclerosis	indication	426373005	DOID:2378
Disorder of lung	contraindication	19829001	DOID:850
Complete atrioventricular block	contraindication	27885002
Sick sinus syndrome	contraindication	36083008	DOID:13884
Macular retinal edema	contraindication	37231002	DOID:4449
Bradycardia	contraindication	48867003
Hepatic failure	contraindication	59927004
Acute infectious disease	contraindication	63171007
Diabetes mellitus	contraindication	73211009	DOID:9351
Leukopenia	contraindication	84828003	DOID:615

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🐶 Veterinary Drug Use

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🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.57	acidic
pKa2	13.18	acidic
pKa3	8.51	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 0.25MG BASE	GILENYA	NOVARTIS	N022527	May 11, 2018	RX	CAPSULE	ORAL	9592208	March 30, 2032	TREATMENT OF MULTIPLE SCLEROSIS IN THE PEDIATRIC PATIENT POPULATION WITH 0.25 MG FINGOLIMOD
EQ 0.5MG BASE	GILENYA	NOVARTIS	N022527	Sept. 21, 2010	RX	CAPSULE	ORAL	9187405	June 25, 2027	TREATMENT OF RELAPSING-REMITTING SCLEROSIS (MS)
EQ 0.5MG BASE	GILENYA	NOVARTIS	N022527	Sept. 21, 2010	RX	CAPSULE	ORAL	10543179	Dec. 25, 2027	TREATMENT OF RELAPSING REMITTING MULTIPLE SCLEROSIS BY DETERMINING VARICELLA ZOSTER VIRUS (VZV) STATUS AND VACCINATING PRIOR TO COMMENCING TREATMENT

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 0.5MG BASE	FINGOLIMOD HYDROCHLORIDE	STRIDES PHARMA	A207971	June 29, 2020	DISCN	CAPSULE	ORAL	March 20, 2023	PATENT CHALLENGE
EQ 0.5MG BASE	FINGOLIMOD HYDROCHLORIDE	GLENMARK PHARMS LTD	A207985	June 18, 2020	RX	CAPSULE	ORAL	March 20, 2023	PATENT CHALLENGE
EQ 0.5MG BASE	FINGOLIMOD HYDROCHLORIDE	ACCORD HLTHCARE	A207991	Oct. 28, 2020	RX	CAPSULE	ORAL	March 20, 2023	PATENT CHALLENGE
EQ 0.5MG BASE	FINGOLIMOD HYDROCHLORIDE	TEVA PHARMS USA	A208008	July 2, 2020	DISCN	CAPSULE	ORAL	March 20, 2023	PATENT CHALLENGE

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sphingosine 1-phosphate receptor 4	GPCR	O95977	S1PR4_HUMAN	AGONIST	EC50	9.52	CHEMBL	CHEMBL
Sphingosine 1-phosphate receptor 1	GPCR	P21453	S1PR1_HUMAN	AGONIST	EC50	9.52	CHEMBL	CHEMBL
Sphingosine 1-phosphate receptor 5	GPCR	Q9H228	S1PR5_HUMAN	AGONIST	EC50	9.52	CHEMBL	CHEMBL
Sphingosine 1-phosphate receptor 3	GPCR	Q99500	S1PR3_HUMAN	AGONIST	EC50	8.52	CHEMBL	CHEMBL
Sphingosine-1-phosphate lyase 1	Enzyme	O95470	SGPL1_HUMAN		IC50	4.77	CHEMBL
Sphingosine-1-phosphate lyase 1, S1PL, SP-lyase 1, SPL 1, mSPL, EC 4.1.2.27	Unclassified		SGPL1_MOUSE		IC50	4.28	CHEMBL
Transient receptor potential cation channel subfamily M member 7	Ion channel		TRPM7_MOUSE	BLOCKER	IC50	6.14	IUPHAR

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External reference:

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ID	Source
013519	NDDF
013520	NDDF
1012891	RXNORM
107970	PUBCHEM_CID
162359-56-0	SECONDARY_CAS_RN
177212	MMSL
2407	IUPHAR_LIGAND_ID
253713	MMSL
27529	MMSL
3QN8BYN5QF	UNII

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Fingolimod	HUMAN PRESCRIPTION DRUG LABEL	1	0378-4525	CAPSULE	0.50 mg	ORAL	ANDA	32 sections
Fingolimod	HUMAN PRESCRIPTION DRUG LABEL	1	0378-4525	CAPSULE	0.50 mg	ORAL	ANDA	32 sections
Fingolimod	Human Prescription Drug Label	1	31722-889	CAPSULE	0.50 mg	ORAL	ANDA	27 sections
FINGOLIMOD	HUMAN PRESCRIPTION DRUG LABEL	1	43547-003	CAPSULE	0.50 mg	ORAL	ANDA	27 sections
Fingolimod	HUMAN PRESCRIPTION DRUG LABEL	1	43598-285	CAPSULE	0.50 mg	ORAL	ANDA	28 sections
Fingolimod	HUMAN PRESCRIPTION DRUG LABEL	1	60505-4332	CAPSULE	0.50 mg	ORAL	ANDA	28 sections
Fingolimod	HUMAN PRESCRIPTION DRUG LABEL	1	60505-4332	CAPSULE	0.50 mg	ORAL	ANDA	28 sections
Fingolimod	Human Prescription Drug Label	1	62756-064	CAPSULE	0.50 mg	ORAL	ANDA	30 sections
FINGOLIMOD	HUMAN PRESCRIPTION DRUG LABEL	1	64380-776	CAPSULE	0.50 mg	ORAL	ANDA	27 sections
FINGOLIMOD	HUMAN PRESCRIPTION DRUG LABEL	1	64380-776	CAPSULE	0.50 mg	ORAL	ANDA	27 sections

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