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

Stem definition	Drug id	CAS RN
immunomodulators, both stimulant/suppressive and stimulant	5326	1230487-00-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: siponimod siponimod fumaric acid mayzent NVP-BAF312-NX BAF-312	Siponimod is a sphingosine-1-phosphate (S1P) receptor modulator. Siponimod binds with high affinity to S1P receptors 1 and 5. Siponimod blocks the capacity of lymphocytes to egress from lymph nodes, reducing the number of lymphocytes in peripheral blood. The mechanism by which siponimod exerts therapeutic effects in multiple sclerosis is unknown, but may involve reduction of lymphocyte migration into the central nervous system. Molecular weight: 516.61 Formula: C29H35F3N2O3 CLOGP: 5.85 LIPINSKI: 1 HAC: 5 HDO: 1 TPSA: 62.13 ALOGS: -6.21 ROTB: 10 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

siponimod
siponimod fumaric acid
mayzent
NVP-BAF312-NX
BAF-312

Siponimod is a sphingosine-1-phosphate (S1P) receptor modulator. Siponimod binds with high affinity to S1P receptors 1 and 5. Siponimod blocks the capacity of lymphocytes to egress from lymph nodes, reducing the number of lymphocytes in peripheral blood. The mechanism by which siponimod exerts therapeutic effects in multiple sclerosis is unknown, but may involve reduction of lymphocyte migration into the central nervous system.

Molecular weight: 516.61
Formula: C29H35F3N2O3
CLOGP: 5.85
LIPINSKI: 1
HAC: 5
HDO: 1
TPSA: 62.13
ALOGS: -6.21
ROTB: 10

Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

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Date	Agency	Company
Jan. 13, 2020	EMA	Novartis Europharm Limited
June 29, 2020	PMDA	Novartis Pharma K.K.
March 26, 2019	FDA	NOVARTIS PHARMS CORP

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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
Lymphocyte count decreased	362.89	27.20	120	4524	30137	63454241
Multiple sclerosis relapse	279.52	27.20	112	4532	48366	63436012
Lymphopenia	220.71	27.20	73	4571	18254	63466124
Gait disturbance	105.20	27.20	95	4549	183083	63301295
Multiple sclerosis	92.66	27.20	42	4602	24330	63460048
Expanded disability status scale score increased	90.50	27.20	18	4626	578	63483800
Basal cell carcinoma	75.19	27.20	38	4606	27953	63456425
Headache	73.76	27.20	150	4494	633091	62851287
Balance disorder	63.07	27.20	51	4593	84371	63400007
Dizziness	54.86	27.20	106	4538	429819	63054559

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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	184.75	36.35	55	1869	13078	34941929
Lymphopenia	116.94	36.35	41	1883	16294	34938713
Gait spastic	113.90	36.35	23	1901	1073	34953934
Muscle spasticity	110.95	36.35	31	1893	5857	34949150
Lymphocyte count decreased	103.93	36.35	41	1883	22581	34932426
Expanded disability status scale score increased	78.84	36.35	14	1910	323	34954684
Multiple sclerosis	68.62	36.35	22	1902	6623	34948384
Needle fatigue	65.42	36.35	14	1910	867	34954140
Relapsing-remitting multiple sclerosis	62.97	36.35	14	1910	1036	34953971
Hypertonic bladder	54.98	36.35	14	1910	1850	34953157

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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
Lymphocyte count decreased	302.56	31.96	109	4257	47180	79692842
Multiple sclerosis relapse	234.25	31.96	90	4276	46443	79693579
Lymphopenia	189.84	31.96	69	4297	30488	79709534
Basal cell carcinoma	145.13	31.96	60	4306	37315	79702707
Multiple sclerosis	118.79	31.96	45	4321	22237	79717785
Gait disturbance	110.44	31.96	91	4275	207415	79532607
Expanded disability status scale score increased	106.38	31.96	20	4346	641	79739381
Balance disorder	94.96	31.96	62	4304	98795	79641227
Central nervous system lesion	82.23	31.96	30	4336	13338	79726684
Urinary tract infection	61.01	31.96	75	4291	274437	79465585

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L04AA42	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Selective immunosuppressants
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
MeSH PA	D000081243	Sphingosine 1 Phosphate Receptor Modulators

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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
Secondary progressive multiple sclerosis	indication	425500002	DOID:0050783
Relapsing remitting multiple sclerosis	indication	426373005	DOID:2378
Sick sinus syndrome	contraindication	36083008	DOID:13884
Atrioventricular block	contraindication	233917008	DOID:0050820

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.28	acidic
pKa2	7.69	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	MAYZENT	NOVARTIS	N209884	March 26, 2019	RX	TABLET	ORAL	8492441	Nov. 30, 2030	A METHOD OF TREATING MULTIPLE SCLEROSIS BY ADMINISTERING SIPONIMOD USING A TITRATION SCHEME TO REACH A MAINTENANCE DOSE
EQ 1MG BASE	MAYZENT	NOVARTIS	N209884	Aug. 24, 2021	RX	TABLET	ORAL	8492441	Nov. 30, 2030	A METHOD OF TREATING MULTIPLE SCLEROSIS BY ADMINISTERING SIPONIMOD USING A TITRATION SCHEME TO REACH A MAINTENANCE DOSE
EQ 2MG BASE	MAYZENT	NOVARTIS	N209884	March 26, 2019	RX	TABLET	ORAL	8492441	Nov. 30, 2030	A METHOD OF TREATING MULTIPLE SCLEROSIS BY ADMINISTERING SIPONIMOD USING A TITRATION SCHEME TO REACH A MAINTENANCE DOSE

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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 0.25MG BASE	MAYZENT	NOVARTIS	N209884	March 26, 2019	RX	TABLET	ORAL	March 26, 2024	NEW CHEMICAL ENTITY
EQ 0.25MG BASE	MAYZENT	NOVARTIS	N209884	March 26, 2019	RX	TABLET	ORAL	March 1, 2025	REVISIONS TO THE LABELING TO INCLUDE RESULTS FROM CLINICAL STUDY CBAF312A2130
EQ 1MG BASE	MAYZENT	NOVARTIS	N209884	Aug. 24, 2021	RX	TABLET	ORAL	March 26, 2024	NEW CHEMICAL ENTITY
EQ 1MG BASE	MAYZENT	NOVARTIS	N209884	Aug. 24, 2021	RX	TABLET	ORAL	March 1, 2025	REVISIONS TO THE LABELING TO INCLUDE RESULTS FROM CLINICAL STUDY CBAF312A2130
EQ 2MG BASE	MAYZENT	NOVARTIS	N209884	March 26, 2019	RX	TABLET	ORAL	March 26, 2024	NEW CHEMICAL ENTITY
EQ 2MG BASE	MAYZENT	NOVARTIS	N209884	March 26, 2019	RX	TABLET	ORAL	March 1, 2025	REVISIONS TO THE LABELING TO INCLUDE RESULTS FROM CLINICAL STUDY CBAF312A2130

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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 1	GPCR	P21453	S1PR1_HUMAN	MODULATOR	EC50	9.41	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Sphingosine 1-phosphate receptor 5	GPCR	Q9H228	S1PR5_HUMAN	MODULATOR	EC50	9.01	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Sphingosine 1-phosphate receptor 4	GPCR	O95977	S1PR4_HUMAN	MODULATOR	EC50	6.13	SCIENTIFIC LITERATURE
Sphingosine 1-phosphate receptor 3	GPCR	Q99500	S1PR3_HUMAN	MODULATOR	EC50	3	SCIENTIFIC LITERATURE
Sphingosine 1-phosphate receptor 2	GPCR	O95136	S1PR2_HUMAN	MODULATOR	EC50	4	SCIENTIFIC LITERATURE

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External reference:

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ID	Source
017942	NDDF
017943	NDDF
1234627-85-0	SECONDARY_CAS_RN
2121085	RXNORM
312581	MMSL
36617	MMSL
4038283	VANDF
44599207	PUBCHEM_CID
786997005	SNOMEDCT_US
787019001	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
MAYZENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0979	TABLET, FILM COATED	0.25 mg	ORAL	NDA	30 sections
MAYZENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0979	TABLET, FILM COATED	0.25 mg	ORAL	NDA	30 sections
MAYZENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0979	TABLET, FILM COATED	0.25 mg	ORAL	NDA	30 sections
MAYZENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0979	TABLET, FILM COATED	0.25 mg	ORAL	NDA	30 sections
MAYZENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0986	TABLET, FILM COATED	2 mg	ORAL	NDA	30 sections
MAYZENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0986	TABLET, FILM COATED	2 mg	ORAL	NDA	30 sections
MAYZENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0986	TABLET, FILM COATED	2 mg	ORAL	NDA	30 sections
MAYZENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0986	TABLET, FILM COATED	2 mg	ORAL	NDA	30 sections
MAYZENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1014	TABLET, FILM COATED	1 mg	ORAL	NDA	30 sections
MAYZENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1014	TABLET, FILM COATED	1 mg	ORAL	NDA	30 sections

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