Details of the Drug

General Information of Drug (ID: DM2OVDT)

Drug Name

TECFIDERA

Synonyms

DIMETHYL FUMARATE

Indication

Disease Entry	ICD 11	Status	REF
Multiple sclerosis	8A40	Approved	[1]
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Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

144.12

Logarithm of the Partition Coefficient (xlogp)

0.7

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Half-life: The concentration or amount of drug in body reduced by one-half in 1 hour [2]
Metabolism: The drug is metabolized via the esterases []
Vd: The volume of distribution (Vd) of drug is 53-73 L []

Chemical Identifiers

Formula: C6H8O4
IUPAC Name: dimethyl (E)-but-2-enedioate
Canonical SMILES: COC(=O)/C=C/C(=O)OC
InChI: InChI=1S/C6H8O4/c1-9-5(7)3-4-6(8)10-2/h3-4H,1-2H3/b4-3+
InChIKey: LDCRTTXIJACKKU-ONEGZZNKSA-N

Cross-matching ID

PubChem CID: 637568
ChEBI ID: CHEBI:76004
CAS Number: 624-49-7
DrugBank ID: DB08908
TTD ID: D0A7MY
ACDINA ID: D00202

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
NFE2-related factor 2 pathway (Nrf2 pathway)	TTK3Q4W	NOUNIPROTAC	Inhibitor	[3]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
C-C motif chemokine 2 (CCL2)	OTAD2HEL	CCL2_HUMAN	Gene/Protein Processing	[4]
Ferritin heavy chain (FTH1)	OT6IFS0O	FRIH_HUMAN	Gene/Protein Processing	[5]
Ferritin light chain (FTL)	OTYQA8A6	FRIL_HUMAN	Gene/Protein Processing	[5]
Heme oxygenase 1 (HMOX1)	OTC1W6UX	HMOX1_HUMAN	Gene/Protein Processing	[4]
Intercellular adhesion molecule 1 (ICAM1)	OTTOIX77	ICAM1_HUMAN	Gene/Protein Processing	[4]
Interleukin-6 receptor subunit alpha (IL6R)	OTCQL07Z	IL6RA_HUMAN	Gene/Protein Processing	[6]
NAD(P)H dehydrogenase 1 (NQO1)	OTZGGIVK	NQO1_HUMAN	Gene/Protein Processing	[7]
Nuclear factor erythroid 2-related factor 2 (NFE2L2)	OT0HENJ5	NF2L2_HUMAN	Protein Interaction/Cellular Processes	[8]
Phospholipid hydroperoxide glutathione peroxidase GPX4 (GPX4)	OTRAFFX2	GPX4_HUMAN	Biochemical Pathways	[9]
Transcription regulator protein BACH1 (BACH1)	OTY8004K	BACH1_HUMAN	Protein Interaction/Cellular Processes	[8]

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Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as TECFIDERA

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Siponimod	DM2R86O	Major	Additive immunosuppressive effects by the combination of Tecfidera and Siponimod.	Multiple sclerosis [8A40]	[10]
Ocrelizumab	DMEZ2KH	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Ocrelizumab.	Multiple sclerosis [8A40]	[11]
Ozanimod	DMT6AM2	Major	Additive immunosuppressive effects by the combination of Tecfidera and Ozanimod.	Multiple sclerosis [8A40]	[12]
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Coadministration of a Drug Treating the Disease Different from TECFIDERA (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Remdesivir	DMBFZ6L	Moderate	Increased risk of hepatotoxicity by the combination of Tecfidera and Remdesivir.	1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019]	[10]
Emapalumab	DMZG5WL	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Emapalumab.	Adaptive immunity immunodeficiency [4A01]	[13]
Siltuximab	DMGEATB	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Siltuximab.	Anemia [3A00-3A9Z]	[13]
Dupilumab	DMOAD2Y	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Dupilumab.	Atopic eczema [EA80]	[13]
Pexidartinib	DMS2J0Z	Major	Increased risk of hepatotoxicity by the combination of Tecfidera and Pexidartinib.	Bone/articular cartilage neoplasm [2F7B]	[14]
Talazoparib	DM1KS78	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Talazoparib.	Breast cancer [2C60-2C6Y]	[13]
LY2835219	DM93VBZ	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and LY2835219.	Breast cancer [2C60-2C6Y]	[13]
Palbociclib	DMD7L94	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Palbociclib.	Breast cancer [2C60-2C6Y]	[13]
Polatuzumab vedotin	DMF6Y0L	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Polatuzumab vedotin.	Diffuse large B-cell lymphoma [2A81]	[13]
Axicabtagene ciloleucel	DMYHN59	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Axicabtagene ciloleucel.	Diffuse large B-cell lymphoma [2A81]	[13]
Cannabidiol	DM0659E	Moderate	Increased risk of hepatotoxicity by the combination of Tecfidera and Cannabidiol.	Epileptic encephalopathy [8A62]	[12]
Bay 80-6946	DMLOS5R	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Bay 80-6946.	Follicular lymphoma [2A80]	[13]
Avapritinib	DMK2GZX	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Avapritinib.	Gastrointestinal stromal tumour [2B5B]	[13]
177Lu-DOTATATE	DMT8GVU	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and 177Lu-DOTATATE.	Hepatitis virus infection [1E50-1E51]	[13]
Brigatinib	DM7W94S	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Brigatinib.	Lung cancer [2C25]	[13]
Lurbinectedin	DMEFRTZ	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Lurbinectedin.	Lung cancer [2C25]	[13]
Osimertinib	DMRJLAT	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Osimertinib.	Lung cancer [2C25]	[13]
Calaspargase pegol	DMQZBXI	Moderate	Increased risk of hepatotoxicity by the combination of Tecfidera and Calaspargase pegol.	Malignant haematopoietic neoplasm [2B33]	[15]
Obinutuzumab	DM3BVAE	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Obinutuzumab.	Mature B-cell leukaemia [2A82]	[13]
Idelalisib	DM602WT	Moderate	Increased risk of hepatotoxicity by the combination of Tecfidera and Idelalisib.	Mature B-cell leukaemia [2A82]	[16]
GDC-0199	DMH0QKA	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and GDC-0199.	Mature B-cell leukaemia [2A82]	[13]
IPI-145	DMWA24P	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and IPI-145.	Mature B-cell leukaemia [2A82]	[13]
Acalabrutinib	DM7GCVW	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Acalabrutinib.	Mature B-cell lymphoma [2A85]	[13]
Blinatumomab	DMGECIJ	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Blinatumomab.	Mature B-cell lymphoma [2A85]	[13]
Ibrutinib	DMHZCPO	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Ibrutinib.	Mature B-cell lymphoma [2A85]	[13]
Tisagenlecleucel	DMM9BJD	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Tisagenlecleucel.	Mature B-cell lymphoma [2A85]	[13]
Selinexor	DMBD4K3	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Selinexor.	Multiple myeloma [2A83]	[13]
Belantamab mafodotin	DMBT3AI	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Belantamab mafodotin.	Multiple myeloma [2A83]	[13]
Daratumumab	DMKCIUZ	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Daratumumab.	Multiple myeloma [2A83]	[13]
Deflazacort	DMV0RNS	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Deflazacort.	Muscular dystrophy [8C70]	[13]
Inebilizumab	DMI0RHA	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Inebilizumab.	Nervous system paraneoplastic/autoimmune disorder [8E4A]	[13]
Atezolizumab	DMMF8U0	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Atezolizumab.	Non-small cell lung cancer [2C25]	[13]
Olaparib	DM8QB1D	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Olaparib.	Ovarian cancer [2C73]	[13]
Rucaparib	DM9PVX8	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Rucaparib.	Ovarian cancer [2C73]	[13]
MK-4827	DMLYGH4	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and MK-4827.	Ovarian cancer [2C73]	[13]
Brodalumab	DMASDQ6	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Brodalumab.	Psoriasis [EA90]	[13]
Tildrakizumab	DMLW9HG	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Tildrakizumab.	Psoriasis [EA90]	[13]
Risankizumab	DMM32GT	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Risankizumab.	Psoriasis [EA90]	[13]
Ixekizumab	DMXW92T	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Ixekizumab.	Psoriasis [EA90]	[13]
Sarilumab	DMOGNXY	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Sarilumab.	Rheumatoid arthritis [FA20]	[13]
Anthrax vaccine	DM9GSWY	Moderate	Antagonize the effect of Tecfidera when combined with Anthrax vaccine.	Sepsis [1G40-1G41]	[17]
Mogamulizumab	DMISH0Z	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Mogamulizumab.	Sezary syndrome [2B02]	[13]
LEE011	DMMX75K	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and LEE011.	Solid tumour/cancer [2A00-2F9Z]	[13]
Pomalidomide	DMTGBAX	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Pomalidomide.	Systemic sclerosis [4A42]	[13]
Durvalumab	DM4PVDY	Moderate	Additive immunosuppressive effects by the combination of Tecfidera and Durvalumab.	Ureteral cancer [2C92]	[13]
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
FD&C blue no. 1	E00263	19700	Colorant
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Carmellose sodium	E00625	Not Available	Disintegrant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Ferrosoferric oxide	E00231	14789	Colorant
Magnesium stearate	E00208	11177	lubricant
Polysorbate 80	E00665	Not Available	Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Triethyl citrate	E00128	6506	Plasticizing agent; Solvent
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⏷ Show the Full List of 11 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Dimethyl fumarate 120 mg capsule	120 mg	Delayed Release Oral Capsule	Oral
Dimethyl fumarate 240 mg capsule	240 mg	Delayed Release Oral Capsule	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1	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: 7045).
2	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
3	Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
4	Dimethyl Fumarate Inhibits the Nuclear Factor B Pathway in Breast Cancer Cells by Covalent Modification of p65 Protein. J Biol Chem. 2016 Feb 12;291(7):3639-47. doi: 10.1074/jbc.M115.679704. Epub 2015 Dec 18.
5	Fumarate Mediates a Chronic Proliferative Signal in Fumarate Hydratase-Inactivated Cancer Cells by Increasing Transcription and Translation of Ferritin Genes. Mol Cell Biol. 2017 May 16;37(11):e00079-17. doi: 10.1128/MCB.00079-17. Print 2017 Jun 1.
6	Dimethyl Fumarate Therapy Significantly Improves the Responsiveness of T Cells in Multiple Sclerosis Patients for Immunoregulation by Regulatory T Cells. Int J Mol Sci. 2017 Jan 28;18(2):271. doi: 10.3390/ijms18020271.
7	Enhanced cytotoxicity of bioreductive antitumor agents with dimethyl fumarate in human glioblastoma cells. Anticancer Drugs. 2005 Feb;16(2):167-74.
8	Distinct Nrf2 Signaling Mechanisms of Fumaric Acid Esters and Their Role in Neuroprotection against 1-Methyl-4-Phenyl-1,2,3,6-Tetrahydropyridine-Induced Experimental Parkinson's-Like Disease. J Neurosci. 2016 Jun 8;36(23):6332-51. doi: 10.1523/JNEUROSCI.0426-16.2016.
9	Fumarate hydratase inactivation in hereditary leiomyomatosis and renal cell cancer is synthetic lethal with ferroptosis induction. Cancer Sci. 2018 Sep;109(9):2757-2766. doi: 10.1111/cas.13701. Epub 2018 Jul 20.
10	Cerner Multum, Inc. "Australian Product Information.".
11	Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA.
12	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
13	Product Information. Vumerity (diroximel fumarate). Alkermes, Inc, Cambridge, MA.
14	Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
15	Al-Nawakil C, Willems L, Mauprivez C, et.al "Successful treatment of l-asparaginase-induced severe acute hepatotoxicity using mitochondrial cofactors." Leuk Lymphoma 55 (2014): 1670-4. [PMID: 24090500]
16	Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
17	CDC. Centers for Disease Control and Prevention/ "Recommendations of the advisory committtee on immunization practices (ACIP): use of vaccines and immune globulins in persons with altered immunocompetence." MMWR Morb Mortal Wkly Rep 42(RR-04) (1993): 1-18. [PMID: 20300058]