Details of the Drug

General Information of Drug (ID: DMQ2FKJ)

Drug Name

Teriflunomide

Indication

Disease Entry	ICD 11	Status	REF
Hyperlipidaemia	5C80	Approved	[1]
Multiple sclerosis	8A40	Approved	[2], [3]
Rheumatoid arthritis	FA20	Phase 3	[2], [4]
Hepatitis B virus infection	1E51.0	Phase 1	[1]

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

270.21

Topological Polar Surface Area (xlogp)

3.3

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 4: low solubility and low permeability [5]
Clearance: The total body clearance of drug is 30.5 mL/h [6]
Half-life: The concentration or amount of drug in body reduced by one-half in 18 - 19 days [7]
Metabolism: The drug is not metabolised [8]
Unbound Fraction: The unbound fraction of drug in plasma is 0.01% [7]
Vd: The volume of distribution (Vd) of drug is 11 L [6]

Chemical Identifiers

Formula: C12H9F3N2O2
IUPAC Name: (Z)-2-cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]but-2-enamide
Canonical SMILES: C/C(=C(\\C#N)/C(=O)NC1=CC=C(C=C1)C(F)(F)F)/O
InChI: InChI=1S/C12H9F3N2O2/c1-7(18)10(6-16)11(19)17-9-4-2-8(3-5-9)12(13,14)15/h2-5,18H,1H3,(H,17,19)/b10-7-
InChIKey: UTNUDOFZCWSZMS-YFHOEESVSA-N

Cross-matching ID

PubChem CID: 54684141
ChEBI ID: CHEBI:68540
CAS Number: 163451-81-8
DrugBank ID: DB08880
TTD ID: D07QFP
VARIDT ID: DR00092
ACDINA ID: D00665

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Dihydroorotate dehydrogenase (DHODH)	TTLVP78	PYRD_HUMAN	Modulator	[3]
HMG-CoA reductase (HMGCR)	TTPADOQ	HMDH_HUMAN	Inhibitor	[1]
Plasmodium Dihydroorotate dehydrogenase (Malaria DHOdehase)	TT3PQ2Y	PYRD_PLAF7	Inhibitor	[9], [10]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Breast cancer resistance protein (ABCG2)	DTI7UX6	ABCG2_HUMAN	Substrate	[11]

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Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease

Hyperlipidaemia

ICD Disease Classification

5C80

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
HMG-CoA reductase (HMGCR)	DTT	HMGCR	1.01E-05	0.65	1.53
Breast cancer resistance protein (ABCG2)	DTP	BCRP	2.28E-08	-3.66E-01	-8.07E-01

Molecular Expression Atlas (MEA)

MEA Detail

Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Teriflunomide (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Remdesivir	DMBFZ6L	Moderate	Increased risk of hepatotoxicity by the combination of Teriflunomide and Remdesivir.	1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019]	[41]
Tagraxofusp	DM9HQ5U	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Tagraxofusp.	Acute myeloid leukaemia [2A60]	[42]
Arn-509	DMT81LZ	Moderate	Accelerated clearance of Teriflunomide due to the transporter induction by Arn-509.	Acute myeloid leukaemia [2A60]	[43]
Gilteritinib	DMWQ4MZ	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Gilteritinib.	Acute myeloid leukaemia [2A60]	[42]
Siltuximab	DMGEATB	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Siltuximab.	Anemia [3A00-3A9Z]	[44]
Bedaquiline	DM3906J	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Bedaquiline.	Antimicrobial drug resistance [MG50-MG52]	[42]
Dupilumab	DMOAD2Y	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Dupilumab.	Atopic eczema [EA80]	[44]
Troleandomycin	DMUZNIG	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Troleandomycin.	Bacterial infection [1A00-1C4Z]	[42]
Ag-221	DMS0ZBI	Moderate	Decreased clearance of Teriflunomide due to the transporter inhibition by Ag-221.	BCR-ABL1-negative chronic myeloid leukaemia [2A41]	[41]
Pexidartinib	DMS2J0Z	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Pexidartinib.	Bone/articular cartilage neoplasm [2F7B]	[45]
Talazoparib	DM1KS78	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Talazoparib.	Breast cancer [2C60-2C6Y]	[44]
LY2835219	DM93VBZ	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and LY2835219.	Breast cancer [2C60-2C6Y]	[44]
Fenofibric acid	DMGO2MC	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Fenofibric acid.	Cardiovascular disease [BA00-BE2Z]	[42]
Macitentan	DMP79A1	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Macitentan.	Cardiovascular disease [BA00-BE2Z]	[42]
PF-04449913	DMSB068	Moderate	Decreased clearance of Teriflunomide due to the transporter inhibition by PF-04449913.	Chronic myelomonocytic leukaemia [2A40]	[43]
Regorafenib	DMHSY1I	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Regorafenib.	Colorectal cancer [2B91]	[42]
Intedanib	DMSTA36	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Intedanib.	Colorectal cancer [2B91]	[42]
Aflibercept	DMT3D5I	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Aflibercept.	Colorectal cancer [2B91]	[44]
Polatuzumab vedotin	DMF6Y0L	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Polatuzumab vedotin.	Diffuse large B-cell lymphoma [2A81]	[44]
Lisocabtagene maraleucel	DMP45ME	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Lisocabtagene maraleucel.	Diffuse large B-cell lymphoma [2A81]	[44]
Axicabtagene ciloleucel	DMYHN59	Major	Additive myelosuppressive effects by the combination of Teriflunomide and Axicabtagene ciloleucel.	Diffuse large B-cell lymphoma [2A81]	[44]
Stiripentol	DMMSDOY	Moderate	Increased metabolism of Teriflunomide caused by Stiripentol mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[43]
Cannabidiol	DM0659E	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Cannabidiol.	Epileptic encephalopathy [8A62]	[42]
Bay 80-6946	DMLOS5R	Major	Additive myelosuppressive effects by the combination of Teriflunomide and Bay 80-6946.	Follicular lymphoma [2A80]	[44]
Avapritinib	DMK2GZX	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Avapritinib.	Gastrointestinal stromal tumour [2B5B]	[44]
GS-5885	DMSL3DX	Moderate	Decreased clearance of Teriflunomide due to the transporter inhibition by GS-5885.	Hepatitis virus infection [1E50-1E51]	[46]
177Lu-DOTATATE	DMT8GVU	Major	Additive myelosuppressive effects by the combination of Teriflunomide and 177Lu-DOTATATE.	Hepatitis virus infection [1E50-1E51]	[44]
GS-9857	DMYU6P5	Moderate	Decreased clearance of Teriflunomide due to the transporter inhibition by GS-9857.	Hepatitis virus infection [1E50-1E51]	[47]
Fostemsavir	DM50ILT	Moderate	Decreased clearance of Teriflunomide due to the transporter inhibition by Fostemsavir.	Human immunodeficiency virus disease [1C60-1C62]	[48]
Givosiran	DM5PFIJ	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Givosiran.	Inborn porphyrin/heme metabolism error [5C58]	[42]
Berotralstat	DMWA2DZ	Major	Decreased clearance of Teriflunomide due to the transporter inhibition by Berotralstat.	Innate/adaptive immunodeficiency [4A00]	[49]
Tasimelteon	DMLOQ1V	Moderate	Increased metabolism of Teriflunomide caused by Tasimelteon mediated induction of CYP450 enzyme.	Insomnia [7A00-7A0Z]	[50]
Brigatinib	DM7W94S	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Brigatinib.	Lung cancer [2C25]	[44]
Ceritinib	DMB920Z	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Ceritinib.	Lung cancer [2C25]	[42]
Lurbinectedin	DMEFRTZ	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Lurbinectedin.	Lung cancer [2C25]	[44]
Alectinib	DMP1I6Y	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Alectinib.	Lung cancer [2C25]	[42]
Osimertinib	DMRJLAT	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Osimertinib.	Lung cancer [2C25]	[44]
BIBW 2992	DMTKD7Q	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and BIBW 2992.	Lung cancer [2C25]	[42]
Pralsetinib	DMWU0I2	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Pralsetinib.	Lung cancer [2C25]	[42]
Capmatinib	DMYCXKL	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Capmatinib.	Lung cancer [2C25]	[42]
Selpercatinib	DMZR15V	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Selpercatinib.	Lung cancer [2C25]	[42]
Calaspargase pegol	DMQZBXI	Major	Additive myelosuppressive effects by the combination of Teriflunomide and Calaspargase pegol.	Malignant haematopoietic neoplasm [2B33]	[44]
Obinutuzumab	DM3BVAE	Major	Additive myelosuppressive effects by the combination of Teriflunomide and Obinutuzumab.	Mature B-cell leukaemia [2A82]	[44]
Idelalisib	DM602WT	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Idelalisib.	Mature B-cell leukaemia [2A82]	[44]
GDC-0199	DMH0QKA	Major	Additive myelosuppressive effects by the combination of Teriflunomide and GDC-0199.	Mature B-cell leukaemia [2A82]	[44]
IPI-145	DMWA24P	Major	Additive myelosuppressive effects by the combination of Teriflunomide and IPI-145.	Mature B-cell leukaemia [2A82]	[44]
Acalabrutinib	DM7GCVW	Major	Additive myelosuppressive effects by the combination of Teriflunomide and Acalabrutinib.	Mature B-cell lymphoma [2A85]	[44]
Blinatumomab	DMGECIJ	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Blinatumomab.	Mature B-cell lymphoma [2A85]	[44]
Ibrutinib	DMHZCPO	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Ibrutinib.	Mature B-cell lymphoma [2A85]	[44]
Tisagenlecleucel	DMM9BJD	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Tisagenlecleucel.	Mature B-cell lymphoma [2A85]	[44]
Ponatinib	DMYGJQO	Major	Additive myelosuppressive effects by the combination of Teriflunomide and Ponatinib.	Mature B-cell lymphoma [2A85]	[44]
Arry-162	DM1P6FR	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Arry-162.	Melanoma [2C30]	[42]
Vemurafenib	DM62UG5	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Vemurafenib.	Melanoma [2C30]	[42]
Ubrogepant	DM749I3	Moderate	Decreased clearance of Teriflunomide due to the transporter inhibition by Ubrogepant.	Migraine [8A80]	[51]
Rimegepant	DMHOAUG	Moderate	Decreased clearance of Teriflunomide due to the transporter inhibition by Rimegepant.	Migraine [8A80]	[52]
Lasmiditan	DMXLVDT	Moderate	Decreased clearance of Teriflunomide due to the transporter inhibition by Lasmiditan.	Migraine [8A80]	[53]
Carfilzomib	DM48K0X	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Carfilzomib.	Multiple myeloma [2A83]	[44]
Selinexor	DMBD4K3	Major	Additive myelosuppressive effects by the combination of Teriflunomide and Selinexor.	Multiple myeloma [2A83]	[44]
Belantamab mafodotin	DMBT3AI	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Belantamab mafodotin.	Multiple myeloma [2A83]	[44]
Daratumumab	DMKCIUZ	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Daratumumab.	Multiple myeloma [2A83]	[44]
Tecfidera	DM2OVDT	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Tecfidera.	Multiple sclerosis [8A40]	[44]
Siponimod	DM2R86O	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Siponimod.	Multiple sclerosis [8A40]	[41]
Ocrelizumab	DMEZ2KH	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Ocrelizumab.	Multiple sclerosis [8A40]	[44]
Deflazacort	DMV0RNS	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Deflazacort.	Muscular dystrophy [8C70]	[44]
Fedratinib	DM4ZBK6	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Fedratinib.	Myeloproliferative neoplasm [2A20]	[42]
Rolapitant	DM8XP26	Moderate	Decreased clearance of Teriflunomide due to the transporter inhibition by Rolapitant.	Nausea/vomiting [MD90]	[54]
Inebilizumab	DMI0RHA	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Inebilizumab.	Nervous system paraneoplastic/autoimmune disorder [8E4A]	[44]
Atezolizumab	DMMF8U0	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Atezolizumab.	Non-small cell lung cancer [2C25]	[44]
Entrectinib	DMMPTLH	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Entrectinib.	Non-small cell lung cancer [2C25]	[44]
Olaparib	DM8QB1D	Major	Additive myelosuppressive effects by the combination of Teriflunomide and Olaparib.	Ovarian cancer [2C73]	[44]
Rucaparib	DM9PVX8	Major	Additive myelosuppressive effects by the combination of Teriflunomide and Rucaparib.	Ovarian cancer [2C73]	[44]
MK-4827	DMLYGH4	Major	Additive myelosuppressive effects by the combination of Teriflunomide and MK-4827.	Ovarian cancer [2C73]	[44]
Choline salicylate	DM8P137	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Choline salicylate.	Postoperative inflammation [1A00-CA43]	[55]
Enzalutamide	DMGL19D	Moderate	Decreased metabolism of Teriflunomide caused by Enzalutamide mediated inhibition of CYP450 enzyme.	Prostate cancer [2C82]	[56]
Darolutamide	DMV7YFT	Moderate	Decreased clearance of Teriflunomide due to the transporter inhibition by Darolutamide.	Prostate cancer [2C82]	[57]
Brodalumab	DMASDQ6	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Brodalumab.	Psoriasis [EA90]	[44]
Tildrakizumab	DMLW9HG	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Tildrakizumab.	Psoriasis [EA90]	[44]
Risankizumab	DMM32GT	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Risankizumab.	Psoriasis [EA90]	[44]
Ixekizumab	DMXW92T	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Ixekizumab.	Psoriasis [EA90]	[44]
Selexipag	DMAHSU0	Moderate	Decreased metabolism of Teriflunomide caused by Selexipag mediated inhibition of CYP450 enzyme.	Pulmonary hypertension [BB01]	[41]
Upadacitinib	DM32B5U	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Upadacitinib.	Rheumatoid arthritis [FA20]	[44]
Baricitinib	DM4ONW5	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Baricitinib.	Rheumatoid arthritis [FA20]	[44]
Tofacitinib	DMBS370	Major	Additive myelosuppressive effects by the combination of Teriflunomide and Tofacitinib.	Rheumatoid arthritis [FA20]	[44]
Anthrax vaccine	DM9GSWY	Moderate	Antagonize the effect of Teriflunomide when combined with Anthrax vaccine.	Sepsis [1G40-1G41]	[58]
Mogamulizumab	DMISH0Z	Major	Additive myelosuppressive effects by the combination of Teriflunomide and Mogamulizumab.	Sezary syndrome [2B02]	[44]
Larotrectinib	DM26CQR	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Larotrectinib.	Solid tumour/cancer [2A00-2F9Z]	[42]
LEE011	DMMX75K	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and LEE011.	Solid tumour/cancer [2A00-2F9Z]	[44]
Pomalidomide	DMTGBAX	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Pomalidomide.	Systemic sclerosis [4A42]	[44]
Fostamatinib	DM6AUHV	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Fostamatinib.	Thrombocytopenia [3B64]	[42]
Lusutrombopag	DMH6IKO	Moderate	Decreased clearance of Teriflunomide due to the transporter inhibition by Lusutrombopag.	Thrombocytopenia [3B64]	[59]
Durvalumab	DM4PVDY	Major	Additive immunosuppressive effects by the combination of Teriflunomide and Durvalumab.	Ureteral cancer [2C92]	[44]
Elagolix	DMB2C0E	Major	Increased risk of hepatotoxicity by the combination of Teriflunomide and Elagolix.	Uterine fibroid [2E86]	[42]
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⏷ Show the Full List of 92 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
FD&C blue no. 2	E00446	2723854	Colorant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
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⏷ Show the Full List of 6 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Teriflunomide 7 mg tablet	7 mg	Oral Tablet	Oral
Teriflunomide 14 mg tablet	14 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

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47	Product Information. Vosevi (sofosbuvir/velpatasvir/voxilaprevir). Gilead Sciences, Foster City, CA.
48	Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC.
49	Ace LN, Jaffe JM, Kunka RL "Effect of food and an antacid on quinidine bioavailability." Biopharm Drug Dispos 4 (1983): 183-90. [PMID: 6882885]
50	Product Information. Hetlioz (tasimelteon). Vanda Pharmaceuticals Inc, Rockville, MD.
51	Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
52	Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT.
53	Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
54	Product Information. Varubi (rolapitant). Tesaro Inc., Waltham, MA.
55	EMEA "EMEA public statement on leflunomide (ARAVA) - severe and serious hepatic reactions.".
56	Product Information. Xtandi (enzalutamide). Astellas Pharma US, Inc, Deerfield, IL.
57	Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
58	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]
59	EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".