Details of the Drug

General Information of Drug (ID: DM7J6OR)

Drug Name
Tocilizumab
Synonyms Actemra; Actemra (TN); Tocilizumab (USAN/INN); Tocilizumab (genetical recombination); Tocilizumab (genetical recombination) (JAN); humanized IgG1 monoclonal antibody
Indication
Disease Entry ICD 11 Status REF
Giant cell arteritis 4A44.2 Approved [1]
Rheumatoid arthritis FA20 Approved [2]
Coronavirus Disease 2019 (COVID-19) 1D6Y Phase 3 [3]
Juvenile idiopathic arthritis FA24 Phase 3 [2]
Castleman's disease 4B2Y Investigative [4]
Affected Organisms
Humans and other mammals
ATC Code
L04AC07: Tocilizumab
L04AC: Interleukin inhibitors
L04A: IMMUNOSUPPRESSANTS
L04: IMMUNOSUPPRESSANTS
L: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Drug Type
Monoclonal antibody
Sequence
>light chain
DIQMTQSPSSLSASVGDRVTITCRASQDISSYLNWYQQKPGKAPKLLIYYTSRLHSGVPS
RFSGSGSGTDFTFTISSLQPEDIATYYCQQGNTLPYTFGQGTKVEIKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
>heavy chain
QVQLQESGPGLVRPSQTLSLTCTVSGYSITSDHAWSWVRQPPGRGLEWIGYISYSGITTY
NPSLKSRVTMLRDTSKNQFSLRLSSVTAADTAVYYCARSLARTTAMDYWGQGSLVTVSSA
STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG
LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGP
SVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNS
TYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEM
TKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQ
QGNVFSCSVMHEALHNHYTQKSLSLSPG
Cross-matching ID
UNII
I031V2H011
DrugBank ID
DB06273
TTD ID
D08HPZ
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Interleukin 6 receptor (IL6R) TT0E5SK IL6RA_HUMAN ; IL6RB_HUMAN Modulator [5]
HUMAN interleukin-6 receptor (IL6R) TTDVAKP IL6RA_HUMAN ; IL6RB_HUMAN Inhibitor [6]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Giant cell arteritis
ICD Disease Classification 4A44.2
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Interleukin 6 receptor (IL6R) DTT IL6R; IL6ST 1.13E-04 1.32 1.28
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Tocilizumab
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Upadacitinib DM32B5U Major Additive immunosuppressive effects by the combination of Tocilizumab and Upadacitinib. Rheumatoid arthritis [FA20] [7]
Coadministration of a Drug Treating the Disease Different from Tocilizumab (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Tocilizumab and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [8]
Oliceridine DM6MDCF Moderate Altered metabolism of Tocilizumab due to Oliceridine alters the formation of CYP450 enzymes. Acute pain [MG31] [7]
Bedaquiline DM3906J Moderate Increased risk of hepatotoxicity by the combination of Tocilizumab and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [9]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Tocilizumab and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [10]
Levonorgestrel DM1DP7T Moderate Altered metabolism of Tocilizumab due to Levonorgestrel alters the formation of CYP450 enzymes. Contraceptive management [QA21] [7]
Oestradiol valerate and dienogest DMZK0FQ Moderate Altered metabolism of Tocilizumab due to Oestradiol valerate and dienogest alters the formation of CYP450 enzymes. Endometriosis [GA10] [11]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Tocilizumab and Cannabidiol. Epileptic encephalopathy [8A62] [7]
Brentuximab vedotin DMWLC57 Moderate Increased risk of hepatotoxicity by the combination of Tocilizumab and Brentuximab vedotin. Hodgkin lymphoma [2B30] [12]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Tocilizumab and BMS-201038. Hyper-lipoproteinaemia [5C80] [13]
Levamlodipine DM92S6N Moderate Altered metabolism of Tocilizumab due to Levamlodipine alters the formation of CYP450 enzymes. Hypertension [BA00-BA04] [7]
Denosumab DMNI0KO Moderate Additive immunosuppressive effects by the combination of Tocilizumab and Denosumab. Low bone mass disorder [FB83] [14]
Lurbinectedin DMEFRTZ Moderate Additive immunosuppressive effects by the combination of Tocilizumab and Lurbinectedin. Lung cancer [2C25] [7]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Tocilizumab and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [15]
Idelalisib DM602WT Moderate Increased risk of hepatotoxicity by the combination of Tocilizumab and Idelalisib. Mature B-cell leukaemia [2A82] [16]
GDC-0199 DMH0QKA Moderate Altered metabolism of Tocilizumab due to GDC-0199 alters the formation of CYP450 enzymes. Mature B-cell leukaemia [2A82] [7]
Tecfidera DM2OVDT Moderate Additive immunosuppressive effects by the combination of Tocilizumab and Tecfidera. Multiple sclerosis [8A40] [17]
Siponimod DM2R86O Major Additive immunosuppressive effects by the combination of Tocilizumab and Siponimod. Multiple sclerosis [8A40] [8]
Fingolimod DM5JVAN Major Additive immunosuppressive effects by the combination of Tocilizumab and Fingolimod. Multiple sclerosis [8A40] [18]
Ocrelizumab DMEZ2KH Moderate Additive immunosuppressive effects by the combination of Tocilizumab and Ocrelizumab. Multiple sclerosis [8A40] [19]
Ozanimod DMT6AM2 Major Additive immunosuppressive effects by the combination of Tocilizumab and Ozanimod. Multiple sclerosis [8A40] [7]
Temsirolimus DMS104F Moderate Additive myelosuppressive effects by the combination of Tocilizumab and Temsirolimus. Renal cell carcinoma [2C90] [7]
Anthrax vaccine DM9GSWY Moderate Antagonize the effect of Tocilizumab when combined with Anthrax vaccine. Sepsis [1G40-1G41] [20]
Apixaban DM89JLN Moderate Altered metabolism of Tocilizumab due to Apixaban alters the formation of CYP450 enzymes. Thrombosis [DB61-GB90] [7]
⏷ Show the Full List of 23 DDI Information 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: 6881).
3 ClinicalTrials.gov (NCT04320615) A Study to Evaluate the Safety and Efficacy of Tocilizumab in Patients With Severe COVID-19 Pneumonia. U.S. National Institutes of Health.
4 Interleukin-6: A Masterplayer in the Cytokine Network. Oncology. 2020;98(3):131-137.
5 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
6 Tocilizumab, an anti-IL6 receptor antibody, to treat Covid-19-related respiratory failure: a case report. Ann Oncol. 2020 Apr 2. pii: S0923-7534(20)36387-0.
7 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
8 Cerner Multum, Inc. "Australian Product Information.".
9 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
10 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
11 Product Information. Cosentyx (secukinumab). Novartis Pharmaceuticals, East Hanover, NJ.
12 Product Information. Accolate (zafirlukast). Zeneca Pharmaceuticals, Wilmington, DE.
13 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
14 Product Information. Prolia (denosumab). Amgen USA, Thousand Oaks, CA.
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 Product Information. Vumerity (diroximel fumarate). Alkermes, Inc, Cambridge, MA.
18 Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
19 Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA.
20 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]