Details of the Drug

General Information of Drug (ID: DMHTYK3)

Drug Name
Ustekinumab
Synonyms
6,6-Dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,6-dihydro-1,3,5-triazine-2,4-diamine; WR99210; WR-99210; 6,6-DIMETHYL-1-[3-(2,4,5-TRICHLOROPHENOXY)PROPOXY]-1,6-DIHYDRO-1,3,5-TRIAZINE-2,4-DIAMINE; 47326-86-3; BRN 0629517; WR 99210; 1,3,5-Triazine-2,4-diamine, 1,6-dihydro-6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-; WR-99,210; CHEMBL129788; BRL 6231; 1,6-Dihydro-6,6-dimethyl-1-(3-(2,4,5-trichlorophenoxy)-propoxy)-1,3,5-triazine-2 ,4-diamine; 1-(2',4',5'-Trichlorophenoxypropoxy)-1,2-dihydro-2,2-dimethyl-4,6-diamino-s-triazine; Stelara (TN)
Indication
Disease Entry ICD 11 Status REF
Plaque psoriasis EA90.0 Approved [1]
Psoriasis EA90 Approved [2]
Psoriatic arthritis FA21 Approved [3]
Psoriasis vulgaris EA90 Phase 3 [1]
Inflammatory bowel disease DD72 Phase 2/3 [1]
Malaria 1F40-1F45 Investigative [4]
⏷ Show the Full List of Indication(s)
Affected Organisms
Humans and other mammals
ATC Code
L04AC05: Ustekinumab
L04AC: Interleukin inhibitors
L04A: IMMUNOSUPPRESSANTS
L04: IMMUNOSUPPRESSANTS
L: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Drug Type
Antibody
Sequence
>heavy chain
EVQLVQSGAEVKKPGESLKISCKGSGYSFTTYWLGWVRQMPGKGLDWIGIMSPVDSDIRY
SPSFQGQVTMSVDKSITTAYLQWNSLKASDTAMYYCARRRPGQGYFDFWGQGTLVTVSSS
STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG
LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTH
>light chain
DIQMTQSPSSLSASVGDRVTITCRASQGISSWLAWYQQKPEKAPKSLIYAASSLQSGVPS
RFSGSGSGTDFTLTISSLQPEDFATYYCQQYNIYPYTFGQGTKLEIKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
ADMET Property
Bioavailability
The bioavailability of drug is 57.2% [5]
Clearance
The clearance of drug is 2.7-5.3 mL/day/kg [5]
Half-life
The concentration or amount of drug in body reduced by one-half in 19.8 days (adminutesistration of a single subcutaneous dose of 45 mg), and 21.2 days (adminutesistration of a single subcutaneous dose of 90 mg) [5]
Metabolism
The drug is metabolized via the catabolic pathways in the same manner as endogenous IgG [6]
Vd
The volume of distribution (Vd) of drug is 4.62 L [7]
Cross-matching ID
UNII
FU77B4U5Z0
DrugBank ID
DB05679
TTD ID
D0A2UV
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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-12 alpha (IL12A) TTRTK6Y IL12A_HUMAN Not Available [8]
Interleukin-23 (IL23) TTC1GLB IL23A_HUMAN Not Available [8]
Polypeptide deformylase (PDF) TT9SL3Q DEFM_HUMAN Inhibitor [4]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Plaque psoriasis
ICD Disease Classification EA90.0
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Interleukin-12 alpha (IL12A) DTT IL12A 2.41E-04 -0.12 -0.49
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 Disease Different from Ustekinumab (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Oliceridine DM6MDCF Moderate Altered metabolism of Ustekinumab due to Oliceridine alters the formation of CYP450 enzymes. Acute pain [MG31] [9]
Levonorgestrel DM1DP7T Moderate Altered metabolism of Ustekinumab due to Levonorgestrel alters the formation of CYP450 enzymes. Contraceptive management [QA21] [9]
Rivaroxaban DMQMBZ1 Moderate Altered metabolism of Ustekinumab due to Rivaroxaban alters the formation of CYP450 enzymes. Deep vein thrombosis [BD71] [9]
Oestradiol valerate and dienogest DMZK0FQ Moderate Altered metabolism of Ustekinumab due to Oestradiol valerate and dienogest alters the formation of CYP450 enzymes. Endometriosis [GA10] [10]
Teriflunomide DMQ2FKJ Major Additive immunosuppressive effects by the combination of Ustekinumab and Teriflunomide. Hyper-lipoproteinaemia [5C80] [11]
Levamlodipine DM92S6N Moderate Altered metabolism of Ustekinumab due to Levamlodipine alters the formation of CYP450 enzymes. Hypertension [BA00-BA04] [9]
Denosumab DMNI0KO Moderate Additive immunosuppressive effects by the combination of Ustekinumab and Denosumab. Low bone mass disorder [FB83] [12]
Lurbinectedin DMEFRTZ Moderate Additive myelosuppressive effects by the combination of Ustekinumab and Lurbinectedin. Lung cancer [2C25] [9]
Siponimod DM2R86O Major Additive immunosuppressive effects by the combination of Ustekinumab and Siponimod. Multiple sclerosis [8A40] [13]
Fingolimod DM5JVAN Major Additive immunosuppressive effects by the combination of Ustekinumab and Fingolimod. Multiple sclerosis [8A40] [14]
Ocrelizumab DMEZ2KH Moderate Additive immunosuppressive effects by the combination of Ustekinumab and Ocrelizumab. Multiple sclerosis [8A40] [15]
Ozanimod DMT6AM2 Major Additive immunosuppressive effects by the combination of Ustekinumab and Ozanimod. Multiple sclerosis [8A40] [9]
Temsirolimus DMS104F Moderate Additive immunosuppressive effects by the combination of Ustekinumab and Temsirolimus. Renal cell carcinoma [2C90] [9]
Canakinumab DM8HLO5 Moderate Additive immunosuppressive effects by the combination of Ustekinumab and Canakinumab. Rheumatoid arthritis [FA20] [16]
Rilonacept DMGLUQS Moderate Additive immunosuppressive effects by the combination of Ustekinumab and Rilonacept. Rheumatoid arthritis [FA20] [16]
Golimumab DMHZV7X Major Additive immunosuppressive effects by the combination of Ustekinumab and Golimumab. Rheumatoid arthritis [FA20] [17]
Anthrax vaccine DM9GSWY Moderate Antagonize the effect of Ustekinumab when combined with Anthrax vaccine. Sepsis [1G40-1G41] [18]
Apixaban DM89JLN Moderate Altered metabolism of Ustekinumab due to Apixaban alters the formation of CYP450 enzymes. Thrombosis [DB61-GB90] [9]
⏷ Show the Full List of 18 DDI Information 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: 6885).
2 Efficacy and safety of ustekinumab, a human interleukin-12/23 monoclonal antibody, in patients with psoriasis: 76-week results from a randomised, double-blind, placebo-controlled trial (PHOENIX 1). Lancet. 2008 May 17;371(9625):1665-74.
3 Pathophysiology, Clinical Presentation, and Treatment of Psoriasis: A Review. JAMA. 2020 May 19;323(19):1945-1960.
4 Novel Saccharomyces cerevisiae screen identifies WR99210 analogues that inhibit Mycobacterium tuberculosis dihydrofolate reductase. Antimicrob Agents Chemother. 2002 Nov;46(11):3362-9.
5 STELARA? (ustekinumab) Product Monograph - Janssen Inc.
6 STELARA? (ustekinumab) injection - FDA Label
7 STELARA? (ustekinumab) injection -Janssen Full Prescribing Information
8 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
9 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
10 Product Information. Cosentyx (secukinumab). Novartis Pharmaceuticals, East Hanover, NJ.
11 Product Information. Arava (leflunomide). Hoechst Marion-Roussel Inc, Kansas City, MO.
12 Product Information. Prolia (denosumab). Amgen USA, Thousand Oaks, CA.
13 Cerner Multum, Inc. "Australian Product Information.".
14 Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
15 Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA.
16 Product Information. Arcalyst (rilonacept). Regeneron Pharmaceuticals Inc, Tarrytown, NY.
17 Product Information. Cimzia (certolizumab). UCB Pharma Inc, Smyrna, GA.
18 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]