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)

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

DrugBank ID: DB05679
TTD ID: D0A2UV

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)

MIA Detail

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)

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 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]