Peringatan Keamanan

Signs of dose-limiting toxicity were not observed with intravenous administration of single doses up to 6 mg/kg in clinical trials. Information on overdose of ustekinumab is limited: in the event of overdose, patients should be monitored for any signs and symptoms of drug-related adverse events and appropriate symptomatic treatment should be initiated.L9386

Ustekinumab

DB05679

biotech approved investigational

Deskripsi

Ustekinumab is a human immunoglobulin (Ig) G1 kappa monoclonal antibody directed against interleukin(IL)-12 and IL-23, which are cytokines that are involved in immune and inflammatory responses.A187349 It was generated via recombinant human IL-12 immunization of human Ig (hu-Ig) transgenic mice.A187349 It is a targeted biologic disease-modifying anti-rheumatic drug (bDMARDs) that is used in the management of various inflammatory conditions that involve the activation of IL-12 and IL-23 signalling pathways.A187346

The therapeutic use of the drug started in Canada, the US, and Europe since 2009 when it was first approved for the treatment of adult patients with moderate to severe plaque psoriasis and active psoriatic arthritis, alone or in combination with methotrexate. In September 2016, ustekinumab was additionally approved for the management of moderate to severe Crohn's disease in selected adult patients. In October 2019, it was also approved by the FDA for use to manage moderately to severely active ulcerative colitis in adults. Ustekinumab is currently the first and only approved biologic therapy for ulcerative colitis that targets the interleukin (IL)-12 and IL-23 cytokines.L9392 The dosing regimen for ustekinumab is based on the patient's weight and there are intravenous and subcutaneous formulations of the drug based on the dosing schedule and condition being treated. Ustekinumab is commonly marketed under the trade name STELARA.

Ustekinumab biosimilars are available in some markets, including Wezlana (ustekinumab-auub) in the USL49071 and Jamteki (AVT04) in Canada.L49076

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following administration of a single subcutaneous dose of 45 mg or 90 mg in patients with psoriasis, the median half-life was 19.8 days and 21.2, respectively.[L9491] The estimated median terminal half-life of approximately 19 days in patients with Crohn’s disease or ulcerative colitis.[L9386]
Volume Distribusi The total volume of distribution at steady-state was 4.62 L in patients with Crohn’s disease and 4.4 L in patients with ulcerative colitis.[L9386] The median apparent volume of distribution during the terminal phase (Vz/F) ranged from 76 to 161 mL/kg in patients with psoriasis receiving a single subcutaneous dose.[L9491]
Klirens (Clearance) The median apparent clearance (CL/F) following a single subcutaneous administration to patients with psoriasis ranged from 2.7 to 5.3 mL/day/kg.[L9491] In patients with Crohn’s disease, the clearance was 0.19 L/day in patients with Crohn’s disease or ulcerative colitis.[L9386]

Absorpsi

The median Tmax following a single subcutaneous dose administration of 45mg and 90mg in adults with psoriasis was 13.5 days and 7 days, respectively. The median Cmax in the same group of patients was 2.4 ?g/mL and 5.3 ?g/mL at doses of 45mg and 90mg, respectively. The median AUC was 84.9 ?g·day/mL and 226.9 ?g·day/mL, respectively.L9491 Following an intravenous induction dose administration, the mean ± SD Cmax was 125.2 ± 33.6 mcg/mL in patients with Crohn’s disease and 129.1 ± 27.6 mcg/mL in patients with ulcerative colitis.L9386 The systemic exposure of ustekinumab (Cmax and AUC) increases in a linear or dose-proportional manner following a single subcutaneous administration at doses ranging from approximately 24 mg to 240 mg in patients with psoriasis. The estimated absolute bioavailability (F) of ustekinumab following a single subcutaneous dose administration in patients with psoriasis is 57.2%.L9491

Metabolisme

The metabolic pathway of ustekinumab has not been fully characterized; it is expected to undergo nonspecific protein degradation via catabolic pathways in the same manner as endogenous IgG.L9386

Rute Eliminasi

There is limited information on the main route of elimination of ustekinumab; it is expected to undergo renal excretion following degradation.

Interaksi Obat

374 Data
Diethylstilbestrol Diethylstilbestrol may increase the thrombogenic activities of Ustekinumab.
Chlorotrianisene Chlorotrianisene may increase the thrombogenic activities of Ustekinumab.
Conjugated estrogens Conjugated estrogens may increase the thrombogenic activities of Ustekinumab.
Estrone Estrone may increase the thrombogenic activities of Ustekinumab.
Estradiol Estradiol may increase the thrombogenic activities of Ustekinumab.
Dienestrol Dienestrol may increase the thrombogenic activities of Ustekinumab.
Ethinylestradiol Ethinylestradiol may increase the thrombogenic activities of Ustekinumab.
Mestranol Mestranol may increase the thrombogenic activities of Ustekinumab.
Estriol Estriol may increase the thrombogenic activities of Ustekinumab.
Estrone sulfate Estrone sulfate may increase the thrombogenic activities of Ustekinumab.
Quinestrol Quinestrol may increase the thrombogenic activities of Ustekinumab.
Hexestrol Hexestrol may increase the thrombogenic activities of Ustekinumab.
Tibolone Tibolone may increase the thrombogenic activities of Ustekinumab.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may increase the thrombogenic activities of Ustekinumab.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may increase the thrombogenic activities of Ustekinumab.
Polyestradiol phosphate Polyestradiol phosphate may increase the thrombogenic activities of Ustekinumab.
Esterified estrogens Esterified estrogens may increase the thrombogenic activities of Ustekinumab.
Zeranol Zeranol may increase the thrombogenic activities of Ustekinumab.
Equol Equol may increase the thrombogenic activities of Ustekinumab.
Promestriene Promestriene may increase the thrombogenic activities of Ustekinumab.
Methallenestril Methallenestril may increase the thrombogenic activities of Ustekinumab.
Epimestrol Epimestrol may increase the thrombogenic activities of Ustekinumab.
Moxestrol Moxestrol may increase the thrombogenic activities of Ustekinumab.
Estradiol acetate Estradiol acetate may increase the thrombogenic activities of Ustekinumab.
Estradiol benzoate Estradiol benzoate may increase the thrombogenic activities of Ustekinumab.
Estradiol cypionate Estradiol cypionate may increase the thrombogenic activities of Ustekinumab.
Estradiol valerate Estradiol valerate may increase the thrombogenic activities of Ustekinumab.
Biochanin A Biochanin A may increase the thrombogenic activities of Ustekinumab.
Formononetin Formononetin may increase the thrombogenic activities of Ustekinumab.
Estetrol Estetrol may increase the thrombogenic activities of Ustekinumab.
Cetuximab The risk or severity of adverse effects can be increased when Cetuximab is combined with Ustekinumab.
Human immunoglobulin G The risk or severity of adverse effects can be increased when Human immunoglobulin G is combined with Ustekinumab.
Omalizumab The risk or severity of adverse effects can be increased when Omalizumab is combined with Ustekinumab.
Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Ustekinumab.
Indium In-111 satumomab pendetide The risk or severity of adverse effects can be increased when Indium In-111 satumomab pendetide is combined with Ustekinumab.
Digoxin Immune Fab (Ovine) The risk or severity of adverse effects can be increased when Digoxin Immune Fab (Ovine) is combined with Ustekinumab.
Capromab pendetide The risk or severity of adverse effects can be increased when Capromab pendetide is combined with Ustekinumab.
Palivizumab The risk or severity of adverse effects can be increased when Palivizumab is combined with Ustekinumab.
Technetium Tc-99m arcitumomab The risk or severity of adverse effects can be increased when Technetium Tc-99m arcitumomab is combined with Ustekinumab.
Panitumumab The risk or severity of adverse effects can be increased when Panitumumab is combined with Ustekinumab.
Ranibizumab The risk or severity of adverse effects can be increased when Ranibizumab is combined with Ustekinumab.
Galiximab The risk or severity of adverse effects can be increased when Galiximab is combined with Ustekinumab.
Pexelizumab The risk or severity of adverse effects can be increased when Pexelizumab is combined with Ustekinumab.
Epratuzumab The risk or severity of adverse effects can be increased when Epratuzumab is combined with Ustekinumab.
Bectumomab The risk or severity of adverse effects can be increased when Bectumomab is combined with Ustekinumab.
Oregovomab The risk or severity of adverse effects can be increased when Oregovomab is combined with Ustekinumab.
IGN311 The risk or severity of adverse effects can be increased when IGN311 is combined with Ustekinumab.
Adecatumumab The risk or severity of adverse effects can be increased when Adecatumumab is combined with Ustekinumab.
Labetuzumab The risk or severity of adverse effects can be increased when Labetuzumab is combined with Ustekinumab.
Matuzumab The risk or severity of adverse effects can be increased when Matuzumab is combined with Ustekinumab.
Fontolizumab The risk or severity of adverse effects can be increased when Fontolizumab is combined with Ustekinumab.
Bavituximab The risk or severity of adverse effects can be increased when Bavituximab is combined with Ustekinumab.
CR002 The risk or severity of adverse effects can be increased when CR002 is combined with Ustekinumab.
Rozrolimupab The risk or severity of adverse effects can be increased when Rozrolimupab is combined with Ustekinumab.
Girentuximab The risk or severity of adverse effects can be increased when Girentuximab is combined with Ustekinumab.
Obiltoxaximab The risk or severity of adverse effects can be increased when Obiltoxaximab is combined with Ustekinumab.
XTL-001 The risk or severity of adverse effects can be increased when XTL-001 is combined with Ustekinumab.
NAV 1800 The risk or severity of adverse effects can be increased when NAV 1800 is combined with Ustekinumab.
Otelixizumab The risk or severity of adverse effects can be increased when Otelixizumab is combined with Ustekinumab.
AMG 108 The risk or severity of adverse effects can be increased when AMG 108 is combined with Ustekinumab.
Iratumumab The risk or severity of adverse effects can be increased when Iratumumab is combined with Ustekinumab.
Enokizumab The risk or severity of adverse effects can be increased when Enokizumab is combined with Ustekinumab.
Ramucirumab The risk or severity of adverse effects can be increased when Ramucirumab is combined with Ustekinumab.
Farletuzumab The risk or severity of adverse effects can be increased when Farletuzumab is combined with Ustekinumab.
Veltuzumab The risk or severity of adverse effects can be increased when Veltuzumab is combined with Ustekinumab.
PRO-542 The risk or severity of adverse effects can be increased when Ustekinumab is combined with PRO-542.
TNX-901 The risk or severity of adverse effects can be increased when Ustekinumab is combined with TNX-901.
Inotuzumab ozogamicin The risk or severity of adverse effects can be increased when Ustekinumab is combined with Inotuzumab ozogamicin.
RI 624 The risk or severity of adverse effects can be increased when Ustekinumab is combined with RI 624.
Stamulumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with MYO-029.
CT-011 The risk or severity of adverse effects can be increased when Ustekinumab is combined with CT-011.
Leronlimab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Leronlimab.
Glembatumumab vedotin The risk or severity of adverse effects can be increased when Ustekinumab is combined with Glembatumumab vedotin.
Olaratumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Olaratumab.
IPH 2101 The risk or severity of adverse effects can be increased when Ustekinumab is combined with IPH 2101.
TB-402 The risk or severity of adverse effects can be increased when Ustekinumab is combined with TB-402.
Caplacizumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Caplacizumab.
IMC-1C11 The risk or severity of adverse effects can be increased when Ustekinumab is combined with IMC-1C11.
Eldelumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Eldelumab.
Lumiliximab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Lumiliximab.
Ipilimumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Ipilimumab.
Nimotuzumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Nimotuzumab.
Clenoliximab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Clenoliximab.
BIIB015 The risk or severity of adverse effects can be increased when Ustekinumab is combined with BIIB015.
Sonepcizumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Sonepcizumab.
Motavizumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Motavizumab.
Elotuzumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Elotuzumab.
AVE9633 The risk or severity of adverse effects can be increased when Ustekinumab is combined with AVE9633.
Carotuximab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Carotuximab.
XmAb 2513 The risk or severity of adverse effects can be increased when Ustekinumab is combined with XmAb 2513.
Coltuximab ravtansine The risk or severity of adverse effects can be increased when Ustekinumab is combined with Coltuximab ravtansine.
Lucatumumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Lucatumumab.
Pertuzumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Pertuzumab.
Siplizumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Siplizumab.
Apolizumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Apolizumab.
Sibrotuzumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Sibrotuzumab.
Bivatuzumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Bivatuzumab.
Lerdelimumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Lerdelimumab.
Lexatumumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Lexatumumab.
Reslizumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Reslizumab.

Target Protein

Interleukin-23 IL12B
Interleukin-12 subunit beta IL12B

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29949399
    Thibodaux RJ, Triche MW, Espinoza LR: Ustekinumab for the treatment of psoriasis and psoriatic arthritis: a drug evaluation and literature review. Expert Opin Biol Ther. 2018 Jul;18(7):821-827. doi: 10.1080/14712598.2018.1492545. Epub 2018 Jul 9.
  • PMID: 22123062
    Benson JM, Peritt D, Scallon BJ, Heavner GA, Shealy DJ, Giles-Komar JM, Mascelli MA: Discovery and mechanism of ustekinumab: a human monoclonal antibody targeting interleukin-12 and interleukin-23 for treatment of immune-mediated disorders. MAbs. 2011 Nov-Dec;3(6):535-45. doi: 10.4161/mabs.3.6.17815. Epub 2011 Nov 1.
  • PMID: 20421912
    Koutruba N, Emer J, Lebwohl M: Review of ustekinumab, an interleukin-12 and interleukin-23 inhibitor used for the treatment of plaque psoriasis. Ther Clin Risk Manag. 2010 Apr 15;6:123-41. doi: 10.2147/tcrm.s5599.
  • PMID: 20691190
    Luo J, Wu SJ, Lacy ER, Orlovsky Y, Baker A, Teplyakov A, Obmolova G, Heavner GA, Richter HT, Benson J: Structural basis for the dual recognition of IL-12 and IL-23 by ustekinumab. J Mol Biol. 2010 Oct 8;402(5):797-812. doi: 10.1016/j.jmb.2010.07.046. Epub 2010 Aug 4.
  • PMID: 12411982
    Frye RF, Schneider VM, Frye CS, Feldman AM: Plasma levels of TNF-alpha and IL-6 are inversely related to cytochrome P450-dependent drug metabolism in patients with congestive heart failure. J Card Fail. 2002 Oct;8(5):315-9.
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