Etrolizumab

DB12189

biotech investigational

Deskripsi

Inflammatory bowel disease (IBD), including ulcerative colitis and Crohn's disease, is typified by a chronic gastrointestinal inflammatory microenvironment, driven in part by the excessive infiltration and retention of intestinal-homing lymphocytes.A244564, A244569, A244579, A244584 A recent class of drugs designed to impair lymphocyte homing, so-called "anti-trafficking agents" (ATAs), have shown some success and include approved drugs such as natalizumab and vedolizumab, which target integrins and impair their interaction with adhesion molecules on epithelial cells.A244574 In the case of natalizumab, which targets the ?4 integrin subunit, this has also resulted in undesirable blockade of lymphocyte CNS trafficking and reported cases of progressive multifocal leukoencephalopathy (PML).A244564, A244584 Etrolizumab is a humanized IgG1? monoclonal antibody directed against the ?7 subunit of gastrointestinal ?4?7 and ?E?7 integrins that, due to its target specificity, appears as or more efficacious than vedolizumab and without the CNS effects of natalizumab.A244564, A244569, A244574, A244584

Etrolizumab is currently under investigation for the treatment of ulcerative colitis and Crohn's disease.

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) Etrolizumab administered as a single 105 mg subcutaneous injection by prefilled syringe or autoinjector device in healthy adults aged 18-55 resulted in a similar mean half-life of 11.8 ± 3.85 days for the injector and 12.2 ± 4.39 days for the syringe.[A244689] In adult ulcerative colitis patients, the half-life was similar at higher doses (10.6-13.1 days for 3-10 mg/kg) but shorter at smaller doses (4.8-7.4 days at 0.3-1.0 mg/kg).[A244694] The half-life in pediatric patients was similar at 7.3 ± 1.76 days at the 1.5 mg/kg q4w level and 8.7 ± 3.74 at the 3.0 mg/kg q8w level.[A244684]
Volume Distribusi Modelling of etrolizumab pharmacokinetic data from adult patients with moderate to severe ulcerative colitis yielded a central volume of distribution of either 2570 mL (from the quasi-steady-state target-mediated drug disposition model) or 3200 mL (from the linear model).[A244589] Subcutaneous administration of either 1.5 mg/kg q4w or 3.0 mg/kg q8w etrolizumab in pediatric patients with ulcerative colitis or Crohn's disease yielded an apparent volume of distribution of 4920 ± 2440 mL and 3910 ± 1830 mL, respectively.[A244684]
Klirens (Clearance) Etrolizumab has a mean clearance in adult patients of ~300 mL/day, which appears higher in pediatric patients (385-505 mL/day).[A244589, A244684, A244689]

Absorpsi

Etrolizumab administered as a single 105 mg subcutaneous injection by prefilled syringe or autoinjector device in healthy adults aged 18-55 resulted in a geometric mean (%CV) Cmax of 12.2-12.5 ?g/mL (28.3-32.0), AUClast of 319-325 ?g\*day/mL (33.1-35.3), and AUC0-? of 329-337 ?g\*day/mL (35.2-36.0). The median time to maximum serum concentration (Tmax) was 5.04 days (range 2.98-14.0) for the autoinjector and 6.97 days (range 3.00-14.0) for the syringe.A244689 Studies in adult patients with ulcerative colitis revealed approximately linear pharmacokinetics at doses >1.0 mg/kg and an accumulation ratio over three doses (four weeks apart) of 1.2-fold for intravenous dosing and 2.0-fold for subcutaneous dosing. The apparent bioavailability of subcutaneous etrolizumab was estimated at 67% at the 3 mg/kg level.A244694 Etrolizumab pharmacokinetics were also evaluated in pediatric patients aged 4-17 years with moderately to severely active ulcerative colitis or Crohn's disease given either 1.5 mg/kg etrolizumab every four weeks (q4w) for four doses or 3.0 mg/kg every eight weeks (q8w) for two doses by subcutaneous injection. The 1.5 mg/kg dose resulted in a mean Cmax of 7.7 ± 2.18 ?g/mL after the first dose and 9.8 ± 4.86 ?g/mL after the last dose and an AUC84-112d of 167 ± 86.9 ?g\*day/mL. The 3.0 mg/kg dose resulted in a mean Cmax of 19.0 ± 8.21 ?g/mL after the first dose and 18.1 ± 6.25 ?g/mL after the last dose and an AUC56-112d of 521 ± 306 ?g\*day/mL.A244684

Metabolisme

Etrolizumab, as a monoclonal antibody, is expected to undergo proteolytic degradation in multiple locations throughout the body.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

373 Data
Diethylstilbestrol Diethylstilbestrol may increase the thrombogenic activities of Etrolizumab.
Chlorotrianisene Chlorotrianisene may increase the thrombogenic activities of Etrolizumab.
Conjugated estrogens Conjugated estrogens may increase the thrombogenic activities of Etrolizumab.
Estrone Estrone may increase the thrombogenic activities of Etrolizumab.
Estradiol Estradiol may increase the thrombogenic activities of Etrolizumab.
Dienestrol Dienestrol may increase the thrombogenic activities of Etrolizumab.
Ethinylestradiol Ethinylestradiol may increase the thrombogenic activities of Etrolizumab.
Mestranol Mestranol may increase the thrombogenic activities of Etrolizumab.
Estriol Estriol may increase the thrombogenic activities of Etrolizumab.
Estrone sulfate Estrone sulfate may increase the thrombogenic activities of Etrolizumab.
Quinestrol Quinestrol may increase the thrombogenic activities of Etrolizumab.
Hexestrol Hexestrol may increase the thrombogenic activities of Etrolizumab.
Tibolone Tibolone may increase the thrombogenic activities of Etrolizumab.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may increase the thrombogenic activities of Etrolizumab.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may increase the thrombogenic activities of Etrolizumab.
Polyestradiol phosphate Polyestradiol phosphate may increase the thrombogenic activities of Etrolizumab.
Esterified estrogens Esterified estrogens may increase the thrombogenic activities of Etrolizumab.
Zeranol Zeranol may increase the thrombogenic activities of Etrolizumab.
Equol Equol may increase the thrombogenic activities of Etrolizumab.
Promestriene Promestriene may increase the thrombogenic activities of Etrolizumab.
Methallenestril Methallenestril may increase the thrombogenic activities of Etrolizumab.
Epimestrol Epimestrol may increase the thrombogenic activities of Etrolizumab.
Moxestrol Moxestrol may increase the thrombogenic activities of Etrolizumab.
Estradiol acetate Estradiol acetate may increase the thrombogenic activities of Etrolizumab.
Estradiol benzoate Estradiol benzoate may increase the thrombogenic activities of Etrolizumab.
Estradiol cypionate Estradiol cypionate may increase the thrombogenic activities of Etrolizumab.
Estradiol valerate Estradiol valerate may increase the thrombogenic activities of Etrolizumab.
Biochanin A Biochanin A may increase the thrombogenic activities of Etrolizumab.
Formononetin Formononetin may increase the thrombogenic activities of Etrolizumab.
Estetrol Estetrol may increase the thrombogenic activities of Etrolizumab.
Cetuximab The risk or severity of adverse effects can be increased when Cetuximab is combined with Etrolizumab.
Human immunoglobulin G The risk or severity of adverse effects can be increased when Human immunoglobulin G is combined with Etrolizumab.
Omalizumab The risk or severity of adverse effects can be increased when Omalizumab is combined with Etrolizumab.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Etrolizumab.
Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Etrolizumab.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Etrolizumab.
Indium In-111 satumomab pendetide The risk or severity of adverse effects can be increased when Indium In-111 satumomab pendetide is combined with Etrolizumab.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Etrolizumab.
Trastuzumab The risk or severity of adverse effects can be increased when Trastuzumab is combined with Etrolizumab.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Etrolizumab.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Etrolizumab.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Etrolizumab.
Digoxin Immune Fab (Ovine) The risk or severity of adverse effects can be increased when Digoxin Immune Fab (Ovine) is combined with Etrolizumab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Etrolizumab.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Etrolizumab.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Etrolizumab.
Capromab pendetide The risk or severity of adverse effects can be increased when Capromab pendetide is combined with Etrolizumab.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Etrolizumab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Etrolizumab.
Natalizumab The risk or severity of adverse effects can be increased when Natalizumab is combined with Etrolizumab.
Palivizumab The risk or severity of adverse effects can be increased when Palivizumab is combined with Etrolizumab.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Etrolizumab.
Bevacizumab The risk or severity of adverse effects can be increased when Bevacizumab is combined with Etrolizumab.
Technetium Tc-99m arcitumomab The risk or severity of adverse effects can be increased when Technetium Tc-99m arcitumomab is combined with Etrolizumab.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Etrolizumab.
Panitumumab The risk or severity of adverse effects can be increased when Panitumumab is combined with Etrolizumab.
Ranibizumab The risk or severity of adverse effects can be increased when Ranibizumab is combined with Etrolizumab.
Galiximab The risk or severity of adverse effects can be increased when Galiximab is combined with Etrolizumab.
Pexelizumab The risk or severity of adverse effects can be increased when Pexelizumab is combined with Etrolizumab.
Afelimomab The risk or severity of adverse effects can be increased when Afelimomab is combined with Etrolizumab.
Epratuzumab The risk or severity of adverse effects can be increased when Epratuzumab is combined with Etrolizumab.
Bectumomab The risk or severity of adverse effects can be increased when Bectumomab is combined with Etrolizumab.
Oregovomab The risk or severity of adverse effects can be increased when Oregovomab is combined with Etrolizumab.
IGN311 The risk or severity of adverse effects can be increased when IGN311 is combined with Etrolizumab.
Adecatumumab The risk or severity of adverse effects can be increased when Adecatumumab is combined with Etrolizumab.
Labetuzumab The risk or severity of adverse effects can be increased when Labetuzumab is combined with Etrolizumab.
Matuzumab The risk or severity of adverse effects can be increased when Matuzumab is combined with Etrolizumab.
Fontolizumab The risk or severity of adverse effects can be increased when Fontolizumab is combined with Etrolizumab.
Bavituximab The risk or severity of adverse effects can be increased when Bavituximab is combined with Etrolizumab.
CR002 The risk or severity of adverse effects can be increased when CR002 is combined with Etrolizumab.
Rozrolimupab The risk or severity of adverse effects can be increased when Rozrolimupab is combined with Etrolizumab.
Girentuximab The risk or severity of adverse effects can be increased when Girentuximab is combined with Etrolizumab.
Obiltoxaximab The risk or severity of adverse effects can be increased when Obiltoxaximab is combined with Etrolizumab.
XTL-001 The risk or severity of adverse effects can be increased when XTL-001 is combined with Etrolizumab.
NAV 1800 The risk or severity of adverse effects can be increased when NAV 1800 is combined with Etrolizumab.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Etrolizumab.
Otelixizumab The risk or severity of adverse effects can be increased when Otelixizumab is combined with Etrolizumab.
AMG 108 The risk or severity of adverse effects can be increased when AMG 108 is combined with Etrolizumab.
Iratumumab The risk or severity of adverse effects can be increased when Iratumumab is combined with Etrolizumab.
Enokizumab The risk or severity of adverse effects can be increased when Enokizumab is combined with Etrolizumab.
Ramucirumab The risk or severity of adverse effects can be increased when Ramucirumab is combined with Etrolizumab.
Farletuzumab The risk or severity of adverse effects can be increased when Farletuzumab is combined with Etrolizumab.
Veltuzumab The risk or severity of adverse effects can be increased when Veltuzumab is combined with Etrolizumab.
Ustekinumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Etrolizumab.
Trastuzumab emtansine The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Etrolizumab.
PRO-542 The risk or severity of adverse effects can be increased when PRO-542 is combined with Etrolizumab.
TNX-901 The risk or severity of adverse effects can be increased when TNX-901 is combined with Etrolizumab.
Inotuzumab ozogamicin The risk or severity of adverse effects can be increased when Inotuzumab ozogamicin is combined with Etrolizumab.
RI 624 The risk or severity of adverse effects can be increased when RI 624 is combined with Etrolizumab.
Stamulumab The risk or severity of adverse effects can be increased when MYO-029 is combined with Etrolizumab.
CT-011 The risk or severity of adverse effects can be increased when CT-011 is combined with Etrolizumab.
Leronlimab The risk or severity of adverse effects can be increased when Leronlimab is combined with Etrolizumab.
Glembatumumab vedotin The risk or severity of adverse effects can be increased when Glembatumumab vedotin is combined with Etrolizumab.
Olaratumab The risk or severity of adverse effects can be increased when Olaratumab is combined with Etrolizumab.
IPH 2101 The risk or severity of adverse effects can be increased when IPH 2101 is combined with Etrolizumab.
TB-402 The risk or severity of adverse effects can be increased when TB-402 is combined with Etrolizumab.
Caplacizumab The risk or severity of adverse effects can be increased when Caplacizumab is combined with Etrolizumab.
IMC-1C11 The risk or severity of adverse effects can be increased when IMC-1C11 is combined with Etrolizumab.
Eldelumab The risk or severity of adverse effects can be increased when Eldelumab is combined with Etrolizumab.
Lumiliximab The risk or severity of adverse effects can be increased when Lumiliximab is combined with Etrolizumab.

Target Protein

Integrin beta-7 ITGB7

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29601644
    Tang MT, Keir ME, Erickson R, Stefanich EG, Fuh FK, Ramirez-Montagut T, McBride JM, Danilenko DM: Review article: nonclinical and clinical pharmacology, pharmacokinetics and pharmacodynamics of etrolizumab, an anti-beta7 integrin therapy for inflammatory bowel disease. Aliment Pharmacol Ther. 2018 Jun;47(11):1440-1452. doi: 10.1111/apt.14631. Epub 2018 Mar 30.
  • PMID: 30774593
    Lichnog C, Klabunde S, Becker E, Fuh F, Tripal P, Atreya R, Klenske E, Erickson R, Chiu H, Reed C, Chung S, Neufert C, Atreya I, McBride J, Neurath MF, Zundler S: Cellular Mechanisms of Etrolizumab Treatment in Inflammatory Bowel Disease. Front Pharmacol. 2019 Feb 1;10:39. doi: 10.3389/fphar.2019.00039. eCollection 2019.
  • PMID: 31567498
    Zundler S, Wiendl M, Neurath MF: Anti-trafficking agents in the treatment of inflammatory bowel disease. Curr Opin Gastroenterol. 2019 Nov;35(6):499-506. doi: 10.1097/MOG.0000000000000579.
  • PMID: 31327399
    Biswas S, Bryant RV, Travis S: Interfering with leukocyte trafficking in Crohn's disease. Best Pract Res Clin Gastroenterol. 2019 Feb - Apr;38-39:101617. doi: 10.1016/j.bpg.2019.05.004. Epub 2019 May 28.
  • PMID: 21232034
    Stefanich EG, Danilenko DM, Wang H, O'Byrne S, Erickson R, Gelzleichter T, Hiraragi H, Chiu H, Ivelja S, Jeet S, Gadkari S, Hwang O, Fuh F, Looney C, Howell K, Albert V, Balazs M, Refino C, Fong S, Iyer S, Williams M: A humanized monoclonal antibody targeting the beta7 integrin selectively blocks intestinal homing of T lymphocytes. Br J Pharmacol. 2011 Apr;162(8):1855-70. doi: 10.1111/j.1476-5381.2011.01205.x.
  • PMID: 29178491
    Wei X, Gibiansky L, Wang Y, Fuh F, Erickson R, O'Byrne S, Tang MT: Pharmacokinetic and Pharmacodynamic Modeling of Serum Etrolizumab and Circulating beta7 Receptor Occupancy in Patients With Ulcerative Colitis. J Clin Pharmacol. 2018 Mar;58(3):386-398. doi: 10.1002/jcph.1031. Epub 2017 Nov 26.
  • PMID: 34849918
    Zhang W, Scalori A, Fuh F, McBride J, She G, Kierkus J, Korczowksi B, Li R, Abouhossein M, Kadva A, Park KT, Tang MT: Pharmacokinetics, Pharmacodynamics, and Safety of Etrolizumab in Children With Moderately to Severely Active Ulcerative Colitis or Crohn's Disease: Results from a Phase 1 Randomized Trial. Inflamm Bowel Dis. 2021 Nov 29. pii: 6446094. doi: 10.1093/ibd/izab275.
  • PMID: 33778929
    Zhang W, Tyrrell H, Ding HT, Pulley J, Boruvka A, Erickson R, Abouhossein M, Ravanello R, Tang MT: Comparable Pharmacokinetics, Safety, and Tolerability of Etrolizumab Administered by Prefilled Syringe or Autoinjector in a Randomized Trial in Healthy Volunteers. Adv Ther. 2021 May;38(5):2418-2434. doi: 10.1007/s12325-021-01661-6. Epub 2021 Mar 29.
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