Peringatan Keamanan

The intravenous LD50 is > 300 mg/kg in mice and > 200 mg/kg in rats.L31408 There is limited information on the overdose from cetuximab.

In clinical trials, cetuximab was associated with serious and fatal infusion reactions, cardiopulmonary arrest or sudden death, and serious dermatologic toxicities. Pulmonary toxicities, such as interstitial lung disease, interstitial pneumonitis with non-cardiogenic pulmonary edema, and exacerbation of pre-existing fibrotic lung disease have been reported.L30448

Cetuximab

DB00002

biotech approved

Deskripsi

Cetuximab is a recombinant chimeric human/mouse IgG1 monoclonal antibody that competitively binds to epidermal growth factor receptor (EGFR) and competitively inhibits the binding of epidermal growth factor (EGF).A227973 EGFR is a member of the ErbB family of receptor tyrosine kinases found in both normal and tumour cells; it is responsible for regulating epithelial tissue development and homeostasis.A228083 EGFR has been implicated in various types of cancer, as it is often overexpressed in malignant cells A227973 and EGFR overexpression has been linked to more advanced disease and poor prognosis.A227963 EGFR is often mutated in certain types of cancer and serves as a driver of tumorigenesis.A228083 In vitro, cetuximab was shown to mediate anti-tumour effects in numerous cancer cell lines and human tumour xenografts.A227963

Approved by the FDA in February 2004 under the brand name ERBITUX, cetuximab is used for the treatment of head and neck cancer and metastatic, KRAS wild-type colorectal cancer, and metastatic colorectal cancer with a BRAF V600E mutation.A227963,L39045 It has also been investigated in advanced colorectal cancer, EGFR-expressing non-small cell lung cancer (NSCLC), and unresectable squamous cell skin cancer.L31418 Cetuximab is administered via intravenous infusion and is used as monotherapy or in combination with other chemotherapies, including platinum agents, radiation therapy, leucovorin, fluorouracil, and irinotecan.L30448

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) After administration of a 400 mg/m<sup>2</sup> initial dose followed by a 250 mg/m<sup>2</sup> weekly dose, the mean half-life for cetuximab was approximately 112 hours, with a range of 63 to 230 hours.[L30448]
Volume Distribusi The volume of the distribution is about 2-3 L/m<sup>2</sup> and is independent of dose.[L30448]
Klirens (Clearance) In patients with recurrent and/or metastatic squamous cell carcinoma of the head and neck, the estimated clearance rate was 0.103 L/h.[A228003] At doses ranging from 200 to 400 mg/m<sup>2</sup>, complete saturation of systemic clearance was observed. In a population pharmacokinetic study, female patients had a 25% lower intrinsic cetuximab clearance than male patients, although there was no evidence of the need for dose modification based on sex.[A227963]

Absorpsi

After administration of a 400 mg/m2 initial dose followed by a 250 mg/m2 weekly dose, the steady-state levels of cetuximab was reached by the third weekly infusion with mean peak and trough concentrations across studies ranging from 168 µg/mL to 235 µg/mL and 41 µg/mL to 85 µg/mL, respectively.L30448 Tmax is about 3 hours.A227963

Metabolisme

Like other monoclonal antibodies, cetuximab is expected to undergo lysosomal degradation by the reticuloendothelial system and protein catabolism by a target?mediated disposition pathway.A40006

Rute Eliminasi

There is limited information available.

Farmakogenomik

2 Varian
FCGR2A (rs1801274)

Patients with this genotype may have increased progression-free survival time when using cetuximab to treat colorectal cancer.

FCGR3A (rs396991)

Patients with this genotype have increased progression-free survival time when using cetuximab to treat colorectal cancer.

Interaksi Obat

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

Target Protein

Epidermal growth factor receptor EGFR
Low affinity immunoglobulin gamma Fc region receptor III-B FCGR3B
Complement C1q subcomponent subunit A C1QA
Complement C1q subcomponent subunit B C1QB
Complement C1q subcomponent subunit C C1QC
Low affinity immunoglobulin gamma Fc region receptor III-A FCGR3A
High affinity immunoglobulin gamma Fc receptor I FCGR1A
Low affinity immunoglobulin gamma Fc region receptor II-a FCGR2A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 11752352
    Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.
  • PMID: 16336752
    Snyder LC, Astsaturov I, Weiner LM: Overview of monoclonal antibodies and small molecules targeting the epidermal growth factor receptor pathway in colorectal cancer. Clin Colorectal Cancer. 2005 Nov;5 Suppl 2:S71-80.
  • PMID: 16117976
    Wong SF: Cetuximab: an epidermal growth factor receptor monoclonal antibody for the treatment of colorectal cancer. Clin Ther. 2005 Jun;27(6):684-94. doi: 10.1016/j.clinthera.2005.06.003.
  • PMID: 15821783
    Harding J, Burtness B: Cetuximab: an epidermal growth factor receptor chemeric human-murine monoclonal antibody. Drugs Today (Barc). 2005 Feb;41(2):107-27. doi: 10.1358/dot.2005.41.2.882662.
  • PMID: 16428506
    Kim S, Prichard CN, Younes MN, Yazici YD, Jasser SA, Bekele BN, Myers JN: Cetuximab and irinotecan interact synergistically to inhibit the growth of orthotopic anaplastic thyroid carcinoma xenografts in nude mice. Clin Cancer Res. 2006 Jan 15;12(2):600-7. doi: 10.1158/1078-0432.CCR-05-1325.
  • PMID: 28653357
    Ryman JT, Meibohm B: Pharmacokinetics of Monoclonal Antibodies. CPT Pharmacometrics Syst Pharmacol. 2017 Sep;6(9):576-588. doi: 10.1002/psp4.12224. Epub 2017 Jul 29.
  • PMID: 18218786
    Dirks NL, Nolting A, Kovar A, Meibohm B: Population pharmacokinetics of cetuximab in patients with squamous cell carcinoma of the head and neck. J Clin Pharmacol. 2008 Mar;48(3):267-78. doi: 10.1177/0091270007313393. Epub 2008 Jan 24.
  • PMID: 20088790
    Vincenzi B, Zoccoli A, Pantano F, Venditti O, Galluzzo S: Cetuximab: from bench to bedside. Curr Cancer Drug Targets. 2010 Feb;10(1):80-95. doi: 10.2174/156800910790980241.
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Contoh Produk & Brand

Produk: 5 • International brands: 0
Produk
  • Erbitux
    Solution • 2 mg/1mL • Intravenous • US • Approved
  • Erbitux
    Solution • 2 mg/1mL • Intravenous • US • Approved
  • Erbitux
    Solution • 2 mg / mL • Intravenous • Canada • Approved
  • Erbitux
    Injection, solution • 5 mg/ml • Intravenous • EU • Approved
  • Erbitux
    Injection, solution • 5 mg/ml • Intravenous • EU • Approved

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