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Cetuximab | CAS No: 205923-56-4 | GMP-certified suppliers
A medication that treats advanced squamous cell carcinoma of the head and neck and metastatic colorectal cancer by targeting EGFR-expressing tumors in combination with chemotherapy or radiation.
Therapeutic categories
Primary indications
- Cetuximab indicated for the treatment of locally or regionally advanced squamous cell carcinoma of the head and neck in combination with radiation therapy
- It is indicated for treating a recurrent locoregional disease or metastatic squamous cell carcinoma of the head and neck in combination with platinum-based therapy with fluorouracil
- It is indicated for recurrent or metastatic squamous cell carcinoma of the head and neck progressing after platinum-based therapy
Product Snapshot
- Cetuximab is an intravenous injectable monoclonal antibody formulation
- It is primarily used for the treatment of squamous cell carcinoma of the head and neck and metastatic colorectal cancer with specific genetic markers
- Cetuximab is approved for use in key regulatory markets including the US, Canada, and the EU
Clinical Overview
The clinical indications for cetuximab include treatment of locally or regionally advanced squamous cell carcinoma of the head and neck in combination with radiation therapy, recurrent or metastatic squamous cell carcinoma of the head and neck combined with platinum-based chemotherapy and fluorouracil, and cases progressing after platinum therapy. Cetuximab is also indicated for K-Ras wild-type, EGFR-expressing metastatic colorectal cancer, either in combination with FOLFIRI chemotherapy (leucovorin, fluorouracil, and irinotecan) or as monotherapy in patients refractory or intolerant to irinotecan. Additionally, it is approved for metastatic colorectal cancer with the BRAF V600E mutation in combination with encorafenib following prior therapy. Cetuximab is not recommended for tumors harboring mutated Ras or when Ras status is unknown.
Pharmacodynamically, cetuximab competitively inhibits binding of natural ligands such as epidermal growth factor (EGF) and transforming growth factor-alpha (TGF-α) to EGFR with higher affinity, preventing receptor dimerization, autophosphorylation, and activation of downstream signaling pathways including MAPK, PI3K/Akt, and Jak/Stat. This leads to reduced cell proliferation, survival, angiogenesis, and tumor invasiveness. Cetuximab also induces antibody-dependent cellular cytotoxicity and receptor internalization, resulting in EGFR downregulation. Its antitumor activity is limited to EGFR-expressing cells and is ineffective in the presence of downstream K-Ras mutations that constitutively activate the pathway independent of EGFR.
Cetuximab is administered intravenously and can be used as monotherapy or in combination with chemotherapy agents and radiation. Key ADME data indicate typical monoclonal antibody pharmacokinetics with distribution confined primarily to the vascular and interstitial spaces, and elimination via proteolytic catabolism rather than renal or hepatic clearance.
Safety considerations include infusion reactions, dermatologic toxicities, and hypomagnesemia; close monitoring is required. It carries a narrow therapeutic index and immunogenicity potential due to its chimeric structure. Cetuximab is marketed under the brand name ERBITUX.
For API sourcing, consistent quality and purity standards are essential to meet regulatory expectations for monoclonal antibody therapeutics. Suppliers must demonstrate compliance with Good Manufacturing Practice (GMP), including control of critical quality attributes such as glycosylation patterns and product-related impurities to ensure batch-to-batch consistency and clinical safety.
Identification & chemistry
| Generic name | Cetuximab |
|---|---|
| Molecule type | Biotech |
| CAS | 205923-56-4 |
| UNII | PQX0D8J21J |
| DrugBank ID | DB00002 |
Pharmacology
| Summary | Cetuximab is a monoclonal antibody that targets the epidermal growth factor receptor (EGFR), inhibiting ligand binding and receptor activation to disrupt downstream signaling pathways involved in cell proliferation, survival, migration, and angiogenesis. By preventing EGFR activation and promoting receptor internalization, cetuximab reduces tumor cell growth and induces apoptosis in EGFR-expressing cancers. Its efficacy is limited to tumors with wild-type K-Ras, as activating mutations in K-Ras can constitutively activate downstream signaling independently of EGFR inhibition. |
|---|---|
| Mechanism of action | The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein and a type I receptor tyrosine kinase expressed on both normal and malignant cells. It has been investigated as a therapeutic target for anticancer treatment, as it is often upregulated in cancer types, including head and neck, colon, and rectal cancers. When activated by its ligand, EGFR undergoes a conformational change and dimerization to form homodimers or heterodimers with another member of the ErbB family of receptors. Dimerization of EGFR activates the intracellular tyrosine kinase region of EGFR and promotes autophosphorylation, initiating a series of downstream signalling cascades, including cell differentiation, proliferation, migration, angiogenesis, and apoptosis. This EGFR signalling pathway is often dysregulated in cancer cells, leading to aberrant cell growth and enhanced cell survival. Cetuximab is a monoclonal antibody that binds specifically to the EGFR on both normal and tumour cells to competitively inhibit the binding of epidermal growth factor (EGF) and other ligands that are produced by normal and tumour tissue epithelial cells.[A11, L30448] Upon binding to domain III of EGFR - which is the binding site for its growth factor ligands - cetuximab prevents the receptor from adopting an extended conformation and thereby inhibits EGFR activation, as well as phosphorylation and activation of receptor-associated kinases (MAPK, PI3K/Akt, Jak/Stat).[A11, A228078] Inhibition of the EGFR signalling pathway ultimately leads to inhibition of cell cycle progression, cell survival pathways, and tumour cell motility and invasion. Cetuximab also induces cell apoptosis and decreases matrix metalloproteinase and vascular endothelial growth factor (VEGF) production.[A228078, L30448] _In vitro_, cetuximab was shown to inhibit tumour angiogenesis. Binding of cetuximab to EGFR also results in internalization of the antibody-receptor complex, leading to an overall downregulation of EGFR expression. K-ras is a small G-protein downstream of EGFR that plays an important role in promoting the EGFR signalling cascade: in some malignant cells, K-ras can acquire activating mutations in exon 2 and thus be continuously active regardless of EGFR regulation. Since mutant Ras proteins can isolate the pathway from the effect of EGFR, K-Ras mutations can render EGFR inhibitors like cetuximab ineffective in exerting anti-tumour effects.[L30448, L31418] Cetuximab is thus only limited in its use for K-Ras wild-type, EGFR-expressing cancers. |
| Pharmacodynamics | Cetuximab is an anticancer agent that works by inhibiting the growth and survival of epidermal growth factor receptor (EGFR)-expressing tumour cells with high specificity and higher affinity than epidermal growth factor (EGF) and transforming growth factor-alpha (TGF-α), which are natural ligands of EGFR. Cetuximab works by inhibiting the growth and survival of EGFR-positive tumours. _In vitro_, it promotes antibody-dependent cellular cytotoxicity (ADCC) against certain human tumour types. On the contrary, cetuximab does not exert its anti-tumour effects on human tumour xenografts lacking EGFR expression.[A227963, L30448] Cetuximab potentiates the cytotoxic effects of chemotherapeutics and radiation therapy when used in combination. In human tumour xenograft models in mice, cetuximab and irinotecan synergistically inhibited the growth of orthotopic anaplastic thyroid carcinoma xenografts _in vitro_ and _in vivo_. Cetuximab potentiated the _in vitro_ anti-proliferative and pro-apoptotic effect of irinotecan and achieved 93% _in vivo_ inhibition of tumour growth when combined with irinotecan, compared to 77% and 79% inhibition when cetuximab and irinotecan were used alone, respectively. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Epidermal growth factor receptor | Humans | binder |
| Low affinity immunoglobulin gamma Fc region receptor III-B | Humans | binder |
| Complement C1q subcomponent subunit A | Humans | binder |
ADME / PK
| Absorption | After administration of a 400 mg/m<sup>2</sup> initial dose followed by a 250 mg/m<sup>2</sup> 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. T<sub>max</sub> is about 3 hours. |
|---|---|
| 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. |
| Protein binding | There is no information available. |
| Metabolism | Like other monoclonal antibodies, cetuximab is expected to undergo lysosomal degradation by the reticuloendothelial system and protein catabolism by a target‐mediated disposition pathway. |
| Route of elimination | There is limited information available. |
| Volume of distribution | The volume of the distribution is about 2-3 L/m<sup>2</sup> and is independent of dose. |
| 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. 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. |
Formulation & handling
- Cetuximab is a biotech product formulated as an intravenous injection, suitable only for parenteral administration.
- Being a monoclonal antibody, it requires careful handling to maintain protein stability and prevent degradation.
- Storage and preparation should adhere to cold chain requirements to preserve biologic activity prior to use.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient's primary patent in Canada expired in March 2016, indicating established market availability. The API is currently marketed in the US, Canada, and the EU, reflecting a mature product lifecycle in these regions. |
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| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Cetuximab is produced by multiple originator companies with packaging support from several contract manufacturers. Its branded product, Erbitux, is marketed across the US, Canada, and EU regions. The patent expiry date in Canada (March 2016) indicates the potential for existing generic competition in some markets. |
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Safety
| Toxicity | The intravenous LD<sub>50</sub> is > 300 mg/kg in mice and > 200 mg/kg in rats. 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. |
|---|
- Cetuximab has an intravenous LD50 of ›300 mg/kg in mice and ›200 mg/kg in rats, indicating moderate acute toxicity
- Serious and fatal infusion-related reactions, including cardiopulmonary arrest and sudden death, have been reported
- Pulmonary adverse effects include interstitial lung disease, pneumonitis with pulmonary edema, and exacerbation of pre-existing fibrotic lung conditions
Cetuximab is a type of Monoclonal antibodies
Monoclonal antibodies are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in the field of biopharmaceuticals. These antibodies are produced by cloning a single type of immune cell to create identical copies, allowing for targeted treatment of various diseases.
Monoclonal antibodies have gained significant attention in recent years due to their potential in treating a wide range of conditions, including cancer, autoimmune disorders, and infectious diseases. Their specificity and ability to bind to specific antigens make them highly effective therapeutic agents.
These pharmaceutical APIs are typically developed using hybridoma technology or recombinant DNA technology. Hybridoma technology involves fusing antibody-producing cells with immortalized cells to create hybrid cells that produce large quantities of monoclonal antibodies. Recombinant DNA technology, on the other hand, utilizes genetically engineered organisms such as bacteria or mammalian cells to produce monoclonal antibodies.
The production of monoclonal antibodies requires stringent quality control measures to ensure purity, potency, and safety. Extensive characterization and validation tests are conducted to assess their binding specificity, stability, and absence of contaminants.
Monoclonal antibodies have revolutionized the pharmaceutical industry, offering personalized treatment options and improving patient outcomes. They provide targeted therapy with fewer side effects compared to traditional treatments. The development and use of monoclonal antibodies continue to expand, with ongoing research aiming to enhance their effectiveness and broaden their applications.
In summary, monoclonal antibodies represent a significant advancement in the field of biopharmaceuticals, offering targeted therapy for a variety of diseases. Their precise mechanism of action and potential for personalized treatment make them a promising class of pharmaceutical APIs.
Cetuximab (Monoclonal antibodies), classified under Immunomodulators
Immunomodulators, a category of pharmaceutical active pharmaceutical ingredients (APIs), are substances that help regulate and modify the immune response of an individual. These compounds play a crucial role in treating various immune-related disorders and diseases. Immunomodulators work by either enhancing or suppressing the immune system, depending on the specific condition being treated.
Immunomodulators are used in the treatment of autoimmune disorders, such as rheumatoid arthritis, multiple sclerosis, and psoriasis. By suppressing the immune system, these APIs help reduce the overactive immune response associated with these conditions, thereby alleviating symptoms and preventing further damage to the body's tissues.
On the other hand, immunomodulators are also employed to boost the immune system in cases of immunodeficiency disorders. These APIs stimulate the immune response, enabling the body to better fight off infections and diseases. Additionally, immunomodulators are utilized in the prevention and treatment of organ transplant rejection, where they help modulate the immune system to accept the transplanted organ.
The development and production of immunomodulators require rigorous testing and quality control to ensure their safety and efficacy. Pharmaceutical companies carefully formulate these APIs into various dosage forms, including tablets, capsules, injections, and topical preparations, to cater to different patient needs.
In summary, immunomodulators form a vital category of pharmaceutical APIs that regulate and modify the immune system. With their ability to modulate immune responses, these compounds contribute significantly to the management and treatment of various immune-related disorders and diseases, improving the quality of life for many patients.
Cetuximab API manufacturers & distributors
Compare qualified Cetuximab API suppliers worldwide. We currently have 2 companies offering Cetuximab API, with manufacturing taking place in 2 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, MSDS, USDMF | 229 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
When sending a request, specify which Cetuximab API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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