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Th1207 details

Primary information
ID 1816
ThPP ID Th1207
Therapeutic Peptide/Protein Name Necitumumab
Sequence NA view full sequnce in fasta
Functional Classification IIIc
Molecular Weight 144800
Chemical Formula NA
Isoelectric Point NA
Hydrophobicity NA
Melting Point (℃) NA
Half Life Approx 14 days
Description Necitumumab is an intravenously administered recombinant monoclonal IgG1 antibody used in the treatment of non-small cell lung cancer (NSCLC) as an EGFR antagonist. It functions by binding to epidermal growth factor receptor (EGFR) and prevents binding of its ligands, a process that is involved in cell proliferation, metastasis, angiogenesis, and malignant progression. Binding of necitumumab to EGFR induces receptor internalization and degradation, thereby preventing further activation of EGFR which is beneficial in NSCLC as many patients have increased protein expression of EGFR. Necitumumab is approved for use in combination with cisplatin and gemcitabine as a first-line treatment for metastatic squamous non-small cell lung cancer (NSCLC).
Indication/Disease Necitumumab is approved for use in combination with cisplatin and gemcitabine as a first-line treatment for metastatic squamous non-small cell lung cancer (NSCLC). It is not indicated for treatment of non-squamous NSCLC.
Pharmacodynamics In animal models administration of necitumumab to implanted mice resulted in increased antitumor activity in combination with gemcitabine and cisplatin as compared to mice receiving gemcitabine and cisplatin alone.
Mechanism of Action Necitumumab is a recombinant human lgG1 monoclonal antibody that binds to the human epidermal growth factor receptor (EGFR) and blocks the binding of EGFR to its ligands. Expression and activation of EGFR has been correlated with malignant progression, induction of angiogenesis, and inhibition of apoptosis. Binding of necitumumab induces EGFR internalization and degradation in vitro. In vitro, binding of necitumumab also led to antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells.
Toxicity 6 cycles showed the absence of disease progression or unacceptable toxicity.
Metabolism NA
Absorption NA
Volume of Distribution Steady state volume of distribution (Vss) is 7.0 L
Clearance Mean total systemic clearance (CLtot) at steady state is 14.1 mL/h
Categories NA
Patents Number NA
Date of Issue NA
Date of Expiry NA
Drug Interaction NA
Target NA
Information of corresponding available drug in the market
Brand Name Portrazza
Company Eli Lilly and Company
Brand Discription Necitumumab is an anti-EGFR recombinant human monoclonal antibody of the IgG1 kappa isotype that specifically binds to the ligand binding site of the human EGFR.
Prescribed for PORTRAZZAâ„¢ is indicated, in combination with gemcitabine and cisplatin, for first-line treatment of patients with metastatic squamous non-small cell lung cancer.
Chemical Name NA
Formulation Each vial contains 800 mg PORTRAZZA in 50 mL (16 mg/mL)
Physcial Appearance Sterile, preservative free, clear to slightly opalescent and colorless to slightly yellow solution
Route of Administration intravenous
Recommended Dosage The recommended dose of PORTRAZZA is 800 mg administered as an intravenous infusion over 60 minutes on Days 1 and 8 of each 3-week cycle prior to gemcitabine and cisplatin infusion. Continue PORTRAZZA until disease progression or unacceptable toxicity.
Contraindication NA
Side Effects Cardiopulmonary Arrest; Hypomagnesemia; Venous and Arterial Thromboembolic Events; Dermatologic Toxicities; nfusion-Related Reactions; Non-Squamous NSCLC - Increased Toxicity and Increased Mortality .
Useful Link http://www.rxlist.com/portrazza-drug/side-effects-interactions.htm
PubMed ID 28293124, 28277882, 28111429, 27913776, 27912834, 27628194, 27575423, 27729681, 27696220
3-D Structure N.A.

OSDDlinux

Raghava's Group

IMTECH

CSIR

CRDD
CPPSITE 2.0

Primary information
ID	1816
ThPP ID	Th1207
Therapeutic Peptide/Protein Name	Necitumumab
Sequence	NA view full sequnce in fasta
Functional Classification	IIIc
Molecular Weight	144800
Chemical Formula	NA
Isoelectric Point	NA
Hydrophobicity	NA
Melting Point (℃)	NA
Half Life	Approx 14 days
Description	Necitumumab is an intravenously administered recombinant monoclonal IgG1 antibody used in the treatment of non-small cell lung cancer (NSCLC) as an EGFR antagonist. It functions by binding to epidermal growth factor receptor (EGFR) and prevents binding of its ligands, a process that is involved in cell proliferation, metastasis, angiogenesis, and malignant progression. Binding of necitumumab to EGFR induces receptor internalization and degradation, thereby preventing further activation of EGFR which is beneficial in NSCLC as many patients have increased protein expression of EGFR. Necitumumab is approved for use in combination with cisplatin and gemcitabine as a first-line treatment for metastatic squamous non-small cell lung cancer (NSCLC).
Indication/Disease	Necitumumab is approved for use in combination with cisplatin and gemcitabine as a first-line treatment for metastatic squamous non-small cell lung cancer (NSCLC). It is not indicated for treatment of non-squamous NSCLC.
Pharmacodynamics	In animal models administration of necitumumab to implanted mice resulted in increased antitumor activity in combination with gemcitabine and cisplatin as compared to mice receiving gemcitabine and cisplatin alone.
Mechanism of Action	Necitumumab is a recombinant human lgG1 monoclonal antibody that binds to the human epidermal growth factor receptor (EGFR) and blocks the binding of EGFR to its ligands. Expression and activation of EGFR has been correlated with malignant progression, induction of angiogenesis, and inhibition of apoptosis. Binding of necitumumab induces EGFR internalization and degradation in vitro. In vitro, binding of necitumumab also led to antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells.
Toxicity	6 cycles showed the absence of disease progression or unacceptable toxicity.
Metabolism	NA
Absorption	NA
Volume of Distribution	Steady state volume of distribution (Vss) is 7.0 L
Clearance	Mean total systemic clearance (CLtot) at steady state is 14.1 mL/h
Categories	NA
Patents Number	NA
Date of Issue	NA
Date of Expiry	NA
Drug Interaction	NA
Target	NA
Information of corresponding available drug in the market
Brand Name	Portrazza
Company	Eli Lilly and Company
Brand Discription	Necitumumab is an anti-EGFR recombinant human monoclonal antibody of the IgG1 kappa isotype that specifically binds to the ligand binding site of the human EGFR.
Prescribed for	PORTRAZZAâ„¢ is indicated, in combination with gemcitabine and cisplatin, for first-line treatment of patients with metastatic squamous non-small cell lung cancer.
Chemical Name	NA
Formulation	Each vial contains 800 mg PORTRAZZA in 50 mL (16 mg/mL)
Physcial Appearance	Sterile, preservative free, clear to slightly opalescent and colorless to slightly yellow solution
Route of Administration	intravenous
Recommended Dosage	The recommended dose of PORTRAZZA is 800 mg administered as an intravenous infusion over 60 minutes on Days 1 and 8 of each 3-week cycle prior to gemcitabine and cisplatin infusion. Continue PORTRAZZA until disease progression or unacceptable toxicity.
Contraindication	NA
Side Effects	Cardiopulmonary Arrest; Hypomagnesemia; Venous and Arterial Thromboembolic Events; Dermatologic Toxicities; nfusion-Related Reactions; Non-Squamous NSCLC - Increased Toxicity and Increased Mortality .
Useful Link	http://www.rxlist.com/portrazza-drug/side-effects-interactions.htm
PubMed ID	28293124, 28277882, 28111429, 27913776, 27912834, 27628194, 27575423, 27729681, 27696220
3-D Structure	N.A.