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Th1093 details

Primary information
ID 1473
ThPP ID Th1093
Therapeutic Peptide/Protein Name Eculizumab
Sequence N.A. view full sequnce in fasta
Functional Classification Ia
Molecular Weight 148000
Chemical Formula N.A.
Isoelectric Point N.A.
Hydrophobicity N.A.
Melting Point (℃) N.A.
Half Life 272 Â± 82 hrs (mean Â± SD)
Description Soliris is a formulation of eculizumab which is a recombinant humanized monoclonal IgG2/4;K antibody. Recombinant; produced in murine myeloma cell culture. Eculizumab contains human constant regions from human IgG2 sequences and human IgG4 sequences and murine complementarity-determining regions grafted onto the human framework light- and heavy-chain variable regions and has a molecular weight of approximately 148 kDa.
Indication/Disease For the treatment of patients with paroxysmal nocturnal hemoglobinuria (PNH) to reduce hemolysis.
Pharmacodynamics Eculizumab is a monoclonal antibody directed against the complement protein C5. This antibody blocks the cleavage of C5 and halts the process of complement-mediated cell destruction. Eculizumab is a product of Alexion Pharmaceuticals and has been shown to be effective in treating paroxysmal nocturnal hemoglobinuria. Eculizumab was approved by the FDA in March, 2007.
Mechanism of Action A genetic mutation in PNH patients leads to the generation of populations of abnormal RBCs (known as PNH cells) that are deficient in terminal complement inhibitors (CD-59), rendering PNH RBCs sensitive to persistent terminal complement-mediated destruction. The destruction and loss of these PNH cells (intravascular hemolysis) results in low RBC counts (anemia) and also fatigue, difficulty in functioning, pain, dark urine, shortness of breath, and blood clots. Eculizumab, the active ingredient in Soliris, is a monoclonal antibody that binds to the complement protein C5 specifically and with high affinity, thereby inhibiting its cleavage to C5a and C5b and subsequent generation of the terminal complement complex C5b-9. Soliris inhibits terminal complement mediated intravascular hemolysis in PNH patients and therefore the destruction of PNH erythrocytes that lack complement protection with CD-59.
Toxicity N.A.
Metabolism N.A.
Absorption N.A.
Volume of Distribution 7.7 L
Clearance 22 mL/hr [typical PNH patient weighing 70 kg]
Categories N.A.
Patents Number CA2189015
Date of Issue 14/04/14
Date of Expiry 01/05/19
Drug Interaction N.A.
Target Complement C5
Information of corresponding available drug in the market
Brand Name Soliris
Company Alexion, Inc
Brand Discription Soliris, a complement inhibitor, is a formulation of eculizumab which is a recombinant humanized monoclonal IgG2/4Îº antibody produced by murine myeloma cell culture and purified by standard bioprocess technology. Eculizumab contains human constant regions from human IgG2 sequences and human IgG4 sequences and murine complementarity-determining regions grafted onto the human framework light- and heavy-chain variable regions. Eculizumab is composed of two 448 amino acid heavy chains and two 214 amino acid light chains and has a molecular weight of approximately 148 kDa.
Prescribed for indicated for the treatment of patients with paroxysmal nocturnal hemoglobinuria (PNH) to reduce hemolysis
Chemical Name N.A.
Formulation The product is formulated at pH 7 and each vial contains 300 mg of eculizumab, 13.8 mg sodium phosphate monobasic, 53.4 mg sodium phosphate dibasic, 263.1 mg sodium chloride, 6.6 mg polysorbate 80 (vegetable origin) and Water for Injection, USP.
Physcial Appearance Sterile, clear, colorless, preservative-free 10 mg/mL solution for Intravenous infusion and is supplied in 30-mL single-use vials
Route of Administration N.A.
Recommended Dosage 600 mg weekly for the first 4 weeks, followed by 900 mg for the fifth dose 1 week later, then 900 mg every 2 weeks thereafter.
Contraindication N.A.
Side Effects Life-threatening and fatal meningococcal infections have occurred in patients treated with Soliris. Meningococcal infection may become rapidly life-threatening or fatal if not recognized and treated early.
Useful Link http://www.rxlist.com/soliris-drug/side-effects-interactions.htm http://www.fda.gov/AboutFDA/CentersOffices/OfficeofMedicalProductsandTobacco/CDER/ucm273089.htm http://www.drugs.com/cdi/eculizumab.html https://en.wikipedia.org/wiki/Eculizumab
PubMed ID 18784156, 17989688, 16990386
3-D Structure N.A.

OSDDlinux

Raghava's Group

IMTECH

CSIR

CRDD
CPPSITE 2.0

Primary information
ID	1473
ThPP ID	Th1093
Therapeutic Peptide/Protein Name	Eculizumab
Sequence	N.A. view full sequnce in fasta
Functional Classification	Ia
Molecular Weight	148000
Chemical Formula	N.A.
Isoelectric Point	N.A.
Hydrophobicity	N.A.
Melting Point (℃)	N.A.
Half Life	272 Â± 82 hrs (mean Â± SD)
Description	Soliris is a formulation of eculizumab which is a recombinant humanized monoclonal IgG2/4;K antibody. Recombinant; produced in murine myeloma cell culture. Eculizumab contains human constant regions from human IgG2 sequences and human IgG4 sequences and murine complementarity-determining regions grafted onto the human framework light- and heavy-chain variable regions and has a molecular weight of approximately 148 kDa.
Indication/Disease	For the treatment of patients with paroxysmal nocturnal hemoglobinuria (PNH) to reduce hemolysis.
Pharmacodynamics	Eculizumab is a monoclonal antibody directed against the complement protein C5. This antibody blocks the cleavage of C5 and halts the process of complement-mediated cell destruction. Eculizumab is a product of Alexion Pharmaceuticals and has been shown to be effective in treating paroxysmal nocturnal hemoglobinuria. Eculizumab was approved by the FDA in March, 2007.
Mechanism of Action	A genetic mutation in PNH patients leads to the generation of populations of abnormal RBCs (known as PNH cells) that are deficient in terminal complement inhibitors (CD-59), rendering PNH RBCs sensitive to persistent terminal complement-mediated destruction. The destruction and loss of these PNH cells (intravascular hemolysis) results in low RBC counts (anemia) and also fatigue, difficulty in functioning, pain, dark urine, shortness of breath, and blood clots. Eculizumab, the active ingredient in Soliris, is a monoclonal antibody that binds to the complement protein C5 specifically and with high affinity, thereby inhibiting its cleavage to C5a and C5b and subsequent generation of the terminal complement complex C5b-9. Soliris inhibits terminal complement mediated intravascular hemolysis in PNH patients and therefore the destruction of PNH erythrocytes that lack complement protection with CD-59.
Toxicity	N.A.
Metabolism	N.A.
Absorption	N.A.
Volume of Distribution	7.7 L
Clearance	22 mL/hr [typical PNH patient weighing 70 kg]
Categories	N.A.
Patents Number	CA2189015
Date of Issue	14/04/14
Date of Expiry	01/05/19
Drug Interaction	N.A.
Target	Complement C5
Information of corresponding available drug in the market
Brand Name	Soliris
Company	Alexion, Inc
Brand Discription	Soliris, a complement inhibitor, is a formulation of eculizumab which is a recombinant humanized monoclonal IgG2/4Îº antibody produced by murine myeloma cell culture and purified by standard bioprocess technology. Eculizumab contains human constant regions from human IgG2 sequences and human IgG4 sequences and murine complementarity-determining regions grafted onto the human framework light- and heavy-chain variable regions. Eculizumab is composed of two 448 amino acid heavy chains and two 214 amino acid light chains and has a molecular weight of approximately 148 kDa.
Prescribed for	indicated for the treatment of patients with paroxysmal nocturnal hemoglobinuria (PNH) to reduce hemolysis
Chemical Name	N.A.
Formulation	The product is formulated at pH 7 and each vial contains 300 mg of eculizumab, 13.8 mg sodium phosphate monobasic, 53.4 mg sodium phosphate dibasic, 263.1 mg sodium chloride, 6.6 mg polysorbate 80 (vegetable origin) and Water for Injection, USP.
Physcial Appearance	Sterile, clear, colorless, preservative-free 10 mg/mL solution for Intravenous infusion and is supplied in 30-mL single-use vials
Route of Administration	N.A.
Recommended Dosage	600 mg weekly for the first 4 weeks, followed by 900 mg for the fifth dose 1 week later, then 900 mg every 2 weeks thereafter.
Contraindication	N.A.
Side Effects	Life-threatening and fatal meningococcal infections have occurred in patients treated with Soliris. Meningococcal infection may become rapidly life-threatening or fatal if not recognized and treated early.
Useful Link	http://www.rxlist.com/soliris-drug/side-effects-interactions.htm http://www.fda.gov/AboutFDA/CentersOffices/OfficeofMedicalProductsandTobacco/CDER/ucm273089.htm http://www.drugs.com/cdi/eculizumab.html https://en.wikipedia.org/wiki/Eculizumab
PubMed ID	18784156, 17989688, 16990386
3-D Structure	N.A.