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Th1139 details
Primary information
ID1628
ThPP IDTh1139
Therapeutic Peptide/Protein NameCertolizumab pegol
SequenceLight chain: DIQMTQSPSSLSASVGDRVTITCKASQNVGTNVAWYQ view full sequnce in fasta
Functional ClassificationIIb
Molecular Weight91000
Chemical FormulaC2115H3252N556O673S16
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half LifeElimination half life- 14 days
DescriptionRecombinant Fab' antibody fragment against TNF-alpha, which is conjugated to a ~40kDa Polyethylene glycol (PEG2MAL40K) moiety. PEG helps delay drug elimination. The light chain is made up of 214 amino acid residues while the heavy chain is composed of 229 amino acid residues. The molecular mass of the Fab' antibody fragment itself is 47.8 kDa (i.e. Excluding the PEG moiety). FDA approved on April 22, 2008.
Indication/DiseaseReducing signs and symptoms of Crohn's disease and treatment of moderately to severely active rheumatoid arthritis (RA).
PharmacodynamicsTNFα is a key pro-inflammatory cytokine with a central role in inflammatory processes. Biological activity associated to TNFα include the upregulation of cellular adhesion molecules and chemokines, upregulation of major histocompatibility complex (MHC) class I and class II molecules, and direct leukocyte activation. TNFα stimulates the production of downstream inflammatory mediators, including interleukin-1, prostaglandins, platelet activating factor, and nitric oxide. After treatment with certolizumab pegol, patients with Crohn's disease demonstrated a decrease in the levels of C-reactive protein (CRP).
Mechanism of ActionN.A.
ToxicityThe most common adverse reactions: upper respiratory tract infection, rash, and urinary tract infection.
MetabolismMetabolism has not been studied in humans.
AbsorptionThere is a linear relationship between dose administered and Cmax and AUC. A mean Cmax of approximately 43 to 49 mcg/mL occurred at Week 5 during the initial loading dose period using the recommended dose regimen for the treatment of patients with rheumatoid arthritis (400 mg sc at Weeks 0, 2 and 4 followed by 200 mg every other week). Tmax, SubQ dose = 54 - 171 hours; Bioavailability, SubQ dose = 80% (range of 76% - 88%)
Volume of DistributionVd, steady state, Crohn's and RA patients = 6 - 8 L
ClearanceIV dose, healthy subjects = 9.21 mL/h to 14.38 mL/h;SC dose, Crohn's disease patients = 17 mL/h;SC dose, RA patients = 21.0 mL/h;
CategoriesTNF inhibitor
Patents NumberCA2380298
Date of Issue29/09/14
Date of Expiry06/06/25
Drug InteractionN.A.
TargetTumor necrosis factor
Information of corresponding available drug in the market
Brand NameCimzia
CompanyUCB
Brand DiscriptionCIMZIA (certolizumab pegol) is a TNF blocker. CIMZIA is a recombinant, humanized antibody Fab' fragment, with specificity for human tumor necrosis factor alpha (TNFα), conjugated to an approximately 40kDa polyethylene glycol (PEG2MAL40K). The Fab' fragment is manufactured in E. coli and is subsequently subjected to purification and conjugation to PEG2MAL40K, to generate certolizumab pegol. The Fab' fragment is composed of a light chain with 214 amino acids and a heavy chain with 229 amino acids. The molecular weight of certolizumab pegol is approximately 91 kiloDaltons
Prescribed forCrohn's Disease, Rheumatoid Arthritis, Psoriatic Arthritis
Chemical NameN.A.
FormulationEach single-use prefilled syringe of CIMZIA delivers 200 mg in 1 mL of solution with a pH of approximately 4.7 for subcutaneous use. Each 1 mL syringe of CIMZIA contains certolizumab pegol (200 mg), sodium acetate (1.36 mg), sodium chloride (7.31 mg), and Water for Injection, USP.
Physcial AppearanceCIMZIA is supplied as either a sterile, white, lyophilized powder for solution or as a sterile, solution in a single-use prefilled 1 mL glass syringe for subcutaneous injection
Route of AdministrationSubcutaneous
Recommended Dosage400 mg dose is needed (given as two subcutaneous injections of 200 mg), injections should occur at separate sites in the thigh or abdomen.
ContraindicationN.A.
Side EffectsSerious Infections, Malignancies, Heart Failure
Useful Linkhttp://www.rxlist.com/cimzia-drug.htm http://www.cimzia.com/ http://www.drugs.com/cimzia.html
PubMed ID25651776, 25645901, 25586216, 25555459, 23620660, 23451881
3-D StructureTh1139 light Chainor (Download)Th1139 Heavy Chain (View) or (Download)
Primary information
ID1629
ThPP IDTh1139
Therapeutic Peptide/Protein NameCertolizumab pegol
SequenceLight chain: DIQMTQSPSSLSASVGDRVTITCKASQNVGTNVAWYQ view full sequnce in fasta
Functional ClassificationIIb
Molecular Weight91000
Chemical FormulaC2115H3252N556O673S16
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half LifeElimination half life- 14 days
DescriptionRecombinant Fab' antibody fragment against TNF-alpha, which is conjugated to a ~40kDa Polyethylene glycol (PEG2MAL40K) moiety. PEG helps delay drug elimination. The light chain is made up of 214 amino acid residues while the heavy chain is composed of 229 amino acid residues. The molecular mass of the Fab' antibody fragment itself is 47.8 kDa (i.e. Excluding the PEG moiety). FDA approved on April 22, 2008
Indication/DiseaseReducing signs and symptoms of Crohn's disease and treatment of moderately to severely active rheumatoid arthritis (RA).
PharmacodynamicsTNFα is a key pro-inflammatory cytokine with a central role in inflammatory processes. Biological activity associated to TNFα include the upregulation of cellular adhesion molecules and chemokines, upregulation of major histocompatibility complex (MHC) class I and class II molecules, and direct leukocyte activation. TNFα stimulates the production of downstream inflammatory mediators, including interleukin-1, prostaglandins, platelet activating factor, and nitric oxide. After treatment with certolizumab pegol, patients with Crohn's disease demonstrated a decrease in the levels of C-reactive protein (CRP).
Mechanism of ActionN.A.
ToxicityThe most common adverse reactions: upper respiratory tract infection, rash, and urinary tract infection.
MetabolismMetabolism has not been studied in humans.
AbsorptionThere is a linear relationship between dose administered and Cmax and AUC. A mean Cmax of approximately 43 to 49 mcg/mL occurred at Week 5 during the initial loading dose period using the recommended dose regimen for the treatment of patients with rheumatoid arthritis (400 mg sc at Weeks 0, 2 and 4 followed by 200 mg every other week). Tmax, SubQ dose = 54 - 171 hours; Bioavailability, SubQ dose = 80% (range of 76% - 88%)
Volume of DistributionVd, steady state, Crohn's and RA patients = 6 - 8 L
ClearanceIV dose, healthy subjects = 9.21 mL/h to 14.38 mL/h;SC dose, Crohn's disease patients = 17 mL/h;SC dose, RA patients = 21.0 mL/h;
CategoriesTNF inhibitor
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameN.A.
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful LinkN.A.
PubMed ID25651776, 25645901, 25586216, 25555459, 23620660, 23451881
3-D StructureTh1139 light Chainor (Download)Th1139 Heavy Chain (View) or (Download)
Primary information
ID1630
ThPP IDTh1139
Therapeutic Peptide/Protein NameCertolizumab pegol
SequenceLight chain: DIQMTQSPSSLSASVGDRVTITCKASQNVGTNVAWYQ view full sequnce in fasta
Functional ClassificationIIb
Molecular Weight91000
Chemical FormulaC2115H3252N556O673S16
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half LifeElimination half life- 14 days
DescriptionRecombinant Fab' antibody fragment against TNF-alpha, which is conjugated to a ~40kDa Polyethylene glycol (PEG2MAL40K) moiety. PEG helps delay drug elimination. The light chain is made up of 214 amino acid residues while the heavy chain is composed of 229 amino acid residues. The molecular mass of the Fab' antibody fragment itself is 47.8 kDa (i.e. Excluding the PEG moiety). FDA approved on April 22, 2008
Indication/DiseaseReducing signs and symptoms of Crohn's disease and treatment of moderately to severely active rheumatoid arthritis (RA).
PharmacodynamicsTNFα is a key pro-inflammatory cytokine with a central role in inflammatory processes. Biological activity associated to TNFα include the upregulation of cellular adhesion molecules and chemokines, upregulation of major histocompatibility complex (MHC) class I and class II molecules, and direct leukocyte activation. TNFα stimulates the production of downstream inflammatory mediators, including interleukin-1, prostaglandins, platelet activating factor, and nitric oxide. After treatment with certolizumab pegol, patients with Crohn's disease demonstrated a decrease in the levels of C-reactive protein (CRP).
Mechanism of ActionN.A.
ToxicityThe most common adverse reactions: upper respiratory tract infection, rash, and urinary tract infection.
MetabolismMetabolism has not been studied in humans.
AbsorptionThere is a linear relationship between dose administered and Cmax and AUC. A mean Cmax of approximately 43 to 49 mcg/mL occurred at Week 5 during the initial loading dose period using the recommended dose regimen for the treatment of patients with rheumatoid arthritis (400 mg sc at Weeks 0, 2 and 4 followed by 200 mg every other week). Tmax, SubQ dose = 54 - 171 hours; Bioavailability, SubQ dose = 80% (range of 76% - 88%)
Volume of DistributionVd, steady state, Crohn's and RA patients = 6 - 8 L
ClearanceIV dose, healthy subjects = 9.21 mL/h to 14.38 mL/h;SC dose, Crohn's disease patients = 17 mL/h;SC dose, RA patients = 21.0 mL/h;
CategoriesTNF inhibitor
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameN.A.
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful LinkN.A.
PubMed ID25651776, 25645901, 25586216, 25555459, 23620660, 23451881
3-D StructureTh1139 light Chainor (Download)Th1139 Heavy Chain (View) or (Download)
Primary information
ID1631
ThPP IDTh1139
Therapeutic Peptide/Protein NameCertolizumab pegol
SequenceLight chain: DIQMTQSPSSLSASVGDRVTITCKASQNVGTNVAWYQ view full sequnce in fasta
Functional ClassificationIIb
Molecular Weight91000
Chemical FormulaC2115H3252N556O673S16
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half LifeElimination half life- 14 days
DescriptionRecombinant Fab' antibody fragment against TNF-alpha, which is conjugated to a ~40kDa Polyethylene glycol (PEG2MAL40K) moiety. PEG helps delay drug elimination. The light chain is made up of 214 amino acid residues while the heavy chain is composed of 229 amino acid residues. The molecular mass of the Fab' antibody fragment itself is 47.8 kDa (i.e. Excluding the PEG moiety). FDA approved on April 22, 2008
Indication/DiseaseReducing signs and symptoms of Crohn's disease and treatment of moderately to severely active rheumatoid arthritis (RA).
PharmacodynamicsTNFα is a key pro-inflammatory cytokine with a central role in inflammatory processes. Biological activity associated to TNFα include the upregulation of cellular adhesion molecules and chemokines, upregulation of major histocompatibility complex (MHC) class I and class II molecules, and direct leukocyte activation. TNFα stimulates the production of downstream inflammatory mediators, including interleukin-1, prostaglandins, platelet activating factor, and nitric oxide. After treatment with certolizumab pegol, patients with Crohn's disease demonstrated a decrease in the levels of C-reactive protein (CRP).
Mechanism of ActionN.A.
ToxicityThe most common adverse reactions: upper respiratory tract infection, rash, and urinary tract infection.
MetabolismMetabolism has not been studied in humans.
AbsorptionThere is a linear relationship between dose administered and Cmax and AUC. A mean Cmax of approximately 43 to 49 mcg/mL occurred at Week 5 during the initial loading dose period using the recommended dose regimen for the treatment of patients with rheumatoid arthritis (400 mg sc at Weeks 0, 2 and 4 followed by 200 mg every other week). Tmax, SubQ dose = 54 - 171 hours; Bioavailability, SubQ dose = 80% (range of 76% - 88%)
Volume of DistributionVd, steady state, Crohn's and RA patients = 6 - 8 L
ClearanceIV dose, healthy subjects = 9.21 mL/h to 14.38 mL/h;SC dose, Crohn's disease patients = 17 mL/h;SC dose, RA patients = 21.0 mL/h;
CategoriesTNF inhibitor
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameN.A.
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful LinkN.A.
PubMed ID25651776, 25645901, 25586216, 25555459, 23620660, 23451881
3-D StructureTh1139 light Chainor (Download)Th1139 Heavy Chain (View) or (Download)
Primary information
ID1632
ThPP IDTh1139
Therapeutic Peptide/Protein NameCertolizumab pegol
SequenceLight chain: DIQMTQSPSSLSASVGDRVTITCKASQNVGTNVAWYQ view full sequnce in fasta
Functional ClassificationIIb
Molecular Weight91000
Chemical FormulaC2115H3252N556O673S16
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half LifeElimination half life- 14 days
DescriptionRecombinant Fab' antibody fragment against TNF-alpha, which is conjugated to a ~40kDa Polyethylene glycol (PEG2MAL40K) moiety. PEG helps delay drug elimination. The light chain is made up of 214 amino acid residues while the heavy chain is composed of 229 amino acid residues. The molecular mass of the Fab' antibody fragment itself is 47.8 kDa (i.e. Excluding the PEG moiety). FDA approved on April 22, 2008
Indication/DiseaseReducing signs and symptoms of Crohn's disease and treatment of moderately to severely active rheumatoid arthritis (RA).
PharmacodynamicsTNFα is a key pro-inflammatory cytokine with a central role in inflammatory processes. Biological activity associated to TNFα include the upregulation of cellular adhesion molecules and chemokines, upregulation of major histocompatibility complex (MHC) class I and class II molecules, and direct leukocyte activation. TNFα stimulates the production of downstream inflammatory mediators, including interleukin-1, prostaglandins, platelet activating factor, and nitric oxide. After treatment with certolizumab pegol, patients with Crohn's disease demonstrated a decrease in the levels of C-reactive protein (CRP).
Mechanism of ActionN.A.
ToxicityThe most common adverse reactions: upper respiratory tract infection, rash, and urinary tract infection.
MetabolismMetabolism has not been studied in humans.
AbsorptionThere is a linear relationship between dose administered and Cmax and AUC. A mean Cmax of approximately 43 to 49 mcg/mL occurred at Week 5 during the initial loading dose period using the recommended dose regimen for the treatment of patients with rheumatoid arthritis (400 mg sc at Weeks 0, 2 and 4 followed by 200 mg every other week). Tmax, SubQ dose = 54 - 171 hours; Bioavailability, SubQ dose = 80% (range of 76% - 88%)
Volume of DistributionVd, steady state, Crohn's and RA patients = 6 - 8 L
ClearanceIV dose, healthy subjects = 9.21 mL/h to 14.38 mL/h;SC dose, Crohn's disease patients = 17 mL/h;SC dose, RA patients = 21.0 mL/h;
CategoriesTNF inhibitor
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameN.A.
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful LinkN.A.
PubMed ID25651776, 25645901, 25586216, 25555459, 23620660, 23451881
3-D StructureTh1139 light Chainor (Download)Th1139 Heavy Chain (View) or (Download)
Primary information
ID1633
ThPP IDTh1139
Therapeutic Peptide/Protein NameCertolizumab pegol
SequenceLight chain: DIQMTQSPSSLSASVGDRVTITCKASQNVGTNVAWYQ view full sequnce in fasta
Functional ClassificationIIb
Molecular Weight91000
Chemical FormulaC2115H3252N556O673S16
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half LifeElimination half life- 14 days
DescriptionRecombinant Fab' antibody fragment against TNF-alpha, which is conjugated to a ~40kDa Polyethylene glycol (PEG2MAL40K) moiety. PEG helps delay drug elimination. The light chain is made up of 214 amino acid residues while the heavy chain is composed of 229 amino acid residues. The molecular mass of the Fab' antibody fragment itself is 47.8 kDa (i.e. Excluding the PEG moiety). FDA approved on April 22, 2008
Indication/DiseaseReducing signs and symptoms of Crohn's disease and treatment of moderately to severely active rheumatoid arthritis (RA).
PharmacodynamicsTNFα is a key pro-inflammatory cytokine with a central role in inflammatory processes. Biological activity associated to TNFα include the upregulation of cellular adhesion molecules and chemokines, upregulation of major histocompatibility complex (MHC) class I and class II molecules, and direct leukocyte activation. TNFα stimulates the production of downstream inflammatory mediators, including interleukin-1, prostaglandins, platelet activating factor, and nitric oxide. After treatment with certolizumab pegol, patients with Crohn's disease demonstrated a decrease in the levels of C-reactive protein (CRP).
Mechanism of ActionN.A.
ToxicityThe most common adverse reactions: upper respiratory tract infection, rash, and urinary tract infection.
MetabolismMetabolism has not been studied in humans.
AbsorptionThere is a linear relationship between dose administered and Cmax and AUC. A mean Cmax of approximately 43 to 49 mcg/mL occurred at Week 5 during the initial loading dose period using the recommended dose regimen for the treatment of patients with rheumatoid arthritis (400 mg sc at Weeks 0, 2 and 4 followed by 200 mg every other week). Tmax, SubQ dose = 54 - 171 hours; Bioavailability, SubQ dose = 80% (range of 76% - 88%)
Volume of DistributionVd, steady state, Crohn's and RA patients = 6 - 8 L
ClearanceIV dose, healthy subjects = 9.21 mL/h to 14.38 mL/h;SC dose, Crohn's disease patients = 17 mL/h;SC dose, RA patients = 21.0 mL/h;
CategoriesTNF inhibitor
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameN.A.
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful LinkN.A.
PubMed ID25651776, 25645901, 25586216, 25555459, 23620660, 23451881
3-D StructureTh1139 light Chainor (Download)Th1139 Heavy Chain (View) or (Download)