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Th1222 details

Primary information
ID 1832
ThPP ID Th1222
Therapeutic Peptide/Protein Name Canakinumab
Sequence H-GAMMA-1 Chain: QVQLVESGGGVVQPGRSLRLSCAASGFTFSVYG view full sequnce in fasta
Functional Classification IIa
Molecular Weight 145200
Chemical Formula C6452H9958N1722O2010S42
Isoelectric Point NA
Hydrophobicity NA
Melting Point (℃) NA
Half Life 26 days
Description Canakinumab is a recombinant, human anti-human-IL-1Î² monoclonal antibody that belongs to the IgG1/Îº isotype subclass. It is expressed in a murine Sp2/0-Ag14 cell line and comprised of two 447- (or 448-) residue heavy chains and two 214-residue light chains, with a molecular mass of 145157 Daltons when deglycosylated. Both heavy chains of canakinumab contain oligosaccharide chains linked to the protein backbone at asparagine 298 (Asn 298). Canakinumab binds to human IL-1Î² and neutralizes its inflammatory activity by blocking its interaction with IL-1 receptors, but it does not bind IL-1alpha or IL-1 receptor antagonist (IL-1ra). Canakinumab is marketed under the brand name Ilaris and indicated for patients 4 years of age and older to treat Familial Cold Autoinflammatory Syndrome (FCAS) and Muckle-Wells Syndrome (MWS), which are both part of the Cryopyrin-Associated Periodic Syndromes (CAPS) as well as for patients 2 years of age and older to treat systemic juvenile idiopathic arthritis (SJIA). Clinical trials have established the administration of canakinumab every 2 weeks to be safe and effective, offering a considerable advantage over the existing treatment with the human IL-1 receptor antagonist, anakinra, which must be injected daily and which is often poorly tolerated by patients.
Indication/Disease Used in patients 4 years of age and older to treat Familial Cold Autoinflammatory Syndrome (FCAS) and Muckle-Wells Syndrome (MWS), which are both part of the Cryopyrin-Associated Periodic Syndromes (CAPS) as well as for patients 2 years of age and older to treat systemic juvenile idiopathic arthritis (SJIA).
Pharmacodynamics Novartis AG has developed canakinumab as a subcutaneous injection and fully human mAb that neutralizes the bioactivity of human IL-1beta, which is involved in several inflammatory disorders. Canakinumab has promising clinical safety and pharmacokinetic properties, and demonstrated potential for the treatment of cryopyrin-associated periodic syndromes (CAPS), systemic juvenile idiopathic arthritis (SJIA), and possibly for other complex inflammatory diseases, such as rheumatoid arthritis, COPD disease and ocular diseases.
Mechanism of Action In inflammatory diseases involving Cryopyrin-Associated Periodic Syndromes (CAPS), interleukin-1 beta (IL-1Î²) is excessively activated and drives inflammation. The protein cryopyrin controls the activation of IL-1Î², and mutations in cryopyrin's gene, NLRP-3, up-regulate IL-1Î² activation. Canakinumab is a human monoclonal anti-human IL-1Î² antibody of the IgG1/Îº isotype. Canakinumab binds to human IL-1Î² and neutralizes its inflammatory activity by blocking its interaction with IL-1 receptors, but it does not bind IL-1Î± or IL-1 receptor antagonist (IL-1ra).
Toxicity The most common adverse reactions involved the central nervous system (headache and vertigo), gastrointestinal system (diarrhea and nausea), neuromuscular and skeletal system (musculoskeletal pain), and respiratory system (rhinitis, nasopharyngitis and bronchitis). Influenza was also reported.
Metabolism The metabolism of canakinumab is not yet determined.
Absorption The absolute bioavailability of subcutaneous canakinumab is estimated to be 70%.
Volume of Distribution 6.01 L
Clearance 0.174 L/day [typical CAPS patient weighing 70 kg]
Categories Antineoplastic and Immunomodulating Agents
Patents Number NA
Date of Issue NA
Date of Expiry NA
Drug Interaction The risk or severity of adverse effects can be increased when Canakinumab is combined with Adalimumab, Afelimomab, Anakinra, BCG, Certolizumab pegol, Denosumab, Etanercept, Fingolimod, G17DT, GI-5005 etc
Target Interleukin-1 beta
Information of corresponding available drug in the market
Brand Name Ilaris
Company Novartis
Brand Discription Ilaris (canakinumab) is a monoclonal antibody that blocks certain proteins in the body that can affect inflammation and other immune responses.
Prescribed for Ilaris is used to treat certain types of periodic fever syndromes, sometimes called auto-inflammatory syndromes.
Chemical Name NA
Formulation Each vial of sterile, white, preservative-free, lyophilized powder contains canakinumab 150Â mg. Nonmedicinal ingredients: sucrose, L-histidine, L-histidine HCL monohydrate, polysorbate 80.
Physcial Appearance Lyphilized powder
Route of Administration Subcutaneous
Recommended Dosage The recommended dose of Ilaris is 150 mg for CAPS patients with body weight greater than 40 kg.Â For CAPS patients with body weight greater than or equal to 15 kg and less than or equal to 40 kg, the recommended dose is 2 mg/kg.Â ForÂ children 15 to 40 kg with an inadequate response, the dose can be increased to 3 mg
Contraindication Confirmed hypersensitivity to the active substance or to any of the excipients.
Side Effects The most common adverse reactionsgreater than 10% reported by patients treated with ILARISare nasopharyngitis, diarrhea, influenza, rhinitis, nausea, headache, bronchitis, gastroenteritis, pharyngitis, weight increased, musculoskeletal pain, and vertigo.
Useful Link https://www.pharma.us.novartis.com/sites/www.pharma.us.novartis.com/files/ilaris.pdf , https://www.drugs.com/ilaris.html , http://www.medbroadcast.com/drug/getdrug/ilaris
PubMed ID 19169963, 19494217
3-D Structure N.A.

OSDDlinux

Raghava's Group

IMTECH

CSIR

CRDD
CPPSITE 2.0

Primary information
ID	1832
ThPP ID	Th1222
Therapeutic Peptide/Protein Name	Canakinumab
Sequence	H-GAMMA-1 Chain: QVQLVESGGGVVQPGRSLRLSCAASGFTFSVYG view full sequnce in fasta
Functional Classification	IIa
Molecular Weight	145200
Chemical Formula	C6452H9958N1722O2010S42
Isoelectric Point	NA
Hydrophobicity	NA
Melting Point (℃)	NA
Half Life	26 days
Description	Canakinumab is a recombinant, human anti-human-IL-1Î² monoclonal antibody that belongs to the IgG1/Îº isotype subclass. It is expressed in a murine Sp2/0-Ag14 cell line and comprised of two 447- (or 448-) residue heavy chains and two 214-residue light chains, with a molecular mass of 145157 Daltons when deglycosylated. Both heavy chains of canakinumab contain oligosaccharide chains linked to the protein backbone at asparagine 298 (Asn 298). Canakinumab binds to human IL-1Î² and neutralizes its inflammatory activity by blocking its interaction with IL-1 receptors, but it does not bind IL-1alpha or IL-1 receptor antagonist (IL-1ra). Canakinumab is marketed under the brand name Ilaris and indicated for patients 4 years of age and older to treat Familial Cold Autoinflammatory Syndrome (FCAS) and Muckle-Wells Syndrome (MWS), which are both part of the Cryopyrin-Associated Periodic Syndromes (CAPS) as well as for patients 2 years of age and older to treat systemic juvenile idiopathic arthritis (SJIA). Clinical trials have established the administration of canakinumab every 2 weeks to be safe and effective, offering a considerable advantage over the existing treatment with the human IL-1 receptor antagonist, anakinra, which must be injected daily and which is often poorly tolerated by patients.
Indication/Disease	Used in patients 4 years of age and older to treat Familial Cold Autoinflammatory Syndrome (FCAS) and Muckle-Wells Syndrome (MWS), which are both part of the Cryopyrin-Associated Periodic Syndromes (CAPS) as well as for patients 2 years of age and older to treat systemic juvenile idiopathic arthritis (SJIA).
Pharmacodynamics	Novartis AG has developed canakinumab as a subcutaneous injection and fully human mAb that neutralizes the bioactivity of human IL-1beta, which is involved in several inflammatory disorders. Canakinumab has promising clinical safety and pharmacokinetic properties, and demonstrated potential for the treatment of cryopyrin-associated periodic syndromes (CAPS), systemic juvenile idiopathic arthritis (SJIA), and possibly for other complex inflammatory diseases, such as rheumatoid arthritis, COPD disease and ocular diseases.
Mechanism of Action	In inflammatory diseases involving Cryopyrin-Associated Periodic Syndromes (CAPS), interleukin-1 beta (IL-1Î²) is excessively activated and drives inflammation. The protein cryopyrin controls the activation of IL-1Î², and mutations in cryopyrin's gene, NLRP-3, up-regulate IL-1Î² activation. Canakinumab is a human monoclonal anti-human IL-1Î² antibody of the IgG1/Îº isotype. Canakinumab binds to human IL-1Î² and neutralizes its inflammatory activity by blocking its interaction with IL-1 receptors, but it does not bind IL-1Î± or IL-1 receptor antagonist (IL-1ra).
Toxicity	The most common adverse reactions involved the central nervous system (headache and vertigo), gastrointestinal system (diarrhea and nausea), neuromuscular and skeletal system (musculoskeletal pain), and respiratory system (rhinitis, nasopharyngitis and bronchitis). Influenza was also reported.
Metabolism	The metabolism of canakinumab is not yet determined.
Absorption	The absolute bioavailability of subcutaneous canakinumab is estimated to be 70%.
Volume of Distribution	6.01 L
Clearance	0.174 L/day [typical CAPS patient weighing 70 kg]
Categories	Antineoplastic and Immunomodulating Agents
Patents Number	NA
Date of Issue	NA
Date of Expiry	NA
Drug Interaction	The risk or severity of adverse effects can be increased when Canakinumab is combined with Adalimumab, Afelimomab, Anakinra, BCG, Certolizumab pegol, Denosumab, Etanercept, Fingolimod, G17DT, GI-5005 etc
Target	Interleukin-1 beta
Information of corresponding available drug in the market
Brand Name	Ilaris
Company	Novartis
Brand Discription	Ilaris (canakinumab) is a monoclonal antibody that blocks certain proteins in the body that can affect inflammation and other immune responses.
Prescribed for	Ilaris is used to treat certain types of periodic fever syndromes, sometimes called auto-inflammatory syndromes.
Chemical Name	NA
Formulation	Each vial of sterile, white, preservative-free, lyophilized powder contains canakinumab 150Â mg. Nonmedicinal ingredients: sucrose, L-histidine, L-histidine HCL monohydrate, polysorbate 80.
Physcial Appearance	Lyphilized powder
Route of Administration	Subcutaneous
Recommended Dosage	The recommended dose of Ilaris is 150 mg for CAPS patients with body weight greater than 40 kg.Â For CAPS patients with body weight greater than or equal to 15 kg and less than or equal to 40 kg, the recommended dose is 2 mg/kg.Â ForÂ children 15 to 40 kg with an inadequate response, the dose can be increased to 3 mg
Contraindication	Confirmed hypersensitivity to the active substance or to any of the excipients.
Side Effects	The most common adverse reactionsgreater than 10% reported by patients treated with ILARISare nasopharyngitis, diarrhea, influenza, rhinitis, nausea, headache, bronchitis, gastroenteritis, pharyngitis, weight increased, musculoskeletal pain, and vertigo.
Useful Link	https://www.pharma.us.novartis.com/sites/www.pharma.us.novartis.com/files/ilaris.pdf , https://www.drugs.com/ilaris.html , http://www.medbroadcast.com/drug/getdrug/ilaris
PubMed ID	19169963, 19494217
3-D Structure	N.A.