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10682 details
Primary information
ID10682
Therapeutic IDTh1150
Protein NameSecukinumab
Sequence>Th1150_Secukinumab EVQLVESGGGLVQPGGSLRLSCAASGFTFSNYWMNWVRQAPGKGLEWVAAINQDGSEKYYVGSVKGRFTISRDNAKNSLYLQMNSLRVEDTAVYYCVRDYYDILTDYYIHYWYFDLWGRGTLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
Molecular Weight147940
Chemical FormulaC6584H10134N1754O2042S44
Isoelectric PointNA
HydrophobicityNA
Melting pointNA
Half-life22-31 days
DescriptionA human monoclonal antibody, secukinumab (cosentyx) was designed for the treatment of uveitis, rheumatoid arthritis, ankylosing spondylitis, and psoriasis. Secukinumab is an interleukin-17A inhibitor marketed by Novartis. On January 19, 2015, secukinumab was approved by the European Commission as a first line systemic treatment in moderate to severe adult plaque psoriasis. On January 21, 2015, the United States Food and Drug Administration announced that it had approved secukinumab to treat adults with moderate-to-severe plaque psoriasis.
Indication/DiseaseIt is a human interleukin-17A antagonist indicated for the treatment of moderate to severe plaque psoriasis in adult patients who are candidates for systemic therapy or phototherapy.
PharmacodynamicsElevated levels of IL-17A are found in psoriatic plaques. Treatment with cosentyx may reduce epidermal neutrophils and IL-17A levels in psoriatic plaques. Serum levels of total IL-17A (free and secukinumab-bound IL-17A) measured at Week 4 and Week 12 were increased following secukinumab treatment. These pharmacodynamic activities are based on small exploratory studies. The relationship between these pharmacodynamic activities and the mechanism(s) by which secukinumab exerts its clinical effects is unknown.
Mechanism of ActionSecukinumab is a human IgG1 monoclonal antibody that selectively binds to the interleukin-17A (IL-17A) cytokine and inhibits its interaction with the IL-17 receptor. IL-17A is a naturally occurring cytokine that is involved in normal inflammatory and immune responses. Secukinumab inhibits the release of proinflammatory cytokines and chemokines.
ToxicityNA
MetabolismMainly intracellular breakdown.
AbsorptionBioavailability after subcutaneous administration was 55-77%.
Volume of distribution (Vd) in interstitial fluid of skin (+/- psoriasis) was 27-40% of that in serum after single subcutaneous dose of 300 mg. Vd increased at higher body weights.
ClearanceSerum clearance was increased with higher body weights.
CategoriesInhibitor
Patents NumberUS20130202610
Date of Issue10-Aug-2010
Date of Expiry10-Aug-2020
Drug InteractionNA
TargetInterleukin-17A
Brand NameCosentyx
CompanyNovartis Pharmaceuticals Corporation
Brand DescriptionNovartis Pharmaceuticals Corporation
Prescribed ForCosentyx is indicated for the treatment of moderate to severe plaque psoriasis in adult patients who are candidates for systemic therapy or phototherapy.
Chemical NameNA
FormulationEach cosentyx sensoready pen or prefilled syringe contains 150 mg of secukinumab formulated in: Lhistidine/ histidine hydrochloride monohydrate (3.103 mg), L-methionine (0.746 mg), polysorbate 80 (0.2 mg), trehalose dihydrate (75.67 mg), and Sterile Water for Injection, USP, at pH of 5.8.
Physical Appearance Cosentyx injection is a sterile, preservative-free, clear to slightly opalescent, colorless to slightly yellow solution.
Route of AdministrationSubcutaneous injection
Recommended DosageThe recommended dose is 300 mg by subcutaneous injection at Weeks 0, 1, 2, 3, and 4 followed by 300 mg every 4 weeks. Each 300 mg dose is given as 2 subcutaneous injections of 150 mg. For some patients, a dose of 150 mg may be acceptable.
ContraindicationPatients with a previous serious hypersensitivity reaction to secukinumab or to any of the excipientsÂÂ
Side EffectsCrohn’s disease “flare-ups” (worsening Crohn’s disease), serious allergic reactions, chest tightness, swelling of your face, eyelids, lips, mouth, tongue, or throat, trouble breathing or throat tightness, skin rash and upper respiratory infections
Useful Link 1Link
Useful Link 2NA
RemarksNA