==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

Detailed description page of THPdb

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1257 details
Primary information
ThPP IDTh1036
Therapeutic Peptide/Protein NameAldesleukin
SequenceMAPTSSSTKKTQLQLEHLLLDLQMILNGINNYKNPKLTRMLTFKFYMPKK view full sequnce in fasta
Functional ClassificationIb
Molecular Weight15314.8
Chemical FormulaC690H1115N177O202S6
Isoelectric Point7.31
Hydrophobicity-0.192
Melting Point (℃)N.A.
Half Life0.22-1.42 hours
DescriptionAldesleukin, a lymphokine, is produced by recombinant DNA technology using a genetically engineered E. coli strain containing an analog of the human interleukin-2 gene. Genetic engineering techniques were used to modify the human IL-2 gene, and the resulting expression clone encodes a modified human interleukin-2. This recombinant form differs from native interleukin-2 in the following ways: a) Aldesleukin is not glycosylated because it is derived from E. coli; b) the molecule has no N-terminal alanine; the codon for this amino acid was deleted during the genetic engineering procedure; c) the molecule has serine substituted for cysteine at amino acid position 125.
Indication/DiseaseFor treatment of adults with metastatic renal cell carcinoma.
PharmacodynamicsAldesleukin is used to treat renal cell carcinoma, it induces the enhancement of lymphocyte mitogenesis and stimulation of long-term growth of human interleukin-2 dependent cell lines, the enhancement of lymphocyte cytotoxicity, the induction of killer cell (lymphokine-activated (LAK) and natural (NK)) activity; and the induction of interferon-gamma production. IL-2 is normally produced by the body, secreted by T cells, and stimulates growth and differentiation of T cell response. It can be used in immunotherapy to treat cancer. It enhances the ability of the immune system to kill tumor cells and may interfere with blood flow to the tumor.
Mechanism of ActionAldesleukin binds to the IL-2 receptor which leads to heterodimerization of the cytoplasmic domains of the IL-2R beta and gamma chains, activation of the tyrosine kinase Jak3, and phosphorylation of tyrosine residues on the IL-2R beta chain. These events led to the creation of an activated receptor complex, to which various cytoplasmic signaling molecules are recruited and become substrates for regulatory enzymes (especially tyrosine kinases) that are associated with the receptor. These events stimulate growth and differentiation of T cells.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of Distribution0.18 l/kg
ClearanceThe pharmacokinetic profile of Proleukin is characterized by high plasma concentrations following a short IV infusion, rapid distribution into the extravascular space and elimination from the body by metabolism in the kidneys with little or no bioactive p
CategoriesAntineoplastic Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionCorticosteroids such as clobetasol propionate may diminish the antineoplastic effect of aldesleukin. Avoid conccurent use of corticosteroids with aldesleukin.
TargetInterleukin-2 receptor subunit beta,Interleukin-2 receptor subunit alpha,Cytokine receptor common subunit gamma
Information of corresponding available drug in the market
Brand NameProleukin
CompanyChiron Corp
Brand DiscriptionProleukin, a human recombinant interleukin-2 product, is a highly purified protein with a molecular weight of approximately 15,300 daltons. It is produced by recombinant DNA technology using a genetically engineered E. coli strain containing an analog of
Prescribed forTreating skin cancer and kidney cancer that has spread to other parts of the body.
Chemical Namedesalanyl-1, serine-125 human interleukin-2
FormulationProleukin is supplied in single-use vials intended for intravenous administration. When reconstituted with 1.2 mL Sterile Water for Injection, USP, each mL contains 18 million International Units (1.1 mg) Proleukin, 50 mg mannitol, and 0.18 mg sodium dod
Physcial AppearnceSterile, white to off-white, lyophilized cake
Route of AdministrationIntravenous administration
Recommended DosageThe recommended Proleukin treatment regimen is administered by a 15 minute Intravenous infusion every 8 hours. 600,000 International Units/kg (0.037 mg/kg) dose administered every 8 hours by a 15 minute Intravenous infusion for a maximum of 14 doses. ollowing 9 days of rest, the schedule is repeated for another 14 doses, for a maximum of 28 doses per course, as tolerated.
ContraindicationProleukin is contraindicated in patients with a known history of hypersensitivity to interleukin-2 or any component of the Proleukin formulation.
Side EffectsAnxiety; dizziness; general body discomfort; increased cough; infection; loss of appetite; pain; runny nose; weakness.
Useful Linkhttp://www.rxlist.com/proleukin-drug.htm
PubMed ID25589384, 25270293, 25270293, 24598453, 11980386, 25270293, 23386066, 11980386
3-D StructureTh1036 (View) or (Download)