==== 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


Details of Th1004 which contains 3 entries.


Entry 1
(1) Primary information
ID1025
ThPP IDTh1004
Therapeutic Peptide/Protein NameDenileukin diftitox
SequenceMGADDVVDSSKSFVMENFSSYHGTKPGYVDSIQKGIQKPKSGTQGNYDDD view full sequnce in fasta
Functional ClassificationIIb
Molecular Weight57647.3
Chemical FormulaC2560H4042N678O799S17
Isoelectric Point5.45
Hydrophobicity-0.301
Melting Point (℃)N.A.
Half Life1.16-1.3 hours
DescriptionA recombinant (using E. coli expression system) DNA-derived cytotoxic protein containing amino acid sequences for diphtheria toxin fragments A and B (Met 1-Thr 387)-His and sequences for interleukin-2 (Ala 1-Thr 133).
Indication/DiseaseUsed in the treatment of cutaneous T-cell lymphoma.
PharmacodynamicsDenileukin diftitox (Ontak) uses the cytocidal action of diphtheria toxin on cells which express the IL-2 receptor. The human IL-2 receptor exists in three forms on basis of affinity, low (CD25), intermediate (CD122/CD132) and high (CD25/CD122/CD132). Malignant cells expressing one or more of the subunits of the IL-2 receptor are found in certain leukemias and lymphomas including cutaneous T-cell lymphoma (CTCL). Ontak interacts with the high affinity IL-2 receptor on the cell surface and inhibits cellular protein synthesis, resulting in cell death within hours.
Mechanism of ActionDenileukin diftitox binds to the high-affinity IL-2 receptor. The IL-2 receptor (Tac) subunit is expressed on activated lymphocytes. The diphtheria toxin associated with Ontak selectively kills the IL-2 bearing cells.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of Distribution0.06 to 0.09 L/kg
Clearance0.6 - 2.0 mL/min/kg [Lymphoma]
CategoriesAntineoplastic Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionRilonacept decreases effects of toxoids by pharmacodynamic antagonism
TargetInterleukin-2 receptor subunit alpha,Interleukin-2 receptor subunit beta,Cytokine receptor common subunit gamma
Information of corresponding available drug in the market
Brand NameOntak
CompanySeragen Inc
Brand DiscriptionOntak is a recombinant DNA-derived cytotoxic protein composed of the amino acid sequences of diphtheria toxin fragments A and B (Met1-Thr387)-His followed by sequences for human interleukin-2 (IL-2; Ala1-Thr133)
Prescribed forTreating leukemia and lymphomas, including cutaneous (of the skin) T-cell lymphoma.
Chemical NameN.A.
FormulationOntak contains 300 mcg of recombinant denileukin diftitox in a sterile solution of citric acid (20 mM), EDTA (0.05 mM) and polysorbate 20 ( < 1%) in Water for Injection, USP. The solution has a pH range of 6.9-7.2.
Physcial AppearanceSterile, white, preservative-free, lyophilized powder.
Route of AdministrationIntravenous (Intravenous) administration
Recommended DosageN.A.
Contraindicationallergic
Side EffectsCommon side effects include:headache, dizziness, or nervousness, numbness or tingling, skin itching or rash, runny or stuffy nose; weight gain or loss; mild diarrhea or constipation, or nausea, vomiting, loss of appetite.
Useful Linkhttp://www.drugs.com/mtm/ontak.html
PubMed ID17454642, 17187516
3-D StructureTh1004 (View) or (Download)


Entry 2
(2) Primary information
ID1026
ThPP IDTh1004
Therapeutic Peptide/Protein NameDenileukin diftitox
SequenceMGADDVVDSSKSFVMENFSSYHGTKPGYVDSIQKGIQKPKSGTQGNYDDD view full sequnce in fasta
Functional ClassificationIIb
Molecular Weight57647.3
Chemical FormulaC2560H4042N678O799S17
Isoelectric Point5.45
Hydrophobicity-0.301
Melting Point (℃)N.A.
Half Life1.16-1.3 hours
DescriptionA recombinant (using E. coli expression system) DNA-derived cytotoxic protein containing amino acid sequences for diphtheria toxin fragments A and B (Met 1-Thr 387)-His and sequences for interleukin-2 (Ala 1-Thr 133).
Indication/DiseaseUsed in the treatment of cutaneous T-cell lymphoma.
PharmacodynamicsDenileukin diftitox (Ontak) uses the cytocidal action of diphtheria toxin on cells which express the IL-2 receptor. The human IL-2 receptor exists in three forms on basis of affinity, low (CD25), intermediate (CD122/CD132) and high (CD25/CD122/CD132). Malignant cells expressing one or more of the subunits of the IL-2 receptor are found in certain leukemias and lymphomas including cutaneous T-cell lymphoma (CTCL). Ontak interacts with the high affinity IL-2 receptor on the cell surface and inhibits cellular protein synthesis, resulting in cell death within hours.
Mechanism of ActionDenileukin diftitox binds to the high-affinity IL-2 receptor. The IL-2 receptor (Tac) subunit is expressed on activated lymphocytes. The diphtheria toxin associated with Ontak selectively kills the IL-2 bearing cells.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of Distribution0.06 to 0.09 L/kg
Clearance0.6 - 2.0 mL/min/kg [Lymphoma]
CategoriesAntineoplastic Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionTrastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
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 Linkhttp://www.rxlist.com/ontak-drug.htm
PubMed ID17454642, 17187516
3-D StructureTh1004 (View) or (Download)


Entry 3
(3) Primary information
ID1027
ThPP IDTh1004
Therapeutic Peptide/Protein NameDenileukin diftitox
SequenceMGADDVVDSSKSFVMENFSSYHGTKPGYVDSIQKGIQKPKSGTQGNYDDD view full sequnce in fasta
Functional ClassificationIIb
Molecular Weight57647.3
Chemical FormulaC2560H4042N678O799S17
Isoelectric Point5.45
Hydrophobicity-0.301
Melting Point (℃)N.A.
Half Life1.16-1.3 hours
DescriptionA recombinant (using E. coli expression system) DNA-derived cytotoxic protein containing amino acid sequences for diphtheria toxin fragments A and B (Met 1-Thr 387)-His and sequences for interleukin-2 (Ala 1-Thr 133).
Indication/DiseaseUsed in the treatment of cutaneous T-cell lymphoma.
PharmacodynamicsDenileukin diftitox (Ontak) uses the cytocidal action of diphtheria toxin on cells which express the IL-2 receptor. The human IL-2 receptor exists in three forms on basis of affinity, low (CD25), intermediate (CD122/CD132) and high (CD25/CD122/CD132). Malignant cells expressing one or more of the subunits of the IL-2 receptor are found in certain leukemias and lymphomas including cutaneous T-cell lymphoma (CTCL). Ontak interacts with the high affinity IL-2 receptor on the cell surface and inhibits cellular protein synthesis, resulting in cell death within hours.
Mechanism of ActionDenileukin diftitox binds to the high-affinity IL-2 receptor. The IL-2 receptor (Tac) subunit is expressed on activated lymphocytes. The diphtheria toxin associated with Ontak selectively kills the IL-2 bearing cells.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of Distribution0.06 to 0.09 L/kg
Clearance0.6 - 2.0 mL/min/kg [Lymphoma]
CategoriesAntineoplastic Agents
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 Linkhttp://www.drugs.com/dosage/ontak.html
PubMed ID17454642, 17187516
3-D StructureTh1004 (View) or (Download)