==== 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 Th1159 which contains 2 entries.


Entry 1
(1) Primary information
ID1671
ThPP IDTh1159
Therapeutic Peptide/Protein NameGemtuzumab ozogamicin
SequenceLight Chain 1: QIVLTQSPAIMSASPGEKVTITCSASSSISYMHWF view full sequnce in fasta
Functional ClassificationIIb
Molecular Weight151000 to 153000
Chemical FormulaN.A.
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)61 (FAB fr
Half LifeN.A.
DescriptionRecombinant humanized IgG4, kappa antibody conjugated with a cytotoxic antitumor antibiotic, calicheamicin, isolated from fermentation of a bacterium, Micromonospora echinospora ssp. calichensis. The antibody portion of Mylotarg binds specifically to the CD33 antigen, The anti-CD33 hP67.6 antibody is produced by mammalian cell suspension culture using a myeloma NS0 cell line.
Indication/DiseaseFor treatment of CD33-positive acute myeloid leukemia in patients 60 and over who are not candidates for other chemotherapy.
PharmacodynamicsUsed for the treatment of acute myeloid leukemia (AML), mylotarg binds to the CD33 antigen, which is expressed on the surface of leukemic cells in more than 80% of patients with AML. The CD33 antigen is not expressed on pluripotent hematopoietic stem cells or nonhematopoietic cells. This gives mylotarg the selectivity needed to target leukemic cells.
Mechanism of ActionMylotarg is directed against the CD33 antigen expressed by hematopoietic cells. Binding of the anti-CD33 antibody portion of Mylotarg with the CD33 antigen results in the formation of a complex that is internalized. Upon internalization, the calicheamicin derivative is released inside the lysosomes of the myeloid cell. The released calicheamicin derivative binds to DNA in the minor groove resulting in DNA double strand breaks and cell death.
ToxicityThe most frequently reported toxicities are myelosuppression and hepatic veno-occlusive disorder.
MetabolismMost likely removed by opsonization via the reticuloendothelial system
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesAntineoplastic agents and Immunotoxins
Patents NumberUS5585089
Date of Issue17/12/93
Date of Expiry17/12/13
Drug InteractionBelizumab, Clozapine, Denosumab, Leflunomide, Natalizumab due to adverse effects of these drugs with Gemtuzumab; Pimecrolimus, Roflumilast, Sipuleucel-T, Tacrolimus, Tofacitinib, Trastuzumab due to adverse effects of above immmunosupressants
TargetMyeloid cell surface antigen CD33, Low affinity immunoglobulin gamma Fc region receptor III-B, Complement C1r subcomponent, Complement C1q subcomponent subunit A, Complement C1q subcomponent subunit B, Complement C1q subcomponent subunit C, Low affinity immunoglobulin gamma Fc region receptor III-A, Complement C1s subcomponent, High affinity immunoglobulin gamma Fc receptor I, Low affinity immunoglobulin gamma Fc region receptor II-a, Low affinity immunoglobulin gamma Fc region receptor II-b, Low affinity immunoglobulin gamma Fc region receptor II-c
Information of corresponding available drug in the market
Brand NameMylotarg
CompanyWyeth pharmaceuticals inc
Brand DiscriptionMylotarg (gemtuzumab ozogamicin for Injection) is a chemotherapy agent composed of a recombinant humanized IgG4, kappa antibody conjugated with a cytotoxic antitumor antibiotic, calicheamicin, isolated from fermentation of a bacterium, Micromonospora echinospora subsp. calichensis.
Prescribed forMylotarg (gemtuzumab ozogamicin for injection) is indicated for the treatment of patients with CD33 positive acute myeloid leukemia
Chemical NameN.A.
Formulation5 mg of drug conjugate (protein equivalent) in an amber vial. The inactive ingredients are: dextran 40; sucrose; sodium chloride; monobasic and dibasic sodium phosphate.
Physcial AppearanceMylotarg (gemtuzumab ozogamicin for injection) is a sterile, white, preservative-free lyophilized powder
Route of AdministrationIntravenous infusion
Recommended DosageThe recommended dose of Mylotarg (gemtuzumab ozogamicin for injection) is 9 mg/m² , infused over a 2-hour period.
ContraindicationMylotarg (gemtuzumab ozogamicin for injection) is contraindicated in patients with a known hypersensitivity to gemtuzumab ozogamicin or any of its components: anti-CD33 antibody (hP67.6), calicheamicin derivatives, or inactive ingredients. Mylotarg is contraindicated in lactating mothers.
Side EffectsFever, Nausea, Chills, Vomiting, Headache,Dyspnea, Hypotension, Hypertension, Hypoxia
Useful Linkhttp://www.rxlist.com/mylotarg-drug.htm
PubMed ID12738663, 11466696, 11410481
3-D StructureTh1159 (View) or (Download)


Entry 2
(2) Primary information
ID1672
ThPP IDTh1159
Therapeutic Peptide/Protein NameGemtuzumab ozogamicin
SequenceLight Chain 1: QIVLTQSPAIMSASPGEKVTITCSASSSISYMHWF view full sequnce in fasta
Functional ClassificationIIb
Molecular Weight151000 to 153000
Chemical FormulaN.A.
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)61 (FAB fr
Half LifeN.A.
DescriptionN.A.
Indication/DiseaseN.A.
PharmacodynamicsN.A.
Mechanism of ActionN.A.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesN.A.
Patents NumberUS5773001
Date of Issue30/06/95
Date of Expiry30/06/15
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 ID12738663, 11466696, 11410481
3-D StructureTh1159 (View) or (Download)