==== 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.====

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Th1178 details
Primary information
ID1738
ThPP IDTh1178
Therapeutic Peptide/Protein NameElotuzumab
SequenceAPQPPNILLLLMDDMGWGDLGVYGEPSRETPLCSPSRAALLTGRLPIRNG view full sequnce in fasta
Functional ClassificationIIIc
Molecular Weight148100
Chemical FormulaC6476H9982N1714O2016S42
Isoelectric PointNA
HydrophobicityNA
Melting Point (℃)NA
Half LifeNA
DescriptionElotuzumab is a humanized IgG1 (Immunoglobulin G) monoclonal antibody indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received one to three prior therapies. Elotuzumab targets SLAMF7, also known as Signaling Lymphocytic Activation Molecule Family member 7, a cell surface glycoprotein. Elotuzumab consists of the complementary determining regions (CDR) of the mouse antibody, MuLuc63, grafted onto human IgG1 heavy and kappa light chain frameworks. Elotuzumab is produced in NS0 cells by recombinant DNA technology. Elotuzumab has a theoretical mass of 148.1 kDa for the intact antibody. Elotuzumab was approved on November 30, 2015 by the U.S. Food and Drug Administration. Elotuzumab is marketed under the brand Emplicitiâ„¢ by Bristol-Myers Squibb.
Indication/DiseaseIndicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received one to three prior therapies.
PharmacodynamicsIt does not prolong the QT interval to any clinically relevant extent in combination with lenalidomide and dexamethasone at the recommended dose or as monotherapy (at a dose 2 times the recommended dose).
Mechanism of ActionElotuzumab is a humanized IgG1 monoclonal antibody that specifically targets the SLAMF7 (Signaling Lymphocytic Activation Molecule Family member 7) protein. SLAMF7 is expressed on myeloma cells independent of cytogenetic abnormalities. SLAMF7 is also expressed on Natural Killer cells, plasma cells, and at lower levels on specific immune cell subsets of differentiated cells within the hematopoietic lineage. Elotuzumab directly activates Natural Killer cells through both the SLAMF7 pathway and Fc receptors. Elotuzumab also targets SLAMF7 on myeloma cells and facilitates the interaction with Natural Killer cells to mediate the killing of myeloma cells through antibody-dependent cellular cytotoxicity (ADCC). In preclinical models, the combination of elotuzumab and lenalidomide resulted in enhanced activation of Natural Killer cells that was greater than the effects of either agent alone and increased anti-tumor activity in vitro and in vivo.
ToxicityNA
MetabolismNA
AbsorptionNA
Volume of DistributionNA
ClearanceThe clearance of elotuzumab decreased from a geometric mean (CV%) of 17.5 (21.2%) to 5.8 (31%) mL/day/kg with an increase in dose from 0.5 (i.e., 0.05 times the recommended dosage) to 20 mg/kg (i.e., 2 times the recommended dosage). Based on a population PK model, when elotuzumab is given in combination with lenalidomide and dexamethasone, approximately 97% of the maximum steady-state concentration is predicted to be eliminated with a geometric mean (CV%) of 82.4 (48%) days.
CategoriesNA
Patents NumberUS2014055370
Date of Issue01/10/12
Date of Expiry01/10/32
Drug InteractionNA
TargetSLAM family member 7
Information of corresponding available drug in the market
Brand NameNA
CompanyNA
Brand DiscriptionNA
Prescribed forNA
Chemical NameNA
Formulation300 mg/1; 400 mg/1
Physcial Appearanceinjection, powder, lyophilized, for solution
Route of AdministrationIV
Recommended DosageNA
ContraindicationNA
Side EffectsNA
Useful Link
PubMed ID28259300, 27195659, 26651519, 26362528, 23254906, 27363832, 27195659, 26445358, 26362528
3-D StructureTh1178 Heavy chianor (Download)Th1178 Light chian (View) or (Download)
Primary information
ID1739
ThPP IDTh1178
Therapeutic Peptide/Protein NameElotuzumab
SequenceAPQPPNILLLLMDDMGWGDLGVYGEPSRETPLCSPSRAALLTGRLPIRNG view full sequnce in fasta
Functional ClassificationIIIc
Molecular Weight148100
Chemical FormulaC6476H9982N1714O2016S43
Isoelectric PointNA
HydrophobicityNA
Melting Point (℃)NA
Half LifeNA
DescriptionElotuzumab is a humanized IgG1 (Immunoglobulin G) monoclonal antibody indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received one to three prior therapies. Elotuzumab targets SLAMF7, also known as Signaling Lymphocytic Activation Molecule Family member 7, a cell surface glycoprotein. Elotuzumab consists of the complementary determining regions (CDR) of the mouse antibody, MuLuc63, grafted onto human IgG1 heavy and kappa light chain frameworks. Elotuzumab is produced in NS0 cells by recombinant DNA technology. Elotuzumab has a theoretical mass of 148.1 kDa for the intact antibody. Elotuzumab was approved on November 30, 2015 by the U.S. Food and Drug Administration. Elotuzumab is marketed under the brand Emplicitiâ„¢ by Bristol-Myers Squibb.
Indication/DiseaseIndicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received one to three prior therapies.
PharmacodynamicsIt does not prolong the QT interval to any clinically relevant extent in combination with lenalidomide and dexamethasone at the recommended dose or as monotherapy (at a dose 2 times the recommended dose).
Mechanism of ActionElotuzumab is a humanized IgG1 monoclonal antibody that specifically targets the SLAMF7 (Signaling Lymphocytic Activation Molecule Family member 7) protein. SLAMF7 is expressed on myeloma cells independent of cytogenetic abnormalities. SLAMF7 is also expressed on Natural Killer cells, plasma cells, and at lower levels on specific immune cell subsets of differentiated cells within the hematopoietic lineage. Elotuzumab directly activates Natural Killer cells through both the SLAMF7 pathway and Fc receptors. Elotuzumab also targets SLAMF7 on myeloma cells and facilitates the interaction with Natural Killer cells to mediate the killing of myeloma cells through antibody-dependent cellular cytotoxicity (ADCC). In preclinical models, the combination of elotuzumab and lenalidomide resulted in enhanced activation of Natural Killer cells that was greater than the effects of either agent alone and increased anti-tumor activity in vitro and in vivo.
ToxicityNA
MetabolismNA
AbsorptionNA
Volume of DistributionNA
ClearanceThe clearance of elotuzumab decreased from a geometric mean (CV%) of 17.5 (21.2%) to 5.8 (31%) mL/day/kg with an increase in dose from 0.5 (i.e., 0.05 times the recommended dosage) to 20 mg/kg (i.e., 2 times the recommended dosage). Based on a population PK model, when elotuzumab is given in combination with lenalidomide and dexamethasone, approximately 97% of the maximum steady-state concentration is predicted to be eliminated with a geometric mean (CV%) of 82.4 (48%) days.
CategoriesNA
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetSLAM family member 8
Information of corresponding available drug in the market
Brand NameEmpliciti
CompanyE.R. Squibb & Sons, L.L.C.
Brand DiscriptionEMPLICITI (elotuzumab) is a sterile, nonpyrogenic, preservative-free lyophilized powder that is white to off-white, whole or fragmented cake in single-dose vials. EMPLICITI for Injection is supplied as 300 mg per vial and 400 mg per vial and requires reconstitution with Sterile Water for Injection, USP (13 mL and 17 mL, respectively) to obtain a solution with a concentration of 25 mg/mL. After reconstitution, each vial contains overfill to allow for withdrawal of 12 mL (300 mg) and 16 mL (400 mg). The reconstituted solution is colorless to slightly yellow, clear to slightly opalescent. Prior to intravenous infusion, the reconstituted solution is diluted with 230 mL of either 0.9% Sodium Chloride Injection, USP or 5% Dextrose Injection, USP
Prescribed forEMPLICITI is indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received one to three prior therapies.
Chemical NameNA
Formulation300 mg/1
Physcial AppearancePowder lyophilized for solution
Route of AdministrationIV
Recommended DosageThe recommended dosage of EMPLICITI is 10 mg/kg administered intravenously every week for the first two cycles and every 2 weeks thereafter in conjunction with the recommended dosing of lenalidomide and low-dose dexamethasone as described below.
ContraindicationThere are no contraindications to EMPLICITI. Because EMPLICITI is indicated for use in combination with lenalidomide and dexamethasone, healthcare providers should consult the prescribing information of these products for a complete description of contraindications before starting therapy.
Side EffectsInfusion reaction; Infections; Second Primary Malignancies; Hepatotoxicity; Interference with determination of complete response
Useful Linkhttp://www.rxlist.com/empliciti-drug.htm
PubMed ID28259300, 27195659, 26651519, 26362528, 23254906, 27363832, 27195659, 26445358, 26362528
3-D StructureTh1178 Heavy chianor (Download)Th1178 Light chian (View) or (Download)
Primary information
ID1740
ThPP IDTh1178
Therapeutic Peptide/Protein NameElotuzumab
SequenceAPQPPNILLLLMDDMGWGDLGVYGEPSRETPLCSPSRAALLTGRLPIRNG view full sequnce in fasta
Functional ClassificationIIIc
Molecular Weight148100
Chemical FormulaC6476H9982N1714O2016S44
Isoelectric PointNA
HydrophobicityNA
Melting Point (℃)NA
Half LifeNA
DescriptionElotuzumab is a humanized IgG1 (Immunoglobulin G) monoclonal antibody indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received one to three prior therapies. Elotuzumab targets SLAMF7, also known as Signaling Lymphocytic Activation Molecule Family member 7, a cell surface glycoprotein. Elotuzumab consists of the complementary determining regions (CDR) of the mouse antibody, MuLuc63, grafted onto human IgG1 heavy and kappa light chain frameworks. Elotuzumab is produced in NS0 cells by recombinant DNA technology. Elotuzumab has a theoretical mass of 148.1 kDa for the intact antibody. Elotuzumab was approved on November 30, 2015 by the U.S. Food and Drug Administration. Elotuzumab is marketed under the brand Emplicitiâ„¢ by Bristol-Myers Squibb.
Indication/DiseaseIndicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received one to three prior therapies.
PharmacodynamicsIt does not prolong the QT interval to any clinically relevant extent in combination with lenalidomide and dexamethasone at the recommended dose or as monotherapy (at a dose 2 times the recommended dose).
Mechanism of ActionElotuzumab is a humanized IgG1 monoclonal antibody that specifically targets the SLAMF7 (Signaling Lymphocytic Activation Molecule Family member 7) protein. SLAMF7 is expressed on myeloma cells independent of cytogenetic abnormalities. SLAMF7 is also expressed on Natural Killer cells, plasma cells, and at lower levels on specific immune cell subsets of differentiated cells within the hematopoietic lineage. Elotuzumab directly activates Natural Killer cells through both the SLAMF7 pathway and Fc receptors. Elotuzumab also targets SLAMF7 on myeloma cells and facilitates the interaction with Natural Killer cells to mediate the killing of myeloma cells through antibody-dependent cellular cytotoxicity (ADCC). In preclinical models, the combination of elotuzumab and lenalidomide resulted in enhanced activation of Natural Killer cells that was greater than the effects of either agent alone and increased anti-tumor activity in vitro and in vivo.
ToxicityNA
MetabolismNA
AbsorptionNA
Volume of DistributionNA
ClearanceThe clearance of elotuzumab decreased from a geometric mean (CV%) of 17.5 (21.2%) to 5.8 (31%) mL/day/kg with an increase in dose from 0.5 (i.e., 0.05 times the recommended dosage) to 20 mg/kg (i.e., 2 times the recommended dosage). Based on a population PK model, when elotuzumab is given in combination with lenalidomide and dexamethasone, approximately 97% of the maximum steady-state concentration is predicted to be eliminated with a geometric mean (CV%) of 82.4 (48%) days.
CategoriesNA
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetSLAM family member 9
Information of corresponding available drug in the market
Brand NameEmpliciti
CompanyE.R. Squibb & Sons, L.L.C.
Brand DiscriptionEMPLICITI (elotuzumab) is a sterile, nonpyrogenic, preservative-free lyophilized powder that is white to off-white, whole or fragmented cake in single-dose vials. EMPLICITI for Injection is supplied as 300 mg per vial and 400 mg per vial and requires reconstitution with Sterile Water for Injection, USP (13 mL and 17 mL, respectively) to obtain a solution with a concentration of 25 mg/mL. After reconstitution, each vial contains overfill to allow for withdrawal of 12 mL (300 mg) and 16 mL (400 mg). The reconstituted solution is colorless to slightly yellow, clear to slightly opalescent. Prior to intravenous infusion, the reconstituted solution is diluted with 230 mL of either 0.9% Sodium Chloride Injection, USP or 5% Dextrose Injection, USP
Prescribed forEMPLICITI is indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received one to three prior therapies.
Chemical NameNA
Formulation400 mg/1
Physcial AppearancePowder lyophilized for solution
Route of AdministrationIV
Recommended DosageThe recommended dosage of EMPLICITI is 10 mg/kg administered intravenously every week for the first two cycles and every 2 weeks thereafter in conjunction with the recommended dosing of lenalidomide and low-dose dexamethasone as described below.
ContraindicationThere are no contraindications to EMPLICITI. Because EMPLICITI is indicated for use in combination with lenalidomide and dexamethasone, healthcare providers should consult the prescribing information of these products for a complete description of contraindications before starting therapy.
Side EffectsInfusion reaction; Infections; Second Primary Malignancies; Hepatotoxicity; Interference with determination of complete response
Useful Linkhttp://www.rxlist.com/empliciti-drug.htm
PubMed ID28259300, 27195659, 26651519, 26362528, 23254906, 27363832, 27195659, 26445358, 26362528
3-D StructureTh1178 Heavy chianor (Download)Th1178 Light chian (View) or (Download)