A database of FDA approved therapeutic peptides and proteins
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1738 details |
| Primary information | |
|---|---|
| ThPP ID | Th1178 |
| Therapeutic Peptide/Protein Name | Elotuzumab |
| Sequence | APQPPNILLLLMDDMGWGDLGVYGEPSRETPLCSPSRAALLTGRLPIRNG view full sequnce in fasta |
| Functional Classification | IIIc |
| Molecular Weight | 148100 |
| Chemical Formula | C6476H9982N1714O2016S42 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting Point (℃) | NA |
| Half Life | NA |
| Description | Elotuzumab 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/Disease | Indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received one to three prior therapies. |
| Pharmacodynamics | It 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 Action | Elotuzumab 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. |
| Toxicity | NA |
| Metabolism | NA |
| Absorption | NA |
| Volume of Distribution | NA |
| Clearance | The 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. |
| Categories | NA |
| Patents Number | US2014055370 |
| Date of Issue | 01/10/12 |
| Date of Expiry | 01/10/32 |
| Drug Interaction | NA |
| Target | SLAM family member 7 |
| Information of corresponding available drug in the market | |
| Brand Name | NA |
| Company | NA |
| Brand Discription | NA |
| Prescribed for | NA |
| Chemical Name | NA |
| Formulation | 300 mg/1; 400 mg/1 |
| Physcial Appearnce | injection, powder, lyophilized, for solution |
| Route of Administration | IV |
| Recommended Dosage | NA |
| Contraindication | NA |
| Side Effects | NA |
| Useful Link | |
| PubMed ID | 28259300, 27195659, 26651519, 26362528, 23254906, 27363832, 27195659, 26445358, 26362528 |
| 3-D Structure | Th1178 Heavy chianor (Download)Th1178 Light chian (View) or (Download) |