Elotuzumab
Identification
- Summary
Elotuzumab is an antineoplastic agent and SLAMF7-directed immunostimulatory antibody used for the treatment of refractory multiple myeloma in combination with other antineoplastic agents.
- Brand Names
- Empliciti
- Generic Name
- Elotuzumab
- DrugBank Accession Number
- DB06317
- Background
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 Empliciti™ by Bristol-Myers Squibb.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Structure
- Protein Chemical Formula
- C6476H9982N1714O2016S42
- Protein Average Weight
- 148100.0 Da
- Sequences
>Elotuzumab heavy chain EVQLVESGGGLVQPGGSLRLSCAASGFDFSRYWMSWVRQAPGKGLEWIGEINPDSSTINY APSLKDKFIISRDNAKNSLYLQMNSLRAEDTAVYYCARPDGNYWYFDVWGQGTLVTVSSA STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGP SVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNS TYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDEL TKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQ QGNVFSCSVMHEALHNHYTQKSLSLSPGK
>Elotuzumab light chain DIQMTQSPSSLSASVGDRVTITCKASQDVGIAVAWYQQKPGKVPKLLIYWASTRHTGVPD RFSGSGSGTDFTLTISSLQPEDVATYYCQQYSSYPYTFGQGTKVEIKRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format- Synonyms
- Elotuzumab
- HuLuc63
- Immunoglobulin G1, anti-(human protein CS1) (human-mouse HuLuc63 heavy chain), disulfide with human-mouse HuLuc63 kappa-chain, dimer
- External IDs
- BMS-901608
- PDL 063
- PDL063
Pharmacology
- Indication
Indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received one to three prior therapies.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Refractory multiple myeloma Regimen in combination with: Dexamethasone (DB01234), Lenalidomide (DB00480) •••••••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Not Available
- 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.
Target Actions Organism ASLAM family member 7 modulatorHumans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- 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.
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Elotuzumab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Elotuzumab. Aducanumab The risk or severity of adverse effects can be increased when Elotuzumab is combined with Aducanumab. Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Elotuzumab. Alirocumab The risk or severity of adverse effects can be increased when Elotuzumab is combined with Alirocumab. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Elotuzumab Injection, powder, lyophilized, for solution 300 mg/1 Intravenous Bristol-Myers Squibb Holdings Pharma, Ltd. Liability Company 2015-11-30 2015-11-30 US Elotuzumab Injection, powder, lyophilized, for solution 300 mg/1 Intravenous Bristol-Myers Squibb Holdings Pharma, Ltd. Liability Company 2015-11-30 2015-11-30 US Empliciti Injection, powder, lyophilized, for solution 400 mg/1 Intravenous E.R. Squibb & Sons, L.L.C. 2015-11-30 Not applicable US Empliciti Injection, powder, for solution 300 mg Intravenous Bristol Myers Squibb Pharma Eeig 2016-09-08 Not applicable EU Empliciti Powder, for solution 340 mg / vial Intravenous Bristol Myers Squibb Not applicable Not applicable Canada
Categories
- ATC Codes
- L01FX08 — Elotuzumab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Blood Proteins
- Cancer immunotherapy
- Globulins
- Immunoglobulins
- Immunoproteins
- Immunotherapy
- MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
- Narrow Therapeutic Index Drugs
- Proteins
- Serum Globulins
- SLAMF7-directed Antibody Interactions
- SLAMF7-directed Immunostimulatory Antibody
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 1351PE5UGS
- CAS number
- 915296-00-3
References
- Synthesis Reference
"Patent Link":https://www.google.com/patents/WO2014055370A1?cl=en
- General References
- Hsi ED, Steinle R, Balasa B, Szmania S, Draksharapu A, Shum BP, Huseni M, Powers D, Nanisetti A, Zhang Y, Rice AG, van Abbema A, Wong M, Liu G, Zhan F, Dillon M, Chen S, Rhodes S, Fuh F, Tsurushita N, Kumar S, Vexler V, Shaughnessy JD Jr, Barlogie B, van Rhee F, Hussein M, Afar DE, Williams MB: CS1, a potential new therapeutic antibody target for the treatment of multiple myeloma. Clin Cancer Res. 2008 May 1;14(9):2775-84. doi: 10.1158/1078-0432.CCR-07-4246. [Article]
- Tai YT, Dillon M, Song W, Leiba M, Li XF, Burger P, Lee AI, Podar K, Hideshima T, Rice AG, van Abbema A, Jesaitis L, Caras I, Law D, Weller E, Xie W, Richardson P, Munshi NC, Mathiot C, Avet-Loiseau H, Afar DE, Anderson KC: Anti-CS1 humanized monoclonal antibody HuLuc63 inhibits myeloma cell adhesion and induces antibody-dependent cellular cytotoxicity in the bone marrow milieu. Blood. 2008 Aug 15;112(4):1329-37. Epub 2007 Sep 28. [Article]
- Markham A: Elotuzumab: First Global Approval. Drugs. 2016 Mar;76(3):397-403. doi: 10.1007/s40265-016-0540-0. [Article]
- External Links
- KEGG Drug
- D09337
- PubChem Substance
- 347910347
- 1726104
- ChEMBL
- CHEMBL1743010
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Elotuzumab
- FDA label
- Download (245 KB)
- MSDS
- Download (381 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 3 Active Not Recruiting Treatment Multiple Myeloma (MM) 1 3 Active Not Recruiting Treatment Newly Diagnosed Multiple Myeloma 1 3 Completed Treatment Lymphoma / Multiple Myeloma (MM) 1 3 Completed Treatment Multiple Myeloma (MM) 3 3 Not Yet Recruiting Treatment Multiple Myeloma (MM) 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, lyophilized, for solution Intravenous 300 mg/1 Injection, powder, for solution Intravenous 300 mg Injection, powder, for solution Intravenous 400 mg Injection, powder, for solution Intravenous; Parenteral 300 MG Injection, powder, for solution Intravenous; Parenteral 400 MG Injection, powder, lyophilized, for solution Intravenous 25 mg Injection, powder, lyophilized, for solution Intravenous 400 mg/1 Powder, for solution Intravenous 340 mg / vial Powder, for solution Intravenous 440 mg / vial - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US2014055370 No 2012-10-01 2032-10-01 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Modulator
- General Function
- Not Available
- Specific Function
- Self-ligand receptor of the signaling lymphocytic activation molecule (SLAM) family. SLAM receptors triggered by homo- or heterotypic cell-cell interactions are modulating the activation and differ...
- Gene Name
- SLAMF7
- Uniprot ID
- Q9NQ25
- Uniprot Name
- SLAM family member 7
- Molecular Weight
- 37420.62 Da
References
- Markham A: Elotuzumab: First Global Approval. Drugs. 2016 Mar;76(3):397-403. doi: 10.1007/s40265-016-0540-0. [Article]
Drug created at March 19, 2008 16:24 / Updated at February 20, 2024 23:54