Elranatamab
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Identification
- Summary
Elranatamab is a bispecific antibody used to treat adults with relapsed or refractory multiple myeloma.
- Brand Names
- Elrexfio
- Generic Name
- Elranatamab
- DrugBank Accession Number
- DB15395
- Background
Elranatamab is a bispecific B-cell maturation antigen (BCMA)-directed CD3 T-cell engager. It is a humanized immunoglobulin 2-alanine kappa antibody derived from two monoclonal antibodies (mAbs), an anti-BCMA mAb and an anti-CD3 mAb,1 each of which contributes one heavy chain and one light chain to drug structure. The resulting 4-chain bispecific antibody is covalently linked via five inter-chain disulfide bonds.4 On August 14, 2023, the FDA granted accelerated approval to elranatamab for the treatment of multiple myeloma.5 Elranatamab was also approved by the European Commission on December 8, 2023.7
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Chemical Formula
- C6440H9958N1738O2010S49
- Protein Average Weight
- 148500.0 Da (approximate)
- Sequences
>Elranatamab heavy chain 1 EVQLVESGGGLVQPGGSLRLSCAASGFTFSDYYMTWVRQAPGKGLEWVAFIRNRARGYTS DHNPSVKGRFTISRDNAKNSLYLQMNSLRAEDTAVYYCARDRPSYYVLDYWGQGTTVTVS SASTKGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQS SGLYSLSSVVTVPSSNFGTQTYTCNVDHKPSNTKVDKTVERKCRVRCPRCPAPPVAGPSV FLFPPKPKDTLMISRTPEVTCVVVAVSHEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTF RVVSVLTVVHQDWLNGKEYKCKVSNKGLPSSIEKTISKTKGQPREPQVYTLPPSREEMTK NQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPMLDSDGSFFLYSRLTVDKSRWQQG NVFSCSVMHEALHNHYTQKSLSLSPGK
>Elranatamab heavy chain 2 EVQLLESGGGLVQPGGSLRLSCAASGFTFSSYPMSWVRQAPGKGLEWVSAIGGSGGSLPY ADIVKGRFTISRDNSKNTLYLQMNSLRAEDTAVYYCARYWPMDIWGQGTLVTVSSASTKG PSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSL SSVVTVPSSNFGTQTYTCNVDHKPSNTKVDKTVERKCEVECPECPAPPVAGPSVFLFPPK PKDTLMISRTPEVTCVVVAVSHEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTFRVVSVL TVVHQDWLNGKEYKCKVSNKGLPSSIEKTISKTKGQPREPQVYTLPPSREEMTKNQVSLT CEVKGFYPSDIAVEWESNGQPENNYKTTPPMLDSDGSFFLYSKLTVDKSRWQQGNVFSCS VMHEALHNHYTQKSLSLSPGK
>Elranatamab light chain 1 DIVMTQSPDSLAVSLGERATINCKSSQSLFNVRSRKNYLAWYQQKPGQPPKLLISWASTR ESGVPDRFSGSGSGTDFTLTISSLQAEDVAVYYCKQSYDLFTFGSGTKLEIKRTVAAPSV FIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSL SSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
>Elranatamab light chain 2 EIVLTQSPGTLSLSPGERATLSCRASQSVSSSYLAWYQQKPGQAPRLLMYDASIRATGIP DRFSGSGSGTDFTLTISRLEPEDFAVYYCQQYQSWPLTFGQGTKVEIKRTVAAPSVFIFP PSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTL TLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA FormatReferences:
- KEGG DRUG: Elranatamab [Link]
- Synonyms
- ANTI-CD3/ANTI-BCMA BISPECIFIC MONOCLONAL ANTIBODY PF-06863135
- B-CELL MATURATION ANTIGEN (BCMA) CLUSTER OF DIFFERENTIATION 3 (CD3) BISPECIFIC MONOCLONAL ANTIBODY (MAB) ANTI-BCMA/ANTI-CD3 BISPECIFIC MAB
- IMMUNOGLOBULIN G2 (224-ARGININE,265-ALANINE,330-SERINE,331-SERINE), ANTI-(HUMAN CD3 ANTIGEN .EPSILON.-CHAIN) (HUMAN-MUS MUSCULUS MONOCLONAL PF-06863059 .GAMMA.2-CHAIN), DISULFIDE WITH HUMAN-MUS MUSCULUS MONOCLONAL PF-06863059 .KAPPA.-CHAIN, (223->217')(2
- IMMUNOGLOBULIN G2-KAPPA, ANTI-(HOMO SAPIENS T-CELL SURFACE GLYCOPROTEIN CD3 EPSILON CHAIN CD3E (T-CELL SURFACE ANTIGEN T3/LEU-4 EPSILON CHAIN)), HUMAN-MUS MUSCULUS MONOCLONAL DISULFIDE WITH IMMUNOGLOBULIN G2-KAPPA, ANTI-(HOMO SAPIENS-TUMOR NECROSIS FACTO
- External IDs
- PF-06863135
- RN 613
- RN-613
- RN613
Pharmacology
- Indication
Elranatamab is indicated for the treatment of adult patients with relapsed or refractory multiple myeloma. In the US, it is approved in patients who have received at least four prior lines of therapy, including a proteasome inhibitor, an immunomodulatory agent, and an anti-CD38 monoclonal antibody.4 In Europe, it is approved in patients who received at least three prior therapies.6
In the US, elranatamab is approved under accelerated approval based on response rate and durability of response. Continued approval for this indication may be contingent upon verification of clinical benefit in a confirmatory trial(s).4
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 Treatment of Refractory multiple myeloma •••••••••••• ••••• •••••••• ••••••••• •••••••••• •••••••• •••••••••• •••••••• •• ••••• ••••• ••••• ••••• •• •••••••• •••••••• •••••••• •••••••••• ••••••••• •••••••••• •••••••• •••••••••••••••• ••••• ••••••••• Treatment of Refractory multiple myeloma •••••••••••• ••••• •••••••• •••••••••••••••• ••••• •••••••••• •••••••• ••••••••• •••••••••• •••••••• •••••••••• •• ••••• •••• ••••• ••••• •• •••••••• •••••••• •••••••••• ••••••••• ••••••••• Treatment of Relapsed multiple myeloma •••••••••••• ••••• •••••••• •••••••••••••••• ••••• •••••••••• •••••••• •• ••••• ••••• ••••• ••••• •• •••••••• •••••••• •••••••• •••••••••• ••••••••• •••••••••• •••••••• ••••••••• •••••••••• •••••••• ••••••••• Treatment of Relapsed multiple myeloma •••••••••••• ••••• •• ••••• •••• ••••• ••••• •• •••••••• •••••••• •••••••••• ••••••••• •••••••••• •••••••• ••••••••• •••••••••• •••••••• •••••••••• •••••••• •••••••••••••••• ••••• ••••••••• - Contraindications & Blackbox Warnings
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- Pharmacodynamics
Elranatamab works to prevent multiple myeloma tumour growth. It causes a transient elevation of circulating cytokines IL-2, IL-6, IL-8, IL-10, TNF-α, and IFN-γ.4
- Mechanism of action
BCMA is a B cell maturation antigen that binds several ligands to activate various survival signalling pathways, including NF-kappa B, STAT3, ERK1/2, and AKT/PI3K signalling pathways. It is often overexpressed in malignant plasma B cells, including multiple myeloma cells, making it a promising therapeutic target for T-cell engaging antibodies.3 Elranatamab is a bispecific B-cell maturation antigen (BCMA)-directed T-cell engaging antibody.1,2 It binds BCMA on plasma cells, plasmablasts, and multiple myeloma cells and CD3 on T-cells leading to cytolysis of the BCMA-expressing cells. Elranatamab activated T-cells, caused pro-inflammatory cytokine release, and resulted in multiple myeloma cell lysis.4
Target Actions Organism UTumor necrosis factor receptor superfamily member 17 antibodyHumans UT-cell surface glycoprotein CD3 antibodyHumans - Absorption
Elranatamab exhibits dose-proportional pharmacokinetics over the dose range of 6 to 76 mg, which is 0.079 to 1 times the approved recommended dosage. In subjects who received a weekly dosing of 76 mg over 24 weeks, the maximum concentration of 33.6 mcg/mL was achieved at the end of the weekly dosing regimen. The mean (coefficient of variation [CV]%) Cmax was 3.8 (94%) mcg/mL at the first full 76 mg dose. At 24 weeks and steady-state, the Cmax was 33.6 (48%) mcg/mL and 20.1 (55%) mcg/mL.4
Following subcutaneous administration, the mean bioavailability of elranatamab was 56.2%. The Tmax ranged from three to seven days.
- Volume of distribution
The mean (CV%) steady-state volume of distribution of elranatamab was 7.76 L (33%).4
- Protein binding
Not Available
- Metabolism
Elranatamab is expected to be metabolized into small peptides by catabolic pathways.4
- Route of elimination
Not Available
- Half-life
The mean (CV%) half-life of elranatamab is 22 (64%) days at a dose of 76 mg.4
- Clearance
The mean (CV%) clearance is 0.324 L/day (100%) following 24 weeks dosing.4
- Adverse Effects
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- Toxicity
There is no information available regarding the acute toxicity and overdose of elranatamab.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- 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.Not Available
- 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 Elrexfio Injection, solution 44 mg/1.1mL Subcutaneous Pfizer Laboratories Div Pfizer Inc 2023-08-15 Not applicable US Elrexfio Injection, solution 40 mg/ml Subcutaneous Pfizer Europe Ma Eeig 2024-07-10 Not applicable EU Elrexfio Injection, solution 44 mg/1.1mL Subcutaneous U.S. Pharmaceuticals 2023-08-15 Not applicable US Elrexfio Solution 76 mg / 1.9 mL Subcutaneous Pfizer Canada Ulc 2024-01-23 Not applicable Canada Elrexfio Injection, solution 76 mg/1.9mL Subcutaneous Pfizer Laboratories Div Pfizer Inc 2023-08-15 Not applicable US
Categories
- Drug Categories
- 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
- Not Available
Chemical Identifiers
- UNII
- L0HR9A577V
- CAS number
- 2408850-14-4
References
- General References
- Grosicki S, Bednarczyk M, Kociszewska K: Elranatamab: a new promising BispAb in multiple myeloma treatment. Expert Rev Anticancer Ther. 2023 Jul 20:1-8. doi: 10.1080/14737140.2023.2236303. [Article]
- Lesokhin AM, Tomasson MH, Arnulf B, Bahlis NJ, Miles Prince H, Niesvizky R, Rodriotaguez-Otero P, Martinez-Lopez J, Koehne G, Touzeau C, Jethava Y, Quach H, Depaus J, Yokoyama H, Gabayan AE, Stevens DA, Nooka AK, Manier S, Raje N, Iida S, Raab MS, Searle E, Leip E, Sullivan ST, Conte U, Elmeliegy M, Czibere A, Viqueira A, Mohty M: Elranatamab in relapsed or refractory multiple myeloma: phase 2 MagnetisMM-3 trial results. Nat Med. 2023 Aug 15. doi: 10.1038/s41591-023-02528-9. [Article]
- Wu L, Huang Y, Sienkiewicz J, Sun J, Guiang L, Li F, Yang L, Golubovskaya V: Bispecific BCMA-CD3 Antibodies Block Multiple Myeloma Tumor Growth. Cancers (Basel). 2022 May 20;14(10). pii: cancers14102518. doi: 10.3390/cancers14102518. [Article]
- FDA Approved Drug Products: ELREXFIO (elranatamab-bcmm) injection, for subcutaneous use [Link]
- FDA: FDA grants accelerated approval to elranatamab-bcmm for multiple myeloma [Link]
- EMA Approved Drug Products: LREXFIO (elranatamab) Subcutaneous Injection [Link]
- Pfizer: European Commission Approves Pfizer’s ELREXFIO® for Relapsed and Refractory Multiple Myeloma [Link]
- External Links
- 2644880
- Wikipedia
- Elranatamab
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available Multiple Myeloma (MM) 3 somestatus stop reason just information to hide Not Available No Longer Available Not Available Multiple Myeloma (MM) 1 somestatus stop reason just information to hide Not Available Not Yet Recruiting Not Available Multiple Myeloma (MM) 1 somestatus stop reason just information to hide Not Available Temporarily Not Available Not Available Multiple Myeloma (MM) 1 somestatus stop reason just information to hide 4 Recruiting Treatment Multiple Myeloma (MM) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Subcutaneous 40 mg/ml Injection, solution Subcutaneous 44 mg/1.1mL Injection, solution Subcutaneous 76 mg/1.9mL Solution Subcutaneous 44 mg / 1.1 mL Solution Subcutaneous 76 mg / 1.9 mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antibody
- General Function
- Receptor for TNFSF13B/BLyS/BAFF and TNFSF13/APRIL. Promotes B-cell survival and plays a role in the regulation of humoral immunity. Activates NF-kappa-B and JNK.
- Specific Function
- signaling receptor activity
- Gene Name
- TNFRSF17
- Uniprot ID
- Q02223
- Uniprot Name
- Tumor necrosis factor receptor superfamily member 17
- Molecular Weight
- 20165.065 Da
References
- FDA Approved Drug Products: ELREXFIO (elranatamab-bcmm) injection, for subcutaneous use [Link]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antibody
- General Function
- Part of the TCR-CD3 complex present on T-lymphocyte cell surface that plays an essential role in adaptive immune response. When antigen presenting cells (APCs) activate T-cell receptor (TCR), TCR-mediated signals are transmitted across the cell membrane by the CD3 chains CD3D, CD3E, CD3G and CD3Z. All CD3 chains contain immunoreceptor tyrosine-based activation motifs (ITAMs) in their cytoplasmic domain. Upon TCR engagement, these motifs become phosphorylated by Src family protein tyrosine kinases LCK and FYN, resulting in the activation of downstream signaling pathways (PubMed:2470098). In addition of this role of signal transduction in T-cell activation, CD3D plays an essential role in thymocyte differentiation. Indeed, participates in correct intracellular TCR-CD3 complex assembly and surface expression. In absence of a functional TCR-CD3 complex, thymocytes are unable to differentiate properly. Interacts with CD4 and CD8 and thus serves to establish a functional link between the TCR and coreceptors CD4 and CD8, which is needed for activation and positive selection of CD4 or CD8 T-cells (PubMed:12215456).
- Specific Function
- identical protein binding
Components:
References
- FDA Approved Drug Products: ELREXFIO (elranatamab-bcmm) injection, for subcutaneous use [Link]
Drug created at May 20, 2019 15:24 / Updated at April 10, 2024 17:34