Blinatumomab

Identification

Summary

Blinatumomab is an antineoplastic antibody used to treat Philadelphia chromosome-negative relapsed or refractory B-cell precursor acute lymphoblastic leukemia (ALL).

Brand Names

Blincyto

Generic Name

Blinatumomab

DrugBank Accession Number

DB09052

Background

Blinatumomab is a BiTE-class (bi-specific T-cell engagers) constructed monoclonal antibody indicated for the treatment of Philadelphia chromosome-negative relapsed or refractory B-cell precursor acute lymphoblastic leukemia (ALL). Blinatumomab is manufactured by Amgen Inc. and marketed under the brand Blincyto™. A full treatment regimen consisting of two cycles of four weeks each, is priced at $178 000 USD. Blinatumomab was approved in December 2014 under the FDA’s accelerated approval program, which allows approval of a drug to treat a serious or life-threatening disease based on clinical data showing the drug has an effect on a surrogate endpoint reasonably likely to predict clinical benefit to patients.

Type

Biotech

Groups

Approved, Investigational

Biologic Classification

Protein Based Therapies
Monoclonal antibody (mAb)

Protein Structure

Protein Chemical Formula: C₂₃₆₇H₃₅₇₇N₆₄₉O₇₇₂S₁₉
Protein Average Weight: 54100.0 Da

Sequences

>single chain variable fragment fusion protein 
DIQLTQSPASLAVSLGQRATISCKASQSVDYDGDSYLNWYQQIPGQPPKLLIYDASNLVS
GIPPRFSGSGSGTDFTLNIHPVEKVDAATYHCQQSTEDPWTFGGGTKLEIKGGGGSGGGG
SGGGGSQVQLQQSGAELVRPGSSVKISCKASGYAFSSYWMNWVKQRPGQGLEWIGQIWPG
DGDTNYNGKFKGKATLTADESSSTAYMQLSSLASEDSAVYFCARRETTTVGRYYYAMDYW
GQGTTVTVSSGGGGSDIKLQQSGAELARPGASVKMSCKTSGYTFTRYTMHWVKQRPGQGL
EWIGYINPSRGYTNYNQKFKDKATLTTDKSSSTAYMQLSSLTSEDSAVYYCARYYDDHYC
LDYWGQGTTLTVSSVEGGSGGSGGSGGSGGVDDIQLTQSPAIMSASPGEKVTMTCRASSS
VSYMNWYQQKSGTSPKRWIYDTSKVASGVPYRFSGSGSGTSYSLTISSMEAEDAATYYCQ
QWSSNPLTFGAGTKLELKHHHHHH

Download FASTA Format

Synonyms

Blinatumomab

External IDs

AMG103
MEDI 538
MEDI-538
MEDI538
MT 103
MT-103
MT103

Pharmacology

Indication

Indicated for the treatment of Philadelphia chromosome-negative relapsed or refractory B-cell precursor acute lymphoblastic leukemia (ALL).

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Associated Conditions

Contraindications & Blackbox Warnings

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Pharmacodynamics

Not Available

Mechanism of action

Blinatumomab is a bispecific CD19-directed CD3 T-cell engager that binds to CD19 expressed on the surface of cells of B-lineage origin and CD3 expressed on the surface of T cells. It activates endogenous T cells by connecting CD3 in the T-cell receptor (TCR) complex with CD19 on benign and malignant B cells. Blinatumomab mediates the formation of a synapse between the T cell and the tumor cell, upregulation of cell adhesion molecules, production of cytolytic proteins, release of inflammatory cytokines, and proliferation of T cells, which result in redirected lysis of CD19+ cells.

Target	Actions	Organism
AB-lymphocyte antigen CD19	activator	Humans
AT-cell surface glycoprotein CD3 delta chain	activator	Humans

Absorption

Not Available

Volume of distribution

4.52 L, standard deviation 2.89.

Protein binding

Not Available

Metabolism

The metabolic pathway of blinatumomab has not been characterized. Like other protein therapeutics, blinatumomab is expected to be degraded into small peptides and amino acids via catabolic pathways.

Route of elimination

Not Available

Half-life

2.11 hours, standard deviation 1.42.

Clearance

2.92 L/hour, standard deviation 2.83.

Adverse Effects

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Toxicity

Cytokine Release Syndrome (CRS), which may be life-threatening or fatal, occurred in patients receiving blinatumomab. Interrupt or discontinue blinatumomab as recommended.
Neurological toxicities, which may be severe, life-threatening, or fatal, occurred in patients receiving blinatumomab. Interrupt or discontinue blinatumomab as recommended.
In patients receiving blinatumomab in clinical trials, serious infections such as sepsis, pneumonia, bacteremia, opportunistic infections, and catheter-site infections were observed in approximately 25% of patients, some of which were life-threatening or fatal.
Tumor lysis syndrome (TLS), which may be life-threatening or fatal, has been observed in patients.
Neutropenia and febrile neutropenia, including life-threatening cases, have been observed in patients.
Treatment with blinatumomab was associated with transient elevations in liver enzymes.
Cranial magnetic resonance imaging (MRI) changes showing leukoencephalopathy have been observed in patients receiving blinatumomab, especially in patients with prior treatment with cranial irradiation and antileukemic chemotherapy (including systemic high-dose methotrexate or intrathecal cytarabine).

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.

Drug	Interaction
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Abatacept	The risk or severity of adverse effects can be increased when Abatacept is combined with Blinatumomab.
Abciximab	The risk or severity of bleeding can be increased when Abciximab is combined with Blinatumomab.
Acenocoumarol	The risk or severity of bleeding can be increased when Acenocoumarol is combined with Blinatumomab.
Acetylsalicylic acid	The risk or severity of bleeding can be increased when Acetylsalicylic acid is combined with Blinatumomab.
Adalimumab	The risk or severity of adverse effects can be increased when Adalimumab is combined with Blinatumomab.
Adenovirus type 7 vaccine live	The risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Blinatumomab.
Aducanumab	The risk or severity of adverse effects can be increased when Blinatumomab is combined with Aducanumab.
Aldesleukin	The risk or severity of adverse effects can be increased when Aldesleukin is combined with Blinatumomab.
Alefacept	The risk or severity of adverse effects can be increased when Alefacept is combined with Blinatumomab.
Alemtuzumab	The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Blinatumomab.

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Food Interactions

No interactions found.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Blincyto	Powder, for solution	38.5 mcg / vial	Intravenous	Amgen	2016-03-17	Not applicable
Blincyto	Solution	38.5 mcg	Intravenous	Amgen Europe B.V.	2020-12-22	Not applicable
Blincyto	Kit	12.5 ug/1mL	Intravenous	AMGEN INC	2014-12-18	Not applicable

Chemical Identifiers

UNII: 4FR53SIF3A
CAS number: 853426-35-4

References

General References

Zugmaier G, Klinger M, Schmidt M, Subklewe M: Clinical overview of anti-CD19 BiTE((R)) and ex vivo data from anti-CD33 BiTE((R)) as examples for retargeting T cells in hematologic malignancies. Mol Immunol. 2015 Oct;67(2 Pt A):58-66. doi: 10.1016/j.molimm.2015.02.033. Epub 2015 Apr 13. [Article]
Garber K: Bispecific antibodies rise again. Nat Rev Drug Discov. 2014 Nov;13(11):799-801. doi: 10.1038/nrd4478. [Article]

External Links

KEGG Drug: D09325
PubChem Substance: 347910400
RxNav: 1597258
ChEMBL: CHEMBL1742992
Drugs.com: Drugs.com Drug Page
Wikipedia: Blinatumomab

FDA label

Download (242 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Recruiting	Treatment	Precursor-B Acute Lymphoblastic Leukemia	1
3	Active Not Recruiting	Treatment	Acute Lymphoblastic Leukemia (ALL)	1
3	Active Not Recruiting	Treatment	Acute Lymphoblastic Leukemia (ALL) / B Acute Lymphoblastic Leukemia, Philadelphia Chromosome Negative	1
3	Active Not Recruiting	Treatment	Recurrent B Acute Lymphoblastic Leukemia	1
3	Completed	Treatment	Acute Lymphoblastic Leukemia (ALL)	1
3	Not Yet Recruiting	Treatment	Acute Lymphoblastic Leukemia (Philadelphia Chromosome Positive) / ALL, Adult / Philadelphia-Positive ALL	1
3	Not Yet Recruiting	Treatment	Newly Diagnosed Philadelphia (Ph)-Negative B-cell Precursor Acute Lymphoblastic Leukemia (ALL)	1
3	Recruiting	Treatment	Acute Lymphoblastic Leukemia (ALL)	1
3	Recruiting	Treatment	B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1	1
3	Recruiting	Treatment	B Acute Lymphoblastic Leukemia / B Lymphoblastic Lymphoma / Down Syndrome (DS)	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection, powder, lyophilized, for solution	Intravenous	38.5 mcg/1vial
Kit	Intravenous	12.5 ug/1mL
Powder	Intravenous; Parenteral	38.5 MICROGRAMMI
Powder, for solution	Intravenous	38.5 mcg / vial
Solution	Intravenous	38.5 mcg
Injection	Intravenous
Injection	Parenteral
Injection, powder, lyophilized, for solution	Intravenous	55 mcg/ml
Injection, powder, lyophilized, for solution	Intravenous	38.5 mcg

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US7235641	No	2007-06-26	2023-12-22
US7575923	No	2009-08-18	2018-04-21
US7635472	No	2009-12-22	2023-05-31
US8247194	No	2012-08-21	2024-05-05
US20120328618	No	2009-10-27	2029-10-27
US20130323247	No	2008-11-07	2028-11-07

Properties

State: Solid
Experimental Properties: Not Available

Targets

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Details1. B-lymphocyte antigen CD19

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Activator

General Function: Receptor signaling protein activity
Specific Function: Assembles with the antigen receptor of B-lymphocytes in order to decrease the threshold for antigen receptor-dependent stimulation.
Gene Name: CD19
Uniprot ID: P15391
Uniprot Name: B-lymphocyte antigen CD19
Molecular Weight: 61127.985 Da

References

Zugmaier G, Klinger M, Schmidt M, Subklewe M: Clinical overview of anti-CD19 BiTE((R)) and ex vivo data from anti-CD33 BiTE((R)) as examples for retargeting T cells in hematologic malignancies. Mol Immunol. 2015 Oct;67(2 Pt A):58-66. doi: 10.1016/j.molimm.2015.02.033. Epub 2015 Apr 13. [Article]

Details2. T-cell surface glycoprotein CD3 delta chain

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Activator

General Function: Transmembrane signaling receptor activity
Specific Function: The CD3 complex mediates signal transduction.
Gene Name: CD3D
Uniprot ID: P04234
Uniprot Name: T-cell surface glycoprotein CD3 delta chain
Molecular Weight: 18929.38 Da

References

Zugmaier G, Klinger M, Schmidt M, Subklewe M: Clinical overview of anti-CD19 BiTE((R)) and ex vivo data from anti-CD33 BiTE((R)) as examples for retargeting T cells in hematologic malignancies. Mol Immunol. 2015 Oct;67(2 Pt A):58-66. doi: 10.1016/j.molimm.2015.02.033. Epub 2015 Apr 13. [Article]

Drug created on May 06, 2015 22:29 / Updated on October 19, 2021 07:39

Blinatumomab

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References

References