Identification

Name

Blinatumomab

Accession Number

DB09052

Description

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

Not Available

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).

Associated Conditions

• Precursor B-Lymphoblastic Lymphoma/Leukaemia Refractory
• Relapsed B cell precursor Acute lymphoblastic leukemia

Contraindications & Blackbox Warnings

Learn about our commercial Contraindications & Blackbox Warnings data.

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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

Learn about our commercial Adverse Effects data.

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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).

Affected organisms

• Humans and other mammals

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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
Unlock Additional Data
Abatacept	The risk or severity of adverse effects can be increased when Abatacept is combined with Blinatumomab.
Abciximab	The risk or severity of adverse effects 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.
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.
Alirocumab	The risk or severity of adverse effects can be increased when Blinatumomab is combined with Alirocumab.

Additional Data Available

Extended Description
Extended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
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Severity
Severity
A severity rating for each drug interaction, from minor to major.
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Evidence Level
Evidence Level
A rating for the strength of the evidence supporting each drug interaction.
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Action
Action
An effect category for each drug interaction. Know how this interaction affects the subject drug.
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Food Interactions

Not Available

Products

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Unlock Additional Data
Blincyto	Kit	12.5 ug/1mL	Intravenous	AMGEN INC	2014-12-18	Not applicable
Blincyto	Powder, for solution	38.5 mcg	Intravenous	Amgen	2016-03-17	Not applicable

Additional Data Available

Application Number
Application Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
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Product Code
Product Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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Categories

ATC Codes

L01XC19 — Blinatumomab

• L01XC — Monoclonal antibodies
• L01X — OTHER ANTINEOPLASTIC AGENTS
• L01 — ANTINEOPLASTIC AGENTS
• L — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Drug Categories

• Amides
• Amino Acids, Peptides, and Proteins
• Antibodies
• Antibodies, Monoclonal
• Antineoplastic Agents
• Antineoplastic and Immunomodulating Agents
• Bispecific CD19-directed CD3-directed T Cell Engager
• Blood Proteins
• CD19-directed Antibody Interactions
• CD3 Receptor Agonists
• CD3-directed Antibody Interactions
• Globulins
• Immunoglobulins
• Immunoproteins
• Immunosuppressive Agents
• Monoterpenes
• Myelosuppressive Agents
• Narrow Therapeutic Index Drugs
• Norbornanes
• Proteins
• Serum Globulins
• Sulfones
• Sulfur Compounds
• Terpenes

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

Chemical Identifiers

UNII

4FR53SIF3A

CAS number

853426-35-4

References

General References

1. 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. [PubMed:25883042]
2. Garber K: Bispecific antibodies rise again. Nat Rev Drug Discov. 2014 Nov;13(11):799-801. doi: 10.1038/nrd4478. [PubMed:25359367]

External Links

KEGG Drug

D09325

PubChem Substance

347910400

RxNav

1597258

ChEMBL

CHEMBL1742992

Drugs.com

Drugs.com Drug Page

Wikipedia

Blinatumomab

AHFS Codes

• 10:00.00 — Antineoplastic Agents

FDA label

Download (242 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Not Yet Recruiting	Treatment	B-precursor Acute Lymphoblastic Leukemia	1
3	Active Not Recruiting	Treatment	Acute Lymphoblastic Leukaemias (ALL)	2
3	Active Not Recruiting	Treatment	Acute Lymphoblastic Leukaemias (ALL) / B Acute Lymphoblastic Leukemia, Philadelphia Chromosome Negative	1
3	Active Not Recruiting	Treatment	Recurrent B Acute Lymphoblastic Leukemia	1
3	Not Yet Recruiting	Treatment	B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1	1
3	Recruiting	Treatment	Acute Lymphoblastic Leukemia, Pediatric	1
3	Recruiting	Treatment	B Acute Lymphoblastic Leukemia / B Lymphoblastic Lymphoma / Down Syndrome (DS)	1
3	Terminated	Treatment	Adult Subjects With Relapsed/Refractory B-precursor Acute Lymphoblastic Leukemia / Relapsed/Refractory B-precursor Acute Lymphoblastic Leukemia	1
3	Withdrawn	Treatment	Acute Lymphoblastic Leukaemias (ALL)	1
2	Active Not Recruiting	Treatment	Acute Lymphoblastic Leukaemias (ALL)	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

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

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
Unlock Additional Data
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

Additional Data Available

Filed On
Filed On
The date on which a patent was filed with the relevant government.
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Properties

State

Solid

Experimental Properties

Not Available

×

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There is additional data available for commercial users including Adverse Effects, Contraindications, and Blackbox Warnings. Contact us to learn more about these and other features.

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Drug created on May 06, 2015 16:29 / Updated on September 25, 2020 15:13