Pegaspargase

Identification

Summary

Pegaspargase is a modified form of L-asparagine amidohydrolase used to treat acute lymphoblastic leukemia, which is dependent on an external source of asparagine.

Brand Names

Oncaspar

Generic Name

Pegaspargase

DrugBank Accession Number

DB00059

Background

Pegylated L-asparagine amidohydrolase from E. coli. Pegylation substantially (by a factor of 4) extends the protein half life.

Type

Biotech

Groups

Approved, Investigational

Biologic Classification

Protein Based Therapies
Other protein based therapies

Protein Structure

Protein Chemical Formula

C₁₃₇₇H₂₂₀₈N₃₈₂O₄₄₂S₁₇

Protein Average Weight

31731.9 Da

Sequences

>DB00059 sequence
MEFFKKTALAALVMGFSGAALALPNITILATGGTIAGGGDSATKSNYTVGKVGVENLVNA
VPQLKDIANVKGEQVVNIGSQDMNDNVWLTLAKKINTDCDKTDGFVITHGTDTMEETAYF
LDLTVKCDKPVVMVGAMRPSTSMSADGPFNLYNAVVTAADKASANRGVLVVMNDTVLDGR
DVTKTNTTDVATFKSVNYGPLGYIHNGKIDYQRTPARKHTSDTPFDVSKLNELPKVGIVY
NYANASDLPAKALVDAGYDGIVSAGVGNGNLYKSVFDTLATAAKTGTAVVRSSRVPTGAT
TQDAEVDDAKYGFVASGTLNPQKARVLLQLALTQTKDPQQIQQIFNQY

Download FASTA Format

Synonyms

• Peg-asparaginase
• Peg/L-asparaginase
• Pegaspargasa
• Pegaspargase

Pharmacology

Indication

For treatment of acute lymphoblastic leukemia

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Associated Conditions

• Acute Lymphoblastic Leukaemias (ALL)

Contraindications & Blackbox Warnings

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Pharmacodynamics

In a significant number of patients with acute leukemia, the malignant cells are dependent on an exogenous source of asparagine for survival. Normal cells, however, are able to synthesize asparagine and thus are affected less by the rapid depletion produced by treatment with the enzyme asparaginase. Oncaspar exploits a metabolic defect in asparagine synthesis of some malignant cells.

Mechanism of action

Pegaspargase, more effective than asparaginase, converts asparagine to aspartic acid and ammonia. It facilitates production of oxaloacetate which is needed for general cellular metabolism. Some malignant cells lose the ability to produce asparagine and so the loss of exogenous sources of asparagine leads to cell death.

Target	Actions	Organism
AL-asparagine	other/unknown	Humans

Absorption

Onset of Asparagine depletion by IM is within 4 days Time to peak: IM: 3 to 4 days

Volume of distribution

IV: Adults (asparaginase naive): 2.4 L/m2 Distributes into CSF (reportedly reducing CSF asparagine concentrations to a similar extent as asparaginase

Protein binding

Not Available

Metabolism

Not Available

Route of elimination

Not Available

Half-life

IM: ~6 days; half-life decreased to ~3 days (range: 1.4 to 5 days) in patients with previous hypersensitivity to native L-asparaginase; IV: Adults (asparaginase naive): 7 days

Clearance

Not Available

Adverse Effects

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Toxicity

Adverse effects that occur more than 10% of the time include hepatotoxicity as it is known to increase serum transaminases (ALT, AST). Also known to induce hypersensitivity reactions including anaphylaxis, erythema and bronchospasm.

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
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Abatacept	The risk or severity of adverse effects can be increased when Pegaspargase is combined with Abatacept.
Adalimumab	The risk or severity of adverse effects can be increased when Adalimumab is combined with Pegaspargase.
Adenovirus type 7 vaccine live	The risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Pegaspargase.
Aldesleukin	The risk or severity of adverse effects can be increased when Aldesleukin is combined with Pegaspargase.
Alefacept	The risk or severity of adverse effects can be increased when Pegaspargase is combined with Alefacept.
Alemtuzumab	The risk or severity of adverse effects can be increased when Pegaspargase is combined with Alemtuzumab.
Allantoin	The therapeutic efficacy of Allantoin can be increased when used in combination with Pegaspargase.
Altretamine	The risk or severity of adverse effects can be increased when Pegaspargase is combined with Altretamine.
Amsacrine	The risk or severity of adverse effects can be increased when Pegaspargase is combined with Amsacrine.
Anakinra	The risk or severity of adverse effects can be increased when Anakinra is combined with Pegaspargase.

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Food Interactions

• Avoid excessive or chronic alcohol consumption. Alcohol and pegaspargase can both cause hepatoxicity, therefore if they are used together they may have additive hepatoxic effects.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Lyophilized Pegaspargase	Injection, powder, lyophilized, for solution	750 U/1mL	Intramuscular	Baxalta US Inc.	2018-02-07	2020-05-16
Lyophilized Pegaspargase	Injection, powder, lyophilized, for solution	750 [iU]/1mL	Intravenous	Servier Pharmaceuticals	2020-08-03	Not applicable
Oncaspar		750 U/ml		Les Laboratoires Servier	2020-12-16	Not applicable
Oncaspar	Liquid	750 unit / mL	Intramuscular; Intravenous	Aventis Pharma Ltd.	1998-10-13	2004-01-02
Oncaspar	Injection, solution	750 U/ml	Intramuscular; Intravenous	Les Laboratoires Servier	2016-09-08	Not applicable
Oncaspar	Injection, solution	750 [iU]/1mL	Intramuscular; Intravenous	Servier Pharmaceuticals LLC	2020-01-02	Not applicable
Oncaspar	Injection, solution	750 [iU]/1mL	Intramuscular; Intravenous	Sigma Tau Pharmaceuticals, Inc.	1994-02-01	2016-11-30
Oncaspar	Solution	750 unit / mL	Intramuscular; Intravenous	Servier	2017-06-01	Not applicable
Oncaspar	Injection, solution	750 [iU]/1mL	Intramuscular; Intravenous	Baxalta US Inc.	1994-02-01	2020-05-16

Categories

ATC Codes

L01XX24 — Pegaspargase

• L01XX — Other antineoplastic agents
• L01X — OTHER ANTINEOPLASTIC AGENTS
• L01 — ANTINEOPLASTIC AGENTS
• L — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Drug Categories

• Alcohols
• Amidohydrolases
• Antineoplastic Agents
• Antineoplastic and Immunomodulating Agents
• Asparaginase
• Asparagine-specific Enzyme
• Compounds used in a research, industrial, or household setting
• Delayed-Action Preparations
• Enzymes
• Enzymes and Coenzymes
• Enzymes, Immobilized
• Ethylene Glycols
• Glycols
• Hydrolases
• Immunosuppressive Agents
• Macromolecular Substances
• Pegylated agents
• Polymers
• Thyroxine-binding globulin inhibitors

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

7D96IR0PPM

CAS number

130167-69-0

References

General References

1. Graham ML: Pegaspargase: a review of clinical studies. Adv Drug Deliv Rev. 2003 Sep 26;55(10):1293-302. [Article]

External Links

UniProt

P37595

Genbank

U00096

PubChem Substance

46505366

RxNav

34132

ChEMBL

CHEMBL2108546

PharmGKB

PA164760860

RxList

RxList Drug Page

Drugs.com

Drugs.com Drug Page

Wikipedia

Pegaspargase

AHFS Codes

• 10:00.00 — Antineoplastic Agents

FDA label

Download (400 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Recruiting	Treatment	Hematological Neoplasms	1
4	Unknown Status	Treatment	Acute Lymphoblastic Leukaemias (ALL)	1
4	Unknown Status	Treatment	Nasal and Nasal-type NK/T-cell Lymphoma	1
3	Active Not Recruiting	Treatment	Acute Lymphoblastic Leukaemias (ALL)	2
3	Active Not Recruiting	Treatment	Acute Lymphoblastic Leukaemias (ALL) / Acute Undifferentiated Leukemia (AUL) / Childhood T Acute Lymphoblastic Leukemia / Untreated Childhood Acute Lymphoblastic Leukemia	1
3	Active Not Recruiting	Treatment	Acute Lymphoblastic Leukaemias (ALL) / Adult B Lymphoblastic Lymphoma / Ann Arbor Stage I B Lymphoblastic Lymphoma / Ann Arbor Stage II B Lymphoblastic Lymphoma / Childhood B Acute Lymphoblastic Leukemia / Childhood B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 / Childhood B Lymphoblastic Lymphoma / Down Syndrome (DS) / Hypodiploid B Acute Lymphoblastic Leukemia / Philadelphia Chromosome Positive	1
3	Active Not Recruiting	Treatment	Acute Lymphoblastic Leukaemias (ALL) / B Acute Lymphoblastic Leukemia, Philadelphia Chromosome Negative	1
3	Active Not Recruiting	Treatment	Adult T Acute Lymphoblastic Leukemia / Ann Arbor Stage II Adult Lymphoblastic Lymphoma / Ann Arbor Stage II Childhood Lymphoblastic Lymphoma / Ann Arbor Stage III Adult Lymphoblastic Lymphoma / Ann Arbor Stage III Childhood Lymphoblastic Lymphoma / Ann Arbor Stage IV Adult Lymphoblastic Lymphoma / Ann Arbor Stage IV Childhood Lymphoblastic Lymphoma / Childhood T Acute Lymphoblastic Leukemia	1
3	Active Not Recruiting	Treatment	B Acute Lymphoblastic Leukemia / Central Nervous System Leukemia / Ph-Like Acute Lymphoblastic Leukemia / Testicular Leukemia	1
3	Active Not Recruiting	Treatment	Extranodal NK/T-cell Lymphoma, Nasal Type	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

• Ben Venue Laboratories Inc.
• Enzon Inc.

Dosage Forms

Form	Route	Strength
Injection, powder, lyophilized, for solution	Intramuscular	750 U/1mL
Injection, powder, lyophilized, for solution	Intravenous	750 [iU]/1mL
Injection, powder, for solution	Intramuscular; Intravenous
Injection, solution	Intramuscular; Intravenous
Injection, solution	Intramuscular; Intravenous	750 [iU]/1mL
Injection, solution	Intramuscular; Intravenous	750 U/ml
Liquid	Intramuscular; Intravenous	750 unit / mL
Solution	Intramuscular; Intravenous	750 unit / mL
Solution	Intramuscular; Intravenous	750 IU

Prices

Unit description	Cost	Unit
Oncaspar 750 unit/ml vial	656.0USD	ml

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Not Available

Properties

State

Liquid

Experimental Properties

Property	Value	Source
hydrophobicity	0.059	Not Available
isoelectric point	4.67	Not Available

Targets

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Details1. L-asparagine

Kind

Small molecule

Organism

Humans

Pharmacological action

Yes

Actions

Other/unknown

References

1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
3. Douer D, Yampolsky H, Cohen LJ, Watkins K, Levine AM, Periclou AP, Avramis VI: Pharmacodynamics and safety of intravenous pegaspargase during remission induction in adults aged 55 years or younger with newly diagnosed acute lymphoblastic leukemia. Blood. 2007 Apr 1;109(7):2744-50. [Article]
4. Wetzler M, Sanford BL, Kurtzberg J, DeOliveira D, Frankel SR, Powell BL, Kolitz JE, Bloomfield CD, Larson RA: Effective asparagine depletion with pegylated asparaginase results in improved outcomes in adult acute lymphoblastic leukemia: Cancer and Leukemia Group B Study 9511. Blood. 2007 May 15;109(10):4164-7. Epub 2007 Jan 30. [Article]
5. Dinndorf PA, Gootenberg J, Cohen MH, Keegan P, Pazdur R: FDA drug approval summary: pegaspargase (oncaspar) for the first-line treatment of children with acute lymphoblastic leukemia (ALL). Oncologist. 2007 Aug;12(8):991-8. [Article]

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Drug created on June 13, 2005 13:24 / Updated on June 23, 2021 06:08