NAV

Chymopapain

Identification

Generic Name
Chymopapain
DrugBank Accession Number
DB06752
Background

Chymopapain was first isolated in 1941 from the crude latex derived from the fruit of Carica papaya by squeezing the green papaya while on the plant prior to harvest.6It is an extracellular plant cysteine proteinase similar to papain in specificity.2 Chymopapain was developed by Chart Medcl and FDA approved on November 10, 1982. It is currently discontinued.8

Type
Biotech
Groups
Approved, Withdrawn
Biologic Classification
Protein Based Therapies
Other protein based therapies
Protein Structure
Protein Chemical Formula
Not Available
Protein Average Weight
27000.0 Da
Sequences
>sp|P14080|PAPA2_CARPA Chymopapain OS=Carica papaya OX=3649 PE=1 SV=2
MATMSSISKIIFLATCLIIHMGLSSADFYTVGYSQDDLTSIERLIQLFDSWMLKHNKIYE
SIDEKIYRFEIFRDNLMYIDETNKKNNSYWLGLNGFADLSNDEFKKKYVGFVAEDFTGLE
HFDNEDFTYKHVTNYPQSIDWRAKGAVTPVKNQGACGSCWAFSTIATVEGINKIVTGNLL
ELSEQELVDCDKHSYGCKGGYQTTSLQYVANNGVHTSKVYPYQAKQYKCRATDKPGPKVK
ITGYKRVPSNCETSFLGALANQPLSVLVEAGGKPFQLYKSGVFDGPCGTKLDHAVTAVGY
GTSDGKNYIIIKNSWGPNWGEKGYMRLKRQSGNSQGTCGVYKSSYYPFKGFA
Download FASTA Format
Synonyms
  • Chymopapain
External IDs
  • BAX 1526
  • BAX-1526

Pharmacology

Indication

Chymopapain is indicated for the development of chemonucleolysis which is used for the digestion of the nucleus pulposus in patients with disc herniation confirmed by myelography.1 A disc herniation occurs when the outer portion of the spinal disc breaks down and the inner portion (nucleus pulposus) leaks out pressing surrounding nerves and leading to irradiating pain.9 The chemonucleolysis is a non-surgical treatment that involves the injection of an enzyme to dissolve the nucleus pulposus.6

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Contraindications & Blackbox Warnings
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Pharmacodynamics

The first studies showed that after intradiscal injection of chymopapain the effect involved the removal of the nucleus pulposus leaving the annulus intact.6 The clinical reports indicated a spontaneous remission of symptoms after the administration of chymopapain. It is also highly documented an increased urinary excretion of glycosaminoglycans.3

Mechanism of action

Chymopapain is thought to degrade proteoglycan content of the intervertebral disc causing loss of glycosaminoglycan and water. This effect will cause the shrinkage of the disc and a reduction of the pressure on the nerve root.3

TargetActionsOrganism
ABone marrow proteoglycan
degradation
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Following intra-discal injection, the level of chymopapain decreases gradually and presents a half-life of 2-3 days. The half-life for urinary excretion is reported to be of about 3 days.4

Clearance

Not Available

Adverse Effects
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Toxicity

The median lethal dose of chymopapain in mice is registered to be 82 mg/kg and the toxicity mechanism was caused by hemorrhage due to the destruction of the cement substance in the blood vessels. When administered in an overdosage, chymopapain was able to nearly completely dissolve the nucleus pulposus and cause the disruption of the annulus fibrosus.5

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
Not Available

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Chymodiactin Injection - 4 Nkat Units/2mlPowder, for solution4 unit / vialIntradiscalKnoll Pharma Inc.1996-12-311999-12-31Canada flag

Categories

ATC Codes
M09AB01 — Chymopapain
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
  • Humans and other mammals

Chemical Identifiers

UNII
1UK146T40N
CAS number
9001-09-6

References

General References
  1. Henschke N, Kuijpers T, Rubinstein SM, van Middelkoop M, Ostelo R, Verhagen A, Koes BW, van Tulder MW: Injection therapy and denervation procedures for chronic low-back pain: a systematic review. Eur Spine J. 2010 Sep;19(9):1425-49. doi: 10.1007/s00586-010-1411-0. Epub 2010 Apr 29. [Article]
  2. EBATA M, YASUNOBU KT: Chymopapain. I. Isolation, crystallization, and preliminary characterization. J Biol Chem. 1962 Apr;237:1086-94. [Article]
  3. Jenner JR, Buttle DJ, Dixon AK: Mechanism of action of intradiscal chymopapain in the treatment of sciatica: a clinical, biochemical, and radiological study. Ann Rheum Dis. 1986 Jun;45(6):441-9. [Article]
  4. Kawano K, Tajima N, Hashida S, Ishikawa E: Study of blood metabolism and urinary excretion of chymopapain following intradiscal injection using a high-sensitivity enzyme immunoassay. J Orthop Sci. 2005;10(2):206-13. doi: 10.1007/s00776-004-0872-6. [Article]
  5. Simmons JW, Upman PJ, Stavinoha WB: Pharmacologic and toxicologic profile of chymopapain B (Chemolase). Drug Chem Toxicol. 1984;7(3):299-314. doi: 10.3109/01480548409035110. [Article]
  6. The rise and fall of chemonucleolysis [Link]
  7. Worthington [Link]
  8. FDA approval [Link]
  9. Spine Health [Link]
PubChem Substance
347910365
RxNav
2525
ChEMBL
CHEMBL1201626
Drugs.com
Drugs.com Drug Page
Wikipedia
Chymopapain
MSDS
Download (69.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Powder, for solutionIntradiscal4 unit / vial
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)137-182 ºCEbata and Yasunobu. 1961.
water solubilitySolubleEbata and Yasunobu. 1961.
isoelectric point10.2-10.6Baines and Brocklehurst, 1982.

Targets

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Details1. Bone marrow proteoglycan
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Degradation
General Function
Heparin binding
Specific Function
Cytotoxin and helminthotoxin. Also induces non-cytolytic histamine release from human basophils. Involved in antiparasitic defense mechanisms and immune hypersensitivity reactions. The proform acts...
Gene Name
PRG2
Uniprot ID
P13727
Uniprot Name
Bone marrow proteoglycan
Molecular Weight
25205.345 Da
References
  1. Jenner JR, Buttle DJ, Dixon AK: Mechanism of action of intradiscal chymopapain in the treatment of sciatica: a clinical, biochemical, and radiological study. Ann Rheum Dis. 1986 Jun;45(6):441-9. [Article]

Drug created at September 14, 2010 16:20 / Updated at February 21, 2021 18:52