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Identification
NameCollagenase clostridium histolyticum
Accession NumberDB00048  (BTD00010, BIOD00010)
TypeBiotech
GroupsApproved, Investigational
Description

Collagenase clostridium histolyticum is an enzyme produced by the bacterium Clostridium histolyticum that dismantles collagen. It is used as a powder-and-solvent injection kit for the treatment of Dupuytren’s contracture, a condition where the fingers bend towards the palm and cannot be fully straightened, and Peyronie’s disease, a connective tissue disorder involving the growth of fibrous plaques in the soft tissue of the penis. BioSpecifics Technologies developed the preparation, which is manufactured and marketed by Auxilium Pharmaceuticals as Xiaflex in the US and by Sobi as Xiapex in Europe.

Protein structureDb00048
Related Articles
Protein chemical formulaC5028H7666N1300O1564S21
Protein average weight112023.2 Da
Sequences
> Collagenase Sequence 
MKRKCLSKRLMLAITMATIFTVNSTLPIYAAVDKNNATAAVQNESKRYTVSYLKTLNYYD
LVDLLVKTEIENLPDLFQYSSDAKEFYGNKTRMSFIMDEIGRRAPQYTEIDHKGIPTLVE
VVRAGFYLGFHNKELNEINKRSFKERVIPSILAIQKNPNFKLGTEVQDKIVSATGLLAGN
ETAPPEVVNNFTPILQDCIKNIDRYALDDLKSKALFNVLAAPTYDITEYLRATKEKPENT
PWYGKIDGFINELKKLALYGKINDNNSWIIDNGIYHIAPLGKLHSNNKIGIETLTEVMKV
YPYLSMQHLQSADQIKRHYDSKDAEGNKIPLDKFKKEGKEKYCPKTYTFDDGKVIIKAGA
RVEEEKVKRLYWASKEVNSQFFRVYGIDKPLEEGNPDDILTMVIYNSPEEYKLNSVLYGY
DTNNGGMYIEPEGTFFTYEREAQESTYTLEELFRHEYTHYLQGRYAVPGQWGRTKLYDND
RLTWYEEGGAELFAGSTRTSGILPRKSIVSNIHNTTRNNRYKLSDTVHSKYGASFEFYNY
ACMFMDYMYNKDMGILNKLNDLAKNNDVDGYDNYIRDLSSNYALNDKYQDHMQERIDNYE
NLTVPFVADDYLVRHAYKNPNEIYSEISEVAKLKDAKSEVKKSQYFSTFTLRGSYTGGAS
KGKLEDQKAMNKFIDDSLKKLDTYSWSGYKTLTAYFTNYKVDSSNRVTYDVVFHGYLPNE
GDSKNSLPYGKINGTYKGTEKEKIKFSSEGSFDPDGKIVSYEWDFGDGNKSNEENPEHSY
DKVGTYTVKLKVTDDKGESSVSTTTAEIKDLSENKLPVIYMHVPKSGALNQKVVFYGKGT
YDPDGSIAGYQWDFGDGSDFSSEQNPSHVYTKKGEYTVTLRVMDSSGQMSEKTMKIKITD
PVYPIGTEKEPNNSKETASGPIVPGIPVSGTIENTSDQDYFYFDVITPGEVKIDINKLGY
GGATWVVYDENNNAVSYATDDGQNLSGKFKADKPGRYYIHLYMFNGSYMPYRINIEGSVG
R
Download FASTA Format
SynonymsNot Available
External Identifiers
  • AA4500
  • PF-5076985
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Collagenase Santylointment250 [arb'U]/gtopicalHEALTHPOINT, LTD2006-10-18Not applicableUs
Collagenase Santylointment250 [arb'U]/gtopicalSmith & Nephew, Inc2012-12-21Not applicableUs
Xiaflexpowder for solution0.9 mgintralesionalActelion Pharmaceuticals Canada Inc2012-11-14Not applicableCanada
XiaflexkitAuxilium Pharmaceuticals, Inc.2010-02-22Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
CordaseNot Available
SantylAdvance Biofactures Corp
XiapexSobi
Brand mixturesNot Available
SaltsNot Available
Categories
UNII9X7O8V25IT
CAS number9001-12-1
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationUsed to promote debridement of necrotic tissue in the treatment of severe burns and dermal ulcers including decubitus ulcers.
PharmacodynamicsUsed in the treatment of skin ulcers and sever burns, collagenase is able to digest collagen in necrotic tissue at physiological pH by hydrolyzing the peptide bonds of undenatured and denatured collagen. Collagenase thus contributes towards the formation of granulation tissue and subsequent epithelization of dermal ulcers and severely burned areas. The action of collagenase may remove substrates necessary for bacterial proliferation or may permit antibodies, leukocytes, and antibiotics better access to the infected area.
Mechanism of actionCollagenase is a protease that is specific to collagen. The triple helical region of interstitial collagens is highly resistant to most cell proteinases. However, during remodeling of the connective tissue in such processes as wound healing and metastasis, collagen becomes susceptible to cleavage by collagenases. Collagenase cleaves all 3 alpha helical chains of native Types I, II and III collagens at a single locus by hydrolyzing the peptide bond following the Gly residue of the sequence: Gly 775-(Ile or Leu) 776-(Ala or Leu) 777 located approximately three-fourths of the chain length from each N-terminus
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Ointmenttopical250 [arb'U]/g
Kit
Powder for solutionintralesional0.9 mg
Prices
Unit descriptionCostUnit
Xiaflex 0.9 mg vial3900.0USD vial
Collagenase powder2432.7USD g
Santyl 250 unit/gm Ointment 15 gm Tube62.98USD tube
Santyl ointment4.13USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
hydrophobicity-0.714Not Available
isoelectric point5.58Not Available
References
Synthesis Reference

Hun-Chi Lin, Shau-Ping Lei, “Molecular cloning of the genes responsible for collagenase production from Clostridium histolyticum.” U.S. Patent US5177017, issued December, 1972.

US5177017
General References
  1. Norris DB, Trudgill PW: Multiple forms of cyclohexanone oxygenase from Nocardia globerula CL1. Eur J Biochem. 1976 Mar 16;63(1):193-8. [PubMed:4312 ]
  2. Pajot P: Fluroescence of proteins in 6-M guanidine hydrochloride. A method for the quantitative determination of tryptophan. Eur J Biochem. 1976 Mar 16;63(1):263-9. [PubMed:4317 ]
External Links
ATC CodesM09AB02
AHFS Codes
  • 84:92.00
PDB Entries
FDA labelNot Available
MSDSDownload (72.9 KB)
Interactions
Drug Interactions
Drug
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Collagenase clostridium histolyticum.
AcenocoumarolThe risk or severity of adverse effects can be increased when Acenocoumarol is combined with Collagenase clostridium histolyticum.
Citric AcidThe risk or severity of adverse effects can be increased when Citric Acid is combined with Collagenase clostridium histolyticum.
DalteparinThe risk or severity of adverse effects can be increased when Dalteparin is combined with Collagenase clostridium histolyticum.
DicoumarolThe risk or severity of adverse effects can be increased when Dicoumarol is combined with Collagenase clostridium histolyticum.
Edetic AcidThe risk or severity of adverse effects can be increased when Edetic Acid is combined with Collagenase clostridium histolyticum.
EnoxaparinThe risk or severity of adverse effects can be increased when Enoxaparin is combined with Collagenase clostridium histolyticum.
Ethyl biscoumacetateThe risk or severity of adverse effects can be increased when Ethyl biscoumacetate is combined with Collagenase clostridium histolyticum.
Fondaparinux sodiumThe risk or severity of adverse effects can be increased when Fondaparinux sodium is combined with Collagenase clostridium histolyticum.
HeparinThe risk or severity of adverse effects can be increased when Heparin is combined with Collagenase clostridium histolyticum.
PhenindioneThe risk or severity of adverse effects can be increased when Phenindione is combined with Collagenase clostridium histolyticum.
PhenprocoumonThe risk or severity of adverse effects can be increased when Phenprocoumon is combined with Collagenase clostridium histolyticum.
SulodexideThe risk or severity of adverse effects can be increased when Sulodexide is combined with Collagenase clostridium histolyticum.
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Collagenase clostridium histolyticum.
WarfarinThe risk or severity of adverse effects can be increased when Warfarin is combined with Collagenase clostridium histolyticum.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Platelet-derived growth factor binding
Specific Function:
Type I collagen is a member of group I collagen (fibrillar forming collagen).
Gene Name:
COL1A1
Uniprot ID:
P02452
Molecular Weight:
138941.105 Da
References
  1. Egeblad M, Shen HC, Behonick DJ, Wilmes L, Eichten A, Korets LV, Kheradmand F, Werb Z, Coussens LM: Type I collagen is a genetic modifier of matrix metalloproteinase 2 in murine skeletal development. Dev Dyn. 2007 Jun;236(6):1683-93. [PubMed:17440987 ]
  2. Lindsey ML, Yoshioka J, MacGillivray C, Muangman S, Gannon J, Verghese A, Aikawa M, Libby P, Krane SM, Lee RT: Effect of a cleavage-resistant collagen mutation on left ventricular remodeling. Circ Res. 2003 Aug 8;93(3):238-45. Epub 2003 Jul 10. [PubMed:12855673 ]
  3. Beare AH, O'Kane S, Krane SM, Ferguson MW: Severely impaired wound healing in the collagenase-resistant mouse. J Invest Dermatol. 2003 Jan;120(1):153-63. [PubMed:12535212 ]
  4. Chiu CJ, Chang ML, Chiang CP, Hahn LJ, Hsieh LL, Chen CJ: Interaction of collagen-related genes and susceptibility to betel quid-induced oral submucous fibrosis. Cancer Epidemiol Biomarkers Prev. 2002 Jul;11(7):646-53. [PubMed:12101112 ]
  5. Beare AH, Krane SM, Ferguson MW: Variable impairment of wound healing in the heterozygous collagenase-resistant mouse. Wound Repair Regen. 2005 Jan-Feb;13(1):27-40. [PubMed:15659034 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Platelet-derived growth factor binding
Specific Function:
Type II collagen is specific for cartilaginous tissues. It is essential for the normal embryonic development of the skeleton, for linear growth and for the ability of cartilage to resist compressive forces.
Gene Name:
COL2A1
Uniprot ID:
P02458
Molecular Weight:
141785.08 Da
References
  1. Fraser A, Fearon U, Billinghurst RC, Ionescu M, Reece R, Barwick T, Emery P, Poole AR, Veale DJ: Turnover of type II collagen and aggrecan in cartilage matrix at the onset of inflammatory arthritis in humans: relationship to mediators of systemic and local inflammation. Arthritis Rheum. 2003 Nov;48(11):3085-95. [PubMed:14613270 ]
  2. Imai K, Dalal SS, Hambor J, Mitchell P, Okada Y, Horton WC, D'Armiento J: Bone growth retardation in mouse embryos expressing human collagenase 1. Am J Physiol Cell Physiol. 2007 Oct;293(4):C1209-15. Epub 2007 Jul 25. [PubMed:17652426 ]
  3. Verstappen SM, Poole AR, Ionescu M, King LE, Abrahamowicz M, Hofman DM, Bijlsma JW, Lafeber FP: Radiographic joint damage in rheumatoid arthritis is associated with differences in cartilage turnover and can be predicted by serum biomarkers: an evaluation from 1 to 4 years after diagnosis. Arthritis Res Ther. 2006;8(1):R31. Epub 2006 Jan 10. [PubMed:16507130 ]
  4. Martin G, Bogdanowicz P, Domagala F, Ficheux H, Pujol JP: Articular chondrocytes cultured in hypoxia: their response to interleukin-1beta and rhein, the active metabolite of diacerhein. Biorheology. 2004;41(3-4):549-61. [PubMed:15299286 ]
  5. Pratta MA, Yao W, Decicco C, Tortorella MD, Liu RQ, Copeland RA, Magolda R, Newton RC, Trzaskos JM, Arner EC: Aggrecan protects cartilage collagen from proteolytic cleavage. J Biol Chem. 2003 Nov 14;278(46):45539-45. Epub 2003 Jul 30. [PubMed:12890681 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Platelet-derived growth factor binding
Specific Function:
Collagen type III occurs in most soft connective tissues along with type I collagen. Involved in regulation of cortical development. Is the major ligand of GPR56 in the developing brain and binding to GPR56 inhibits neuronal migration and activates the RhoA pathway by coupling GPR56 to GNA13 and possibly GNA12.
Gene Name:
COL3A1
Uniprot ID:
P02461
Molecular Weight:
138564.005 Da
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. [PubMed:17139284 ]
  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. [PubMed:17016423 ]
  3. Cole WG, Chiodo AA, Lamande SR, Janeczko R, Ramirez F, Dahl HH, Chan D, Bateman JF: A base substitution at a splice site in the COL3A1 gene causes exon skipping and generates abnormal type III procollagen in a patient with Ehlers-Danlos syndrome type IV. J Biol Chem. 1990 Oct 5;265(28):17070-7. [PubMed:2145268 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein binding, bridging
Specific Function:
Type I collagen is a member of group I collagen (fibrillar forming collagen).
Gene Name:
COL1A2
Uniprot ID:
P08123
Molecular Weight:
129313.615 Da
References
  1. Chiu CJ, Chang ML, Chiang CP, Hahn LJ, Hsieh LL, Chen CJ: Interaction of collagen-related genes and susceptibility to betel quid-induced oral submucous fibrosis. Cancer Epidemiol Biomarkers Prev. 2002 Jul;11(7):646-53. [PubMed:12101112 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23