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Collagenase Clostridium Histolyticum - Uses, Interactions, Mechanism of Action - DrugBank Online
Collagenase Clostridium Histolyticum - Uses, Interactions, Mechanism of Action - DrugBank Online
Collagenase Clostridium Histolyticum - Uses, Interactions, Mechanism of Action - DrugBank Online
Drugs
Identification
Pharmacology
Summary Collagenase clostridium histolyticum is a collagenase enzyme used to promote debridement of
Interactions necrotic tissue in burns and skin ulcers as well as to treat Dupuytren's contracture and Peyronie's
Products disease.
Categories
Brand Names Qwo, Santyl, Xiaflex
Chemical Identifiers
Clinical Trials
DrugBank Accession Number DB00048
Pharmacoeconomics
Properties Background Collagenase clostridium histolyticum is an enzyme produced by the bacterium Clostridium
histolyticum. It is beneficial in the breakdown of collagen plaques for the treatment of
Targets (3) Dupuytren's contracture and Peyronie's disease.11 The topical formulation is used for the
debridement of necrotic tissue due to burns or chronic ulcers.14
On July 6, 2020 a combination of injectable bacterial collagenases was approved by the FDA for
the treatment of cellulite in adult women.10 Also known as Qwo, this injection is the first
approved injectable treatment for cellulite and was developed by Endo International.13
Type Biotech
Protein Structure
MKRKCLSKRLMLAITMATIFTVNSTLPIYAAVDKNNATAAVQNESKRYTVSYLKTLNYYD
LVDLLVKTEIENLPDLFQYSSDAKEFYGNKTRMSFIMDEIGRRAPQYTEIDHKGIPTLVE
VVRAGFYLGFHNKELNEINKRSFKERVIPSILAIQKNPNFKLGTEVQDKIVSATGLLAGN
ETAPPEVVNNFTPILQDCIKNIDRYALDDLKSKALFNVLAAPTYDITEYLRATKEKPENT
PWYGKIDGFINELKKLALYGKINDNNSWIIDNGIYHIAPLGKLHSNNKIGIETLTEVMKV
YPYLSMQHLQSADQIKRHYDSKDAEGNKIPLDKFKKEGKEKYCPKTYTFDDGKVIIKAGA
RVEEEKVKRLYWASKEVNSQFFRVYGIDKPLEEGNPDDILTMVIYNSPEEYKLNSVLYGY
DTNNGGMYIEPEGTFFTYEREAQESTYTLEELFRHEYTHYLQGRYAVPGQWGRTKLYDND
RLTWYEEGGAELFAGSTRTSGILPRKSIVSNIHNTTRNNRYKLSDTVHSKYGASFEFYNY
ACMFMDYMYNKDMGILNKLNDLAKNNDVDGYDNYIRDLSSNYALNDKYQDHMQERIDNYE
NLTVPFVADDYLVRHAYKNPNEIYSEISEVAKLKDAKSEVKKSQYFSTFTLRGSYTGGAS
KGKLEDQKAMNKFIDDSLKKLDTYSWSGYKTLTAYFTNYKVDSSNRVTYDVVFHGYLPNE
GDSKNSLPYGKINGTYKGTEKEKIKFSSEGSFDPDGKIVSYEWDFGDGNKSNEENPEHSY
DKVGTYTVKLKVTDDKGESSVSTTTAEIKDLSENKLPVIYMHVPKSGALNQKVVFYGKGT
YDPDGSIAGYQWDFGDGSDFSSEQNPSHVYTKKGEYTVTLRVMDSSGQMSEKTMKIKITD
PVYPIGTEKEPNNSKETASGPIVPGIPVSGTIENTSDQDYFYFDVITPGEVKIDINKLGY
GGATWVVYDENNNAVSYATDDGQNLSGKFKADKPGRYYIHLYMFNGSYMPYRINIEGSVG
PHARMACOLOGY
Indication Collagenase clostridium histolyticum is indicated for the treatment of adults with Dupuytren's
contracture with a palpable cord. Additionally, it is used to treat men with Peyronie's disease
diagnosed with a penile curvature deformity of at least a 30-degree angle at the beginning of
therapy in addition to palpable plaques.11 Collagenase ointment is used for the tissue
debridement of chronic dermal ulcers and severely burned tissues.15
The combination
collagenase product, also known as Qwo, is used for the treatment of moderate to severe cellulite
in the buttocks of adult women.10
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Drugs
Associated Conditions Dupuytren's Contracture of the Hand (Viking's Disease)
View As List
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Peyronie's Disease
Necrotic tissue
Pharmacodynamics Collagenase digests collagen, treating conditions such as Peyronie's disease, cellulite, chronic
ulcers, burns, and contractures.10,11,14
Mechanism of action Peyronie's disease is a fibrous lesion of the tunica albuginea in the penile tissues.4 Cellulite is a
multifactorial condition resulting in the accumulation of fibrotic dermal septae and the expansion
of subcutaneous fat.3 Dupuytren's contracture is a fibroproliferative disease that results in the
fibrous deposition of collagen in the hands, limiting mobility and functionality of the hands.5 The
collagen deposition in the abovementioned conditions is the target of collagenase enzyme
therapy.6,7
Absorption There is currently limited readily available regarding the absorption of collagenase through the
skin.14
In a pharmacokinetic study, the serum concentrations of clostridium type I collagenase
(AUX-I) and clostridium type II collagenase (AUX-II) were measured. Both were detected under the
lower limit of quantitation of 5 ng/mL and 25 ng/mL, respectively, in volunteers administered one
dose of the collagenase histolyticum combination product, Qwo, at a dose of up to 3.36 mg in a
maximum of 4 body areas.10
Volume of distribution There is no currently available information regarding the presence of collagenase in body fluids or
uptake by particular organs and passage through the blood-brain barrier.14 Systemic
pharmacokinetic studies evaluation volume of distribution have not been performed, however,
collagenase histolyticum is likely to have local degradative effects in the region of the application
without effects on the vasculature and elastic tissue.9
Protein binding There is no readily available information regarding the protein binding of collagenase.14
Metabolism No formal systemic metabolism studies have been performed with collagenase histolyticum.9
Adverse Effects
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effects data.
Toxicity No clinical reaction has been attributed to an overdose of collagenase in clinical trials.14 If
required, the collagenase enzymes can be inactivated with a povidone-iodine wash.14
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.
ALL DRUGS
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DRUG ↑↓ INTERACTION ↑↓
Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Collagenase
Drugs
clostridium histolyticum.
Learn to leverage the Clinical API: Therapeutic Alternatives Read Blog! Acenocoumarol The risk or severity of adverse effects can be increased when Acenocoumarol is combined with
Collagenase clostridium histolyticum.
Alteplase The risk or severity of adverse effects can be increased when Alteplase is combined with Collagenase
clostridium histolyticum.
Ancrod The risk or severity of adverse effects can be increased when Ancrod is combined with Collagenase
clostridium histolyticum.
Anistreplase The risk or severity of adverse effects can be increased when Anistreplase is combined with
Collagenase clostridium histolyticum.
Antithrombin Alfa The risk or severity of adverse effects can be increased when Antithrombin Alfa is combined with
Collagenase clostridium histolyticum.
Antithrombin III human The risk or severity of adverse effects can be increased when Antithrombin III human is combined with
Collagenase clostridium histolyticum.
Apixaban The risk or severity of adverse effects can be increased when Apixaban is combined with Collagenase
clostridium histolyticum.
Ardeparin The risk or severity of adverse effects can be increased when Ardeparin is combined with Collagenase
clostridium histolyticum.
Argatroban The risk or severity of adverse effects can be increased when Argatroban is combined with Collagenase
clostridium histolyticum.
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PRODUCTS
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MARKETING MARKETING
NAME ↑↓ DOSAGE ↑↓ STRENGTH ↑↓ ROUTE ↑↓ LABELLER ↑↓ START ↑↓ END ↑↓ ↑↓ ↑↓
Qwo Injection, powder, 0.23 mg/1mL Intralesional Endo Aesthetics 2021-02-01 Not applicable
lyophilized, for LLC
solution
Santyl Ointment 250 unit / g Topical Smith & Nephew, 1994-12-31 Not applicable
Inc.
Xiaflex Powder, for 0.9 mg / vial Intralesional Endo Ventures 2012-11-14 2020-06-11
solution Ltd
Xiaflex Injection, powder, 0.9 mg/1 Intralesional Endo 2010-02-22 Not applicable
lyophilized, for Pharmaceuticals
solution; Kit Inc.
Showing 1 to 7 of 7 entries
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MARKETING MARKETING
NAME ↑↓ DOSAGE ↑↓ STRENGTH ↑↓ ROUTE ↑↓ LABELLER ↑↓ START ↑↓ END ↑↓ ↑↓ ↑↓
IRUXOL Ointment 1.2 IU Topical SMITH & NEPHEW 2020-09-08 Not applicable
MONO HEALTHCARE SDN BHD
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MARKETING MARKETING
NAME ↑↓ INGREDIENTS DOSAGE ↑↓ ROUTE ↑↓ LABELLER ↑↓ START ↑↓ END ↑↓ ↑↓ ↑↓
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MARKETING MARKETING
NAME ↑↓ INGREDIENTS DOSAGE ↑↓ ROUTE ↑↓ LABELLER ↑↓ START ↑↓ END ↑↓ ↑↓ ↑↓
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CATEGORIES
Collagenases
Dermatologicals
Endopeptidases
Enzymes
Hydrolases
Metalloendopeptidases
Metalloproteases
Musculo-Skeletal System
Peptide Hydrolases
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CHEMICAL IDENTIFIERS
CAS
Learn to leverage the Clinical API: number Alternatives Read Blog!9001-12-1
Therapeutic
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. [Article]
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. [Article]
3. Rossi AM, Katz BE: A modern approach to the treatment of cellulite. Dermatol Clin. 2014 Jan;32(1):51-9. doi:
10.1016/j.det.2013.09.005. [Article]
4. Randhawa K, Shukla CJ: Non-invasive treatment in the management of Peyronie's disease. Ther Adv Urol. 2019 Feb
11;11:1756287218823671. doi: 10.1177/1756287218823671. eCollection 2019 Jan-Dec. [Article]
5. Grazina R, Teixeira S, Ramos R, Sousa H, Ferreira A, Lemos R: Dupuytren's disease: where do we stand? EFORT Open Rev. 2019
Feb 20;4(2):63-69. doi: 10.1302/2058-5241.4.180021. eCollection 2019 Feb. [Article]
6. Dhillon S: Collagenase Clostridium Histolyticum: A Review in Peyronie's Disease. Drugs. 2015 Aug;75(12):1405-12. doi:
10.1007/s40265-015-0441-7. [Article]
7. Kaplan FT: Collagenase clostridium histolyticum injection for the treatment of Dupuytren's contracture. Drugs Today (Barc).
2011 Sep;47(9):653-67. doi: 10.1358/dot.2011.47.9.1656502. [Article]
8. Krane SM: Collagenases and collagen degradation. J Invest Dermatol. 1982 Jul;79 Suppl 1:83s-86s. doi: 10.1111/1523-
1747.ep12545849. [Article]
9. Andrew J Watt, Vincent R Hentz: Collagenase clostridium histolyticum: a novel nonoperative treatment for Dupuytren’s disease
Int. J. Clin. Rheumatol.. [Article]
10. FDA Approved Products: Qwo (collagenase clostridium histolyticum-aaes) for subcutaneous injection [Link]
11. FDA Approved Products: Ziaflex (collagenase clostridium histolyticum) for intralesional use [Link]
12. Thermo Fisher SDS: Collagenase, Type II Powder [Link]
13. Endo International website [Link]
14. FDA Approved Products: Santyl (collagenase) ointment [Link]
15. Product monograph: Santyl (collagenase) [Link]
RxNav 58939
PharmGKB PA449107
Wikipedia Collagenase
CLINICAL TRIALS
Search
4 Active Not Recruiting Treatment Dupuytren's Contracture of the Hand (Viking's Disease) 1
Showing 1 to 10 of 58 entries
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PHARMACOECONOMICS
Auxilium Pharmaceuticals
BASF Corp.
Dispensing Solutions
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15/11/22, 13:04 Collagenase clostridium histolyticum: Uses, Interactions, Mechanism of Action | DrugBank Online
Healthpoint Ltd.
Medisca Inc.
Drugs
Dosage Forms Show 10 entries
Ointment Topical
Ointment Topical
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Showing 1 to 4 of 4 entries
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DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PROPERTIES
State Solid
TARGETS
Kind Protein
Organism Humans
Actions Binder
Curator comments Collagenase targets many types of collagen chains. This chain has been selected as a
representative collagen chain, though others may also be targeted.
Specific Function Type I collagen is a member of group I collagen (fibrillar forming collagen).
Uniprot ID P02452
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. [Article]
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15/11/22, 13:04 Collagenase clostridium histolyticum: Uses, Interactions, Mechanism of Action | DrugBank Online
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. [Article]
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. [Article]
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.
Drugs
Cancer Epidemiol Biomarkers Prev. 2002 Jul;11(7):646-53. [Article]
5. Beare AH, Krane SM, Ferguson MW: Variable impairment of wound healing in the heterozygous collagenase-resistant mouse. Wound Repair Regen. 2005 Jan-
Learn to leverage the Clinical API: Therapeutic Alternatives
Feb;13(1):27-40. [Article] Read Blog!
Kind Protein
Organism Humans
Actions Binder
Curator comments Collagenase targets many types of collagen chains. This chain has been selected as a
representative collagen chain, though others may also be targeted.
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 compressiv...
Uniprot ID P02458
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
Kind Protein
Organism Humans
Actions Binder
Curator comments Collagenase targets many types of collagen chains. This chain has been selected as a
representative collagen chain, though others may also be targeted.
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...
Uniprot ID P02461
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. 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. [Article]
Drug created at June 13, 2005 13:24 / Updated at November 15, 2022 08:41
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