Detailed description page of ThPDB2
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11433 details |
| Primary information | |
|---|---|
| ID | 11433 |
| Therapeutic ID | Th1248 |
| Protein Name | Collagenase clostridium histolyticum |
| Sequence | >Th1248_Collagenase_clostridium_histolyticum MKRKCLSKRLMLAITMATIFTVNSTLPIYAAVDKNNATAAVQNESKRYTVSYLKTLNYYDLVDLLVKTEIENLPDLFQYSSDAKEFYGNKTRMSFIMDEIGRRAPQYTEIDHKGIPTLVEVVRAGFYLGFHNKELNEINKRSFKERVIPSILAIQKNPNFKLGTEVQDKIVSATGLLAGNETAPPEVVNNFTPILQDCIKNIDRYALDDLKSKALFNVLAAPTYDITEYLRATKEKPENTPWYGKIDGFINELKKLALYGKINDNNSWIIDNGIYHIAPLGKLHSNNKIGIETLTEVMKVYPYLSMQHLQSADQIKRHYDSKDAEGNKIPLDKFKKEGKEKYCPKTYTFDDGKVIIKAGARVEEEKVKRLYWASKEVNSQFFRVYGIDKPLEEGNPDDILTMVIYNSPEEYKLNSVLYGYDTNNGGMYIEPEGTFFTYEREAQESTYTLEELFRHEYTHYLQGRYAVPGQWGRTKLYDNDRLTWYEEGGAELFAGSTRTSGILPRKSIVSNIHNTTRNNRYKLSDTVHSKYGASFEFYNYACMFMDYMYNKDMGILNKLNDLAKNNDVDGYDNYIRDLSSNYALNDKYQDHMQERIDNYENLTVPFVADDYLVRHAYKNPNEIYSEISEVAKLKDAKSEVKKSQYFSTFTLRGSYTGGASKGKLEDQKAMNKFIDDSLKKLDTYSWSGYKTLTAYFTNYKVDSSNRVTYDVVFHGYLPNEGDSKNSLPYGKINGTYKGTEKEKIKFSSEGSFDPDGKIVSYEWDFGDGNKSNEENPEHSYDKVGTYTVKLKVTDDKGESSVSTTTAEIKDLSENKLPVIYMHVPKSGALNQKVVFYGKGTYDPDGSIAGYQWDFGDGSDFSSEQNPSHVYTKKGEYTVTLRVMDSSGQMSEKTMKIKITDPVYPIGTEKEPNNSKETASGPIVPGIPVSGTIENTSDQDYFYFDVITPGEVKIDINKLGYGGATWVVYDENNNAVSYATDDGQNLSGKFKADKPGRYYIHLYMFNGSYMPYRINIEGSVGR |
| Molecular Weight | 112023.2 |
| Chemical Formula | C5028H7666N1300O1564S21 |
| Isoelectric Point | 5.35-6.20 |
| Hydrophobicity | -0.714 |
| Melting point | 49-54 |
| Half-life | NA |
| Description | 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 Dupuytren's contracture and Peyronie's disease.[L14882] The topical formulation is used for the debridement of necrotic tissue due to burns or chronic ulcers.[L14912] On July 6, 2020 a combination of injectable bacterial collagenases was approved by the FDA for the treatment of cellulite in adult women.[L14872] Also known as Qwo, this injection is the first approved injectable treatment for cellulite and was developed by Endo International.[L14892] |
| Indication/Disease | 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.[L14882] Collagenase ointment is used for the tissue debridement of chronic dermal ulcers and severely burned tissues.[L14952] The combination collagenase product, also known as Qwo, is used for the treatment of moderate to severe cellulite in the buttocks of adult women.[L14872] |
| Pharmacodynamics | Collagenase digests collagen, treating conditions such as Peyronie's disease, cellulite, chronic ulcers, burns, and contractures.[L14872,L14882,L14912] |
| Mechanism of Action | Peyronie's disease is a fibrous lesion of the tunica albuginea in the penile tissues.[A215067] Cellulite is a multifactorial condition resulting in the accumulation of fibrotic dermal septae and the expansion of subcutaneous fat.[A215062] 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.[A215072] The collagen deposition in the abovementioned conditions is the target of collagenase enzyme therapy.[A215157,A215167] These enzymes are proteinases acting to hydrolyze collagen's triple-helical conformation, resulting in the lysis of collagen deposits and relief from the necrotic tissue and plaques associated with several conditions.[L14882,L14912] On a molecular level, collagenases cleave polypeptide chains that make up the collagen triple helix structure at various loci, leading to solubilization from the collagen fibril.[A215197] |
| Toxicity | No clinical reaction has been attributed to an overdose of collagenase in clinical trials.[L14912] If required, the collagenase enzymes can be inactivated with a povidone-iodine wash.[L14912] |
| Metabolism | No formal systemic metabolism studies have been performed with collagenase histolyticum.[A215277] |
| Absorption | There is currently limited readily available regarding the absorption of collagenase through the skin.[L14912] 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.[L14872] |
| NA | |
| Clearance | NA |
| Categories | Collagen-specific Enzyme |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | Bivalirudin,Abciximab,Dicoumarol,Argatroban,Ardeparin,Phenindione,Fondaparinux,Warfarin,Pentosan polysulfate,Phenprocoumon,Edetic acid,Heparin,Enoxaparin,Acenocoumarol,Ximelagatran,Ancrod,Rivaroxaban,Sulodexide,Idraparinux,Apixaban,Otamixaban,Dabigatran etexilate,Danaparoid,Dalteparin,Ferulic acid,Ethyl biscoumacetate,Nadroparin,Edoxaban,Dextran,Desirudin,Protocatechualdehyde,Protein C,Antithrombin III human,Letaxaban,Darexaban,Nafamostat,Gabexate,Troxerutin,Fluindione,Protein S human,Melagatran,Potassium citrate,Sodium citrate,Tenecteplase,Drotrecogin alfa,Defibrotide,Tinzaparin,Brinase,Saruplase,Streptokinase,Desmoteplase,Fibrinolysin,Astaxanthin,Urokinase,Dipyridamole,Epoprostenol,Beraprost,Prasugrel,Cangrelor,Triflusal,Ticagrelor,Ditazole,Vorapaxar,Bemiparin,Parnaparin,Clorindione,Diphenadione,Tioclomarol,Lepirudin,Alteplase,Reteplase,Anistreplase,Tocopherylquinone,Amediplase,4-hydroxycoumarin,(R)-warfarin,(S)-Warfarin,Betrixaban,Edetate calcium disodium anhydrous,Zinc citrate,Antithrombin Alfa,Coumarin,Dabigatran,Semuloparin,Monteplase,Reviparin,Dermatan sulfate,SR-123781A,Dociparstat sodium,Doxycycline,Lymecycline,Clomocycline,Tigecycline,Oxytetracycline,Demeclocycline,Tetracycline,Metacycline,Minocycline,Rolitetracycline,Chlortetracycline,Sarecycline,Eravacycline,Omadacycline,Meclocycline,Penimepicycline |
| Target | Collagen alpha-1(I) chain,Collagen alpha-1(II) chain,Collagen alpha-1(III) chain |
| Brand Name | Collagenase Santyl |
| Company | Healthpoint |
| Brand Description | Healthpoint |
| Prescribed For | Topical |
| Chemical Name | 250 [arb'U]/1g |
| Formulation | Collagenase Santyl® Ointment is contraindicated in patients who have shown local or systemic hypersensitivity to collagenase. |
| Physical Appearance | No allergic sensitivity or toxic reactions have been noted in clinical use when used as directed. However, one case of systemic manifestations of hypersensitivity to collagenase in a patient treated for more than one year with a combination of collagenase and cortisone has been reported. |
| Route of Administration | NA |
| Recommended Dosage | NA |
| Contraindication | NA |
| Side Effects | NA |
| Useful Link 1 | Link |
| Useful Link 2 | Link |
| Remarks | NA |