IP Library Patent Application 15160392
Patent Application
App. No. 15/160,392

COMPOSITIONS AND METHODS FOR TREATING COLLAGEN-MEDIATED DISEASES

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Patent No.
US None
App. No.
15/160,392
Abstract

A drug product comprising a combination of highly purified collagenase I and collagenase II from Clostridium histolyticum is disclosed. The drug product includes collagenase I and collagenase II in a ratio of about 1 to 1, with a purity of greater than at least 95%. The invention further disclosed improved fermentation and purification processes for preparing the said drug product.

Claims (76)

1 . A drug product comprising isolated and purified collagenase I and collagenase II having the sequence of Clostridium histolyticum collagenase I and collagenase II, respectively, wherein the collagenase I and collagenase II have a mass ratio of about 1 to 1 and the drug product is at least 95% by area pure as determined by reverse phase high performance liquid chromatography.

2 . The drug product of claim 1 , wherein the drug product contains less than about 2% by area aggregated protein as determined by reverse phase high performance liquid chromatography.

3 . The drug product of claim 1 , wherein the drug product contains less than about 1% by area of clostripain as determined by reverse phase high performance liquid chromatography.

4 . The drug product of claim 1 , wherein the drug product contains less than about 1% by area of gelatinase as determined by anion exchange chromatography.

5 . The drug product of claim 1 , wherein the drug product contains less than about 1 ug/mg (w/w) of leupeptin.

6 . The drug product of claim 1 , wherein the drug product has a bioburden less than 1 cfu/ml, and wherein the drug product is sterile.

7 . The drug product of claim 6 , wherein the drug product contains less than 10 EU/ml of endotoxin.

8 . The drug product of claim 6 , wherein the drug product contains less than 5 EU/mg of endotoxin.

9 . A drug product comprising isolated and purified collagenase I and collagenase II having the sequence of Clostridium histolyticum collagenase I and collagenase II, respectively, wherein the collagenase I and collagenase II have a mass ratio of about 1 to 1 and the drug product is at least 95% by area pure as determined by reverse phase high performance liquid chromatography, wherein the preparation of the drug product comprises the steps of:

a) fermenting Clostridium histolyticum;

b) harvesting a crude fermentation comprising collagenase I and collagenase II;

c) purifying collagenase I and collagenase II from the crude harvest via filtration and column chromatography comprising the steps of:

i) filtering the crude harvest through an anion exchange filter;

ii) adding ammonium sulphate;

iii) subjecting the harvest through a HIC column;

iv) adding leupeptin to the filtrate;

v) removing the ammonium sulfate;

vi) filtering the mixture of step (v); and

vii) separating collagenase I and collagenase II using ion-exchange;

d) combining the collagenase I and collagenase II purified from step (c) at a ratio of about 1 to 1.

10 . The drug product of claim 9 , wherein the drug product is at least 97% by area pure as determined by reverse phase high performance liquid chromatography.

11 . The drug product of claim 9 , wherein preparation of the drug product further comprises the step of conducting cell bank preparations in the presence of phytone peptone or vegetable peptone.

12 . The drug product of claim 9 , wherein the fermentation step comprises the steps of:

i. inoculating the medium in a first stage with Clostridium histolyticum and agitating the mixture;

ii. incubating the mixture from step (i) to obtain an aliquot;

iii. inoculating the medium in a second stage with aliquots resulting from step (ii) and agitating the mixture;

iv. incubating mixtures from step (iii) to obtain an aliquot;

v. inoculating the medium in a third stage with aliquots resulting from step (iv) and agitating;

vi. incubating mixtures from step (v) to obtain an aliquot;

vii. inoculating the medium in a fourth stage with an aliquot resulting from step (vi) and agitating; and

viii. incubating mixtures from step (vii).

13 . The drug product of claim 9 , wherein the drug product is stored at a temperature of about −70° C.

14 - 18 . (canceled)

19 . A pharmaceutical formulation comprising a pharmaceutically acceptable excipient and a drug product comprising isolated and purified collagenase I and collagenase II having the sequence of Clostridium histolyticum collagenase I and collagenase II, respectively, wherein the collagenase I and collagenase II have a mass ratio of about 1 to 1 and the drug product is at least 95% by area pure as determined by reverse phase high performance liquid chromatography.

20 . The pharmaceutical formulation of claim 19 , wherein the drug product is a sterile lyophilized powder and is stored at a temperature of about 5° C.

21 . The pharmaceutical formulation of claim 19 , wherein the formulation is a lyophilized injectable formulation formulated with Sucrose, Tris and with a pH level of about 8.0.

22 . The pharmaceutical formulation of claim 21 , wherein the formulation is a lyophilized injectable formulation comprising about 0.9 mg of the said drug product, about 18.5 mg of sucrose and about 1.1 mg of Tris, and wherein the targeting vial fill volume is about 0.9 mL.

23 . The pharmaceutical formulation of claim 21 , wherein the formulation is a lyophilized injectable formulation comprising about 0.58 mg of the said drug product, about 12.0 mg of sucrose and about 0.7 mg of Tris.

24 . The pharmaceutical formulation of claim 19 , wherein the preparation of the drug product comprises the steps of:

a) fermenting Clostridium histolyticum;

b) harvesting a crude fermentation comprising collagenase I and collagenase II;

c) purifying collagenase I and collagenase II from the crude harvest via filtration and column chromatography comprising the steps of:

i) filtering the crude harvest through an anion exchange filter;

ii) adding ammonium sulphate;

iii) subjecting the harvest through a HIC column;

iv) adding leupeptin to the filtrate;

v) removing the ammonium sulfate;

vi) filtering the mixture of step (v); and

vii) separating collagenase I and collagenase II using ion-exchange;

d) combining the collagenase I and collagenase II purified from step (c) at a ratio of about 1 to 1.

25 . The pharmaceutical formulation of claim 24 , wherein the formulation is a sterile lyophilized powder.

26 . The pharmaceutical formulation of claim 25 , wherein the formulation is a lyophilized injectable formulation formulated with sucrose, Tris and with a pH level of about 8.0.

27 . The pharmaceutical formulation of claim 26 , wherein the formulation is a lyophilized injectable formulation comprising about 0.9 mg of the said drug product, about 18.5 mg of sucrose and about 1.1 mg of Tris, and wherein the targeting vial fill volume is about 0.9 mL.

28 . The pharmaceutical formulation of claim 26 , wherein the formulation is a lyophilized injectable composition comprising about 0.58 mg of the said drug product, about 12.0 mg of sucrose and about 0.7 mg of Tris.

29 - 46 . (canceled)

47 . The pharmaceutical formulation of claim 19 , wherein the drug product is at least 97% by area pure as determined by reverse phase high performance liquid chromatography.

48 . The pharmaceutical formulation of claim 47 , wherein the formulation is a sterile lyophilized powder and is stored at a temperature of about 5° C.

49 . The pharmaceutical formulation of claim 47 , wherein the formulation is a lyophilized injectable formulation formulated with Sucrose, Tris and with a pH level of about 8.0.

50 . The pharmaceutical formulation of claim 49 , wherein the formulation is a lyophilized injectable formulation comprising about 0.9 mg of the said drug product, about 18.5 mg of sucrose and about 1.1 mg of Tris, and wherein the targeting vial fill volume is about 0.9 mL.

51 . The pharmaceutical formulation of claim 49 , wherein the formulation is a lyophilized injectable formulation comprising about 0.58 mg of the said drug product, about 12.0 mg of sucrose and about 0.7 mg of Tris.

52 . The pharmaceutical formulation of claim 47 , wherein the preparation of the drug product comprises the steps of:

a) fermenting Clostridium histolyticum;

b) harvesting a crude fermentation comprising collagenase I and collagenase II;

c) purifying collagenase I and collagenase II from the crude harvest via filtration and column chromatography comprising the steps of:

i) filtering the crude harvest through an anion exchange filter;

ii) adding ammonium sulphate;

iii) subjecting the harvest through a HIC column;

iv) adding leupeptin to the filtrate;

v) removing the ammonium sulfate;

vi) filtering the mixture of step (v); and

vii) separating collagenase I and collagenase II using ion-exchange;

d) combining the collagenase I and collagenase II purified from step (c) at a ratio of about 1 to 1.

53 . The pharmaceutical formulation of claim 52 , wherein the formulation is a sterile lyophilized powder.

54 . The pharmaceutical formulation of claim 52 , wherein the formulation is a lyophilized injectable formulation formulated with sucrose, Tris and with a pH level of about 8.0.

55 . The pharmaceutical formulation of claim 54 , wherein the formulation is a lyophilized injectable composition comprising about 0.9 mg of the said drug product, about 18.5 mg of sucrose and about 1.1 mg of Tris, and wherein the targeting vial fill volume is about 0.9 mL.

56 . The pharmaceutical formulation of claim 54 , wherein the formulation is a lyophilized injectable composition comprising about 0.58 mg of the said drug product, about 12.0 mg of sucrose and about 0.7 mg of Tris.

Assignments (13)
RELEASE OF SECURITY INTEREST Recorded Apr 26, 2024
From: WILMINGTON TRUST, NATIONAL ASSOCIATION
To: ACTIENT PHARMACEUTICALS LLC; ASTORA WOMEN’S HEALTH HOLDINGS, LLC; ASTORA WOMEN’S HEALTH LLC; AUXILIUM PHARMACEUTICALS, LLC; AUXILIUM US HOLDINGS, LLC; BIOSPECIFICS TECHNOLOGIES CORP.; BIOSPECIFICS TECHNOLOGIES LLC; DAVA INTERNATIONAL, LLC; DAVA PHARMACEUTICALS, LLC; ENDO GENERIC HOLDINGS, INC. (FORMERLY KNOWN AS PAR PHARMACEUTICALS COMPANIES, INC.); ENDO PHARMACEUTICALS INC.; ENDO PHARMACEUTICALS SOLUTIONS INC. (FORMERLY KNOWN AS INDEVUS PHARMACEUTICALS, INC.); GENERICS BIDCO I, LLC; GENERICS INTERNATIONAL (US), INC.; PAR PHARMACEUTICAL, INC.; PAR STERILE PRODUCTS, LLC (FORMERLY KNOWN AS JHP PHARMACEUTICALS, LLC); QUARTZ SPECIALTY PHARMACEUTICALS, LLC; SLATE PHARMACEUTICALS, LLC; VINTAGE PHARMACEUTICALS, LLC
Reel/Frame 067240/0001 →
RELEASE OF SECURITY INTEREST Recorded Apr 25, 2024
From: WILMINGTON TRUST, NATIONAL ASSOCIATION
To: ENDO GLOBAL AESTHETICS LIMITED; ENDO GLOBAL VENTURES; ENDO VENTURES BERMUDA LIMITED; ENDO VENTURES LIMITED; PALADIN LABS INC.
Reel/Frame 067221/0958 →
RELEASE OF SECURITY INTEREST Recorded Apr 24, 2024
From: WILMINGTON TRUST, NATIONAL ASSOCIATION
To: ENDO GLOBAL AESTHETICS LIMITED; ENDO GLOBAL VENTURES; ENDO VENTURES BERMUDA LIMITED; ENDO VENTURES LIMITED; PALADIN LABS INC.
Reel/Frame 067216/0376 →
CONFIRMATORY GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS Recorded Sep 17, 2021
From: ENDO VENTURES LIMITED; ENDO GLOBAL VENTURES; PALADIN LABS INC.
To: WILMINGTON TRUST, NATIONAL ASSOCIATION
Reel/Frame 057538/0893 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 5, 2020
From: ENDO GLOBAL VENTURES
To: ENDO GLOBAL AESTHETICS LIMITED
Reel/Frame 053978/0933 →
CONFIRMATORY GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS Recorded May 26, 2020
From: ENDO GLOBAL VENTURES; ENDO VENTURES LIMITED; PALADIN LABS INC.
To: WILMINGTON TRUST, NATIONAL ASSOCIATION
Reel/Frame 053548/0239 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 11, 2019
From: AUXILIUM PHARMACEUTICALS, INC.
To: AUXILIUM US HOLDINGS, LLC
Reel/Frame 048297/0644 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 11, 2019
From: YU, BO; WEGMAN, THOMAS L.
To: BIOSPECIFICS TECHNOLOGIES CORP.
Reel/Frame 048297/0909 →
CHANGE OF NAME Recorded Feb 11, 2019
From: AUXILIUM BERMUDA UNLIMITED
To: ENDO GLOBAL VENTURES
Reel/Frame 048303/0095 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 11, 2019
From: AUXILIUM US HOLDINGS, LLC
To: AUXILIUM BERMUDA UNLIMITED
Reel/Frame 048297/0765 →
SECURITY INTEREST Recorded Jun 8, 2017
From: AUXILIUM PHARMACEUTICALS, LLC
To: WILMINGTON TRUST, NATIONAL ASSOCIATION, AS COLLATERAL TRUSTEE
Reel/Frame 042742/0855 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 20, 2016
From: SABATINO, GREGORY L.; DEL TITO, BENJAMIN J.; BASSETT, PHILLIP J.; THARIA, HAZEL A.; HITCHCOCK, ANTONY G.
To: AUXILIUM PHARMACEUTICALS, INC.
Reel/Frame 040076/0226 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 19, 2016
From: BIOSPECIFICS TECHNOLOGIES CORP.
To: BIOSPECIFICS TECHNOLOGIES CORP.; AUXILIUM US HOLDINGS, LLC
Reel/Frame 039191/0001 →