IP Library › Granted Patent US 12,467,042
Granted Patent B2
US 12,467,042 · App. 17/999,980 · Granted Nov 11, 2025

Lipase enzyme

Inventors: Christopher Moers (Münster, DE); Ingo Aldag (Münster, DE)
Assignee: DERMAPHARM AKTIENGESELLSCHAFT
C12N9/20A61K38/46
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Quick Facts
Patent No.
US 12,467,042
App. No.
17/999,980
Granted
Nov 11, 2025
Kind
B2
Abstract

The present invention relates to a Lipase enzyme comprising an amino acid sequence that has at least 90% sequence identity with SEQ ID NO 1, or comprising a functional fragment thereof encompassing position Q55, with the proviso that the lipase enzyme has a substitution of an amino acid with a basic side chain at neutral pH in position Q55 ( FIG. 1 ).

Claims (17)

1 . A lipase enzyme comprising an amino acid sequence that has at least 90% sequence identity with SEQ ID NO 1, or comprising a functional fragment thereof encompassing position Q55, with the proviso that the lipase enzyme has a substitution of an amino acid with a basic side chain at neutral pH in position Q55.

2 . The lipase enzyme according to claim 1 , wherein the substitution is by an amino acid selected from the group consisting of Lysine (K), Arginine (R) and Histidine (H).

3 . The lipase enzyme according to claim 1 , wherein the substitution in position Q55 is Q55K.

4 . The lipase enzyme according to claim 1 , which has a lipolytic activity of at least 30,000 U/g.

5 . The lipase enzyme according to claim 1 , which comprises at least one conservative amino acid substitution in addition to the substitution in position Q55, compared to the amino acid according to SEQ ID NO 1.

6 . The lipase enzyme according to claim 1 , wherein the lipase enzyme has an increased lipolytic activity in a medium having a pH of ≥5.5, compared to a lipase enzyme that has the amino acid sequence of SEQ ID NO 1.

7 . The lipase enzyme according to claim 1 , wherein the lipase enzyme has an increased lipolytic activity in a medium having a total bile salt concentration of ≥2.5 mM, compared to a lipase enzyme that has the amino acid sequence of SEQ ID NO 1.

8 . The lipase enzyme according to claim 1 , wherein the lipase enzyme has an increased lipolytic activity in a medium comprising a mixture of two or more different bile acids, compared to a lipase enzyme that has the amino acid sequence of SEQ ID NO 1.

9 . A nucleic acid that encodes for a lipase enzyme comprising an amino acid sequence that has at least 90% sequence identity with SEQ ID NO 1, or comprising a functional fragment thereof encompassing position Q55, with the proviso that the lipase enzyme has a substitution of an amino acid with a basic side chain at neutral pH in position Q55.

10 . A pharmaceutical composition comprising the lipase enzyme according to claim 1 and one or more pharmaceutically acceptable excipients.

11 . A combination comprising (i) the lipase enzyme according to claim 1 and (ii) one or more therapeutically active compounds.

12 . A method for treating or preventing a lipid digestion deficiency, a digestive disorder or an inflammatory condition, which method comprises administration, to a human or animal subject, of the lipase enzyme according to claim 1 in a therapeutically sufficient dose.

13 . A therapeutic kit of parts comprising: a) the lipase enzyme according to claim 1 , b) an apparatus for administering the lipase enzyme, and c) instructions for use.

14 . A method of producing a lipase enzyme according to claim 1 , which method comprises the steps of a) expressing the lipase enzyme in an expression host from the order ciliates, and b) purifying the lipase enzyme expressed in step a).

15 . The method according to claim 14 , which method comprises, before step a), the step of transforming the ciliate with a vector encoding for the lipase enzyme.

16 . The method according to claim 14 , wherein the expression host is from the genus Tetrahymena.

17 . The method according to claim 14 , wherein the expression host is Tetrahymena thermophila.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 21, 2024
From: CILIAN AG
To: DERMAPHARM AKTIENGESELLSCHAFT
Reel/Frame 069743/0432 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 28, 2022
From: MOERS, CHRISTOPHER; ALDAG, INGO
To: CILIAN AG
Reel/Frame 061890/0393 →
Priority Claims (1)
EP 20182077 · Jun 24, 2020 · regional
Continuity (1)
Related Publication 20230220360A1 · Jul 13, 2023
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