Abstract: Methods are provided for producing a PEGylated interleukin 11 (IL-11) by treating a recombinant IL-11 PEGylated with an equimolar to low molar excess of PEG carrying an amine-reactive group to achieve a highly pure monoconjugate preparation, which provides improved half-life in serum while having desirable therapeutic activity and presenting fewer side-effects. Most preferably, the IL-11 is an N-terminally truncated human or humanized IL-11 and has a 20 Kd or 40 Kd branched PEG moiety, Y- or comb-shaped in particular, coupled to the N-terminal amino group. Such compounds are characterized by substantially increased stability in serum and sustained biological activity while exhibiting significantly reduced plasma expansion.
Type:
Grant
Filed:
February 11, 2021
Date of Patent:
March 19, 2024
Assignee:
Nansha Biologics (Hong Kong) Limited
Inventors:
Kuo-Ming Yu, Qui-Lim Choo, Manson Fok, Johnson Yiu-Nam Lau
Abstract: Methods are provided for treating an individual with a pharmaceutical preparation that includes a recombinant IL-11 PEGylated at equimolar to low molar excess of PEG to achieve a highly pure monoconjugate preparation, which provides improved half-life in serum while having desirable therapeutic activity and presenting fewer side-effects. Most preferably, the IL-11 is an N-terminally truncated human or humanized IL-11 and has a 20 Kd or 40 Kd branched PEG moiety, Y- or comb-shaped in particular, coupled to the N-terminal amino group. Such compounds are characterized by substantially increased stability in serum and sustained biological activity while exhibiting significantly reduced plasma expansion.
Type:
Grant
Filed:
May 21, 2019
Date of Patent:
March 16, 2021
Assignee:
Nansha Biologics (Hong Kong) Limited
Inventors:
Kuo-Ming Yu, Qui-Lim Choo, Manson Fok, Johnson Yiu-Nam Lau
Abstract: Compositions and methods are presented in which recombinant IL-11 is PEGylated to achieve improved half-life in serum while having desirable therapeutic activity and presenting less side-effects. Most preferably, the IL-11 is an N-terminally truncated human or humanized IL-11 and has a 20 Kd or 40 Kd branched PEG moiety, Y- or comb-shaped in particular, coupled to the N-terminal amino group. Such compounds are characterized by substantially increased stability in serum and sustained biological activity while exhibiting significantly reduced plasma expansion.
Type:
Grant
Filed:
March 1, 2016
Date of Patent:
July 2, 2019
Assignee:
NANSHA BIOLOGICS (HONG KONG) LIMITED
Inventors:
Kuo-Ming Yu, Qui-Lim Choo, Manson Fok, Johnson Yiu-Nam Lau