公开(公告)号：US20210115159A1

公开(公告)日：2021-04-22

申请号：US16951003

申请日：2020-11-18

Applicant: PFIZER INC. ,  RINAT NEUROSCIENCE CORP.

Inventor： Pavel STROP ,  Magdalena Grazyna DORYWALSKA ,  Arvind RAJPAL ,  David SHELTON ,  Shu-Hui LIU ,  Jaume PONS ,  Russell DUSHIN

IPC: C07K17/02 ,  C07K16/30 ,  A61K47/68

Abstract: The present invention provides engineered polypeptide conjugates (e.g., antibody-drug-conjugates, toxin-(biocompatible polymer) conjugates, antibody-(biocompatible polymer) conjugates, and bispecific antibodies) comprising acyl donor glutamine-containing tags and amine donor agents. In one aspect, the invention provides an engineered Fc-containing polypeptide conjugate comprising the formula (Fc-containing polypeptide)-T-A, wherein T is an acyl donor glutamine-containing tag engineered at a specific site or comprises an endogenous glutamine made reactive by the Fc-containing polypeptide engineering, wherein A is an amine donor agent, and wherein the amine donor agent is site-specifically conjugated to the acyl donor glutamine-containing tag or the endogenous glutamine. The invention also provides methods of making engineered polypeptide conjugates using transglutaminase.

公开(公告)号：US20180002428A1

公开(公告)日：2018-01-04

申请号：US15610417

申请日：2017-05-31

Applicant: PFIZER INC.

Inventor： Shu-Hui LIU ,  Flavia Mercer PERNASETTI ,  Weihsien HO

IPC: C07K16/28 ,  A61K49/00 ,  A61K47/68 ,  A61K39/395 ,  A61K39/00 ,  C07K14/715

CPC classification number: C07K16/2866 ,  A61K39/3955 ,  A61K47/6803 ,  A61K47/6809 ,  A61K47/6847 ,  A61K47/6849 ,  A61K47/6851 ,  A61K49/0002 ,  A61K2039/505 ,  C07H21/04 ,  C07K14/7158 ,  C07K2317/24 ,  C07K2317/33 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/73 ,  C07K2317/732 ,  C07K2317/734 ,  C07K2317/76 ,  C07K2317/92 ,  C12N15/09

Abstract: The present invention provides antibodies and related molecules that bind to chemokine receptor 4 (CXCR4). The invention further provides antibody-drug conjugates comprising such antibodies, antibody encoding nucleic acids, and methods of obtaining such antibodies. The invention further relates to therapeutic methods for use of these antibodies and anti-CXCR4 antibody-drug conjugates for the treatment of a disorder associated with CXCR4 function or expression (e.g., cancer), such as colon, RCC, esophageal, gastric, head and neck, lung, ovarian, pancreatic cancer or hematological cancers.

公开(公告)号：US20150037328A1

公开(公告)日：2015-02-05

申请号：US14449478

申请日：2014-08-01

Applicant: Pfizer Inc.

Inventor： Shu-Hui LIU ,  Flavia Mercer PERNASETTI ,  Wei-Hsien HO

IPC: C07K16/28 ,  A61K47/48

CPC classification number: C07K16/2866 ,  A61K39/3955 ,  A61K47/6803 ,  A61K47/6809 ,  A61K47/6847 ,  A61K47/6849 ,  A61K47/6851 ,  A61K49/0002 ,  A61K2039/505 ,  C07H21/04 ,  C07K14/7158 ,  C07K2317/24 ,  C07K2317/33 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/73 ,  C07K2317/732 ,  C07K2317/734 ,  C07K2317/76 ,  C07K2317/92 ,  C12N15/09

Abstract: The present invention provides antibodies and related molecules that bind to chemokine receptor 4 (CXCR4). The invention further provides antibody-drug conjugates comprising such antibodies, antibody encoding nucleic acids, and methods of obtaining such antibodies. The invention further relates to therapeutic methods for use of these antibodies and anti-CXCR4 antibody-drug conjugates for the treatment of a disorder associated with CXCR4 function or expression (e.g., cancer), such as colon, RCC, esophageal, gastric, head and neck, lung, ovarian, pancreatic cancer or hematological cancers.

Abstract translation: 本发明提供结合趋化因子受体4（CXCR4）的抗体和相关分子。 本发明进一步提供包含此类抗体的抗体 - 药物偶联物，编码抗体的核酸，以及获得此类抗体的方法。 本发明还涉及使用这些抗体和抗CXCR4抗体 - 药物偶联物治疗与CXCR4功能或表达相关的疾病（例如癌症）如结肠，RCC，食管癌，胃癌，头部和/ 颈，肺，卵巢，胰腺癌或血液癌。

公开(公告)号：US20170313787A1

公开(公告)日：2017-11-02

申请号：US15593259

申请日：2017-05-11

Applicant: PFIZER INC. ,  RINAT NEUROSCIENCE CORP.

Inventor： Pavel STROP ,  Magdalena Grazyna DORYWALSKA ,  Arvind RAJPAL ,  David SHELTON ,  Shu-Hui LIU ,  Jaume PONS ,  Russell DUSHIN

IPC: C07K17/02 ,  C07K16/30

CPC classification number: C07K17/02 ,  A61K47/68 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6889 ,  C07K16/30 ,  C07K2317/31 ,  C07K2317/73

Abstract: The present invention provides engineered polypeptide conjugates (e.g., antibody-drug-conjugates, toxin-(biocompatible polymer) conjugates, antibody-(biocompatible polymer) conjugates, and bispecific antibodies) comprising acyl donor glutamine-containing tags and amine donor agents. In one aspect, the invention provides an engineered Fc-containing polypeptide conjugate comprising the formula (Fc-containing polypeptide)-T-A, wherein T is an acyl donor glutamine-containing tag engineered at a specific site or comprises an endogenous glutamine made reactive by the Fc-containing polypeptide engineering, wherein A is an amine donor agent, and wherein the amine donor agent is site-specifically conjugated to the acyl donor glutamine-containing tag or the endogenous glutamine. The invention also provides methods of making engineered polypeptide conjugates using transglutaminase.