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：US20180171018A1

公开(公告)日：2018-06-21

申请号：US15878344

申请日：2018-01-23

Applicant: PFIZER INC.

Inventor： Tracy Chia-Chien KUO ,  Javier Fernando CHAPARRO RIGGERS ,  Wei CHEN ,  Amy Shaw-Ru CHEN ,  Edward Derrick PASCUA ,  Thomas John VAN BLARCOM ,  Leila Marie BOUSTANY ,  Weihsien HO ,  Yik Andy YEUNG ,  Pavel STROP ,  Arvind RAJPAL

IPC: C07K16/28 ,  A61K39/395 ,  A61K47/68 ,  A61K31/454 ,  A61K31/69 ,  A61K31/704 ,  A61K39/00

CPC classification number: C07K16/2878 ,  A61K31/454 ,  A61K31/69 ,  A61K31/704 ,  A61K39/3955 ,  A61K39/39558 ,  A61K47/6801 ,  A61K47/6849 ,  A61K2039/505 ,  C07K16/2803 ,  C07K16/2809 ,  C07K2317/21 ,  C07K2317/31 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/73 ,  C07K2317/732 ,  C07K2317/92 ,  A61K2300/00

Abstract: The present invention relates to antibodies, e.g., full length antibodies or antigen binding fragments thereof, that specifically bind to BCMA (B-Cell Maturation Antigen) and/or CD3 (Cluster of Differentiation 3). The invention also relates to antibody conjugates (e.g., antibody-drug-conjugates) comprising the BCMA antibodies, compositions comprising the BCMA antibodies, and methods of using the BCMA antibodies and their conjugates for treating conditions associated with cells expressing BCMA (e.g., cancer or autoimmune disease). The invention further relates to heteromultimeric antibodies that specifically bind to CD3 and a tumor cell antigen, (e.g., bispecific antibodies that specifically bind to CD3 and BCMA). Compositions comprising such heteromultimeric antibodies, methods for producing and purifying such heterodimeric antibodies, and their use in diagnostics and therapeutics are also provided.

公开(公告)号：US20130129753A1

公开(公告)日：2013-05-23

申请号：US13670612

申请日：2012-11-07

Applicant: PFIZER INC.

Inventor： Matthew David DOROSKI ,  Andreas MADERNA ,  Christopher John O'DONNELL ,  Chakrapani SUBRAMANYAM ,  Beth VETELINO ,  Russell George DUSHIN ,  Pavel STROP ,  Edmund Idris GRAZIANI

IPC: C07K7/02 ,  C07K5/02 ,  C07K16/00

CPC classification number: C07K7/06 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K47/6803 ,  A61K47/6811 ,  A61K47/6851 ,  A61K47/6855 ,  A61K47/6863 ,  A61K47/6889 ,  C07K5/0205 ,  C07K5/0808 ,  C07K7/02 ,  C07K16/00 ,  C07K2319/30

Abstract: The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.

公开(公告)号：US20210054087A1

公开(公告)日：2021-02-25

申请号：US17005073

申请日：2020-08-27

Applicant: PFIZER INC.

Inventor： Tracy Chia-Chien KUO ,  Javier Fernando CHAPARRO RIGGERS ,  Wei CHEN ,  Amy Shaw-Ru CHEN ,  Edward Derrick PASCUA ,  Thomas John VAN BLARCOM ,  Leila Marie BOUSTANY ,  Weihsien HO ,  Yik Andy YEUNG ,  Pavel STROP ,  Arvind RAJPAL

IPC: C07K16/28 ,  A61K39/395 ,  A61K31/454 ,  A61K31/704 ,  A61K31/69 ,  A61K47/68

Abstract: The present invention relates to antibodies, e.g., full length antibodies or antigen binding fragments thereof, that specifically bind to BCMA (B-Cell Maturation Antigen) and/or CD3 (Cluster of Differentiation 3). The invention also relates to antibody conjugates (e.g., antibody-drug-conjugates) comprising the BCMA antibodies, compositions comprising the BCMA antibodies, and methods of using the BCMA antibodies and their conjugates for treating conditions associated with cells expressing BCMA (e.g., cancer or autoimmune disease). The invention further relates to heteromultimeric antibodies that specifically bind to CD3 and a tumor cell antigen, (e.g., bispecific antibodies that specifically bind to CD3 and BCMA). Compositions comprising such heteromultimeric antibodies, methods for producing and purifying such heterodimeric antibodies, and their use in diagnostics and therapeutics are also provided.

公开(公告)号：US20170151341A1

公开(公告)日：2017-06-01

申请号：US15356750

申请日：2016-11-21

Applicant: Pfizer Inc.

Inventor： Dangshe MA ,  Frank LOGANZO, JR. ,  Kimberly Ann MARQUETTE ,  Edmund Idris GRAZIANI ,  Puja SAPRA ,  Pavel STROP

IPC: A61K47/48 ,  C07K16/30 ,  C07K16/32

Abstract: The present invention provides site specific HER2 antibody drug conjugates and methods for preparing and using the same.

公开(公告)号：US20170043033A1

公开(公告)日：2017-02-16

申请号：US15306481

申请日：2015-04-21

Applicant: Rinat Neuroscience Corp. ,  Pfizer Inc.

Inventor： Pavel STROP ,  Katherine Anne DELARIA ,  Magdalena DORYWALSKA ,  Davide Luciano FOLETTI ,  Russell George DUSHIN ,  David Louis SHELTON ,  Arvind RAJPAL

IPC: A61K47/48 ,  G01N33/574 ,  C07K16/30 ,  A61K31/427

CPC classification number: A61K31/427 ,  A61K47/65 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6889 ,  A61K2039/505 ,  C07K16/3076 ,  G01N33/57492 ,  G01N2333/705

Abstract: The present invention provides transglutaminase-mediated antibody-drug conjugates with high anti-body-drug ratio (DAR) comprising 1) glutamine-containing tags, endogenous glutamines, and/or endogenous glutamines made reactive by antibody engineering or an engineered transglutaminase (e.g., with altered substrate specifity); and 2) amine donor agents comprising amine donor units, linkers, and agent moieties, wherein the DAR is at least about 5. The invention also provides methods of making and methods of using such higher drug loaded antibody-drug conjugates.

Abstract translation: 本发明提供了具有高抗体药物比例（DAR）的转谷氨酰胺酶介导的抗体 - 药物偶联物，其包含1）含有抗体工程或工程化转谷氨酰胺酶（例如，谷氨酰胺）的反应产生的含谷氨酰胺的标签，内源性谷氨酰胺和/或内源性谷氨酰胺， 改变底物特异性）; 和2）包含胺供体单元，接头和试剂部分的胺供体试剂，其中DAR为至少约5.本发明还提供了制备方法和使用这种高加载药物的抗体 - 药物共轭物的方法。

公开(公告)号：US20160297885A1

公开(公告)日：2016-10-13

申请号：US15085644

申请日：2016-03-30

Applicant: PFIZER INC.

Inventor： Tracy Chia-Chien KUO ,  Javier Fernando CHAPARRO RIGGERS ,  Wei CHEN ,  Amy Shaw-Ru CHEN ,  Edward Derrick PASCUA ,  Thomas John VAN BLARCOM ,  Leila Marie BOUSTANY ,  Weihsien HO ,  Yik Andy YEUNG ,  Pavel STROP ,  Arvind RAJPAL

IPC: C07K16/28 ,  A61K31/704 ,  A61K38/07 ,  A61K38/05 ,  A61K39/395 ,  A61K31/454

CPC classification number: C07K16/2878 ,  A61K31/454 ,  A61K31/69 ,  A61K31/704 ,  A61K39/3955 ,  A61K39/39558 ,  A61K47/6801 ,  A61K47/6849 ,  A61K2039/505 ,  C07K16/2803 ,  C07K16/2809 ,  C07K2317/21 ,  C07K2317/31 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/73 ,  C07K2317/732 ,  C07K2317/92 ,  A61K2300/00

Abstract: The present invention relates to antibodies, e.g., full length antibodies or antigen binding fragments thereof, that specifically bind to BCMA (B-Cell Maturation Antigen) and/or CD3 (Cluster of Differentiation 3). The invention also relates to antibody conjugates (e.g., antibody-drug-conjugates) comprising the BCMA antibodies, compositions comprising the BCMA antibodies, and methods of using the BCMA antibodies and their conjugates for treating conditions associated with cells expressing BCMA (e.g., cancer or autoimmune disease). The invention further relates to heteromultimeric antibodies that specifically bind to CD3 and a tumor cell antigen, (e.g., bispecific antibodies that specifically bind to CD3 and BCMA). Compositions comprising such heteromultimeric antibodies, methods for producing and purifying such heterodimeric antibodies, and their use in diagnostics and therapeutics are also provided.

Abstract translation: 本发明涉及特异性结合BCMA（B细胞成熟抗原）和/或CD3（分化群3）的抗体，例如全长抗体或其抗原结合片段。 本发明还涉及包含BCMA抗体的抗体缀合物（例如，抗体 - 药物偶联物），包含BCMA抗体的组合物，以及使用BCMA抗体及其缀合物治疗与表达BCMA的细胞相关的病症的方法（例如癌症或 自身免疫性疾病）。 本发明还涉及特异性结合CD3和肿瘤细胞抗原的异源多聚体抗体（例如，特异性结合CD3和BCMA的双特异性抗体）。 还提供了包含这种异源多聚体抗体的组合物，用于产生和纯化此类异二聚体抗体的方法及其在诊断和治疗中的应用。

公开(公告)号：US20240018252A1

公开(公告)日：2024-01-18

申请号：US18456399

申请日：2023-08-25

Applicant: PFIZER INC.

Inventor： Tracy Chia-Chien KUO ,  Javier Fernando CHAPARRO RIGGERS ,  Wei CHEN ,  Amy Shaw-Ru CHEN ,  Edward Derrick PASCUA ,  Thomas John VAN BLARCOM ,  Leila Marie BOUSTANY ,  Weihsien HO ,  Yik Andy YEUNG ,  Pavel STROP ,  Arvind RAJPAL

IPC: C07K16/28 ,  A61K31/454 ,  A61K39/395 ,  A61K38/07 ,  A61P35/00 ,  A61K31/704

CPC classification number: C07K16/2878 ,  C07K16/2809 ,  A61K31/454 ,  A61K39/3955 ,  A61K38/07 ,  A61P35/00 ,  A61K31/704 ,  C07K2317/31 ,  A61K39/00

Abstract: The present invention relates to antibodies, e.g., full length antibodies or antigen binding fragments thereof, that specifically bind to BCMA (B-Cell Maturation Antigen) and/or CD3 (Cluster of Differentiation 3). The invention also relates to antibody conjugates (e.g., antibody-drug-conjugates) comprising the BCMA antibodies, compositions comprising the BCMA antibodies, and methods of using the BCMA antibodies and their conjugates for treating conditions associated with cells expressing BCMA (e.g., cancer or autoimmune disease). The invention further relates to heteromultimeric antibodies that specifically bind to CD3 and a tumor cell antigen, (e.g., bispecific antibodies that specifically bind to CD3 and BCMA). Compositions comprising such heteromultimeric antibodies, methods for producing and purifying such heterodimeric antibodies, and their use in diagnostics and therapeutics are also provided.

公开(公告)号：US20180298108A1

公开(公告)日：2018-10-18

申请号：US16017974

申请日：2018-06-25

Applicant: PFIZER INC.

Inventor： Tracy Chia-Chien KUO ,  Javier Fernando CHAPARRO RIGGERS ,  Wei CHEN ,  Amy Shaw-Ru CHEN ,  Edward Derrick PASCUA ,  Thomas John VAN BLARCOM ,  Leila Marie BOUSTANY ,  Weihsien HO ,  Yik Andy YEUNG ,  Pavel STROP ,  Arvind RAJPAL

IPC: C07K16/28 ,  A61K39/395 ,  A61K31/704 ,  A61K31/454 ,  A61K47/68

Abstract: The present invention relates to antibodies, e.g., full length antibodies or antigen binding fragments thereof, that specifically bind to BCMA (B-Cell Maturation Antigen) and/or CD3 (Cluster of Differentiation 3). The invention also relates to antibody conjugates (e.g., antibody-drug-conjugates) comprising the BCMA antibodies, compositions comprising the BCMA antibodies, and methods of using the BCMA antibodies and their conjugates for treating conditions associated with cells expressing BCMA (e.g., cancer or autoimmune disease). The invention further relates to heteromultimeric antibodies that specifically bind to CD3 and a tumor cell antigen, (e.g., bispecific antibodies that specifically bind to CD3 and BCMA). Compositions comprising such heteromultimeric antibodies, methods for producing and purifying such heterodimeric antibodies, and their use in diagnostics and therapeutics are also provided.

公开(公告)号：US20150307551A1

公开(公告)日：2015-10-29

申请号：US14793942

申请日：2015-07-08

Applicant: PFIZER INC.

Inventor： Matthew David DOROSKI ,  Andreas MADERNA ,  Christopher John O'DONNELL ,  Chakrapani SUBRAMANYAM ,  Beth VETELINO ,  Russell George DUSHIN ,  Pavel STROP ,  Edmund Idris GRAZIANI

IPC: C07K7/06

CPC classification number: C07K7/06 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K47/6803 ,  A61K47/6811 ,  A61K47/6851 ,  A61K47/6855 ,  A61K47/6863 ,  A61K47/6889 ,  C07K5/0205 ,  C07K5/0808 ,  C07K7/02 ,  C07K16/00 ,  C07K2319/30

Abstract: The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.

Abstract translation: 本发明涉及细胞毒性五肽，其抗体药物偶联物及其用于治疗癌症的方法。