Title:
TROP2 ANTIBODY, PREPARATION METHOD THEREFOR, AND CONJUGATE AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/027851
Kind Code:
A1
Abstract:
A TROP2 antibody, a preparation method therefor, and a conjugate and a use thereof. The TROP2 antibody comprises a heavy-chain variable region and a light-chain variable region, the heavy-chain variable region comprising a heavy-chain CDR1, a heavy-chain CDR2, and a heavy-chain CDR3, and/or, the light-chain variable region comprising a light-chain CDR1, a light-chain CDR2, and a light-chain CDR3. The TROP2 antibody features a high affinity and a strong specificity, and a conjugate produced from coupling with a small molecule drug toxin such as MMAF is able to have a cytotoxic effect on TROP2-positive cells, and therefore can be used in the preparation of a drug for treating tumors and the like.
Inventors:
PENG FEI (CN)
QU BAOYUAN (CN)
ZHANG LI (CN)
SHENG QIRAN (CN)
YAN YUPING (CN)
CHEN HAIXIA (CN)
RUAN WENJING (CN)
YANG TATCHI TEDDY (CN)
QU BAOYUAN (CN)
ZHANG LI (CN)
SHENG QIRAN (CN)
YAN YUPING (CN)
CHEN HAIXIA (CN)
RUAN WENJING (CN)
YANG TATCHI TEDDY (CN)
Application Number:
PCT/CN2020/108720
Publication Date:
February 18, 2021
Filing Date:
August 12, 2020
Export Citation:
Assignee:
XDCEXPLORER SHANGHAI CO LTD (CN)
International Classes:
C07K16/30; A61K39/395; A61P35/00
Domestic Patent References:
| WO2019039483A1 | 2019-02-28 |
Foreign References:
| CN104053672A | 2014-09-17 | |||
| CN101679526A | 2010-03-24 | |||
| CN105849126A | 2016-08-10 | |||
| CN107446050A | 2017-12-08 |
Other References:
P. STROP, T.-T. TRAN, M. DORYWALSKA, K. DELARIA, R. DUSHIN, O. K. WONG, W.-H. HO, D. ZHOU, A. WU, E. KRAYNOV, L. ASCHENBRENNER, B.: "RN927C, a Site-Specific Trop-2 Antibody-Drug Conjugate (ADC) with Enhanced Stability, Is Highly Efficacious in Preclinical Solid Tumor Models", MOLECULAR CANCER THERAPEUTICS, vol. 15, no. 11, 1 November 2016 (2016-11-01), pages 2698 - 2708, XP055658796, ISSN: 1535-7163, DOI: 10.1158/1535-7163.MCT-16-0431
JOYCE VARUGHESE; EMILIANO COCCO; STEFANIA BELLONE; ELENA RATNER; DAN-ARIN SILASI; MASOUD AZODI; PETER E. SCHWARTZ; THOMAS J. RUTHE: "Cervical carcinomas overexpress human trophoblast cell-surface marker (Trop-2) and are highly sensitive to immunotherapy with hRS7, a humanized monoclonal anti-Trop-2 antibody", AMERICAN JOURNAL OF OBSTETRICS & GYNECOLOGY, vol. 205, no. 6, 29 June 2011 (2011-06-29), MOSBY, ST LOUIS, MO, US, pages 567.e1 - 567.e7, XP028116550, ISSN: 0002-9378, DOI: 10.1016/j.ajog.2011.06.093
LIU JINRONG, BAI LUYUE; TANG QI; WANG YIQUAN; YE CHUNPING; YIN ZHENGNA; ZHU JIN; FENG ZHENQING; TONG HUA; ZHANG HUILIN: "Preparation of a full human anti-Trop-2 IgG and its effect on ovarian cancer cells", ACTA UNIVERSITATIS MEDICINALIS NANJING(NATURAL SCIENCE), NANJING UNIVERSITY, CN, 15 March 2016 (2016-03-15), CN, pages 280 - 286, XP055781679, ISSN: 1007-4368
BARDIA ADITYA, MAYER INGRID A., DIAMOND JENNIFER R., MOROOSE REBECCA L., ISAKOFF STEVEN J., STARODUB ALEXANDER N., SHAH NIKITA C.,: "Efficacy and Safety of Anti-Trop-2 Antibody Drug Conjugate Sacituzumab Govitecan (IMMU-132) in Heavily Pretreated Patients With Metastatic Triple-Negative Breast Cancer", JOURNAL OF CLINICAL ONCOLOGY, vol. 35, no. 19, 1 July 2017 (2017-07-01), American Society of Clinical Oncology, US, pages 2141 - 2148, XP055781665, ISSN: 0732-183X, DOI: 10.1200/JCO.2016.70.8297
LIANG JIE, LIU QIONG-QIONG, ZHANG HUI-LIN, LIN HONG, TANG QI, LIU YU, SU YI-PING, FENG ZHEN-QING, ZHU JIN: "Preparation and immunologic characterization of a monoclonal antibody against human trophoblast cell-surface antigen 2", ACTA UNIVERSITATIS MEDICINALIS NANJING(NATURAL SCIENCE), NANJING UNIVERSITY, CN, vol. 31, no. 5, 15 May 2011 (2011-05-15), CN, pages 645 - 650, XP055781662, ISSN: 1007-4368
STARODUB ALEXANDER N., OCEAN ALLYSON J., SHAH MANISH A., GUARINO MICHAEL J., PICOZZI VINCENT J., VAHDAT LINDA T., THOMAS SAJEVE S.: "First-in-Human Trial of a Novel Anti-Trop-2 Antibody-SN-38 Conjugate, Sacituzumab Govitecan, for the Treatment of Diverse Metastatic Solid Tumors", CLINICAL CANCER RESEARCH, vol. 21, no. 17, 1 September 2015 (2015-09-01), American Association for Cancer Research, US, pages 3870 - 3878, XP055781655, ISSN: 1078-0432, DOI: 10.1158/1078-0432.CCR-14-3321
JOYCE VARUGHESE; EMILIANO COCCO; STEFANIA BELLONE; ELENA RATNER; DAN-ARIN SILASI; MASOUD AZODI; PETER E. SCHWARTZ; THOMAS J. RUTHE: "Cervical carcinomas overexpress human trophoblast cell-surface marker (Trop-2) and are highly sensitive to immunotherapy with hRS7, a humanized monoclonal anti-Trop-2 antibody", AMERICAN JOURNAL OF OBSTETRICS & GYNECOLOGY, vol. 205, no. 6, 29 June 2011 (2011-06-29), MOSBY, ST LOUIS, MO, US, pages 567.e1 - 567.e7, XP028116550, ISSN: 0002-9378, DOI: 10.1016/j.ajog.2011.06.093
LIU JINRONG, BAI LUYUE; TANG QI; WANG YIQUAN; YE CHUNPING; YIN ZHENGNA; ZHU JIN; FENG ZHENQING; TONG HUA; ZHANG HUILIN: "Preparation of a full human anti-Trop-2 IgG and its effect on ovarian cancer cells", ACTA UNIVERSITATIS MEDICINALIS NANJING(NATURAL SCIENCE), NANJING UNIVERSITY, CN, 15 March 2016 (2016-03-15), CN, pages 280 - 286, XP055781679, ISSN: 1007-4368
BARDIA ADITYA, MAYER INGRID A., DIAMOND JENNIFER R., MOROOSE REBECCA L., ISAKOFF STEVEN J., STARODUB ALEXANDER N., SHAH NIKITA C.,: "Efficacy and Safety of Anti-Trop-2 Antibody Drug Conjugate Sacituzumab Govitecan (IMMU-132) in Heavily Pretreated Patients With Metastatic Triple-Negative Breast Cancer", JOURNAL OF CLINICAL ONCOLOGY, vol. 35, no. 19, 1 July 2017 (2017-07-01), American Society of Clinical Oncology, US, pages 2141 - 2148, XP055781665, ISSN: 0732-183X, DOI: 10.1200/JCO.2016.70.8297
LIANG JIE, LIU QIONG-QIONG, ZHANG HUI-LIN, LIN HONG, TANG QI, LIU YU, SU YI-PING, FENG ZHEN-QING, ZHU JIN: "Preparation and immunologic characterization of a monoclonal antibody against human trophoblast cell-surface antigen 2", ACTA UNIVERSITATIS MEDICINALIS NANJING(NATURAL SCIENCE), NANJING UNIVERSITY, CN, vol. 31, no. 5, 15 May 2011 (2011-05-15), CN, pages 645 - 650, XP055781662, ISSN: 1007-4368
STARODUB ALEXANDER N., OCEAN ALLYSON J., SHAH MANISH A., GUARINO MICHAEL J., PICOZZI VINCENT J., VAHDAT LINDA T., THOMAS SAJEVE S.: "First-in-Human Trial of a Novel Anti-Trop-2 Antibody-SN-38 Conjugate, Sacituzumab Govitecan, for the Treatment of Diverse Metastatic Solid Tumors", CLINICAL CANCER RESEARCH, vol. 21, no. 17, 1 September 2015 (2015-09-01), American Association for Cancer Research, US, pages 3870 - 3878, XP055781655, ISSN: 1078-0432, DOI: 10.1158/1078-0432.CCR-14-3321
Attorney, Agent or Firm:
SHANGHAI BESHINING LAW OFFICE (CN)
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