Title:
ANTIBODY-SN-38 IMMUNOCONJUGATES WITH A CL2A LINKER
Document Type and Number:
WIPO Patent Application WO/2015/012904
Kind Code:
A3
Abstract:
The present invention concerns improved methods and compositions for preparing SN-38 conjugates of proteins or peptides, preferably immunoconjugates of antibodies or antigen-binding antibody fragments. More preferably, the SN-38 is attached to the antibody or antibody fragment using a CL2A linker, with 1-12, more preferably 6 or less, most preferably 1-5 SN-38 moieties per antibody or antibody fragment. Most preferably, the immunoconjugate is prepared in large scale batches, with various modifications to the reaction scheme to optimize yield and recovery in large scale. Other embodiments concern optimized dosages and/or schedules of administration of immunoconjugate to maximize efficacy for disease treatment and minimize side effects of administration.
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Inventors:
GOVINDAN SERENGULAM V (US)
GALE JONATHAN B (US)
HOLMAN NICHOLAS J (US)
GOLDENBERG DAVID M (US)
GALE JONATHAN B (US)
HOLMAN NICHOLAS J (US)
GOLDENBERG DAVID M (US)
Application Number:
PCT/US2014/034518
Publication Date:
May 07, 2015
Filing Date:
April 17, 2014
Export Citation:
Assignee:
IMMUNOMEDICS INC (US)
International Classes:
A61K31/4745; A61K39/395; A61K47/48
Domestic Patent References:
| WO2012097081A2 | 2012-07-19 |
Foreign References:
| US20120082617A1 | 2012-04-05 | |||
| CA2471717C | 2013-06-18 | |||
| US20130053334A1 | 2013-02-28 | |||
| CA2428885A1 | 2002-05-30 | |||
| US20130156691A1 | 2013-06-20 | |||
| US20060122113A1 | 2006-06-08 |
Other References:
MOON, SJ ET AL.: "Antibody Conjugates of 7-Ethyl-10-Hydroxycamptothecin (SN-38) for Targeted Cancer Chemotherapy.", JOURNAL OF MEDICAL CHEMISTRY, vol. 51, no. 21, 13 November 2008 (2008-11-13), pages 6916 - 6926, XP055044282, Retrieved from the Internet
COTARCA, L ET AL.: "Phosphogenations- a Handbook.", 2003, WEINHEIM, GERMANY, pages 1 - 656, XP008182767, Retrieved from the Internet
GROTHEY: "Survival of Patients with Advanced Colorectal Cancer Improves with the Availability of Fluorouracil- Leucovorin, Irinotecan, and Oxaliplatin in the Course of Treatment.", JOURNAL OF CLINICAL ONCOLOGY., vol. 22, no. 7, 1 April 2004 (2004-04-01), pages 1209 - 1214, XP055315179, Retrieved from the Internet
COTARCA, L ET AL.: "Phosphogenations- a Handbook.", 2003, WEINHEIM, GERMANY, pages 1 - 656, XP008182767, Retrieved from the Internet
GROTHEY: "Survival of Patients with Advanced Colorectal Cancer Improves with the Availability of Fluorouracil- Leucovorin, Irinotecan, and Oxaliplatin in the Course of Treatment.", JOURNAL OF CLINICAL ONCOLOGY., vol. 22, no. 7, 1 April 2004 (2004-04-01), pages 1209 - 1214, XP055315179, Retrieved from the Internet
Attorney, Agent or Firm:
NAKASHIMA, Richard A. (Morris Plains, New Jersey, US)
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