Title:
SYK INHIBITORS
Document Type and Number:
WIPO Patent Application WO/2018/053189
Kind Code:
A3
Abstract:
The application provides methods reducing the side effects of chemotherapy and radiotherapy, including, hematopoietic toxicity, anemia, myelosuppression, pancytopenia, thrombocytopenia, neutropenia, lymphopenia, leukopenia, stomatitis and alopecia. The application provides a method for increasing the number of, neutrophil counts and platelet counts in a patient in need thereof, comprising administering an effective of an inhibitor of spleen tyrosine kinase (SYKi). The present application provides methods for treating myelosuppresive disorders by the administration of a SYKi. In certain embodiments, the myelosuppression is induced by the administration of one or more myelosuppressive agents, for example, anti-cancer drugs. The present application provides methods for treating AML/ALL in a patient with 11q23/MLL abnormalities comprising the step of administering an effective amount of a SYKi to said patient.
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Inventors:
ABELLA ESTEBAN M (US)
RAO ARATI V (US)
MARCONDES ANTONIO MARIO QUERIDO (US)
RAO ARATI V (US)
MARCONDES ANTONIO MARIO QUERIDO (US)
Application Number:
PCT/US2017/051648
Publication Date:
April 26, 2018
Filing Date:
September 14, 2017
Export Citation:
Assignee:
GILEAD SCIENCES INC (US)
International Classes:
A61K31/5377; A61K31/437; A61K31/4985; A61K31/506; A61K31/5383; A61K45/06; A61P25/04
Domestic Patent References:
| WO2015100217A1 | 2015-07-02 | |||
| WO2009029682A1 | 2009-03-05 |
Foreign References:
| US20150150881A1 | 2015-06-04 | |||
| US20150038504A1 | 2015-02-05 | |||
| EP2010181A1 | 2009-01-07 |
Other References:
J. W. FRIEDBERG ET AL: "Inhibition of Syk with fostamatinib disodium has significant clinical activity in non-Hodgkin lymphoma and chronic lymphocytic leukemia", BLOOD, vol. 115, no. 13, 1 April 2010 (2010-04-01), pages 2578 - 2585, XP055213215, ISSN: 0006-4971, DOI: 10.1182/blood-2009-08-236471
SHARMAN ET AL: "Phase 2 Trial of Entospletinib (GS-9973), a Selective SYK Inhibitor, in Follicular Lymphoma (FL) | Blood Journal", BLOOD 2014; 124: 4419, 1 January 2014 (2014-01-01), XP055426011, Retrieved from the Internet [retrieved on 20171116]
FATIH M. UCKUN ET AL: "Liposomal Nanoparticles of a Spleen Tyrosine Kinase P-Site Inhibitor Amplify the Potency of Low Dose Total Body Irradiation Against Aggressive B-Precursor Leukemia and Yield Superior Survival Outcomes in Mice", EBIOMEDICINE, vol. 2, no. 6, 1 June 2015 (2015-06-01), pages 554 - 562, XP055453936, ISSN: 2352-3964, DOI: 10.1016/j.ebiom.2015.04.005
A WALKER ET AL: "Interim Results of a Phase 1b/2 Study of Entospletinib (GS-9973) Monotherapy and in Combination with Chemotherapy in Patients with Acute Myeloid Leukemia | Blood Journal", 1 December 2016 (2016-12-01), XP055422424, Retrieved from the Internet [retrieved on 20171107]
SHARMAN ET AL: "Phase 2 Trial of Entospletinib (GS-9973), a Selective SYK Inhibitor, in Follicular Lymphoma (FL) | Blood Journal", BLOOD 2014; 124: 4419, 1 January 2014 (2014-01-01), XP055426011, Retrieved from the Internet
FATIH M. UCKUN ET AL: "Liposomal Nanoparticles of a Spleen Tyrosine Kinase P-Site Inhibitor Amplify the Potency of Low Dose Total Body Irradiation Against Aggressive B-Precursor Leukemia and Yield Superior Survival Outcomes in Mice", EBIOMEDICINE, vol. 2, no. 6, 1 June 2015 (2015-06-01), pages 554 - 562, XP055453936, ISSN: 2352-3964, DOI: 10.1016/j.ebiom.2015.04.005
A WALKER ET AL: "Interim Results of a Phase 1b/2 Study of Entospletinib (GS-9973) Monotherapy and in Combination with Chemotherapy in Patients with Acute Myeloid Leukemia | Blood Journal", 1 December 2016 (2016-12-01), XP055422424, Retrieved from the Internet
Attorney, Agent or Firm:
TANNER, Lorna L. et al. (US)
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