Patent application EP16194112A (EP), filed 2016-10-17
Publication number: EP3159007A1
Title: PHARMACEUTICAL COMPOSITION FOR TREATING RHEUMATOID ARTHRITIS
Abstract: An object of the present invention is to provide a pharmaceutical composition comprising an anti-fractalkine antibody, wherein the pharmaceutical composition brings about therapeutically effective amelioration in rheumatoid arthritis after administration to a human subject. The present invention provides a pharmaceutical composition for the treatment of rheumatoid arthritis. The pharmaceutical composition comprises an anti-fractalkine antibody and a pharmaceutically acceptable excipient and is used such that at least 100 mg per dose of the anti-fractalkine antibody is subcutaneously administered to a human in need thereof.
IPC codes: A61K  39/    00            A I
A61K  39/   395            A I
C07K  16/    24            A I
Claims: number: 1
text: A pharmaceutical composition for the treatment of rheumatoid arthritis,
the pharmaceutical composition comprising an anti-fractalkine antibody and a pharmaceutically acceptable excipient, wherein
the anti-fractalkine antibody is an antibody wherein:
number: 2
text: The pharmaceutical composition according to claim 1, wherein
the pharmaceutical composition is used such that 100 mg to 400 mg per dose of the anti-fractalkine antibody is subcutaneously administered to a human.
number: 3
text: The pharmaceutical composition according to claim 1, wherein
the pharmaceutical composition is used such that 100 mg, 200 mg, or 400 mg per dose of the anti-fractalkine antibody is subcutaneously administered to a human.
number: 4
text: The pharmaceutical composition according to claim 1, wherein
when 100 mg of the anti-fractalkine antibody is subcutaneously administered by a single administration to a human,
mean C<max> is a value that falls within the numerical range of 80% to 125% of 10 µg/mL,
mean AUC<(0-336h)> is a value that falls within the numerical range of 80% to 125% of 2.4 × 10<3> µg·h/mL, or
mean AUC<(0-t)> is a value that falls within the numerical range of 80% to 125% of 3.0 × 10<3> µg·h/mL.
number: 5
text: The pharmaceutical composition according to claim 1, wherein
when 200 mg of the anti-fractalkine antibody is subcutaneously administered by a single administration to a human,
mean C<max> is a value that falls within the numerical range of 80% to 125% of 27 µg/mL,
mean AUC<(0-336h)> is a value that falls within the numerical range of 80% to 125% of 7.4 × 10<3> µg·h/mL, or
mean AUC<(0-t)> is a value that falls within the numerical range of 80% to 125% of 1.2 × 10<4> µg·h/mL.
number: 6
text: The pharmaceutical composition according to claim 1, wherein
when 400 mg of the anti-fractalkine antibody is subcutaneously administered by a single administration to a human,
mean C<max> is a value that falls within the numerical range of 80% to 125% of 43 µg/mL,
mean AUC<(0-336h)> is a value that falls within the numerical range of 80% to 125% of 1.2 × 10<4> µg·h/mL, or
mean AUC<(0-t)> is a value that falls within the numerical range of 80% to 125% of 2.7 × 10<4> µg·h/mL.
number: 7
text: The pharmaceutical composition according to claim 1, wherein
the pharmaceutical composition is subcutaneously administered by multiple administrations at dosing intervals of once a week to once every two weeks.
number: 8
text: The pharmaceutical composition according to any one of claims 1 to 7, wherein
the pharmaceutical composition is subcutaneously administered such that the mean trough concentration of the anti-fractalkine antibody is 10 µg/mL or higher.
number: 9
text: The pharmaceutical composition according to any one of claims 1 to 7, wherein
the pharmaceutical composition is subcutaneously administered such that the mean trough concentration of the anti-fractalkine antibody is 20 µg/mL or higher.
number: 10
text: A therapeutic agent for rheumatoid arthritis, comprising an anti-fractalkine antibody, wherein
the therapeutic agent for rheumatoid arthritis is used such that 100 mg to 400 mg of the anti-fractalkine antibody is subcutaneously administered at dosing intervals of once a week to once every two weeks to a human, and
the anti-fractalkine antibody is an antibody wherein:
Office action: search_report, dated 2017-04-26
Rejection reasons: novelty_epc_54
inventive_step_epc_56
Prior art cited: ref_id: WO2006046739A1
ref_type: patent
severity: background
ref_id: WO2011052799A1
ref_type: patent
severity: background
ref_id: - J IMMUNOL., vol. 173, 2004, pages 7010 - 7016
ref_type: npl
severity: background
ref_id: WO2011052799A1
ref_type: patent
severity: background
ref_id: - "Monoclonal Antibodies", 1 January 2015, ELSEVIER, ISBN: 978-0-08-100296-4, article STEVEN J. SHIRE: "Challenges in the subcutaneous (SC) administration of monoclonal antibodies (mAbs)", pages: 131 - 138, XP055344541, DOI: 10.1016/B978-0-08-100296-4.00006-3
ref_type: npl
severity: background
ref_id: - "Therapeutic Fc-Fusion Proteins", 19 February 2014, WILEY-VCH VERLAG GMBH & CO. KGAA, Weinheim, Germany, ISBN: 978-3-52-733317-2, article ARVIND RAJPAL ET AL: "Introduction: Antibody Structure and Function", pages: 1 - 44, XP055198075, DOI: 10.1002/9783527675272.ch01
ref_type: npl
severity: background
ref_id: - TANAKA YOSHIYA ET AL: "Safety and Efficacy of E6011, an Anti-Fractalkine Monoclonal Antibody, in a First-in-Patient Phase 1/2 Study in Rheumatoid Arthritis", ARTHRITIS & RHEUMATOLOGY (HOBOKEN), JOHN WILEY & SONS, INC, US, vol. 67, no. Suppl.10, 27 October 2015 (2015-10-27), XP009193437, ISSN: 2326-5191
ref_type: npl
severity: background
ref_id: - TABUCHI H ET AL: "FIRST-IN-HUMAN (FIH) STUDY OF E6011, A NOVEL HUMANIZED ANTI-FRACTALKINE (CX3CL1) MONOCLONAL ANTIBODY", CLINICAL PHARMACOLOGY & THERAPEUTICS, vol. 99, no. Suppl. 1, February 2016 (2016-02-01), & ANNUAL MEETING OF THE AMERICAN-SOCIETY-FOR-CLINICAL-PHARMACOLOGY-AND-THERAPEUTICS (ASCPT); SAN DIEGO, CA, USA; MARCH 08 -12, 2016, pages S33, XP055344618
ref_type: npl
severity: background
ref_id: - NANKI T ET AL: "Inhibition of fractalkine ameliorates murine collagen-induced arthritis", THE JOURNAL OF IMMUNOLOGY, THE AMERICAN ASSOCIATION OF IMMUNOLOGISTS, US, vol. 173, no. 11, 1 December 2004 (2004-12-01), pages 7010 - 7016, XP002996170, ISSN: 0022-1767
ref_type: npl
severity: background
ref_id: - B. A. JONES ET AL: "Fractalkine/CX3CL1: A Potential New Target for Inflammatory Diseases", MOLECULAR INTERVENTIONS, vol. 10, no. 5, 1 October 2010 (2010-10-01), BETHESDA,MD, US, pages 263 - 270, XP055513674, ISSN: 1534-0384, DOI: 10.1124/mi.10.5.3
* the whole document *
ref_type: npl
severity: background
ref_id: - B. A. JONES ET AL: "Fractalkine/CX3CL1: A Potential New Target for Inflammatory Diseases", MOLECULAR INTERVENTIONS, vol. 10, no. 5, 1 October 2010 (2010-10-01), BETHESDA,MD, US, pages 263 - 270, XP055513674, ISSN: 1534-0384, DOI: 10.1124/mi.10.5.3
ref_type: npl
severity: background
ref_id: WO2011052799
ref_type: patent
severity: obviousness
ref_id: - Steven J. Shire, "Challenges in the subcutaneous (SC) administration of monoclonal antibodies (mAbs)", Monoclonal Antibodies, Elsevier, (20150101), pages 131 - 138, doi:10.1016/B978-0-08-100296-4.00006-3, ISBN 978-0-08-100296-4, XP055344541 [Y] 1-10 * the whole document *
ref_type: npl
severity: obviousness
ref_id: - Arvind Rajpal ET AL, "Introduction: Antibody Structure and Function", Therapeutic Fc-Fusion Proteins, Weinheim, Germany, Wiley-VCH Verlag GmbH & Co. KGaA, (20140219), pages 1 - 44, doi:10.1002/9783527675272.ch01, ISBN 978-3-52-733317-2, XP055198075 [Y] 1-10 * table 1.6 *
ref_type: npl
severity: obviousness
ref_id: - TANAKA YOSHIYA ET AL, "Safety and Efficacy of E6011, an Anti-Fractalkine Monoclonal Antibody, in a First-in-Patient Phase 1/2 Study in Rheumatoid Arthritis", ARTHRITIS & RHEUMATOLOGY (HOBOKEN), JOHN WILEY & SONS, INC, US, (20151027), vol. 67, no. Suppl.10, ISSN 2326-5191, XP009193437 [XP] 1-10 * the whole document *
ref_type: npl
severity: novelty_destroying
ref_id: - TABUCHI H ET AL, "FIRST-IN-HUMAN (FIH) STUDY OF E6011, A NOVEL HUMANIZED ANTI-FRACTALKINE (CX3CL1) MONOCLONAL ANTIBODY", CLINICAL PHARMACOLOGY & THERAPEUTICS, & ANNUAL MEETING OF THE AMERICAN-SOCIETY-FOR-CLINICAL-PHARMACOLOGY-AND-THERAPEUTICS (ASCPT); SAN DIEGO, CA, USA; MARCH 08 -12, 2016, (201602), vol. 99, no. Suppl. 1, page S33, XP055344618 [XP] 1-10 * the whole document *
ref_type: npl
severity: novelty_destroying
Final disposition: pending (2017-04-26)