JPWO2020056232A5 - - Google Patents

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JPWO2020056232A5
JPWO2020056232A5 JP2021514070A JP2021514070A JPWO2020056232A5 JP WO2020056232 A5 JPWO2020056232 A5 JP WO2020056232A5 JP 2021514070 A JP2021514070 A JP 2021514070A JP 2021514070 A JP2021514070 A JP 2021514070A JP WO2020056232 A5 JPWO2020056232 A5 JP WO2020056232A5
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JP2022500431A (en
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(i)１－ベンジル－６－（３，５－ジメチルイソオキサゾル－４－イル）－Ｎ－メチル－１Ｈ－イミダゾ［４，５－ｂ］ピリジン－２－アミン（化合物Ｉ）、１－ベンジル－６－（３，５－ジメチルイソオキサゾル－４－イル）－１Ｈ－イミダゾ［４，５－ｂ］ピリジン－２－アミン、およびその薬学的に許容可能な塩／共結晶から選択されるＢＥＴブロモドメイン阻害剤を含む第一医薬組成物と、(ii)第二の治療剤を含む第二医薬組成物を含む、それを必要とする対象の前立腺がんを治療するための医薬組成物の組み合わせ。 (i) 1-benzyl-6-(3,5-dimethylisoxazol-4-yl)-N-methyl-1H-imidazo[4,5-b]pyridin-2-amine (compound I), 1- benzyl-6-(3,5-dimethylisoxazol-4-yl)-1H-imidazo[4,5-b]pyridin-2-amine, and pharmaceutically acceptable salts/co-crystals thereof; and (ii) a second pharmaceutical composition comprising a second therapeutic agent for treating prostate cancer in a subject in need thereof. combination of things. 前記ＢＥＴブロモドメイン阻害剤が、化合物Ｉである、請求項１に記載の医薬組成物の組み合わせ。 2. A pharmaceutical composition combination according to claim 1, wherein said BET bromodomain inhibitor is Compound I. 前記ＢＥＴブロモドメイン阻害剤が、化合物Ｉの形態Ｉのメシル酸塩／共結晶である、請求項１または請求項２に記載の医薬組成物の組み合わせ。 3. The pharmaceutical composition combination of claim 1 or claim 2, wherein said BET bromodomain inhibitor is Form I mesylate/co-crystal of Compound I. 前記第二の治療剤がアンドロゲン受容体拮抗薬である、請求項１～３のいずれか一項に記載の医薬組成物の組み合わせ。 A pharmaceutical composition combination according to any one of claims 1 to 3, wherein said second therapeutic agent is an androgen receptor antagonist. 前記第二の治療剤がアンドロゲン合成阻害剤である、請求項１～３のいずれか一項に記載の医薬組成物の組み合わせ。 A pharmaceutical composition combination according to any one of claims 1 to 3, wherein said second therapeutic agent is an androgen synthesis inhibitor. 前記第二の治療剤がエンザルタミドである、請求項１～３のいずれか一項に記載の医薬組成物の組み合わせ。 A pharmaceutical composition combination according to any one of claims 1 to 3, wherein said second therapeutic agent is enzalutamide. 前記第二の治療剤がアパルタミドである、請求項１～３のいずれか一項に記載の医薬組成物の組み合わせ。 A combination pharmaceutical composition according to any one of claims 1 to 3, wherein said second therapeutic agent is apalutamide. 前記第二の治療剤がアビラテロンである、請求項１～３のいずれか一項に記載の医薬組成物の組み合わせ。 A combination pharmaceutical composition according to any one of claims 1 to 3, wherein said second therapeutic agent is abiraterone. 前記前立腺がんが、去勢抵抗性前立腺がんまたは転移性去勢抵抗性前立腺がんである、請求項１～８のいずれか一項に記載の医薬組成物の組み合わせ。 The combination of pharmaceutical compositions according to any one of claims 1 to 8, wherein said prostate cancer is castration-resistant prostate cancer or metastatic castration-resistant prostate cancer. 前記対象が以前に前立腺がん療法で治療されている、請求項１～９のいずれか一項に記載の医薬組成物の組み合わせ。 A combination of pharmaceutical compositions according to any one of claims 1 to 9, wherein said subject has been previously treated with prostate cancer therapy. 前記前立腺がん療法がアンドロゲン遮断療法である、請求項１０に記載の医薬組成物の組み合わせ。 11. A combination pharmaceutical composition according to claim 10, wherein said prostate cancer therapy is androgen deprivation therapy. 前記対象が以前に、アンドロゲン遮断療法で疾患の進行を示していた、請求項１１に記載の医薬組成物の組み合わせ。 12. The combination of pharmaceutical compositions according to claim 11, wherein said subject has previously shown disease progression on androgen deprivation therapy. 前記対象が以前に、アンドロゲン遮断療法で治療されていなかった、請求項１～１０のいずれか一項に記載の医薬組成物の組み合わせ。 The combination of pharmaceutical compositions according to any one of claims 1 to 10, wherein said subject has not been previously treated with androgen deprivation therapy. 前記アンドロゲン遮断療法が、エンザルタミド、アパルタミド、またはアビラテロンである、請求項１１または１２に記載の医薬組成物の組み合わせ。 13. A pharmaceutical composition combination according to claim 11 or 12, wherein said androgen deprivation therapy is enzalutamide, apalutamide or abiraterone. 第二医薬組成物がアンドロゲン遮断療法を含み、第一医薬組成物と第二医薬組成物が用量制限毒性として血小板減少症を引き起こすことなく投与されうる、請求項１に記載の医薬組成物の組み合わせ。 2. The combination of pharmaceutical compositions according to claim 1, wherein the second pharmaceutical composition comprises androgen deprivation therapy, and wherein the first pharmaceutical composition and the second pharmaceutical composition can be administered without causing thrombocytopenia as a dose limiting toxicity. . 前記アンドロゲン遮断療法が、エンザルタミド、アパルタミド、ダロルタミド、またはアビラテロンである、請求項１５に記載の医薬組成物の組み合わせ。 16. A pharmaceutical composition combination according to claim 15, wherein said androgen deprivation therapy is enzalutamide, apalutamide, darolutamide or abiraterone. 前記対象が、ＴＭＰＲＳＳ２－ＥＲＧ、ＳＬＣ４５Ａ３－ＥＲＧ、ＮＤＲＧ１－ＥＲＧ、ＤＵＸ４－ＥＲＧ、ＥＬＦ４－ＥＲＧ、ＥＬＫ４－ＥＲＧ、ＢＺＷ２－ＥＲＧ、ＣＩＤＥＣ－ＥＲＧ、ＤＹＲＫ１Ａ－ＥＲＧ、ＥＷＳＲ１－ＥＲＧ、ＦＵＳ－ＥＲＧ、ＧＭＰＲ－ＥＲＧ、ＨＥＲＰＵＤ１－ＥＲＧ、ＫＣＮＪ６－ＥＲＧ、ＺＮＲＦ３－ＥＲＧ、ＥＴＳ２－ＥＲＧ、ＥＴＶ１－ＥＲＧ、ＨＮＲＮＰＨ１－ＥＲＧ、ＰＡＫ１－ＥＲＧ、ＰＲＫＡＢ２－ＥＲＧ、ＳＭＧ６－ＥＲＧ、ＳＬＣ４５Ａ３－ＦＬＩ１、ＴＭＰＲＳＳ２－ＥＴＶ１、ＳＬＣ４５Ａ３－ＥＴＶ１、ＦＯＸＰ１－ＥＴＶ１、ＥＳＴ１４－ＥＴＶ１、ＨＥＲＶｋ１７－ＥＴＶ１、ＥＲＶＫ－２４－ＥＴＶ１、Ｃ１５ＯＲＦ２１－ＥＴＶ１、ＨＮＲＰＡ２Ｂ１－ＥＴＶ１、ＡＣＳＬ３－ＥＴＶ１、ＯＲ５１Ｅ２－ＥＴＶ１、ＥＴＶ１ Ｓ１００Ｒ、ＲＢＭ２５－ＥＴＶ１、ＡＣＰＰ－ＥＴＶ１、ＢＭＰＲ１Ｂ－ＥＴＶ１、ＣＡＮＴ１－ＥＴＶ１、ＥＲＯ１Ａ－ＥＴＶ１、ＣＰＥＤ１－ＥＴＶ１、ＨＭＧＮ２Ｐ４６－ＥＴＶ１、ＨＮＲＮＰＡ２Ｂ１－ＥＴＶ１、ＳＭＧ６－ＥＴＶ１、ＦＵＢＰ１－ＥＴＶ１、ＫＬＫ２－ＥＴＶ１、ＭＩＰＯＬ１－ ＥＴＶ１、ＳＬＣ３０Ａ４－ＥＴＶ１、ＥＷＳＲ１－ＥＴＶ１、ＴＭＰＲＳＳ２－ＥＴＶ４、ＫＬＫ２－ＥＴＶ４、ＣＡＮＴ１－ＥＴＶ４、ＤＤＸ５－ＥＴＶ４、ＵＢＴＦ－ＥＴＶ４、ＤＨＸ８－ＥＴＶ４、ＣＣＬ１６－ＥＴＶ４、ＥＤＩＬ３－ＥＴＶ４、ＥＷＳＲ１－ＥＴＶ４、ＳＬＣ４５Ａ３－ＥＴＶ４、ＵＢＴＦ－ＥＴＶ４、ＸＰＯ７－ＥＴＶ４、ＴＭＰＲＳＳ２－ＥＴＶ５、ＳＬＣ４５Ａ３－ＥＴＶ５、ＡＣＴＮ４－ ＥＴＶ５、ＥＰＧ５－ＥＴＶ５、ＬＯＣ２８４８８９－ＥＴＶ５、ＲＮＦ２１３－ＥＴＶ５、ＳＬＣ４５Ａ３－ＥＬＫ４を含む、活性化変異および／または転座のいずれかを介して、ＥＴＳ転写因子ファミリーの活性化を有する、請求項１～１０のいずれか一項に記載の医薬組成物の組み合わせ。 The subject is TMPRSS2-ERG, SLC45A3-ERG, NDRG1-ERG, DUX4-ERG, ELF4-ERG, ELK4-ERG, BZW2-ERG, CIDEC-ERG, DYRK1A-ERG, EWSR1-ERG, FUS-ERG, GMPR- ERG, HERPUD1-ERG, KCNJ6-ERG, ZNRF3-ERG, ETS2-ERG, ETV1-ERG, HNRNPH1-ERG, PAK1-ERG, PRKAB2-ERG, SMG6-ERG, SLC45A3-FLI1, TMPRSS2-ETV1, SLC45A3-ETV1, FOXP1-ETV1, EST14-ETV1, HERVk17-ETV1, ERVK-24-ETV1, C15ORF21-ETV1, HNRPA2B1-ETV1, ACSL3-ETV1, OR51E2-ETV1, ETV1 S100R, RBM25-ETV1, ACPP-ETV1, BMPR1B-ETV1, CANT1 -ETV1, ERO1A-ETV1, CPED1-ETV1, HMGN2P46-ETV1, HNRNPA2B1-ETV1, SMG6-ETV1, FUBP1-ETV1, KLK2-ETV1, MIPOL1-ETV1, SLC30A4-ETV1, EWSR1-ETV1, TMPRSS2-ETV4, KLK2-ETV4 , CANT1-ETV4, DDX5-ETV4, UBTF-ETV4, DHX8-ETV4, CCL16-ETV4, EDIL3-ETV4, EWSR1-ETV4, SLC45A3-ETV4, UBTF-ETV4, XPO7-ETV4, TMPRSS2-ETV5, SLC45A3-ETV5, ACTN4 - having activation of the ETS transcription factor family, either through activating mutations and/or translocations, including ETV5, EPG5-ETV5, LOC284889-ETV5, RNF213-ETV5, SLC45A3-ELK4, claims 1- 11. A combination of pharmaceutical compositions according to any one of 10. 前記対象が、治療４週間または８週間のいずれかでＰＳＡのスパイクを有する、請求項１～１０のいずれか一項に記載の医薬組成物の組み合わせ。 A combination of pharmaceutical compositions according to any one of claims 1 to 10, wherein said subject has a PSA spike at either 4 or 8 weeks of treatment.
JP2021514070A 2018-09-13 2019-09-13 Combination therapy for the treatment of prostate cancer Active JP7441214B2 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201862730869P 2018-09-13 2018-09-13
US62/730,869 2018-09-13
US201862737612P 2018-09-27 2018-09-27
US62/737,612 2018-09-27
US201862778185P 2018-12-11 2018-12-11
US62/778,185 2018-12-11
PCT/US2019/050970 WO2020056232A1 (en) 2018-09-13 2019-09-13 Combination therapy for the treatment of prostate cancer

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JP2022500431A JP2022500431A (en) 2022-01-04
JPWO2020056232A5 true JPWO2020056232A5 (en) 2022-09-22
JP7441214B2 JP7441214B2 (en) 2024-02-29

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US (1) US20220117942A1 (en)
EP (1) EP3849544A4 (en)
JP (1) JP7441214B2 (en)
KR (1) KR20210060515A (en)
CN (1) CN112912075B (en)
AU (1) AU2019338483A1 (en)
CA (1) CA3112396A1 (en)
IL (1) IL281281A (en)
MX (1) MX2021002884A (en)
SG (1) SG11202102492PA (en)
TW (1) TWI816880B (en)
WO (1) WO2020056232A1 (en)

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JP2024507232A (en) * 2021-02-22 2024-02-16 セルジーン・クオンティセル・リサーチ・インコーポレイテッド Bromodomain (BET) inhibitors used to treat prostate cancer
CN114644687B (en) * 2022-04-07 2023-06-27 华中科技大学同济医学院附属协和医院 Polypeptide RBIP-21 capable of antagonizing RBM25 protein RNA binding activity and application thereof

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* Cited by examiner, † Cited by third party
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GB0919434D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
JP2013537918A (en) * 2010-09-27 2013-10-07 エクセリクシス， インク． Dual inhibitors of MET and VEGF for the treatment of castration resistant prostate cancer and osteoblastic bone metastases
ES2806135T3 (en) * 2013-06-21 2021-02-16 Zenith Epigenetics Ltd New bicyclic bromodomain inhibitors
WO2015065919A1 (en) * 2013-10-28 2015-05-07 The Regents Of The University Of California Treatment of metastatic prostate cancer
NO2719005T3 (en) * 2014-07-28 2018-01-20
WO2016171470A1 (en) * 2015-04-21 2016-10-27 Kainos Medicine, Inc. Bromodomain-inhibiting compounds and methods to prevent or treat a cancer
WO2017216772A2 (en) * 2016-06-16 2017-12-21 The University Of Chicago Methods and compositions for treating breast and prostate cancer
WO2018097977A1 (en) * 2016-11-22 2018-05-31 Gilead Sciences, Inc. Crystalline forms of a phosphate complex of a bet inhibitor
US20180153867A1 (en) * 2016-12-06 2018-06-07 Gilead Sciences, Inc. Treatment of prostate cancer by concomitant administration of a bromodomain inhibitor and a second agent

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