JP2015506961A5 - - Google Patents
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- JP2015506961A5 JP2015506961A5 JP2014555801A JP2014555801A JP2015506961A5 JP 2015506961 A5 JP2015506961 A5 JP 2015506961A5 JP 2014555801 A JP2014555801 A JP 2014555801A JP 2014555801 A JP2014555801 A JP 2014555801A JP 2015506961 A5 JP2015506961 A5 JP 2015506961A5
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- JP
- Japan
- Prior art keywords
- renal cell
- cell carcinoma
- optionally
- therapeutic agent
- therapeutic
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 208000006265 Renal Cell Carcinoma Diseases 0.000 claims 23
- 239000003814 drug Substances 0.000 claims 11
- 230000027455 binding Effects 0.000 claims 10
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims 8
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims 8
- 230000002401 inhibitory effect Effects 0.000 claims 7
- 101710027366 ACVRL1 Proteins 0.000 claims 6
- 239000003112 inhibitor Substances 0.000 claims 6
- 230000001225 therapeutic Effects 0.000 claims 6
- 241000124008 Mammalia Species 0.000 claims 5
- 102000004965 antibodies Human genes 0.000 claims 5
- 108090001123 antibodies Proteins 0.000 claims 5
- 102100007311 BMP10 Human genes 0.000 claims 4
- 101700058635 BMP10 Proteins 0.000 claims 4
- 102100003277 GDF2 Human genes 0.000 claims 4
- 101700046122 GDF2 Proteins 0.000 claims 4
- 150000001413 amino acids Chemical class 0.000 claims 4
- 229920001184 polypeptide Polymers 0.000 claims 4
- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims 3
- HKVAMNSJSFKALM-XJFKSLPYSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)C(C)=C[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-XJFKSLPYSA-N 0.000 claims 3
- 239000002147 L01XE04 - Sunitinib Substances 0.000 claims 3
- 239000005511 L01XE05 - Sorafenib Substances 0.000 claims 3
- 239000003798 L01XE11 - Pazopanib Substances 0.000 claims 3
- 239000002118 L01XE12 - Vandetanib Substances 0.000 claims 3
- WINHZLLDWRZWRT-ATVHPVEESA-N Sunitinib Chemical compound CCN(CC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C WINHZLLDWRZWRT-ATVHPVEESA-N 0.000 claims 3
- CBPNZQVSJQDFBE-FUXHJELOSA-N Temsirolimus Chemical compound C1C[C@@H](OC(=O)C(C)(CO)CO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 CBPNZQVSJQDFBE-FUXHJELOSA-N 0.000 claims 3
- SPMVMDHWKHCIDT-UHFFFAOYSA-N Tivozanib Chemical compound C=12C=C(OC)C(OC)=CC2=NC=CC=1OC(C=C1Cl)=CC=C1NC(=O)NC=1C=C(C)ON=1 SPMVMDHWKHCIDT-UHFFFAOYSA-N 0.000 claims 3
- UHTHHESEBZOYNR-UHFFFAOYSA-N Vandetanib Chemical compound COC1=CC(C(/N=CN2)=N/C=3C(=CC(Br)=CC=3)F)=C2C=C1OCC1CCN(C)CC1 UHTHHESEBZOYNR-UHFFFAOYSA-N 0.000 claims 3
- 229960003005 axitinib Drugs 0.000 claims 3
- RITAVMQDGBJQJZ-FMIVXFBMSA-N axitinib Chemical compound CNC(=O)C1=CC=CC=C1SC1=CC=C(C(\C=C\C=2N=CC=CC=2)=NN2)C2=C1 RITAVMQDGBJQJZ-FMIVXFBMSA-N 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 229960005167 everolimus Drugs 0.000 claims 3
- 239000003446 ligand Substances 0.000 claims 3
- 229960000639 pazopanib Drugs 0.000 claims 3
- CUIHSIWYWATEQL-UHFFFAOYSA-N pazopanib Chemical compound C1=CC2=C(C)N(C)N=C2C=C1N(C)C(N=1)=CC=NC=1NC1=CC=C(C)C(S(N)(=O)=O)=C1 CUIHSIWYWATEQL-UHFFFAOYSA-N 0.000 claims 3
- 229960003787 sorafenib Drugs 0.000 claims 3
- 229960001796 sunitinib Drugs 0.000 claims 3
- 229960000235 temsirolimus Drugs 0.000 claims 3
- 229960000940 tivozanib Drugs 0.000 claims 3
- 229960000241 vandetanib Drugs 0.000 claims 3
- 101700016442 GDF5 Proteins 0.000 claims 2
- 102100003274 GDF5 Human genes 0.000 claims 2
- 102100010135 GDF6 Human genes 0.000 claims 2
- 101700040898 GDF6 Proteins 0.000 claims 2
- 102100010137 GDF7 Human genes 0.000 claims 2
- 101700021567 GDF7 Proteins 0.000 claims 2
- 102100015972 IL2 Human genes 0.000 claims 2
- 108010002350 Interleukin-2 Proteins 0.000 claims 2
- 102000005962 receptors Human genes 0.000 claims 2
- 108020003175 receptors Proteins 0.000 claims 2
- 210000000988 Bone and Bones Anatomy 0.000 claims 1
- 210000004556 Brain Anatomy 0.000 claims 1
- 101700046422 IFNA Proteins 0.000 claims 1
- 102000018358 Immunoglobulins Human genes 0.000 claims 1
- 108060003951 Immunoglobulins Proteins 0.000 claims 1
- 102000006992 Interferon-alpha Human genes 0.000 claims 1
- 108010047761 Interferon-alpha Proteins 0.000 claims 1
- 210000004185 Liver Anatomy 0.000 claims 1
- 210000004072 Lung Anatomy 0.000 claims 1
- 210000001165 Lymph Nodes Anatomy 0.000 claims 1
- 206010050513 Metastatic renal cell carcinoma Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 125000003275 alpha amino acid group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 210000004027 cells Anatomy 0.000 claims 1
- 229940079593 drugs Drugs 0.000 claims 1
- 238000007912 intraperitoneal administration Methods 0.000 claims 1
- 210000003292 kidney cell Anatomy 0.000 claims 1
- 102000027656 receptor tyrosine kinases Human genes 0.000 claims 1
- 108091007921 receptor tyrosine kinases Proteins 0.000 claims 1
- 201000010174 renal carcinoma Diseases 0.000 claims 1
- 230000000268 renotropic Effects 0.000 claims 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims 1
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 claims 1
- 229940121358 tyrosine kinase inhibitors Drugs 0.000 claims 1
Claims (11)
- 受容体チロシンキナーゼ阻害剤(RTKI)と
(a) ALK1の細胞外ドメインのリガンド結合部分を含むALK1ポリペプチドであって、任意で、SEQ ID NO:1のアミノ酸22〜120の配列、SEQ ID NO:3の配列またはSEQ ID NO:14の配列と少なくとも90%同一であるアミノ酸配列を有するポリペプチドを含み、かつ任意で、GDF5、GDF6、GDF7、BMP9、およびBMP10より選択されるALK1リガンドに結合する、ALK1ポリペプチド；
(b) ヒトALK1の細胞外ドメインに結合する抗体であって、任意で、SEQ ID NO:1のアミノ酸22〜118の配列内のエピトープに結合し、かつGDF5、GDF6、GDF7、BMP9、およびBMP10より選択されるリガンドの結合を阻害する、抗体；
(c) ヒトBMP9に結合する抗体であって、任意で、SEQ ID NO:12のアミノ酸1〜111の配列内のエピトープに結合し、かつ受容体に対するBMP9の結合を阻害する、抗体；および
(d) ヒトBMP10に結合する抗体であって、任意で、SEQ ID NO:13のアミノ酸1〜108の配列内のエピトープに結合し、かつ受容体に対するBMP10の結合を阻害する、抗体
より選択される薬剤との組み合わせを含み、哺乳動物が任意で以前に腎細胞癌(RCC)治療薬を受けている、腎細胞癌を有する哺乳動物における腎細胞癌治療剤。 - RTKIがスニチニブ、ソラフェニブ、パゾパニブ、アキシチニブ、チボザニブまたはバンデタニブである、請求項1に記載の腎細胞癌治療剤。
- 哺乳類ラパマイシン標的タンパク質(mTOR)標的阻害剤をさらに含み、mTOR標的阻害剤が、任意でエベロリムスまたはテムシロリムスである、請求項1に記載の腎細胞癌治療剤。
- 腎細胞癌が腎明細胞癌である、請求項1に記載の腎細胞癌治療剤。
- 腎細胞癌が腎洞に浸潤している、腎細胞癌が転移性腎細胞癌である、または腎細胞癌が肺、腹腔内リンパ節、骨、脳、または肝臓に転移している、請求項1に記載の腎細胞癌治療剤。
- 哺乳動物が以前にRCC治療薬を受けており、該RCC治療薬がRTKIであり、かつ以前に受けた該RTKIが、任意でスニチニブ、ソラフェニブ、パゾパニブ、アキシチニブ、チボザニブ、およびバンデタニブより選択される、請求項1に記載の腎細胞癌治療剤。
- 哺乳動物が以前にRCC治療薬を受けており、該RCC治療薬が哺乳類ラパマイシン標的タンパク質(mTOR)標的阻害剤であり、かつ以前に受けたmTOR標的阻害剤が、任意でエベロリムスおよびテムシロリムスより選択される、請求項1に記載の腎細胞癌治療剤。
- 哺乳動物が以前にRCC治療薬を受けており、以前に受けた該RCC治療薬がインターフェロンα(IFN-α)またはインターロイキン-2(IL-2)である、請求項1に記載の腎細胞癌治療剤。
- ALK1ポリペプチドが免疫グロブリンの定常ドメインまたはFc部分をさらに含み、該Fc部分が任意でヒトIgG1のFc部分である、請求項1に記載の腎細胞癌治療剤。
- RTKIをさらに含み、かつ、該RTKIが任意で、スニチニブ、ソラフェニブ、パゾパニブ、アキシチニブ、チボザニブ、およびバンデタニブより選択される薬剤である、請求項1〜9のいずれか一項に記載の腎細胞癌治療剤。
- mTOR標的阻害剤をさらに含み、かつ、該mTOR標的阻害剤が任意で、エベロリムスおよびテムシロリムスより選択される薬剤である、請求項1〜9のいずれか一項に記載の腎細胞癌治療剤。
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261593864P | 2012-02-02 | 2012-02-02 | |
| US61/593,864 | 2012-02-02 | ||
| US201261597124P | 2012-02-09 | 2012-02-09 | |
| US61/597,124 | 2012-02-09 | ||
| PCT/US2013/024510 WO2013116781A1 (en) | 2012-02-02 | 2013-02-01 | Alk1 antagonists and their uses in treating renal cell carcinoma |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015506961A JP2015506961A (ja) | 2015-03-05 |
| JP2015506961A5 true JP2015506961A5 (ja) | 2016-03-17 |
Family
ID=48903082
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014555801A Pending JP2015506961A (ja) | 2012-02-02 | 2013-02-01 | Ａｌｋ１アンタゴニストおよび腎細胞癌の治療におけるその使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20130202594A1 (ja) |
| EP (1) | EP2809335A4 (ja) |
| JP (1) | JP2015506961A (ja) |
| KR (1) | KR20140123558A (ja) |
| CN (1) | CN104321070A (ja) |
| AU (1) | AU2013214779A1 (ja) |
| BR (1) | BR112014019151A2 (ja) |
| CA (1) | CA2863188A1 (ja) |
| MX (1) | MX2014009277A (ja) |
| RU (1) | RU2633638C2 (ja) |
| WO (1) | WO2013116781A1 (ja) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10059756B2 (en) | 2006-11-02 | 2018-08-28 | Acceleron Pharma Inc. | Compositions comprising ALK1-ECD protein |
| US8642031B2 (en) | 2006-11-02 | 2014-02-04 | Acceleron Pharma, Inc. | Antagonists of BMP9, BMP10, ALK1 and other ALK1 ligands, and uses thereof |
| WO2015147908A1 (en) * | 2014-03-28 | 2015-10-01 | Acceleron Pharma, Inc. | Use of activin receptor-like kinase 1 (alk-1) antagonists in the treatment of cancer |
| JP2016036322A (ja) * | 2014-08-11 | 2016-03-22 | 日本化薬株式会社 | 血管新生因子と結合するキメラタンパク質 |
| ES2805206T3 (es) * | 2015-03-10 | 2021-02-11 | Univ Massachusetts | Enfoque dirigido a GDF6 y a señalización de BMP para la terapia contra el melanoma |
| US10047155B2 (en) | 2015-06-05 | 2018-08-14 | Novartis Ag | Antibodies targeting bone morphogenetic protein 9 (BMP9) and methods therefor |
| CN106994181A (zh) * | 2017-03-10 | 2017-08-01 | 上海交通大学医学院附属第九人民医院 | Bmp9在制备延缓肝纤维化药物中的应用 |
| WO2019173482A1 (en) * | 2018-03-06 | 2019-09-12 | Sanford Burnham Prebys Medical Discovery Institute | 4-aminoquinoline compounds for the treatment of angiogenesis |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8529014D0 (en) | 1985-11-25 | 1986-01-02 | Biogen Nv | Enhanced secretion of heterologous proteins |
| JPS63502716A (ja) | 1986-03-07 | 1988-10-13 | マサチューセッツ・インステチュート・オブ・テクノロジー | 糖タンパク安定性の強化方法 |
| US6858598B1 (en) * | 1998-12-23 | 2005-02-22 | G. D. Searle & Co. | Method of using a matrix metalloproteinase inhibitor and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia |
| TW200803842A (en) | 2005-11-04 | 2008-01-16 | Wyeth Corp | Antineoplastic combinations of temsirolimus and sunitinib malate |
| CA2656836A1 (en) | 2006-07-13 | 2008-01-17 | Zymogenetics, Inc. | Interleukin 21 and tyrosine kinase inhibitor combination therapy |
| MX2009004718A (es) * | 2006-11-02 | 2009-06-19 | Acceleron Pharma Inc | Antagonistas de receptor de alk1 y ligando y sus usos. |
| US20090017019A1 (en) * | 2007-06-01 | 2009-01-15 | Wyeth | Methods and compositions for modulating bmp-10 activity |
| CA2703099A1 (en) * | 2007-11-09 | 2009-05-14 | Genentech, Inc. | Activin receptor-like kinase-i compositions and methods of use |
| EP2280960A1 (en) | 2008-04-16 | 2011-02-09 | Natco Pharma Limited | Novel polymorphic forms of sunitinib base |
| WO2009134428A2 (en) * | 2008-05-02 | 2009-11-05 | Acceleron Pharma, Inc. | Methods and compositions for modulating angiogenesis and pericyte composition |
| US7998973B2 (en) | 2009-11-13 | 2011-08-16 | Aveo Pharmaceuticals, Inc. | Tivozanib and temsirolimus in combination |
| US20120207671A1 (en) * | 2010-04-15 | 2012-08-16 | Vegenics Pty Limited | Combination treatment with vegf-c antagonists |
-
2013
- 2013-02-01 CA CA2863188A patent/CA2863188A1/en not_active Abandoned
- 2013-02-01 WO PCT/US2013/024510 patent/WO2013116781A1/en active Application Filing
- 2013-02-01 RU RU2014134923A patent/RU2633638C2/ru not_active IP Right Cessation
- 2013-02-01 MX MX2014009277A patent/MX2014009277A/es unknown
- 2013-02-01 AU AU2013214779A patent/AU2013214779A1/en not_active Abandoned
- 2013-02-01 BR BR112014019151A patent/BR112014019151A2/pt not_active Application Discontinuation
- 2013-02-01 US US13/757,672 patent/US20130202594A1/en not_active Abandoned
- 2013-02-01 KR KR1020147024468A patent/KR20140123558A/ko not_active Application Discontinuation
- 2013-02-01 JP JP2014555801A patent/JP2015506961A/ja active Pending
- 2013-02-01 EP EP13744185.3A patent/EP2809335A4/en not_active Withdrawn
- 2013-02-01 CN CN201380013788.3A patent/CN104321070A/zh active Pending
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