JP2016536282A5 - - Google Patents
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- JP2016536282A5 JP2016536282A5 JP2016519762A JP2016519762A JP2016536282A5 JP 2016536282 A5 JP2016536282 A5 JP 2016536282A5 JP 2016519762 A JP2016519762 A JP 2016519762A JP 2016519762 A JP2016519762 A JP 2016519762A JP 2016536282 A5 JP2016536282 A5 JP 2016536282A5
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- JP
- Japan
- Prior art keywords
- item
- regimen
- cancer
- administered
- pharmaceutical
- 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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- 229940124607 PI3Kα inhibitor Drugs 0.000 claims description 45
- 206010006187 Breast cancer Diseases 0.000 claims description 13
- 208000026310 Breast neoplasm Diseases 0.000 claims description 13
- 239000008194 pharmaceutical composition Substances 0.000 claims description 12
- -1 6- (2-aminobenzo [d] oxazol-5-yl) imidazo [1,2-a] pyridin-3-yl Chemical group 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 6
- 201000011510 cancer Diseases 0.000 claims description 6
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 4
- 206010014733 Endometrial cancer Diseases 0.000 claims description 3
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 3
- WSFSSNUMVMOOMR-BJUDXGSMSA-N methanone Chemical compound O=[11CH2] WSFSSNUMVMOOMR-BJUDXGSMSA-N 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 231100000682 maximum tolerated dose Toxicity 0.000 description 18
- 238000000034 method Methods 0.000 description 16
- 230000003442 weekly effect Effects 0.000 description 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 7
- 208000035475 disorder Diseases 0.000 description 7
- 238000003556 assay Methods 0.000 description 6
- 102000015694 estrogen receptors Human genes 0.000 description 6
- 108010038795 estrogen receptors Proteins 0.000 description 6
- 108091008039 hormone receptors Proteins 0.000 description 6
- 239000001257 hydrogen Substances 0.000 description 6
- 229910052739 hydrogen Inorganic materials 0.000 description 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 4
- 102000004190 Enzymes Human genes 0.000 description 4
- 108090000790 Enzymes Proteins 0.000 description 4
- 229940102550 Estrogen receptor antagonist Drugs 0.000 description 4
- VWUXBMIQPBEWFH-WCCTWKNTSA-N Fulvestrant Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC2=C1 VWUXBMIQPBEWFH-WCCTWKNTSA-N 0.000 description 4
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 description 4
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 description 4
- 125000000217 alkyl group Chemical group 0.000 description 4
- 150000001408 amides Chemical class 0.000 description 4
- 125000003118 aryl group Chemical group 0.000 description 4
- 125000000753 cycloalkyl group Chemical group 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 229960002258 fulvestrant Drugs 0.000 description 4
- 125000001072 heteroaryl group Chemical group 0.000 description 4
- 150000002431 hydrogen Chemical class 0.000 description 4
- 239000003112 inhibitor Substances 0.000 description 4
- 210000004185 liver Anatomy 0.000 description 4
- 229940124597 therapeutic agent Drugs 0.000 description 4
- 206010005003 Bladder cancer Diseases 0.000 description 3
- 206010009944 Colon cancer Diseases 0.000 description 3
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 description 3
- 206010033128 Ovarian cancer Diseases 0.000 description 3
- 206010061535 Ovarian neoplasm Diseases 0.000 description 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 description 3
- 206010060862 Prostate cancer Diseases 0.000 description 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 3
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 description 3
- 206010041067 Small cell lung cancer Diseases 0.000 description 3
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 description 3
- 208000005718 Stomach Neoplasms Diseases 0.000 description 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 3
- 208000029742 colonic neoplasm Diseases 0.000 description 3
- 206010017758 gastric cancer Diseases 0.000 description 3
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 description 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 description 3
- 230000001613 neoplastic effect Effects 0.000 description 3
- 201000002120 neuroendocrine carcinoma Diseases 0.000 description 3
- 208000002154 non-small cell lung carcinoma Diseases 0.000 description 3
- 201000002528 pancreatic cancer Diseases 0.000 description 3
- 208000008443 pancreatic carcinoma Diseases 0.000 description 3
- 102000003998 progesterone receptors Human genes 0.000 description 3
- 108090000468 progesterone receptors Proteins 0.000 description 3
- 208000015347 renal cell adenocarcinoma Diseases 0.000 description 3
- 208000000587 small cell lung carcinoma Diseases 0.000 description 3
- 201000011549 stomach cancer Diseases 0.000 description 3
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 3
- 201000005112 urinary bladder cancer Diseases 0.000 description 3
- 102100036475 Alanine aminotransferase 1 Human genes 0.000 description 2
- 108010082126 Alanine transaminase Proteins 0.000 description 2
- 108010003415 Aspartate Aminotransferases Proteins 0.000 description 2
- 102000004625 Aspartate Aminotransferases Human genes 0.000 description 2
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- 229910019142 PO4 Inorganic materials 0.000 description 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 2
- 125000002252 acyl group Chemical group 0.000 description 2
- 125000004423 acyloxy group Chemical group 0.000 description 2
- 125000003342 alkenyl group Chemical group 0.000 description 2
- 125000003545 alkoxy group Chemical group 0.000 description 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 2
- 125000000304 alkynyl group Chemical group 0.000 description 2
- 125000003710 aryl alkyl group Chemical group 0.000 description 2
- 239000004202 carbamide Substances 0.000 description 2
- 125000004122 cyclic group Chemical group 0.000 description 2
- 125000001475 halogen functional group Chemical group 0.000 description 2
- 125000004404 heteroalkyl group Chemical group 0.000 description 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 2
- 230000001404 mediated effect Effects 0.000 description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 2
- 229910052757 nitrogen Inorganic materials 0.000 description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 2
- 239000010452 phosphate Substances 0.000 description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- BLGWHBSBBJNKJO-UHFFFAOYSA-N serabelisib Chemical group C=1C=C2OC(N)=NC2=CC=1C(=CN12)C=CC1=NC=C2C(=O)N1CCOCC1 BLGWHBSBBJNKJO-UHFFFAOYSA-N 0.000 description 2
- 210000002966 serum Anatomy 0.000 description 2
- 229940124530 sulfonamide Drugs 0.000 description 2
- 150000003456 sulfonamides Chemical class 0.000 description 2
- BFYIZQONLCFLEV-DAELLWKTSA-N Aromasine Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC(=C)C2=C1 BFYIZQONLCFLEV-DAELLWKTSA-N 0.000 description 1
- 239000005411 L01XE02 - Gefitinib Substances 0.000 description 1
- 239000005551 L01XE03 - Erlotinib Substances 0.000 description 1
- 229930012538 Paclitaxel Natural products 0.000 description 1
- 229960001686 afatinib Drugs 0.000 description 1
- ULXXDDBFHOBEHA-CWDCEQMOSA-N afatinib Chemical compound N1=CN=C2C=C(O[C@@H]3COCC3)C(NC(=O)/C=C/CN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ULXXDDBFHOBEHA-CWDCEQMOSA-N 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 229960000397 bevacizumab Drugs 0.000 description 1
- LVXJQMNHJWSHET-AATRIKPKSA-N dacomitinib Chemical compound C=12C=C(NC(=O)\C=C\CN3CCCCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 LVXJQMNHJWSHET-AATRIKPKSA-N 0.000 description 1
- 229950002205 dacomitinib Drugs 0.000 description 1
- 210000004696 endometrium Anatomy 0.000 description 1
- 229960001433 erlotinib Drugs 0.000 description 1
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 description 1
- 229960000255 exemestane Drugs 0.000 description 1
- 229960002584 gefitinib Drugs 0.000 description 1
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 description 1
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 description 1
- 229960005277 gemcitabine Drugs 0.000 description 1
- 229950003968 motesanib Drugs 0.000 description 1
- RAHBGWKEPAQNFF-UHFFFAOYSA-N motesanib Chemical compound C=1C=C2C(C)(C)CNC2=CC=1NC(=O)C1=CC=CN=C1NCC1=CC=NC=C1 RAHBGWKEPAQNFF-UHFFFAOYSA-N 0.000 description 1
- XZXHXSATPCNXJR-ZIADKAODSA-N nintedanib Chemical compound O=C1NC2=CC(C(=O)OC)=CC=C2\C1=C(C=1C=CC=CC=1)\NC(C=C1)=CC=C1N(C)C(=O)CN1CCN(C)CC1 XZXHXSATPCNXJR-ZIADKAODSA-N 0.000 description 1
- 229960004378 nintedanib Drugs 0.000 description 1
- 229960001592 paclitaxel Drugs 0.000 description 1
- QOFFJEBXNKRSPX-ZDUSSCGKSA-N pemetrexed Chemical compound C1=N[C]2NC(N)=NC(=O)C2=C1CCC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 QOFFJEBXNKRSPX-ZDUSSCGKSA-N 0.000 description 1
- 229960005079 pemetrexed Drugs 0.000 description 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361886623P | 2013-10-03 | 2013-10-03 | |
| US61/886,623 | 2013-10-03 | ||
| US201462054879P | 2014-09-24 | 2014-09-24 | |
| US62/054,879 | 2014-09-24 | ||
| PCT/US2014/058926 WO2015051193A1 (en) | 2013-10-03 | 2014-10-02 | ENHANCED TREATMENT REGIMENS USING PI3Kα INHIBITORS |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016536282A JP2016536282A (ja) | 2016-11-24 |
| JP2016536282A5 true JP2016536282A5 (2) | 2017-11-02 |
Family
ID=52779165
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016519762A Pending JP2016536282A (ja) | 2013-10-03 | 2014-10-02 | ＰＩ３Ｋα阻害剤を使用する強化された治療レジメン |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20160287601A1 (2) |
| EP (1) | EP3052493A4 (2) |
| JP (1) | JP2016536282A (2) |
| CN (1) | CN105745207A (2) |
| CA (1) | CA2925523A1 (2) |
| WO (1) | WO2015051193A1 (2) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL285928B2 (en) | 2016-05-06 | 2025-06-01 | Eagle Pharmaceuticals Inc | Fulvestrant formulations and methods of their use |
| CA3102279A1 (en) | 2018-06-01 | 2019-12-05 | Cornell University | Combination therapy for pi3k-associated disease or disorder |
| WO2021001427A1 (en) * | 2019-07-02 | 2021-01-07 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the prophylactic treatment of cancer in patients suffering from pancreatitis |
| US20260000658A1 (en) * | 2022-07-06 | 2026-01-01 | Institut National de la Santé et de la Recherche Médicale | Methods for the treatment of proliferative glomerulonephritis |
| WO2025045915A1 (en) * | 2023-08-29 | 2025-03-06 | Institut National de la Santé et de la Recherche Médicale | Methods for inducing muscle hypertrophy |
| CN120550330B (zh) * | 2025-07-29 | 2025-10-24 | 四川省肿瘤医院 | 经皮穴位电刺激调控免疫检查点系统及其方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110105521A1 (en) * | 2008-07-11 | 2011-05-05 | Novartis Ag | Combination of (a) a phosphoinositide 3-kinase inhibitor and (b) a modulator of ras/raf/mek pathway |
| EP2486149B1 (en) * | 2009-08-06 | 2015-06-17 | John Wayne Cancer Institute | Diagnosis of primary and metastatic basal-like breast cancer and other cancer types |
| NZ598220A (en) * | 2009-08-17 | 2014-02-28 | Intellikine Llc | Heterocyclic compounds and uses thereof |
| US9403820B2 (en) * | 2011-11-11 | 2016-08-02 | Intellikine Llc | Kinase inhibitor polymorphs |
| US8611178B2 (en) * | 2011-11-11 | 2013-12-17 | Qualcomm Incorporated | Device and method to perform memory operations at a clock domain crossing |
| JP6130391B2 (ja) * | 2011-11-23 | 2017-05-17 | インテリカイン， エルエルシー | Ｍｔｏｒ阻害剤を使用する強化された治療レジメン |
-
2014
- 2014-10-02 CN CN201480063176.XA patent/CN105745207A/zh active Pending
- 2014-10-02 WO PCT/US2014/058926 patent/WO2015051193A1/en not_active Ceased
- 2014-10-02 CA CA2925523A patent/CA2925523A1/en not_active Abandoned
- 2014-10-02 US US15/026,352 patent/US20160287601A1/en not_active Abandoned
- 2014-10-02 EP EP14850658.7A patent/EP3052493A4/en not_active Withdrawn
- 2014-10-02 JP JP2016519762A patent/JP2016536282A/ja active Pending
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