JPWO2020138370A5 - - Google Patents
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- JPWO2020138370A5 JPWO2020138370A5 JP2020562462A JP2020562462A JPWO2020138370A5 JP WO2020138370 A5 JPWO2020138370 A5 JP WO2020138370A5 JP 2020562462 A JP2020562462 A JP 2020562462A JP 2020562462 A JP2020562462 A JP 2020562462A JP WO2020138370 A5 JPWO2020138370 A5 JP WO2020138370A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- androgen receptor
- phosphorylation
- composition according
- tumor
- 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.)
- Pending
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- 206010028980 Neoplasm Diseases 0.000 claims description 75
- 201000011510 cancer Diseases 0.000 claims description 75
- 108010080146 androgen receptors Proteins 0.000 claims description 58
- 102000001307 androgen receptors Human genes 0.000 claims description 58
- 230000026731 phosphorylation Effects 0.000 claims description 49
- 238000006366 phosphorylation reaction Methods 0.000 claims description 49
- 238000000034 method Methods 0.000 claims description 37
- 239000000203 mixture Substances 0.000 claims description 36
- 239000008194 pharmaceutical composition Substances 0.000 claims description 30
- 206010060862 Prostate cancer Diseases 0.000 claims description 28
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 28
- 210000004027 cell Anatomy 0.000 claims description 19
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims description 18
- 150000003839 salts Chemical class 0.000 claims description 17
- 108091008721 AR-V7 Proteins 0.000 claims description 14
- 229940123407 Androgen receptor antagonist Drugs 0.000 claims description 12
- 206010005003 Bladder cancer Diseases 0.000 claims description 12
- 206010006187 Breast cancer Diseases 0.000 claims description 12
- 208000026310 Breast neoplasm Diseases 0.000 claims description 12
- 206010033128 Ovarian cancer Diseases 0.000 claims description 12
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 12
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 12
- 239000003936 androgen receptor antagonist Substances 0.000 claims description 12
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 12
- 239000004480 active ingredient Substances 0.000 claims description 10
- 239000003098 androgen Substances 0.000 claims description 10
- 230000002280 anti-androgenic effect Effects 0.000 claims description 8
- 239000000051 antiandrogen Substances 0.000 claims description 8
- WXCXUHSOUPDCQV-UHFFFAOYSA-N enzalutamide Chemical group C1=C(F)C(C(=O)NC)=CC=C1N1C(C)(C)C(=O)N(C=2C=C(C(C#N)=CC=2)C(F)(F)F)C1=S WXCXUHSOUPDCQV-UHFFFAOYSA-N 0.000 claims description 8
- 229960004671 enzalutamide Drugs 0.000 claims description 8
- 102000005962 receptors Human genes 0.000 claims description 8
- 108020003175 receptors Proteins 0.000 claims description 8
- 206010000830 Acute leukaemia Diseases 0.000 claims description 6
- 206010061424 Anal cancer Diseases 0.000 claims description 6
- 229940127512 Androgen Synthesis Inhibitors Drugs 0.000 claims description 6
- 208000007860 Anus Neoplasms Diseases 0.000 claims description 6
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims description 6
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 6
- 206010004593 Bile duct cancer Diseases 0.000 claims description 6
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 6
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 6
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 6
- 206010009944 Colon cancer Diseases 0.000 claims description 6
- 206010014733 Endometrial cancer Diseases 0.000 claims description 6
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 6
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 6
- 208000006168 Ewing Sarcoma Diseases 0.000 claims description 6
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims description 6
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims description 6
- 208000032320 Germ cell tumor of testis Diseases 0.000 claims description 6
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 6
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims description 6
- 206010025323 Lymphomas Diseases 0.000 claims description 6
- 208000034578 Multiple myelomas Diseases 0.000 claims description 6
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 6
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 6
- 206010029260 Neuroblastoma Diseases 0.000 claims description 6
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 6
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 6
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 6
- 208000033014 Plasma cell tumor Diseases 0.000 claims description 6
- 208000007452 Plasmacytoma Diseases 0.000 claims description 6
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 6
- 206010038389 Renal cancer Diseases 0.000 claims description 6
- 206010039491 Sarcoma Diseases 0.000 claims description 6
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 6
- 206010041067 Small cell lung cancer Diseases 0.000 claims description 6
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims description 6
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 6
- 208000024313 Testicular Neoplasms Diseases 0.000 claims description 6
- 208000000728 Thymus Neoplasms Diseases 0.000 claims description 6
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 6
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 6
- 208000008383 Wilms tumor Diseases 0.000 claims description 6
- GZOSMCIZMLWJML-VJLLXTKPSA-N abiraterone Chemical group C([C@H]1[C@H]2[C@@H]([C@]3(CC[C@H](O)CC3=CC2)C)CC[C@@]11C)C=C1C1=CC=CN=C1 GZOSMCIZMLWJML-VJLLXTKPSA-N 0.000 claims description 6
- 229960000853 abiraterone Drugs 0.000 claims description 6
- 208000017733 acquired polycythemia vera Diseases 0.000 claims description 6
- 238000009167 androgen deprivation therapy Methods 0.000 claims description 6
- 201000011165 anus cancer Diseases 0.000 claims description 6
- 208000026900 bile duct neoplasm Diseases 0.000 claims description 6
- 230000015572 biosynthetic process Effects 0.000 claims description 6
- 201000010881 cervical cancer Diseases 0.000 claims description 6
- 208000006990 cholangiocarcinoma Diseases 0.000 claims description 6
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims description 6
- 208000029742 colonic neoplasm Diseases 0.000 claims description 6
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims description 6
- 201000004101 esophageal cancer Diseases 0.000 claims description 6
- 210000000232 gallbladder Anatomy 0.000 claims description 6
- 201000010175 gallbladder cancer Diseases 0.000 claims description 6
- 206010017758 gastric cancer Diseases 0.000 claims description 6
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims description 6
- 201000010536 head and neck cancer Diseases 0.000 claims description 6
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 6
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 6
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 6
- 239000003112 inhibitor Substances 0.000 claims description 6
- 201000010982 kidney cancer Diseases 0.000 claims description 6
- 201000007270 liver cancer Diseases 0.000 claims description 6
- 208000014018 liver neoplasm Diseases 0.000 claims description 6
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 6
- 201000001441 melanoma Diseases 0.000 claims description 6
- 208000025189 neoplasm of testis Diseases 0.000 claims description 6
- 201000008026 nephroblastoma Diseases 0.000 claims description 6
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 6
- 201000008968 osteosarcoma Diseases 0.000 claims description 6
- 208000021284 ovarian germ cell tumor Diseases 0.000 claims description 6
- 201000002528 pancreatic cancer Diseases 0.000 claims description 6
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 6
- 208000010626 plasma cell neoplasm Diseases 0.000 claims description 6
- 208000037244 polycythemia vera Diseases 0.000 claims description 6
- 206010038038 rectal cancer Diseases 0.000 claims description 6
- 201000001275 rectum cancer Diseases 0.000 claims description 6
- 201000000849 skin cancer Diseases 0.000 claims description 6
- 208000000587 small cell lung carcinoma Diseases 0.000 claims description 6
- 201000011549 stomach cancer Diseases 0.000 claims description 6
- 238000003786 synthesis reaction Methods 0.000 claims description 6
- 201000003120 testicular cancer Diseases 0.000 claims description 6
- 208000002918 testicular germ cell tumor Diseases 0.000 claims description 6
- 208000008732 thymoma Diseases 0.000 claims description 6
- 201000002510 thyroid cancer Diseases 0.000 claims description 6
- 206010044412 transitional cell carcinoma Diseases 0.000 claims description 6
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 6
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 claims description 4
- 102000007469 Actins Human genes 0.000 claims description 3
- 108010085238 Actins Proteins 0.000 claims description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 2
- 230000010261 cell growth Effects 0.000 claims description 2
- 230000003247 decreasing effect Effects 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 238000002651 drug therapy Methods 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 210000002966 serum Anatomy 0.000 claims description 2
- 229960003604 testosterone Drugs 0.000 claims description 2
- 238000012258 culturing Methods 0.000 description 2
- 238000004113 cell culture Methods 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2018244174 | 2018-12-27 | ||
| JP2018244174 | 2018-12-27 | ||
| PCT/JP2019/051310 WO2020138370A1 (ja) | 2018-12-27 | 2019-12-26 | Ｃｄｋ阻害剤を含有する癌治療用医薬組成物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPWO2020138370A1 JPWO2020138370A1 (ja) | 2021-11-11 |
| JPWO2020138370A5 true JPWO2020138370A5 (https=) | 2022-11-09 |
Family
ID=71126081
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020562462A Pending JPWO2020138370A1 (ja) | 2018-12-27 | 2019-12-26 | Ｃｄｋ阻害剤を含有する癌治療用医薬組成物 |
Country Status (3)
| Country | Link |
|---|---|
| US (1) | US20220071978A1 (https=) |
| JP (1) | JPWO2020138370A1 (https=) |
| WO (1) | WO2020138370A1 (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025217307A1 (en) | 2024-04-09 | 2025-10-16 | Revolution Medicines, Inc. | Methods for predicting response to a ras(on) inhibitor and combination therapies |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2959336A1 (en) * | 2014-08-25 | 2016-03-03 | The Johns Hopkins University | Methods and compositions related to prostate cancer therapeutics |
| JP2018177658A (ja) * | 2017-04-05 | 2018-11-15 | 公立大学法人名古屋市立大学 | 去勢抵抗性前立腺癌の治療 |
-
2019
- 2019-12-26 JP JP2020562462A patent/JPWO2020138370A1/ja active Pending
- 2019-12-26 WO PCT/JP2019/051310 patent/WO2020138370A1/ja not_active Ceased
- 2019-12-26 US US17/417,727 patent/US20220071978A1/en not_active Abandoned
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