JPWO2020118213A5 - - Google Patents
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- Publication number
- JPWO2020118213A5 JPWO2020118213A5 JP2021531818A JP2021531818A JPWO2020118213A5 JP WO2020118213 A5 JPWO2020118213 A5 JP WO2020118213A5 JP 2021531818 A JP2021531818 A JP 2021531818A JP 2021531818 A JP2021531818 A JP 2021531818A JP WO2020118213 A5 JPWO2020118213 A5 JP WO2020118213A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- cdk4
- resistant
- inhibitor
- subject
- 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
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims 21
- 101700008359 CDK4 Proteins 0.000 claims 12
- 102100016692 ESR1 Human genes 0.000 claims 11
- 230000002401 inhibitory effect Effects 0.000 claims 11
- 108010007005 Estrogen Receptor alpha Proteins 0.000 claims 10
- 201000011510 cancer Diseases 0.000 claims 10
- 239000003112 inhibitor Substances 0.000 claims 10
- 206010006187 Breast cancer Diseases 0.000 claims 4
- -1 DDR2 Proteins 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000011780 sodium chloride Substances 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 239000003886 aromatase inhibitor Substances 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- RHXHGRAEPCAFML-UHFFFAOYSA-N 7-cyclopentyl-N,N-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 RHXHGRAEPCAFML-UHFFFAOYSA-N 0.000 claims 2
- 101700006234 AKT1 Proteins 0.000 claims 2
- 102100001248 AKT1 Human genes 0.000 claims 2
- 102100001250 AKT2 Human genes 0.000 claims 2
- 101700006583 AKT2 Proteins 0.000 claims 2
- 229950001573 Abemaciclib Drugs 0.000 claims 2
- 101700004551 BRAF Proteins 0.000 claims 2
- 102100004328 BRAF Human genes 0.000 claims 2
- 102100019398 CDK4 Human genes 0.000 claims 2
- 102100006130 CDK6 Human genes 0.000 claims 2
- 108010025468 Cyclin-Dependent Kinase 6 Proteins 0.000 claims 2
- 101710026102 MIC-ACT-2 Proteins 0.000 claims 2
- 102100013322 MTOR Human genes 0.000 claims 2
- 101700036611 MTOR Proteins 0.000 claims 2
- UZWDCWONPYILKI-UHFFFAOYSA-N N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine Chemical compound C1CN(CC)CCN1CC(C=N1)=CC=C1NC1=NC=C(F)C(C=2C=C3N(C(C)C)C(C)=NC3=C(F)C=2)=N1 UZWDCWONPYILKI-UHFFFAOYSA-N 0.000 claims 2
- 101710027440 PIK3CA Proteins 0.000 claims 2
- 102100019471 PIK3CA Human genes 0.000 claims 2
- 102100014818 PIK3R1 Human genes 0.000 claims 2
- 101710039899 PIK3R1 Proteins 0.000 claims 2
- AHJRHEGDXFFMBM-UHFFFAOYSA-N Palbociclib Chemical compound N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 AHJRHEGDXFFMBM-UHFFFAOYSA-N 0.000 claims 2
- 229960004390 Palbociclib Drugs 0.000 claims 2
- 229950003687 Ribociclib Drugs 0.000 claims 2
- 230000035772 mutation Effects 0.000 claims 2
- 239000000333 selective estrogen receptor modulator Substances 0.000 claims 2
- 102100019002 ABL1 Human genes 0.000 claims 1
- 101700000782 ABL1 Proteins 0.000 claims 1
- 102100011882 ARID1A Human genes 0.000 claims 1
- 101710037383 ARID1A Proteins 0.000 claims 1
- 101700021058 ASXL1 Proteins 0.000 claims 1
- 102100016224 ASXL1 Human genes 0.000 claims 1
- 102100000648 ATM Human genes 0.000 claims 1
- 108060006202 ATM Proteins 0.000 claims 1
- 108060000721 ATR Proteins 0.000 claims 1
- 229940046836 Anti-estrogens Drugs 0.000 claims 1
- 229940046844 Aromatase inhibitors Drugs 0.000 claims 1
- 102000004000 Aurora Kinase A Human genes 0.000 claims 1
- 108090000461 Aurora Kinase A Proteins 0.000 claims 1
- 108060005926 BAP1 Proteins 0.000 claims 1
- 102100009749 BCR Human genes 0.000 claims 1
- 101700072047 BCR Proteins 0.000 claims 1
- 102100007281 BRCA1 Human genes 0.000 claims 1
- 108010042977 BRCA1 Protein Proteins 0.000 claims 1
- 108010000750 BRCA2 Protein Proteins 0.000 claims 1
- 102000002280 BRCA2 Protein Human genes 0.000 claims 1
- 101710019578 BZIP46 Proteins 0.000 claims 1
- 108010040168 Bcl-2-Like Protein 11 Proteins 0.000 claims 1
- 102000001765 Bcl-2-Like Protein 11 Human genes 0.000 claims 1
- 210000004556 Brain Anatomy 0.000 claims 1
- 206010055113 Breast cancer metastatic Diseases 0.000 claims 1
- 102100019529 CCND1 Human genes 0.000 claims 1
- 102100019530 CCND2 Human genes 0.000 claims 1
- 101700059002 CCND2 Proteins 0.000 claims 1
- 102100016486 CCND3 Human genes 0.000 claims 1
- 101700079292 CCND3 Proteins 0.000 claims 1
- 102100016490 CCNE1 Human genes 0.000 claims 1
- 101700061678 CCNE1 Proteins 0.000 claims 1
- 101700016900 CDH1 Proteins 0.000 claims 1
- 102100003970 CDK8 Human genes 0.000 claims 1
- 102100002974 CDKN1A Human genes 0.000 claims 1
- 102000033243 CDKN2A Human genes 0.000 claims 1
- 102100019348 CEBPA Human genes 0.000 claims 1
- 101700058775 CEBPA Proteins 0.000 claims 1
- 102100002043 CTNNB1 Human genes 0.000 claims 1
- 101710005974 CTNNB1 Proteins 0.000 claims 1
- 108010058546 Cyclin D1 Proteins 0.000 claims 1
- 108010025415 Cyclin-Dependent Kinase 8 Proteins 0.000 claims 1
- 108010009356 Cyclin-Dependent Kinase Inhibitor p15 Proteins 0.000 claims 1
- 102000009512 Cyclin-Dependent Kinase Inhibitor p15 Human genes 0.000 claims 1
- 108010009392 Cyclin-Dependent Kinase Inhibitor p16 Proteins 0.000 claims 1
- 108010016788 Cyclin-Dependent Kinase Inhibitor p21 Proteins 0.000 claims 1
- 108010016777 Cyclin-Dependent Kinase Inhibitor p27 Proteins 0.000 claims 1
- 102000000577 Cyclin-Dependent Kinase Inhibitor p27 Human genes 0.000 claims 1
- 101700011568 DIB1 Proteins 0.000 claims 1
- 102100006402 DNMT3A Human genes 0.000 claims 1
- 101710038368 DNMT3A Proteins 0.000 claims 1
- 102100016362 E2F3 Human genes 0.000 claims 1
- 101700073364 E2F3 Proteins 0.000 claims 1
- 101700028671 E2FA Proteins 0.000 claims 1
- 102100002671 EML4 Human genes 0.000 claims 1
- 101700040935 EML4 Proteins 0.000 claims 1
- 102100009835 EPHB2 Human genes 0.000 claims 1
- 101700024891 EPHB2 Proteins 0.000 claims 1
- 102100016662 ERBB2 Human genes 0.000 claims 1
- 101700025368 ERBB2 Proteins 0.000 claims 1
- 101700041204 ERBB3 Proteins 0.000 claims 1
- 102000027776 ERBB3 Human genes 0.000 claims 1
- 108010062201 F-Box-WD Repeat-Containing Protein 7 Proteins 0.000 claims 1
- 101710019535 FARSA Proteins 0.000 claims 1
- 102100020077 FBXW7 Human genes 0.000 claims 1
- 102100007406 FGF4 Human genes 0.000 claims 1
- 101700036125 FGF4 Proteins 0.000 claims 1
- 102100017996 FGFR1 Human genes 0.000 claims 1
- 102100018000 FGFR2 Human genes 0.000 claims 1
- 102100020191 FGFR3 Human genes 0.000 claims 1
- 102100004573 FLT3 Human genes 0.000 claims 1
- 101710009074 FLT3 Proteins 0.000 claims 1
- 102100004396 FRS2 Human genes 0.000 claims 1
- 101700069831 FRS2 Proteins 0.000 claims 1
- 102100018976 FZR1 Human genes 0.000 claims 1
- 102100003042 HIF1A Human genes 0.000 claims 1
- 101700000053 HIF1A Proteins 0.000 claims 1
- 102100009283 HRAS Human genes 0.000 claims 1
- 101710033925 HRAS Proteins 0.000 claims 1
- 102100004121 IDH1 Human genes 0.000 claims 1
- 101700024037 IDH1 Proteins 0.000 claims 1
- 101700030371 IDH2 Proteins 0.000 claims 1
- 102100002772 IDH2 Human genes 0.000 claims 1
- 101700066748 IDH3B Proteins 0.000 claims 1
- 102100014263 IGF1R Human genes 0.000 claims 1
- 101700025802 IGF1R Proteins 0.000 claims 1
- 101700016050 JAK2 Proteins 0.000 claims 1
- 102100019516 JAK2 Human genes 0.000 claims 1
- 101700004928 KDM6A Proteins 0.000 claims 1
- 102100013867 KDM6A Human genes 0.000 claims 1
- 102100013180 KDR Human genes 0.000 claims 1
- 101700033678 KDR Proteins 0.000 claims 1
- 101710030888 KDR Proteins 0.000 claims 1
- 102100012801 KIF5B Human genes 0.000 claims 1
- 101710024882 KIF5B Proteins 0.000 claims 1
- 102100009279 KRAS Human genes 0.000 claims 1
- 101710033922 KRAS Proteins 0.000 claims 1
- 102100012762 LRP1B Human genes 0.000 claims 1
- 101700083303 LRP1B Proteins 0.000 claims 1
- 102100012659 MAGI1 Human genes 0.000 claims 1
- 108010068342 MAP Kinase Kinase 1 Proteins 0.000 claims 1
- 102100006473 MAP2K1 Human genes 0.000 claims 1
- 102100015874 MAP2K4 Human genes 0.000 claims 1
- 101710027749 MAP2K4 Proteins 0.000 claims 1
- 102100002383 MCL1 Human genes 0.000 claims 1
- 101700031439 MCL1 Proteins 0.000 claims 1
- 102100019155 MDM2 Human genes 0.000 claims 1
- 101700032565 MDM2 Proteins 0.000 claims 1
- 102000017274 MDM4 Human genes 0.000 claims 1
- 108050005300 MDM4 Proteins 0.000 claims 1
- 102100008541 MGMT Human genes 0.000 claims 1
- 102100002001 MSH6 Human genes 0.000 claims 1
- 101700030163 MSH6 Proteins 0.000 claims 1
- 206010027476 Metastasis Diseases 0.000 claims 1
- 102100018287 NKX2-1 Human genes 0.000 claims 1
- 101710012901 NKX2-1 Proteins 0.000 claims 1
- 102100001119 NRAS Human genes 0.000 claims 1
- 101710033916 NRAS Proteins 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 102100004940 PDGFRA Human genes 0.000 claims 1
- 101710018349 PDGFRA Proteins 0.000 claims 1
- 102100000124 PHB2 Human genes 0.000 claims 1
- 102100002428 PML Human genes 0.000 claims 1
- 101700004802 PML Proteins 0.000 claims 1
- 108010011536 PTEN Phosphohydrolase Proteins 0.000 claims 1
- 102000014160 PTEN Phosphohydrolase Human genes 0.000 claims 1
- 101700079089 PTPRD Proteins 0.000 claims 1
- 102100005502 PTPRD Human genes 0.000 claims 1
- 210000002381 Plasma Anatomy 0.000 claims 1
- 206010036807 Progressive multifocal leukoencephalopathy Diseases 0.000 claims 1
- 102100013019 RARA Human genes 0.000 claims 1
- 101700078798 RARA Proteins 0.000 claims 1
- 102100000895 RB1 Human genes 0.000 claims 1
- 101710003919 RB1 Proteins 0.000 claims 1
- 101710017811 RB1 Proteins 0.000 claims 1
- 102100006051 RET Human genes 0.000 claims 1
- 101700001630 RET Proteins 0.000 claims 1
- 108090000740 RNA-Binding Protein EWS Proteins 0.000 claims 1
- 102000004229 RNA-Binding Protein EWS Human genes 0.000 claims 1
- 102100002050 ROS1 Human genes 0.000 claims 1
- 101710027587 ROS1 Proteins 0.000 claims 1
- 101700054115 ROS1A Proteins 0.000 claims 1
- 102100012618 RPTOR Human genes 0.000 claims 1
- 102100013038 RUNX1 Human genes 0.000 claims 1
- 101700025439 RUNX1 Proteins 0.000 claims 1
- 108010061204 Rapamycin-Insensitive Companion of mTOR Protein Proteins 0.000 claims 1
- 102000012007 Rapamycin-Insensitive Companion of mTOR Protein Human genes 0.000 claims 1
- 108010029031 Regulatory-Associated Protein of mTOR Proteins 0.000 claims 1
- 108060007538 SIL1 Proteins 0.000 claims 1
- 101700062085 SMAD4 Proteins 0.000 claims 1
- 102100017680 SMAD4 Human genes 0.000 claims 1
- 102100019447 SMARCA4 Human genes 0.000 claims 1
- 101710025703 SMARCA4 Proteins 0.000 claims 1
- 101700006931 SOX2 Proteins 0.000 claims 1
- 102100018829 SOX2 Human genes 0.000 claims 1
- 102100019330 STK11 Human genes 0.000 claims 1
- 101700065463 STK11 Proteins 0.000 claims 1
- 108060008091 TBP Proteins 0.000 claims 1
- 102100003998 TET2 Human genes 0.000 claims 1
- 101700048164 TET2 Proteins 0.000 claims 1
- 102100019730 TP53 Human genes 0.000 claims 1
- 102100008209 TSC1 Human genes 0.000 claims 1
- 101700061326 TSC1 Proteins 0.000 claims 1
- 102100008210 TSC2 Human genes 0.000 claims 1
- 101700083014 TSC2 Proteins 0.000 claims 1
- 108010078814 Tumor Suppressor Protein p53 Proteins 0.000 claims 1
- 108010081291 Type 1 Fibroblast Growth Factor Receptor Proteins 0.000 claims 1
- 108010081268 Type 2 Fibroblast Growth Factor Receptor Proteins 0.000 claims 1
- 108010081267 Type 3 Fibroblast Growth Factor Receptor Proteins 0.000 claims 1
- 206010046766 Uterine cancer Diseases 0.000 claims 1
- 230000001833 anti-estrogenic Effects 0.000 claims 1
- 230000000593 degrading Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drugs Drugs 0.000 claims 1
- 102000017256 epidermal growth factor-activated receptor activity proteins Human genes 0.000 claims 1
- 108040009258 epidermal growth factor-activated receptor activity proteins Proteins 0.000 claims 1
- 239000000328 estrogen antagonist Substances 0.000 claims 1
- 101700064822 lcb1 Proteins 0.000 claims 1
- 101700085186 lcb2 Proteins 0.000 claims 1
- 231100000682 maximum tolerated dose Toxicity 0.000 claims 1
- 108040008770 methylated-DNA-[protein]-cysteine S-methyltransferase activity proteins Proteins 0.000 claims 1
- 201000002511 pituitary cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862776323P | 2018-12-06 | 2018-12-06 | |
| US62/776,323 | 2018-12-06 | ||
| PCT/US2019/065005 WO2020118213A1 (en) | 2018-12-06 | 2019-12-06 | Methods for treating cancer resistant to cdk4/6 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022511498A JP2022511498A (ja) | 2022-01-31 |
| JPWO2020118213A5 true JPWO2020118213A5 (ru) | 2022-12-19 |
Family
ID=69063871
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021531818A Pending JP2022511498A (ja) | 2018-12-06 | 2019-12-06 | Ｃｄｋ４／６阻害剤に耐性の癌を治療するための方法 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20210330612A1 (ru) |
| EP (1) | EP3890834A1 (ru) |
| JP (1) | JP2022511498A (ru) |
| KR (1) | KR20210100137A (ru) |
| CN (1) | CN113164779A (ru) |
| AU (1) | AU2019395093A1 (ru) |
| BR (1) | BR112021010110A2 (ru) |
| CA (1) | CA3121930A1 (ru) |
| EA (1) | EA202191283A1 (ru) |
| IL (1) | IL283659A (ru) |
| JO (1) | JOP20210137A1 (ru) |
| MA (1) | MA54388A (ru) |
| MX (1) | MX2021006411A (ru) |
| SG (1) | SG11202105531XA (ru) |
| WO (1) | WO2020118213A1 (ru) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW202237117A (zh) * | 2020-12-14 | 2022-10-01 | 美商亞文納營運公司 | 使用四氫萘衍生物作為雌激素受體降解劑治療乳癌之方法 |
| GB202116745D0 (en) * | 2021-11-19 | 2022-01-05 | Institute Of Cancer Res Royal Cancer Hospital | Prognostic and treatment response predictive method |
| CN115369089A (zh) * | 2022-08-11 | 2022-11-22 | 中山大学孙逸仙纪念医院 | 两种er阳性her-2阴性乳腺癌cdk4/6抑制剂耐药株及其构建方法和用途 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL297369B1 (en) * | 2015-04-29 | 2024-02-01 | Radius Pharmaceuticals Inc | RAD for use in a method to treat mutant estrogen receptor positive breast cancer or mutant estrogen receptor positive ovarian cancer |
| KR102322802B1 (ko) * | 2017-01-05 | 2021-11-04 | 래디어스 파마슈티컬스, 인코포레이티드 | Rad1901-2hcl의 다형 형태 |
-
2019
- 2019-12-06 AU AU2019395093A patent/AU2019395093A1/en active Pending
- 2019-12-06 EA EA202191283A patent/EA202191283A1/ru unknown
- 2019-12-06 EP EP19829727.7A patent/EP3890834A1/en active Pending
- 2019-12-06 BR BR112021010110-1A patent/BR112021010110A2/pt unknown
- 2019-12-06 MX MX2021006411A patent/MX2021006411A/es unknown
- 2019-12-06 CA CA3121930A patent/CA3121930A1/en active Pending
- 2019-12-06 KR KR1020217020435A patent/KR20210100137A/ko active Search and Examination
- 2019-12-06 MA MA054388A patent/MA54388A/fr unknown
- 2019-12-06 JP JP2021531818A patent/JP2022511498A/ja active Pending
- 2019-12-06 JO JOP/2021/0137A patent/JOP20210137A1/ar unknown
- 2019-12-06 US US17/299,948 patent/US20210330612A1/en active Pending
- 2019-12-06 WO PCT/US2019/065005 patent/WO2020118213A1/en unknown
- 2019-12-06 SG SG11202105531XA patent/SG11202105531XA/en unknown
- 2019-12-06 CN CN201980081052.7A patent/CN113164779A/zh active Pending
-
2021
- 2021-06-02 IL IL283659A patent/IL283659A/en unknown
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