JP7345151B1 - 癌治療薬 - Google Patents
癌治療薬 Download PDFInfo
- Publication number
- JP7345151B1 JP7345151B1 JP2023522767A JP2023522767A JP7345151B1 JP 7345151 B1 JP7345151 B1 JP 7345151B1 JP 2023522767 A JP2023522767 A JP 2023522767A JP 2023522767 A JP2023522767 A JP 2023522767A JP 7345151 B1 JP7345151 B1 JP 7345151B1
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- Japan
- Prior art keywords
- cancer
- ags8
- cells
- therapeutic agent
- present
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Abstract
Description
ところで、前立腺癌にActivator of G-protein signaling 8(以下、「AGS8」ということもある)の発現が認められ、その発現レベルは進行癌や転移性前立腺癌でより高く、また、発現の有無が生命予後と相関することが報告された(非特許文献1参照)。
そこで本発明においては、AGS8-Gβγ相互作用を阻害することにより癌細胞の増殖を抑える癌治療薬を提供することを課題とする。
すなわち本発明は、上述の課題を解決するためになされたものであり、本発明の実施形態は、以下に挙げる構成を含み得る。
(3)前記癌が前立腺癌である、(1)又は(2)に記載の癌治療薬。
(4)前記癌が転移性前立腺癌である、(1)~(3)のいずれか1項に記載の癌治療薬。
(5)前記癌が、ヒト正常前立腺上皮細胞に比べてAGS8の発現レベルの上昇を伴う癌である、(1)~(4)のいずれか1項に記載の癌治療薬。
<Activator of G-protein signaling 8と癌>
<癌治療薬>
<剤形及び投与量>
併用投与とは、本発明の癌治療薬の投与と同時、又は本発明の癌治療薬投与の前後に投与することである。あるいは、本発明の癌治療薬と、上記他の癌治療薬を混合して一つの製剤とすることもできる。
<適用対象>
(AGS8阻害薬)
(細胞)
(AGS8発現量の確認試験)
ヒトAGS8リアルタイムPCRのプライマー配列は、以下を用いた。
5'-TTCCGTAACCCTCTCCCG-3 '(センス)及び
5'-AACCCACGATCAAGGTCCAC-3'(アンチセンス)
ヒト正常前立腺上皮細胞(PrEC)に対するPC-3及びDU-145のAGS8相対的発現量は、比較Ct値法によって決定された。
(AGS8-Gβγサブユニット会合阻害確認試験)
(細胞毒性試験)
(DU-145細胞の生存率確認試験)
(DU-145細胞の遊走阻害試験)
(in vivoでの腫瘍形成抑制試験)
1週間おきにDU-145細胞移植部分を切開して腫瘍を取り出し、腫瘍体積及び重量を測定した。腫瘍体積(mm3)は、長径、短径をノギスで測定し、長径×(短径)2/2で算出した(各n=6)
コントロールでは、1週目~4週目にかけて腫瘍増殖が見られた。一方、本発明の癌治療薬を投与したところ、腫瘍体積及び重量を有意に(**p <0.01)抑制した。(図6(A)~(C))。なお試験中、いずれのマウスも外観異常は認められず、本発明の安全性が示された。
Claims (5)
- 一般式(1)で表される化合物又はその医薬的に許容される塩を含有してなる、癌治療薬。
- さらに、医薬的に許容される賦形剤を含有してなる、請求項1に記載の癌治療薬。
- 前記癌が前立腺癌である、請求項1又は2に記載の癌治療薬。
- 前記癌が転移性前立腺癌である、請求項1又は2に記載の癌治療薬。
- 前記癌が、ヒト正常前立腺上皮細胞に比べてAGS8の発現レベルの上昇を伴う癌である、請求項1又は2に記載の癌治療薬。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2022008336 | 2022-01-23 | ||
JP2022008336 | 2022-01-23 | ||
PCT/JP2023/001710 WO2023140355A1 (ja) | 2022-01-23 | 2023-01-20 | 癌治療薬 |
Publications (2)
Publication Number | Publication Date |
---|---|
JPWO2023140355A1 JPWO2023140355A1 (ja) | 2023-07-27 |
JP7345151B1 true JP7345151B1 (ja) | 2023-09-15 |
Family
ID=87348348
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2023522767A Active JP7345151B1 (ja) | 2022-01-23 | 2023-01-20 | 癌治療薬 |
Country Status (2)
Country | Link |
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JP (1) | JP7345151B1 (ja) |
WO (1) | WO2023140355A1 (ja) |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2014150252A1 (en) | 2013-03-15 | 2014-09-25 | Ligand Pharmaceuticals Incorporated | Methods of treatment associated with the granulocyte colony-stimulating factor receptor |
-
2023
- 2023-01-20 JP JP2023522767A patent/JP7345151B1/ja active Active
- 2023-01-20 WO PCT/JP2023/001710 patent/WO2023140355A1/ja active Application Filing
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2014150252A1 (en) | 2013-03-15 | 2014-09-25 | Ligand Pharmaceuticals Incorporated | Methods of treatment associated with the granulocyte colony-stimulating factor receptor |
Non-Patent Citations (3)
Title |
---|
DAS, Dibash K. et al,miR-1207-3p regulates the androgen receptor in prostate cancer via FNDC1/fibronectin,Experimental Cell Research,2016年,Vol.348,pp.190-200 |
DATABASE REGISTRY [Online] US: American Chemical Society [retrieved on 2023.03.09],Retrieved from STN,Registry No. 331244-90-7,(Entered STN 2001.04.13) |
SATO, Motohiko et al.,Protection of Cardiomyocytes from the Hypoxia-Mediated Injury by a Peptide Targeting the Activator o,PLOS ONE,2014年,Vol.9, No.3,e91980 |
Also Published As
Publication number | Publication date |
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WO2023140355A1 (ja) | 2023-07-27 |
JPWO2023140355A1 (ja) | 2023-07-27 |
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