From Wikipedia, the free encyclopedia
CREB-binding protein/β-catenin inhibitor
Foscenvivint
![](https://upload.wikimedia.org/wikipedia/commons/thumb/f/f7/Foscenvivint.svg/220px-Foscenvivint.svg.png) |
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Other names | PRI 724; OP 724 |
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[4-[[(6S,9S,9aS)-1-(Benzylcarbamoyl)-2,9-dimethyl-4,7-dioxo-8-(quinolin-8-ylmethyl)-3,6,9,9a-tetrahydropyrazino[2,1-c][1,2,4]triazin-6-yl]methyl]phenyl] dihydrogen phosphate
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CAS Number | |
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PubChem
CID | |
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DrugBank | |
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Formula | C33H35N6O7P |
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Molar mass | 658.652 g·mol−1 |
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3D model (
JSmol) | |
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C[C@H]1[C@H]2N([C@H](C(=O)N1CC3=CC=CC4=C3N=CC=C4)CC5=CC=C(C=C5)OP(=O)(O)O)C(=O)CN(N2C(=O)NCC6=CC=CC=C6)C
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InChI=1S/C33H35N6O7P/c1-22-31-38(29(40)21-36(2)39(31)33(42)35-19-24-8-4-3-5-9-24)28(18-23-13-15-27(16-14-23)46-47(43,44)45)32(41)37(22)20-26-11-6-10-25-12-7-17-34-30(25)26/h3-17,22,28,31H,18-21H2,1-2H3,(H,35,42)(H2,43,44,45)/t22-,28-,31-/m0/s1 Key:VHOZWHQPEJGPCC-AZXNYEMZSA-N
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Foscenvivint (PRI 724 or OP 724)
[1] is a
CREB-binding protein/
β-catenin inhibitor that is developed for the treatment of liver diseases
[2] such as
primary biliary cholangitis,
[3]
hepatocellular carcinoma,
[4]
[5] and
hepatitis C and
B virus-induced liver cirrhosis.
[6]
[7]
References
-
^
"Foscenvivint - PRISM Pharma Co - AdisInsight". adisinsight.springer.com. Retrieved 23 November 2023.
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^ Ouchi, Hirofumi; Mizutani, Yuki; Yoshimura, Kaori; Sato, Yasunori; Kimura, Kiminori; Haruyama, Yushi; Harada, Kenichi (June 2023). "Anti-inflammatory and antifibrotic effects of CBP/β-catenin inhibitor for hepatocytes: small molecular inhibitor, OP-724 possibly improves liver function". Medical Molecular Morphology. 56 (2): 94–105.
doi:
10.1007/s00795-022-00343-8.
PMID
36645521.
S2CID
255847780.
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^ Kimura, Masamichi; Ogawa, Eiichi; Harada, Kenichi; Imamura, Jun; Saio, Masanao; Ikura, Yoshihiro; Yatsuhashi, Hiroshi; Murata, Kazumoto; Miura, Kouichi; Ieiri, Ichiro; Tanaka, Atsushi; Kimura, Kiminori (1 November 2022).
"Feasibility, safety and tolerability of the CREB-binding protein/β-catenin inhibitor OP-724 in patients with advanced primary biliary cholangitis: an investigator-initiated, open-label, non-randomised, two-centre, phase 1 study". BMJ Open Gastroenterology. 9 (1): e001001.
doi:
10.1136/bmjgast-2022-001001.
ISSN
2054-4774.
PMC
9710334.
PMID
36442892.
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^ El-Khoueiry, Anthony B.; Ning, Yan; Yang, Dongyun; Cole, Sarah; Kahn, Michael; Zoghbi, Marwan; Berg, Jennifer; Fujimori, Masamoto; Inada, Tetsuhi; Kouji, Hiroyuki; Lenz, Heinz-Josef (20 May 2013). "A phase I first-in-human study of PRI-724 in patients (pts) with advanced solid tumors". Journal of Clinical Oncology. 31 (15_suppl): 2501.
doi:
10.1200/jco.2013.31.15_suppl.2501.
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^ Gabata, Ryosuke; Harada, Kenichi; Mizutani, Yuki; Ouchi, Hirofumi; Yoshimura, Kaori; Sato, Yasunori; Kitao, Azusa; Kimura, Kiminori; Kouji, Hiroyuki; Miyashita, Tomoharu; Tajima, Hidehiro; Ohta, Tetsuo (September 2020).
"Anti-tumor Activity of the Small Molecule Inhibitor PRI-724 Against β-Catenin-activated Hepatocellular Carcinoma". Anticancer Research. 40 (9): 5211–5219.
doi:
10.21873/anticanres.14524.
PMID
32878809.
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^ Kimura, Kiminori; Kanto, Tatsuya; Shimoda, Shinji; Harada, Kenichi; Kimura, Masamichi; Nishikawa, Koji; Imamura, Jun; Ogawa, Eiichi; Saio, Masanao; Ikura, Yoshihiro; Okusaka, Takuji; Inoue, Kazuaki; Ishikawa, Tetsuya; Ieiri, Ichiro; Kishimoto, Junji; Todaka, Koji; Kamisawa, Terumi (June 2022).
"Safety, tolerability, and anti-fibrotic efficacy of the CBP/β-catenin inhibitor PRI-724 in patients with hepatitis C and B virus-induced liver cirrhosis: An investigator-initiated, open-label, non-randomised, multicentre, phase 1/2a study". eBioMedicine. 80: 104069.
doi:
10.1016/j.ebiom.2022.104069.
PMC
9126795.
PMID
35605429.
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^ Kimura, Kiminori; Ikoma, Akemi; Shibakawa, Maki; Shimoda, Shinji; Harada, Kenichi; Saio, Masanao; Imamura, Jun; Osawa, Yosuke; Kimura, Masamichi; Nishikawa, Koji; Okusaka, Takuji; Morita, Satoshi; Inoue, Kazuaki; Kanto, Tatsuya; Todaka, Koji; Nakanishi, Yoichi; Kohara, Michinori; Mizokami, Masashi (September 2017).
"Safety, Tolerability, and Preliminary Efficacy of the Anti-Fibrotic Small Molecule PRI-724, a CBP/β-Catenin Inhibitor, in Patients with Hepatitis C Virus-related Cirrhosis: A Single-Center, Open-Label, Dose Escalation Phase 1 Trial". eBioMedicine. 23: 79–87.
doi:
10.1016/j.ebiom.2017.08.016.
PMC
5605374.
PMID
28844410.