Foscenvivint Explained

Legal Status:Investigational
Synonyms:PRI 724; OP 724
Unii:43Y934BBZ6
Cas Number:1422253-38-0
Pubchem:71509318
Drugbank:DB15034
Stdinchi: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
Stdinchikey:VHOZWHQPEJGPCC-AZXNYEMZSA-N
Smiles: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
Iupac Name:[4-[[(6''S'',9''S'',9a''S'')-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
C:33
H:35
N:6
O:7
P:1

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]

Notes and References

  1. Web site: Foscenvivint - PRISM Pharma Co - AdisInsight . adisinsight.springer.com . 23 November 2023.
  2. Ouchi . Hirofumi . Mizutani . Yuki . Yoshimura . Kaori . Sato . Yasunori . Kimura . Kiminori . Haruyama . Yushi . Harada . Kenichi . Anti-inflammatory and antifibrotic effects of CBP/β-catenin inhibitor for hepatocytes: small molecular inhibitor, OP-724 possibly improves liver function . Medical Molecular Morphology . June 2023 . 56 . 2 . 94–105 . 10.1007/s00795-022-00343-8. 36645521 . 255847780 .
  3. Kimura . Masamichi . Ogawa . Eiichi . Harada . Kenichi . Imamura . Jun . Saio . Masanao . Ikura . Yoshihiro . Yatsuhashi . Hiroshi . Murata . Kazumoto . Miura . Kouichi . Ieiri . Ichiro . Tanaka . Atsushi . Kimura . Kiminori . 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 . 1 November 2022 . 9 . 1 . e001001 . 10.1136/bmjgast-2022-001001 . 36442892 . 9710334 . en . 2054-4774. free .
  4. 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 . A phase I first-in-human study of PRI-724 in patients (pts) with advanced solid tumors. . Journal of Clinical Oncology . 20 May 2013 . 31 . 15_suppl . 2501 . 10.1200/jco.2013.31.15_suppl.2501.
  5. Gabata . Ryosuke . Harada . Kenichi . Mizutani . Yuki . Ouchi . Hirofumi . Yoshimura . Kaori . Sato . Yasunori . Kitao . Azusa . Kimura . Kiminori . Kouji . Hiroyuki . Miyashita . Tomoharu . Tajima . Hidehiro . Ohta . Tetsuo . Anti-tumor Activity of the Small Molecule Inhibitor PRI-724 Against β-Catenin-activated Hepatocellular Carcinoma . Anticancer Research . September 2020 . 40 . 9 . 5211–5219 . 10.21873/anticanres.14524. 32878809 . free .
  6. 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 . 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 . June 2022 . 80 . 104069 . 10.1016/j.ebiom.2022.104069. 35605429 . 9126795 . free .
  7. 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 . 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 . September 2017 . 23 . 79–87 . 10.1016/j.ebiom.2017.08.016. 28844410 . 5605374 . free .