Chemistry:Daporinad
Daporinad (FK866, APO866), is a drug which acts as a selective inhibitor of the enzyme nicotinamide phosphoribosyltransferase (NAMPT). Levels of this enzyme are elevated in certain forms of cancer such as leukemia, and it was hoped that NAMPT inhibitors would be useful in the treatment of cancer. Unfortunately, dapinorad was unsuccessful in clinical trials due to lack of efficacy, but it still has antiinflammatory effects and may be useful for other medical applications such as arthritis, as well as being widely used as a tool compound for the study of NAMPT and its function.[1][2][3][4][5][6][7]
Daporinad was originally identified and developed by Klinge Pharma G.m.b.H.,[8] Development rights then moved through a corporate chain in which Fujisawa Deutschland GmbH[9] which later merged into Astellas held APO866/FK866 and subsequently out-licensed the worldwide development and marketing rights to the Danish oncology company TopoTarget in 2005, after which TopoTarget merged with BioAlliance Pharma to form Onxeo, which later rebranded as Valerio Therapeutics.[10]
References
- ↑ "Nampt/PBEF/visfatin and cancer". Cancer Biology & Therapy 10 (2): 119–125. July 2010. doi:10.4161/cbt.10.2.12581. PMID 20647743.
- ↑ "Nicotinamide phosphoribosyltransferase as a target in inflammation- related disorders". Current Topics in Medicinal Chemistry 13 (23): 2930–2938. 2013. doi:10.2174/15680266113136660208. PMID 24171767.
- ↑ "Medicinal chemistry of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors". Journal of Medicinal Chemistry 56 (16): 6279–6296. August 2013. doi:10.1021/jm4001049. PMID 23679915.
- ↑ "Visfatin as a therapeutic target for rheumatoid arthritis". Expert Opinion on Therapeutic Targets 23 (7): 607–618. July 2019. doi:10.1080/14728222.2019.1617274. PMID 31074669.
- ↑ "Advances in NAD-Lowering Agents for Cancer Treatment". Nutrients 13 (5): 1665. May 2021. doi:10.3390/nu13051665. PMID 34068917.
- ↑ "Review of various NAMPT inhibitors for the treatment of cancer". Frontiers in Pharmacology 13. 2022. doi:10.3389/fphar.2022.970553. PMID 36160449.
- ↑ "The Role of Visfatin in Gastric and Esophageal Cancer: From Biomarker to Therapeutic Target". Cancers 17 (8): 1377. April 2025. doi:10.3390/cancers17081377. PMID 40282553.
- ↑ Biedermann E, Hasmann M, Löser R, Rattel B, Reiter F, Schein B, Seibel K, Vogt K, "Pyridyl alkene- and pyridyl alkyne-acid amides as cytostatics and immunosuppressives", WO patent 1997/048696A1, published 1997-12-24 Example 7: N-[4-(l-benzoylpiperidin-4-yl)-butyl]-3-(pyridin-3-yl)-acrylamide (substance 159)
- ↑ "FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis". Cancer Research 63 (21): 7436–7442. November 2003. PMID 14612543.
- ↑ "Valerio Therapeutics SA". Synapse. PatSnap. https://synapse.patsnap.com/organization/0830f6c82a2e35f87a16074dbcc4a1b8?.
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