From Wikipedia, the free encyclopedia
Chemical compound
Denifanstat
Other names TVB-2640
Legal status
4-[1-[4-Cyclobutyl-2-methyl-5-(5-methyl-1H -1,2,4-triazol-3-yl)benzoyl]piperidin-4-yl]benzonitrile
CAS Number
PubChem
CID
ChemSpider
UNII
ChEMBL
Formula C 27 H 29 N 5 O
Molar mass 439.563 g·mol−1 3D model (
JSmol )
CC1=CC(=C(C=C1C(=O)N2CCC(CC2)C3=CC=C(C=C3)C#N)C4=NNC(=N4)C)C5CCC5
InChI=1S/C27H29N5O/c1-17-14-24(22-4-3-5-22)25(26-29-18(2)30-31-26)15-23(17)27(33)32-12-10-21(11-13-32)20-8-6-19(16-28)7-9-20/h6-9,14-15,21-22H,3-5,10-13H2,1-2H3,(H,29,30,31)
Key:BBGOSBDSLYHMRA-UHFFFAOYSA-N
Denifanstat (TVB-2640 ) is a
small-molecule drug and
fatty acid synthase inhibitor. Developed by Sagimet Biosciences, it has been tested in various types of cancer
[1]
[2]
[3]
[4] and for
non-alcoholic steatohepatitis .
[5]
References
^ Falchook, Gerald; Infante, Jeffrey; Arkenau, Hendrik-Tobias; Patel, Manish R.; Dean, Emma; Borazanci, Erkut; Brenner, Andrew; Cook, Natalie; Lopez, Juanita; Pant, Shubham; Frankel, Arthur; Schmid, Peter; Moore, Kathleen; McCulloch, William; Grimmer, Katharine; O'Farrell, Marie; Kemble, George; Burris, Howard (April 2021).
"First-in-human study of the safety, pharmacokinetics, and pharmacodynamics of first-in-class fatty acid synthase inhibitor TVB-2640 alone and with a taxane in advanced tumors" . eClinicalMedicine . 34 : 100797.
doi :
10.1016/j.eclinm.2021.100797 .
PMC
8040281 .
PMID
33870151 .
^ Konkel, Brandon; Michalek, Joel; Diaz Duque, Enrique; Liu, Qiangia; Caflisch, Laura; Madhu, Vinu; Brenner, Andrew (11 November 2019).
"Actr-45. Fatty Acid Synthase Inhibitor TVB-2640 Increases Progression Free Survival in Recurrent GBM" . Neuro-Oncology . 21 (Supplement_6): vi23.
doi :
10.1093/neuonc/noz175.087 .
PMC
6847162 .
^ Dean, Emma Jane; Falchook, Gerald Steven; Patel, Manish R.; Brenner, Andrew Jacob; Infante, Jeffrey R.; Arkenau, Hendrik-Tobias; Borazanci, Erkut Hasan; Lopez, Juanita Suzanne; Pant, Shubham; Schmid, Peter; Frankel, Arthur E.; Jones, Suzanne Fields; McCulloch, William; Kemble, George; O'Farrell, Marie; Burris, Howard (20 May 2016). "Preliminary activity in the first in human study of the first-in-class fatty acid synthase (FASN) inhibitor, TVB-2640". Journal of Clinical Oncology . 34 (15_suppl): 2512.
doi :
10.1200/JCO.2016.34.15_suppl.2512 .
^ Kelly, William; Diaz Duque, Adolfo Enrique; Michalek, Joel; Konkel, Brandon; Caflisch, Laura; Chen, Yidong; Pathuri, Sarath Chand; Madhusudanannair-Kunnuparampil, Vinu; Floyd, John; Brenner, Andrew (5 July 2023).
"Phase II Investigation of TVB-2640 (Denifanstat) with Bevacizumab in Patients with First Relapse High-Grade Astrocytoma" . Clinical Cancer Research . 29 (13): 2419–2425.
doi :
10.1158/1078-0432.CCR-22-2807 .
PMC
10320469 .
PMID
37093199 .
^
"CTG Labs - NCBI" . clinicaltrials.gov .