Troriluzole

Troriluzole
Clinical data
Other names	Trigriluzole, BHV-4157, FC-4157
Routes of; administration	By mouth
ATC code	N07XX23 (WHO) ;
Identifiers
	IUPAC name 2-amino-N-[2-[methyl-[2-oxo-2-[[6-(trifluoromethoxy)-1,3-benzothiazol-2-yl]amino]ethyl]amino]-2-oxoethyl]acetamide;
CAS Number	1926203-09-9;
PubChem CID	121488186;
DrugBank	DB15079;
ChemSpider	58828005;
UNII	S7H48S6K7H;
KEGG	D11414;
ChEMBL	ChEMBL4297586;
Chemical and physical data
Formula	C15H16F3N5O4S
Molar mass	419.38 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN(CC(=O)NC1=NC2=C(S1)C=C(C=C2)OC(F)(F)F)C(=O)CNC(=O)CN;
	InChI InChI=1S/C15H16F3N5O4S/c1-23(13(26)6-20-11(24)5-19)7-12(25)22-14-21-9-3-2-8(4-10(9)28-14)27-15(16,17)18/h2-4H,5-7,19H2,1H3,(H,20,24)(H,21,22,25); Key:YBZSGIWIPOUSHY-UHFFFAOYSA-N;

Troriluzole is an experimental medication that has been investigated as a potential treatment for Machado–Joseph disease (MJD),^[1] obsessive–compulsive disorder (OCD),^[2]^[3] and glioblastoma.^[4] It is a prodrug formulation of the medication riluzole.^[2]^[4]

Pharmacology

Pharmacokinetics

While riluzole is typically taken twice-daily and on an empty stomach, troriluzole may offer a potential once-daily dosing with or without food along with greater bioavailability.^[2]^[4]

Research

In 2024, researchers published a study in the Journal of Neurochemistry that reported troriluzole could reverse some early Alzheimer's disease brain changes in mice, reduce harmful glutamate levels, and improve memory and learning abilities.^[5]^[6]

References

^ Meglio, Marco (25 June 2023). "Biohaven Submits New Drug Application for Troriluzole as Spinocerebellar Ataxia Type 3 Therapy". NeurologyLive. Retrieved 17 February 2024.
^ ^a ^b ^c Grassi G, Cecchelli C, Vignozzi L, Pacini S (2020). "Investigational and Experimental Drugs to Treat Obsessive-Compulsive Disorder". Journal of Experimental Pharmacology. 12: 695–706. doi:10.2147/JEP.S255375. PMC 7801912. PMID 33447096.
^ van Roessel PJ, Grassi G, Aboujaoude EN, Menchón JM, Van Ameringen M, Rodríguez CI (January 2023). "Treatment-resistant OCD: Pharmacotherapies in adults". Comprehensive Psychiatry. 120: 152352. doi:10.1016/j.comppsych.2022.152352. hdl:2445/192315. PMID 36368186.
^ ^a ^b ^c Silk AW, Saraiya B, Groisberg R, Chan N, Spencer K, Girda E, Shih W, Palmeri M, Saunders T, Berman RM, Coric V, Chen S, Zloza A, Vieth J, Mehnert JM, Malhotra J (July 2022). "A phase Ib dose-escalation study of troriluzole (BHV-4157), an oral glutamatergic signaling modulator, in combination with nivolumab in patients with advanced solid tumors". European Journal of Medical Research. 27 (1): 107. doi:10.1186/s40001-022-00732-w. PMC 9250196. PMID 35780243.
^ Pfitzer J, Pinky PD, Perman S, Redmon E, Cmelak L, Suppiramaniam V, Coric V, Qureshi IA, Gramlich MW, Reed MN (August 2024). "Troriluzole rescues glutamatergic deficits, amyloid and tau pathology, and synaptic and memory impairments in 3xTg-AD mice". Journal of Neurochemistry. doi:10.1111/jnc.16215. PMID 39214859.
^ "New Drug Shows Promise in Reversing Memory Loss and Cognitive Decline". SciTech (magazine). September 5, 2024. Retrieved September 6, 2024.

[Meglio_2023-1] Meglio, Marco (25 June 2023). "Biohaven Submits New Drug Application for Troriluzole as Spinocerebellar Ataxia Type 3 Therapy". NeurologyLive. Retrieved 17 February 2024.

[pmid33447096-2] Grassi G, Cecchelli C, Vignozzi L, Pacini S (2020). "Investigational and Experimental Drugs to Treat Obsessive-Compulsive Disorder". Journal of Experimental Pharmacology. 12: 695–706. doi:10.2147/JEP.S255375. PMC 7801912. PMID 33447096.

[pmid36368186-3] van Roessel PJ, Grassi G, Aboujaoude EN, Menchón JM, Van Ameringen M, Rodríguez CI (January 2023). "Treatment-resistant OCD: Pharmacotherapies in adults". Comprehensive Psychiatry. 120: 152352. doi:10.1016/j.comppsych.2022.152352. hdl:2445/192315. PMID 36368186.

[pmid35780243-4] Silk AW, Saraiya B, Groisberg R, Chan N, Spencer K, Girda E, Shih W, Palmeri M, Saunders T, Berman RM, Coric V, Chen S, Zloza A, Vieth J, Mehnert JM, Malhotra J (July 2022). "A phase Ib dose-escalation study of troriluzole (BHV-4157), an oral glutamatergic signaling modulator, in combination with nivolumab in patients with advanced solid tumors". European Journal of Medical Research. 27 (1): 107. doi:10.1186/s40001-022-00732-w. PMC 9250196. PMID 35780243.

[pmid39214859-5] Pfitzer J, Pinky PD, Perman S, Redmon E, Cmelak L, Suppiramaniam V, Coric V, Qureshi IA, Gramlich MW, Reed MN (August 2024). "Troriluzole rescues glutamatergic deficits, amyloid and tau pathology, and synaptic and memory impairments in 3xTg-AD mice". Journal of Neurochemistry. doi:10.1111/jnc.16215. PMID 39214859.

[6] "New Drug Shows Promise in Reversing Memory Loss and Cognitive Decline". SciTech (magazine). September 5, 2024. Retrieved September 6, 2024.

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