Ampreloxetine

Ampreloxetine
Clinical data
Other names	TD-9855
Drug class	Norepinephrine reuptake inhibitor; Serotonin–norepinephrine reuptake inhibitor
Pharmacokinetic data
Elimination half-life	30–40 hours
Identifiers
	IUPAC name 4-[2-[(2,4,6-trifluorophenoxy)methyl]phenyl]piperidine;
CAS Number	1227056-84-9 [GSRS];
PubChem CID	46189893;
DrugBank	DB15348;
ChemSpider	64853713;
UNII	19997EZ42I;
KEGG	D11688;
ChEMBL	ChEMBL4297646;
Chemical and physical data
Formula	C18H18F3NO
Molar mass	321.343 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1CNCCC1C2=CC=CC=C2COC3=C(C=C(C=C3F)F)F;
	InChI InChI=1S/C18H18F3NO/c19-14-9-16(20)18(17(21)10-14)23-11-13-3-1-2-4-15(13)12-5-7-22-8-6-12/h1-4,9-10,12,22H,5-8,11H2; Key:TZIALEBTHQWNAO-UHFFFAOYSA-N;

Ampreloxetine (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; developmental code name TD-9855) is a selective norepinephrine reuptake inhibitor (NRI) which is under development for the treatment of symptomatic neurogenic orthostatic hypotension (NOH).^[2]^[3]^[4]

It shows high affinity for both the norepinephrine transporter (NET) and the serotonin transporter (SERT), with 4-fold selectivity for the NET over the SERT, and is thought to act as a dual serotonin–norepinephrine reuptake inhibitor (SNRI) at higher doses.^[4]^[1]

As of November 2023, ampreloxetine is in phase 3 clinical trials for NOH.^[2] The drug was also under development for the treatment of attention deficit hyperactivity disorder (ADHD) and fibromyalgia, but development for these uses was discontinued.^[2]^[5]

References

^ ^a ^b Kanodia J, Lo A, Baldwin RM, Graham RA, Bourdet DL (January 2021). "Pharmacokinetics of Ampreloxetine, a Norepinephrine Reuptake Inhibitor, in Healthy Subjects and Adults with Attention-Deficit/Hyperactive Disorder or Fibromyalgia Pain". Clin Pharmacokinet. 60 (1): 121–131. doi:10.1007/s40262-020-00918-7. PMC 7808980. PMID 32856281.
^ ^a ^b ^c "Ampreloxetine - Theravance Biopharma". AdisInsight. 21 November 2023. Retrieved 26 September 2024.
^ Hoxhaj P, Shah S, Muyolema Arce VE, Khan W, Sadeghzadegan A, Singh S, Collado GF, Goyal A, Khawaja I, Botlaguduru D, Razzaq W, Abdin ZU, Gupta I (May 2023). "Ampreloxetine Versus Droxidopa in Neurogenic Orthostatic Hypotension: A Comparative Review". Cureus. 15 (5): e38907. doi:10.7759/cureus.38907. PMC 10257554. PMID 37303338.
^ ^a ^b Smith JA, Bourdet DL, Daniels OT, Ding YS, Gallezot JD, Henry S, Kim KH, Kshirsagar S, Martin WJ, Obedencio GP, Stangeland E, Tsuruda PR, Williams W, Carson RE, Patil ST (December 2014). "Preclinical to clinical translation of CNS transporter occupancy of TD-9855, a novel norepinephrine and serotonin reuptake inhibitor". Int J Neuropsychopharmacol. 18 (2). doi:10.1093/ijnp/pyu027. PMC 4368888. PMID 25522383.
^ Pozzi M, Bertella S, Gatti E, Peeters GG, Carnovale C, Zambrano S, Nobile M (December 2020). "Emerging drugs for the treatment of attention-deficit hyperactivity disorder (ADHD)". Expert Opin Emerg Drugs. 25 (4): 395–407. doi:10.1080/14728214.2020.1820481. hdl:2434/851076. PMID 32938246.

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[KanodiaLoBaldwin2021-1] Kanodia J, Lo A, Baldwin RM, Graham RA, Bourdet DL (January 2021). "Pharmacokinetics of Ampreloxetine, a Norepinephrine Reuptake Inhibitor, in Healthy Subjects and Adults with Attention-Deficit/Hyperactive Disorder or Fibromyalgia Pain". Clin Pharmacokinet. 60 (1): 121–131. doi:10.1007/s40262-020-00918-7. PMC 7808980. PMID 32856281.

[AdisInsight-2] "Ampreloxetine - Theravance Biopharma". AdisInsight. 21 November 2023. Retrieved 26 September 2024.

[HoxhajShahMuyolema2023-3] Hoxhaj P, Shah S, Muyolema Arce VE, Khan W, Sadeghzadegan A, Singh S, Collado GF, Goyal A, Khawaja I, Botlaguduru D, Razzaq W, Abdin ZU, Gupta I (May 2023). "Ampreloxetine Versus Droxidopa in Neurogenic Orthostatic Hypotension: A Comparative Review". Cureus. 15 (5): e38907. doi:10.7759/cureus.38907. PMC 10257554. PMID 37303338.

[SmithBourdetDaniels2014-4] Smith JA, Bourdet DL, Daniels OT, Ding YS, Gallezot JD, Henry S, Kim KH, Kshirsagar S, Martin WJ, Obedencio GP, Stangeland E, Tsuruda PR, Williams W, Carson RE, Patil ST (December 2014). "Preclinical to clinical translation of CNS transporter occupancy of TD-9855, a novel norepinephrine and serotonin reuptake inhibitor". Int J Neuropsychopharmacol. 18 (2). doi:10.1093/ijnp/pyu027. PMC 4368888. PMID 25522383.

[PozziBertellaGatti2020-5] Pozzi M, Bertella S, Gatti E, Peeters GG, Carnovale C, Zambrano S, Nobile M (December 2020). "Emerging drugs for the treatment of attention-deficit hyperactivity disorder (ADHD)". Expert Opin Emerg Drugs. 25 (4): 395–407. doi:10.1080/14728214.2020.1820481. hdl:2434/851076. PMID 32938246.

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