Ondelopran

Ondelopran
Names
	IUPAC name 6-[2-Fluoro-4-[[2-(oxan-4-yl)ethylamino]methyl]phenoxy]pyridine-3-carboxamide
Identifiers
CAS Number	676501-25-0;
3D model (JSmol)	Interactive image;
ChEMBL	ChEMBL2103878;
ChemSpider	8632801;
DrugBank	DB12585;
KEGG	D10143;
PubChem CID	10457387;
UNII	4VZT670SD9;
	InChI InChI=1S/C20H24FN3O3/c21-17-11-15(12-23-8-5-14-6-9-26-10-7-14)1-3-18(17)27-19-4-2-16(13-24-19)20(22)25/h1-4,11,13-14,23H,5-10,12H2,(H2,22,25) Key: QWNDOCKIKKQJNN-UHFFFAOYSA-N;
	SMILES C1COCCC1CCNCC2=CC(=C(C=C2)OC3=NC=C(C=C3)C(=O)N)F;
Properties
Chemical formula	C20H24FN3O3
Molar mass	373.428 g·mol−1
	Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). Infobox references

Ondelopran (LY-2196044) is an experimental drug being investigated for the treatment of alcoholism.^[1]

Mechanism of action

Ondelopran appears to be an antagonist at opioid receptors,^[2] which means it blocks the action of other opioids (including endogenous opioids like endorphins) by preventing them from binding to the receptor. It antagonizes the three primary opioid receptors with potency of 0.4 (mu), 0.6 (kappa), and 1.9 nM (delta).^[3]

Potential use

A study has shown that treatment with ondelopran reduces the amount of alcohol intake (significantly more than in the placebo group), which means it could be a good path for the treatment of alcoholism.^[4] Another test also displays more results which go in the same conclusion.^[3]

References

^ "ClinicalTrials.gov". clinicaltrials.gov. Retrieved 2024-08-22.
^ Hillemacher, Thomas; Heberlein, Annemarie; Muschler, Marc An; Bleich, Stefan; Frieling, Helge (August 2011). "Opioid modulators for alcohol dependence". Expert Opinion on Investigational Drugs. 20 (8): 1073–1086. doi:10.1517/13543784.2011.592139. ISSN 1744-7658. PMID 21651459.
^ ^a ^b Shagiakhmetov, Farid; Mukhametshina Elvira; Samsonov Mikhail (2019). "Novel triple opioid receptor antagonist ondelopran (LY2196044) for the treatment of alcohol dependence. Phase III study: female subjects subset eﬃcacy and safety analysis". doi:10.13140/RG.2.2.35480.96001. {{cite journal}}: Cite journal requires |journal= (help)
^ Wong, Conrad J.; Witcher, Jennifer; Mallinckrodt, Craig; Dean, Robert A.; Anton, Raymond F.; Chen, Yunfei; Fijal, Bonnie A.; Ouyang, Haojun; Dharia, Sweta; Sundseth, Scott S.; Schuh, Kory J.; Kinon, Bruce J. (February 2014). "A phase 2, placebo-controlled study of the opioid receptor antagonist LY2196044 for the treatment of alcohol dependence". Alcoholism: Clinical and Experimental Research. 38 (2): 511–520. doi:10.1111/acer.12257. ISSN 1530-0277. PMID 24010675.

[1] "ClinicalTrials.gov". clinicaltrials.gov. Retrieved 2024-08-22.

[2] Hillemacher, Thomas; Heberlein, Annemarie; Muschler, Marc An; Bleich, Stefan; Frieling, Helge (August 2011). "Opioid modulators for alcohol dependence". Expert Opinion on Investigational Drugs. 20 (8): 1073–1086. doi:10.1517/13543784.2011.592139. ISSN 1744-7658. PMID 21651459.

[:0-3] Shagiakhmetov, Farid; Mukhametshina Elvira; Samsonov Mikhail (2019). "Novel triple opioid receptor antagonist ondelopran (LY2196044) for the treatment of alcohol dependence. Phase III study: female subjects subset eﬃcacy and safety analysis". doi:10.13140/RG.2.2.35480.96001. {{cite journal}}: Cite journal requires |journal= (help)

[4] Wong, Conrad J.; Witcher, Jennifer; Mallinckrodt, Craig; Dean, Robert A.; Anton, Raymond F.; Chen, Yunfei; Fijal, Bonnie A.; Ouyang, Haojun; Dharia, Sweta; Sundseth, Scott S.; Schuh, Kory J.; Kinon, Bruce J. (February 2014). "A phase 2, placebo-controlled study of the opioid receptor antagonist LY2196044 for the treatment of alcohol dependence". Alcoholism: Clinical and Experimental Research. 38 (2): 511–520. doi:10.1111/acer.12257. ISSN 1530-0277. PMID 24010675.

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