Absorption, metabolism and excretion of opicapone in human healthy volunteers

Aims The absorption, metabolism and excretion of opicapone (2,5‐dichloro‐3‐(5‐[3,4‐dihydroxy‐5‐nitrophenyl]‐1,2,4‐oxadiazol‐3‐yl)‐4,6‐dimethylpyridine 1‐oxide), a selective catechol‐O‐methyltransferase inhibitor, were investigated. Methods Plasma, urine and faeces were collected from healthy male su...

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Bibliographic Details
Published in:British journal of clinical pharmacology 2022-10, Vol.88 (10), p.4540-4551
Main Authors: Loureiro, Ana I., Rocha, Francisco, Santos, Ana T., Singh, Nand, Bonifácio, Maria João, Pinto, Rui, Kiss, Laszlo E., Soares‐da‐Silva, Patrício
Format: Article
Language:English
Subjects:
COMT inhibitor
human
mass balance
metabolism
opicapone
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Summary:Aims The absorption, metabolism and excretion of opicapone (2,5‐dichloro‐3‐(5‐[3,4‐dihydroxy‐5‐nitrophenyl]‐1,2,4‐oxadiazol‐3‐yl)‐4,6‐dimethylpyridine 1‐oxide), a selective catechol‐O‐methyltransferase inhibitor, were investigated. Methods Plasma, urine and faeces were collected from healthy male subjects following a single oral dose of 100 mg [14C]‐opicapone. The mass balance of [14C]‐opicapone and metabolic profile were evaluated. Results The recovery of total administered radioactivity averaged >90% after 144 hours. Faeces were the major route of elimination, representing 70% of the administered dose; 5% and 20% were excreted in urine and expired air, respectively. The Cmax of total radioactivity matched that of unchanged opicapone, whereas the total radioactivity remained quantifiable for a longer period, attributed to the contribution of opicapone metabolites, involving primarily 3‐O‐sulfate conjugation (58.6% of total circulating radioactivity) at the nitrocatechol ring. Other circulating metabolites, accounting for
ISSN:0306-5251
1365-2125
DOI:10.1111/bcp.15383