Objective: To determine the ADME profile an open-label, single-dose, single period study was conducted with six healthy male subjects.

Background: BIA 28-6156 is an allosteric activator of beta-glucocerebrosidase (GCase) and is being developed by BIAL – Portela & Cª, S.A. as a potential treatment for PD patients who have PD-risk associated variant in the GBA1 gene.

Method: All subjects received 60 mg ¹⁴C-BIA 28-6156, containing not more than 3.7 MBq ¹⁴C. Blood, urine and faecal samples were collected from pre-dose up to 288 h post-dose.

Results: Following administration of ¹⁴C-BIA 28-6156, approximately 93% of the radioactivity was recovered over 288 h. Approximately 71% of total radioactivity (TR) was recovered from urine, indicating renal excretion as the main route of elimination. Exposure to BIA 28-6156 accounted for approximately 92% of circulating plasma TR, indicating that BIA 28-6156 was the main circulating component with no systemic metabolites accounting for >10% of TR. In urine two components accounted for greater than 10% of the dose; metabolites U11 and U12, accounting for 31.84% and 10.80 % of the dose, respectively. In faeces only U11 accounted for more than >10% of the dose. Those metabolites were pharmacologically inactive to GCase up to 30 µM. BIA 28-6156 was well tolerated by healthy male subjects. Three subjects reported a total of 4 AEs, none of which were related to the BIA 28-6156.

Conclusion: Following a single oral administration of ¹⁴C-BIA 28-6156, BIA 28-6156 was identified as the predominant circulating compound. Total radioactivity recovery was nearly complete, with the majority excreted via urine.

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MDS Abstracts - https://www.mdsabstracts.org/abstract/mass-balance-and-metabolism-of-bia-28-6156-an-allosteric-activator-of-beta-glucocerebrosidase-in-humans/