Investigation of the absolute bioavailability and human mass balance of navoximod, a novel IDO1 inhibitor.

ABSTRACT:

Aims

Navoximod (GDC-0919, NLG-919) is a small molecule inhibitor of indoleamine-2,3-dioxygenase 1 (IDO1), developed to treat the acquired immune tolerance associated with cancer. The primary objectives of this study were to assess navoximod's absolute bioavailability (aBA), determine the mass balance and routes of elimination of [¹⁴ C]-navoximod, and characterize navoximod's metabolite profile.

Methods

A phase 1, open-label, two-part study was conducted in healthy volunteers. In Part 1 (aBA), subjects (n = 16) were randomized to receive oral (200 mg tablet) or intravenous (5 mg solution) navoximod in a crossover design with a 5-day washout. In Part 2 (mass balance), subjects (n = 8) were administered [¹⁴ C]-navoximod (200 mg/600 μCi) as an oral solution

SUBMITTER: Ma S 

PROVIDER: S-EPMC6624388 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature