Avila Therapeutics announced results from two Phase 1a studies of AVL-292 for the treatment of B-cell cancers. This was a double-blind, placebo-controlled, single-ascending dose study in healthy volunteers. The study showed that AVL-292 achieved statistically significant levels of target occupancy at all dose levels, with >80% Bruton’s tyrosine kinase (Btk) target site occupancy achieved at doses as low as 1.0mg/kg. It was well absorbed with good systemic exposure, and demonstrated a dose-proportional pharmacokinetic profile across all dose levels (ranging from 0.5–7.0mg/kg) with low inter-subject variability.
AVL-292 is an orally available, covalent drug that targets Btk. Inhibition of Btk is a new approach to treatment of diseases that are driven by B-cells, including certain cancers and autoimmune diseases. AVL-292 selectively and covalently binds to Btk to inactivate and silence its activity.
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