Policy & Regulation
PureTech's LYT-100 Demonstrates Tolerability and Pharmacokinetic Proof-of-Concept in Phase 1 Multiple Ascending Dose and Food Effect Study
20 November 2020 - - US-based biotherapeutics company PureTech Health plc (LSE: PRTC) (NASDAQ: PRTC) has completed a Phase 1 multiple ascending dose and food effect study for LYT-100 (deupirfenidone), the company said.

The study demonstrated favourable proof-of-concept for LYT-100's tolerability and pharmacokinetic profile, which will also enable twice-a-day dosing of LYT-100 in future studies.

LYT-100 is PureTech's wholly-owned product candidate that is being advanced for the potential treatment of conditions involving inflammation and fibrosis and disorders of lymphatic flow.

LYT-100 is a deuterated, oral small molecule designed to overcome the challenges associated with pirfenidone, an approved and marketed anti-inflammatory and anti-fibrotic drug.

Pirfenidone is currently approved for the treatment of idiopathic pulmonary fibrosis, but it is associated with significant tolerability issues and dose-limiting toxicities leading approximately 50% of patients to discontinue use, dose adjust or switch therapies, which results in suboptimal disease management.

LYT-100, a new chemical entity, retains the pharmacology of pirfenidone but has a differentiated PK profile, which is designed to enable improved tolerability, less frequent dosing and potentially increased efficacy.

The Phase 1 multiple ascending dose and food effect study was a randomized, double-blind study designed to evaluate the safety, tolerability and PK profile of LYT-100 in healthy participants. In the multiple ascending dose part of the study, participants were initially scheduled to receive increasing doses of LYT-100 up to 750 mg BID.

LYT-100 was well-tolerated at all pre-specified doses, so an additional cohort receiving 1000 mg BID was assessed. LYT-100 was well-tolerated at that dose as well. In the food effect portion of the study, participants received a single dose of 500 mg of LYT-100 with or without food.

All adverse events that were possibly or probably related to LYT-100 were mild and transient and there were no discontinuations.

The most common AEs across all multiple ascending dose cohorts were headache (23.3% with LYT-100 vs. 20.0% with placebo), abdominal distension (10.0% with LYT-100 vs. 0% with placebo), nausea (10.0% with LYT-100 vs. 0% with placebo) and abdominal discomfort (6.7% with LYT-100 vs. 10.0% with placebo).