LTSE-2578 / Structure Therap, Schrodinger - LARVOL DELTA

A Phase I, Randomized, Double-Blind, Placebo-Controlled, First in Human Study of the Safety, Tolerability, and Pharmacokinetics of Single and Multiple Ascending Doses of LTSE-2578 in Healthy Participants (ANZCTR) - P1 | N=64 | Completed | Sponsor: Lhotse Bio, Inc. | Not yet recruiting ➔ Completed

Trial completion • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease • Respiratory Diseases

Structure Therapeutics Reports Second Quarter 2025 Financial Results and Recent Highlights (GlobeNewswire) - P1 | N=64 | ACTRN12624000535572 | "Structure Therapeutics has successfully finished a Phase 1 single and multiple ascending dose clinical study of LTSE-2578, an oral small molecule antagonist that targets the LPA1R for the treatment of IPF. In the study there was no evidence of any dose-dependent LTSE-2578-related adverse events, including clinical, laboratory and electrocardiogram recordings. No SAEs were observed in the study."

P1 data • Trial status • Idiopathic Pulmonary Fibrosis

A Phase I, Randomized, Placebo-Controlled, First in Human Study of the Safety, Tolerability, and Pharmacokinetics of Single and Multiple Ascending Doses of LTSE-2578 in Healthy Participants (ANZCTR) - P1 | N=64 | Not yet recruiting | Sponsor: Lhotse Bio, Inc.

New P1 trial • Fibrosis • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease • Respiratory Diseases

Structure Based Discovery and Anti-fibrotic Activity of Novel Antagonists of Lysophosphatidic Acid Receptor 1 (LPAR1) (ATS 2023) - "The 1st generation LPAR1 antagonist, BMS-986020, demonstrated a significant reduction in forced vital capacity (FVC) decline in a 6-month phase II trial in IPF patients but was terminated due to compound-specific hepatobiliary toxicity...Lead compounds were evaluated for LPAR1 antagonist activity in a mouse model of LPA-mediated histamine release, anti-fibrotic efficacy in a mouse model of bleomycin induced lung fibrosis, and toxicity in preclinical species. Structure-based drug design and Schrödinger FEP modeling dramatically shortened compound synthesis and testing cycles resulting in the identification of multiple novel LPAR1 antagonist chemical series with nanomolar potency in LPAR1 Ca2+ flux assay...Two lead compounds LTSE A and B showed potent in vitro activity with nanomolar IC50 in Ca2+ flux assay and fibroblast migration inhibition... Novel oral LPAR1 antagonists were discovered through structure-based drug design. The advanced leads with superior potency..."

Fibrosis • Hepatology • Idiopathic Pulmonary Fibrosis • Immunology • Respiratory Diseases • ABCC3