LY3509754 / Eli Lilly - LARVOL DELTA

Discovery and In Vivo Exploration of 1,3,4-Oxadiazole and α-Fluoroacrylate Containing IL-17 Inhibitors. (PubMed, J Med Chem) - "IL-17 blocking antibodies like secukinumab (Cosentyx) have been developed and are used to treat conditions like psoriasis, psoriatic arthritis, and ankylosing spondylitis. Both compounds effectively reduced knee swelling in a rat arthritis model. However, early rat and dog toxicity studies revealed adverse findings, preventing their further development and indicating that furazan might not be responsible for the adverse effects of LY3509754."

Journal • Preclinical • Ankylosing Spondylitis • Dermatology • Immunology • Infectious Disease • Inflammation • Inflammatory Arthritis • Psoriasis • Psoriatic Arthritis • Rheumatology • Seronegative Spondyloarthropathies • IL17A

Safety, Tolerability, and Pharmacokinetics of an Oral Small Molecule Inhibitor of IL-17A (LY3509754): A Phase I Randomized Placebo-Controlled Study. (PubMed, Clin Pharmacol Ther) - P1 | "We theorize that the DILI relates to an off-target effect rather than IL-17A inhibition. In conclusion, despite strong target engagement and a PK profile that supported once-daily administration, this study showed that oral dosing with LY3509754 was poorly tolerated."

Journal • P1 data • PK/PD data • Dermatology • Hepatology • Immunology • Inflammation • Liver Failure • Psoriasis • IL17A

A Study of LY3509754 in Healthy Non-Japanese and Japanese Participants (clinicaltrials.gov) - P1 | N=104 | Terminated | Sponsor: Eli Lilly and Company | Suspended ➔ Terminated; Terminated due to safety findings

Trial termination

A Study of LY3509754 in Healthy Non-Japanese and Japanese Participants (clinicaltrials.gov) - P1 | N=105 | Suspended | Sponsor: Eli Lilly and Company | Trial completion date: Feb 2022 ➔ Sep 2022 | Trial primary completion date: Feb 2022 ➔ Sep 2022

Trial completion date • Trial primary completion date

A Safety Study of LY3462817 and LY3509754 in Participants With Psoriasis (clinicaltrials.gov) - P1 | N=30 | Terminated | Sponsor: Eli Lilly and Company | N=94 ➔ 30 | Active, not recruiting ➔ Terminated; Terminated due to liver findings

Enrollment change • Trial termination • Dermatology • Immunology • Psoriasis

A Safety Study of LY3462817 and LY3509754 in Participants With Psoriasis (clinicaltrials.gov) - P1 | N=94 | Active, not recruiting | Sponsor: Eli Lilly and Company | Suspended ➔ Active, not recruiting

Enrollment closed • Dermatology • Immunology • Psoriasis

A Safety Study of LY3462817 and LY3509754 in Participants With Psoriasis (clinicaltrials.gov) - P1; N=94; Suspended; Sponsor: Eli Lilly and Company; Trial completion date: Jul 2022 ➔ Mar 2022; Trial primary completion date: Jul 2022 ➔ Mar 2022

Clinical • Trial completion date • Trial primary completion date • Dermatology • Immunology • Psoriasis

A Study of LY3509754 in Healthy Non-Japanese and Japanese Participants (clinicaltrials.gov) - P1; N=105; Suspended; Sponsor: Eli Lilly and Company; Trial completion date: Oct 2021 ➔ Feb 2022; Active, not recruiting ➔ Suspended; Trial primary completion date: Oct 2021 ➔ Feb 2022

Clinical • Trial completion date • Trial primary completion date • Trial suspension

A Safety Study of LY3462817 and LY3509754 in Participants With Psoriasis (clinicaltrials.gov) - P1; N=94; Suspended; Sponsor: Eli Lilly and Company; Trial completion date: Apr 2022 ➔ Jul 2022; Trial primary completion date: Apr 2022 ➔ Jul 2022

Clinical • Trial completion date • Trial primary completion date • Dermatology • Immunology • Psoriasis