June 5, 2025 – Leadingtac Pharmaceutical Co., Ltd. ("Leadingtac"), a clinical stage biotech company focused on innovative drug discovery and development in autoimmune disease and oncology, announced today that the first patient has been dosed in the Phase Ic clinical study of its independently developed IRAK4 protein degrader LT-002 for the treatment of atopic dermatitis (AD). This marks another significant milestone following the completion of the Phase I trial in healthy volunteers, signifying the project's official entry into the patient clinical trial stage.

The Phase I clinical trial of LT-002 (randomized, double-blind, placebo-controlled) included over 120 healthy volunteers. The results showed that LT-002 demonstrated a favorable safety and tolerability profile, superior PK characteristics, and achieved over 99% IRAK4 degradation in PBMC and over 95% in the skin after multiple doses. LT-002 also showed excellent inhibition on pro-inflammatory cytokines. These data provide a solid foundation for the Phase Ic trial design and dose exploration, and reinforce our confidence in the further clinical development of LT-002.

The multi-center open-label, dose-escalation Phase Ic clinical trial of LT-002 is currently evaluating the safety, tolerability, pharmacokinetics and preliminary efficacy of LT-002 in patients with moderate-to-severe AD. This study will provide crucial evidence for dose selection and trial design for the subsequent Phase II study.

Dr. Yan Feng, Founder and CEO of Leadingtac, said, "The completion of the first patient dosing in the Phase IC clinical trial represents a significant milestone of LT-002 program in our mission to bring innovative and urgently needed therapies to patients in need. We are excited to accelerate the pace of clinical development and bringing this innovative drug to patients as soon as possible. According to the unblinded data from the Phase I trial in healthy volunteers, LT-002 not only proves a good safety, tolerability, and PK profile, but also demonstrates potent IRAK4 protein degradation and significant anti-inflammatory activity in skin tissue. This strengthens our confidence in advancing the Phase Ic clinical study. We look forward to the data from this Phase 1c trial, which will add to the understanding of the safety and efficacy of LT-002 in patients, bringing a new treatment option to the vast number of individuals affected."

About Atopic Dermatitis (AD)

Atopic Dermatitis is a chronic, relapsing disease characterized by epidermal barrier disruption, T-cell activation, and imbalance of the skin microbiome. One characteristic symptom of atopic dermatitis is pruritus, which diminishes quality of life. Patients with AD suffer burdensome itch, sleep disturbance, symptoms of anxiety and depression, and diminished health-related quality of life (QOL), all of which are worsen with increasing disease severity. Furthermore, when AD is progressed to moderate or severe, it often can be difficult to manage.

In Europe and USA, recent data suggests that the prevalence of AD is approximately 20% among children and ranges from 7% to 14% among adults, with substantial variation across different countries (Bylund S., et al, 2020). Treatment options for moderate-to-severe AD include topical therapies, phototherapy, systemic corticosteroids, immunosuppressants, and Dupilumab. Despite these treatments, AD remains a major societal burden and a significant unmet medical need.

About Us:

Leadingtac is a leading company in the field of PROTAC drug discovery and development in China. Founded at the end of 2019, Leadingtac has established R&D centers in Zhangjiang, Pudong, Shanghai and Keqiao, Shaoxing, Zhejiang. The company focuses on the field of Targeted Protein Degradation and has independently developed the unique SPUD® (Specific Protein Ubiquitination and Degradation) technology platform for the efficient and rapid screening of proteasomal degradation, new E3 ligase ligands, and lysosomal degradation.

Nano-SPUD® for Target Proteins

Nano-SPUD® for E3 Ligases

Lyso-SPUD® for Lysosome

Based on this platform, Leadingtac has independently developed its first pipeline of IRAK4 degrader LT-002 for the treatment of autoimmune diseases. With significant market potential, it has received approvals from both the CDE and FDA to enter clinical trials in China and the US, the first in China and second globally in terms of development progress.

Leadingtac's follow-on pipelines includes the JAK-STAT pathway, KRAS and other ‘undruggable’ proteins for the treatment of autoimmune diseases, as well as solid tumors such as lung, pancreatic, and colorectal cancers, a with its R&D progress also being among the world's leading.