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Overview

Tags

Neoplasms

Immune System Diseases

Skin and Musculoskeletal Diseases

Small molecule drug

Disease domain score

A glimpse into the focused therapeutic areas

Technology Platform

Most used technologies in drug development

Targets

Most frequently developed targets

Disease Domain	Count

Neoplasms	4
Immune System Diseases	1

Top 5 Drug Type	Count

Small molecule drug	6

Top 5 Target	Count

CSF-2R x PDL1	1
CSF-1R(Colony stimulating factor 1 receptor)	1
PDL1(Programmed death-ligand 1)	1
TNF-α(Tumor necrosis factor α)	1
IL-6(Interleukin-6)	1

Randomized, Double-Blind, Placebo-Controlled, Multiple Ascending Dose Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of IA-14069 in Healthy Subjects, With an Extension to Explore Any Drug-Drug Interaction Potential With Methotrexate (Part 1), and in Patients With Rheumatoid Arthritis, With Preliminary Assessment of Efficacy in Patients (Part 2)

The purpose of this study is to assess the safety, tolerability, pharmacokinetics, and pharmacodynamics of multiple ascending oral doses of IA-14069 in healthy subjects and in patients with RA on stable dosese of MTX, with preliminary assessment of efficacy in RA patients.

Start Date10 Oct 2022

Sponsor / Collaborator

iLab Co., Ltd

NCT05317741

/ CompletedPhase 1

A Phase 1, First-in-human, Double-Blind, Placebo-Controlled, Single Ascending Dose Study to Evaluate the Safety, Tolerability, Pharmacokinetics, Food Effect, and Pharmacodynamics Following a Single Oral Dose of IA-14069 in Healthy Male Subjects

The purpose of this study is to assess the safety, tolerability, pharmacokinetics, food effect, and pharmacodynamics following a single oral dose of IA-14069 in healthy male subjects.

Start Date23 Aug 2021

Sponsor / Collaborator

iLab Co., Ltd

100 Clinical Results associated with iLab Co., Ltd

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0 Patents (Medical) associated with iLab Co., Ltd

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1

Literatures (Medical) associated with iLab Co., Ltd

21 Apr 2025·Cancer Research

Abstract 3213: IA-05592: A breakthrough oral PD-L1 inhibitor with exceptional anti-tumor efficacy and immune activation potential

Author: Yang, Deokmo ; Kim, Ye Eun ; Heo, Tae-Hwe ; Choi, Garam ; Kim, Myung Jin ; Lee, Sol ; Shin, Kye Jung ; Oh, Taegwon ; Sung, Jongmin ; Kang, Yeo Wool

AbstractProgrammed death-ligand 1 (PD-L1) is a key immune checkpoint protein that interacts with PD-1 on T cells to suppress anti-tumor immunity. While PD-1/PD-L1 antibodies have become a cornerstone of cancer therapy, their limitations, including poor tumor penetration, immunogenicity, immune-related risks due to long half-life, and high production costs, have driven interest in small-molecule alternatives. IA-05592, a novel orally bioavailable small-molecule PD-L1 inhibitor, was developed using structure-based drug design to disrupt PD-1/PD-L1 interactions. This compound offers advantages such as oral bioavailability, reduced costs, and a novel mechanism of action involving PD-L1 internalization and degradation. Biochemical assays using fluorescence resonance energy transfer (FRET) demonstrated IA-05592’s potency in disrupting PD-1/PD-L1 interactions, while cellular activity assays confirmed its ability to activate T cells, with an EC50 of 14 nM in NFAT reporter assays. IA-05592 reduced PD-L1 expression on tumor cells by inducing internalization and degradation, a mechanism confirmed in MC38 cells engineered to express human PD-L1 (MC38-hPD-L1). In vivo, daily oral administration of IA-05592 in a human PD-L1 knock-in MC38 syngeneic mouse model at doses of 10, 30, and 90 mg/kg resulted in dose-dependent tumor reduction. Combination studies with Fingolimod confirmed that IA-05592’s anti-tumor effects are immune-mediated. Pharmacokinetic and ADME studies in rodents revealed high oral bioavailability and systemic exposure, further supporting its therapeutic potential. These findings position IA-05592 as a promising candidate for next-generation cancer immunotherapy, offering a unique mechanism of action and robust preclinical anti-tumor efficacy comparable to anti-PD-L1 antibodies. Ongoing studies aim to advance IA-05592 as a key component of all-oral cancer immunotherapy regimens.Citation Format:Yeo Wool Kang, Ye Eun Kim, Garam Choi, Sol Lee, Deokmo Yang, Jongmin Sung, Kye Jung Shin, Tae-Hwe Heo, Taegwon Oh, Myung Jin Kim. IA-05592: A breakthrough oral PD-L1 inhibitor with exceptional anti-tumor efficacy and immune activation potential [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2025; Part 1 (Regular Abstracts); 2025 Apr 25-30; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2025;85(8_Suppl_1):Abstract nr 3213.

100 Deals associated with iLab Co., Ltd

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100 Translational Medicine associated with iLab Co., Ltd

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Pipeline

Pipeline Snapshot as of 11 May 2025

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

Discovery

4

1

Preclinical

Phase 1 Clinical

1

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

IA-14069 ( TNF-α )	Rheumatoid Arthritis More	Phase 1
IA-05592 ( PDL1 )	Neoplasms More	Preclinical
Anti-inflammatory project (ILAb) ( IL-6 )	Inflammation More	Discovery
Cancer therapeutics project (iLab) ( CSF-2R x PDL1 )	Neoplasms More	Discovery
CSF1R program (iLab) ( CSF-1R )	Neoplasms More	Discovery