Drug intelligence / Profile preview

LCB-03-0110

Development stage
Preclinical
Lead developer
Georgetown University Medical Center
Modality
Small Molecules
Administration
Topical, Oral, Systemic
01

Overview

LCB-03-0110 is a **potent multi-tyrosine kinase inhibitor** developed as a small molecule drug targeting several key kinases, including Discoidin domain receptor 1 (DDR1), C-terminal Src kinase (CSK), Janus kinase (JAK), Signal transducer and activator of transcription 3 (STAT3), and Vascular endothelial growth factor receptor 2 (VEGFR2). It acts via **ATP-competitive inhibition** at the kinase active site, suppressing multiple pro-inflammatory and pro-angiogenic signaling pathways. LCB-03-0110 shows anti-inflammatory activity by significantly inhibiting phosphorylation of ERK and P38 and reducing expression of inflammatory cytokines (IL-6, IL-8, IL-17A), with efficacy demonstrated in models for dry eye disease, tumor angiogenesis, and neurodegenerative pathology. It additionally inhibits Tie2, BTK, SYK, FLT1, FLT3, FLT4, EphA3, EphB4, and c-Abl. Studies show benefits over tacrolimus and tofacitinib without cytotoxicity to tested cells, and promising anti-angiogenic and anti-metastatic effects in preclinical models[1][2][3][5].

Other names
LCB-03-0110LCB03-0110LCB 03-0110LCB-03-110LCB03-110LCB 03-110
02

Targets

BTK (Bruton tyrosine kinase)DDR1 (Discoidin domain receptor 1)DDR2 (Discoidin domain receptor tyrosine kinase 2)SYK (Spleen Tyrosine Kinase)TEK (Tie2)VEGFR2 (Vascular endothelial growth factor receptor 2)CSK (C-terminal Src kinase)JAK (Janus kinase family)STAT3 (Signal Transducer and Activator of Transcription 3)EPHA3 (Ephrin Receptor A3)EPHB4 (Ephrin type-B receptor 4)FLT3 (Fms related receptor tyrosine kinase 3)RET (Rearranged during transfection receptor tyrosine kinase)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)SRC (Proto-oncogene tyrosine-protein kinase Src)

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