Drug intelligence / Profile preview

LUS009

Development stage
Preclinical
Lead developer
Qilu Pharmaceutical
Modality
Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules
Administration
Oral
01

Overview

LUS009 is a proprietary, potent, and orally bioavailable molecular glue degrader (MGD) that specifically targets and degrades the guanine nucleotide exchange factor VAV1 [0971]. Developed by Qilu Pharmaceutical, LUS009 inhibits both T and B cell functions by blocking downstream signaling of the T-cell receptor (TCR) and B-cell receptor (BCR) [0971]. In preclinical evaluations, LUS009 demonstrated superior VAV1 degradation potency in human PBMCs, T cells, and B cells compared to other degraders like MRT-6160, and showed strong anti-inflammatory efficacy in mouse models of colitis [0971]. It is being developed for the potential treatment of inflammatory bowel disease (IBD), rheumatoid arthritis (RA), systemic lupus erythematosus (SLE), and other autoimmune disorders [0971].

02

Targets

VAV1 (Guanine nucleotide exchange factor VAV1)

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