Drug intelligence / Profile preview

PBS-1086

Development stage
Preclinical
Lead developer
Aurobindo Pharma
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

PBS-1086 (also known as REM-1086) is a small-molecule, dual inhibitor of both the canonical and non-canonical NF-κB (nuclear factor kappa-light-chain-enhancer of activated B cells) signaling pathways. It acts as a 'pan-Rel' inhibitor, blocking the DNA-binding activity of all five Rel family transcription factor subunits: RelA/p65, RelB, c-Rel, NF-κB1/p50, and NF-κB2/p52. Originally developed by Profectus BioSciences and later spun out to Rel-MD, PBS-1086 has been investigated preclinically for its therapeutic potential in multiple myeloma, chronic lymphocytic leukemia (CLL), non-small cell lung cancer (NSCLC), breast cancer, and rheumatoid arthritis. It has demonstrated the ability to induce apoptosis in cancer cells, overcome microenvironment-mediated drug resistance, and act as a radiosensitizer or chemosensitizer (e.g., in combination with bortezomib or EGFR inhibitors).

02

Targets

RELB (Nuclear factor kappa-light-chain-enhancer of activated B cells subunit RelB)REL (Proto-oncogene c-Rel)RELA (Nuclear Factor Kappa B Subunit p65)NFKB2 (NF-κB2)NFKB1 (NF-κB1)

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