Drug intelligence / Profile preview

FV-162

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

**FV-162** is a novel, orally bioavailable, irreversible tripeptide epoxyketone proteasome inhibitor developed using fluorine-based medicinal chemistry to enhance metabolic stability and pharmacokinetics. It selectively inhibits the chymotrypsin-like (CT-L) activity of the proteasome, exhibiting potent cytotoxicity against human multiple myeloma cell lines, primary myeloma patient cells, and drug-resistant cells while sparing normal hematopoietic cells at lower concentrations. In preclinical mouse xenograft models, daily oral dosing reduced tumor burden with favorable tolerability, lower peak plasma concentrations, longer half-life, and higher AUC compared to benchmarks like ONX-0912, positioning it as a promising candidate for blood cancer therapy.[1][2][7]

02

Targets

PSMB5 (Proteasome subunit beta Type-5)

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