Drug intelligence / Profile preview

FHND6091

Development stage
Phase 1
Lead developer
Jiangsu Chia Tai Fenghai Pharmaceutical
Modality
Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

FHND6091 is a novel, selective oral proteasome inhibitor that acts as a prodrug, being entirely converted into its active form (FHND6081) under physiological conditions. It is an N-capped dipeptidyl boronic acid compound that binds irreversibly to the β5 subunit of the 20S proteasome, thereby inhibiting proteasomal activity and exerting anti-cancer effects. The drug is primarily under development for the treatment of multiple myeloma and has demonstrated promising pharmacological properties in preclinical studies, including significant immunomodulatory activity. Mechanistically, FHND6091 not only inhibits the proteasome but also activates the cGAS-STING pathway in multiple myeloma cells, leading to increased type-I interferon production and enhanced natural killer (NK) cell-mediated tumor cell killing. Clinical trials are ongoing to evaluate its safety and efficacy in patients with relapsed or refractory multiple myeloma[1][2][3][4][5][7].

Other names
FHND91FHND-91FHND 91
02

Targets

PSMB5 (Proteasome subunit beta Type-5)STING (Stimulator of interferon genes protein)

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