Drug intelligence / Profile preview

MPT-0118

Development stage
Phase 1
Lead developer
Monopteros Therapeutics
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

MPT-0118 is an orally bioavailable, small molecule inhibitor of mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1), developed as a potential antineoplastic agent. It is a phenothiazine derivative, specifically the S-enantiomer of mepazine (S-mepazine succinate), and demonstrates approximately tenfold greater MALT1 inhibitory activity than its R-enantiomer. The drug acts by inhibiting the protease activity of MALT1, which plays a key role in regulatory T cell (Treg) function within the tumor microenvironment. By reprogramming Tregs and inducing their fragility, MPT-0118 may enhance anti-tumor immune responses and improve outcomes with checkpoint inhibitor immunotherapies. Preclinical studies have shown single-agent anticancer activity as well as synergy with PD-1 pathway-targeted therapies. Clinical development is ongoing for advanced or metastatic treatment-refractory solid tumors, B-cell lymphoma, brain metastases, and ovarian cancer[1][3][4][5][6].

Other names
S-mepazine succinate
02

Targets

MALT1 (Mucosa-associated lymphoid tissue lymphoma translocation protein 1)

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