Drug intelligence / Profile preview

RGT-068A

Development stage
Preclinical
Lead developer
Regor Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

RGT-068A is a potent, selective, and orally bioavailable small molecule inhibitor of mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1). Developed by Regor Therapeutics (also referred to as Ruagen), RGT-068A is designed as a preclinical candidate for the potential treatment of autoimmune diseases and MALT1-dependent cancers, such as diffuse large B-cell lymphoma (DLBCL). The compound features a pyrazoloaminopyrimidine core, and its synthesis involves a highly efficient Heck reaction and N-directed asymmetric hydrogenation to construct its chiral ether unit.

02

Targets

BCL10 (B-cell lymphoma/leukemia 10 protein)NF-κBMALT1 (Mucosa-associated lymphoid tissue lymphoma translocation protein 1)

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