Drug intelligence / Profile preview

TG02 + carfilzomib

Development stage
Preclinical
Lead developer
Cothera Bioscience
Modality
Small Molecules
Administration
Intravenous
01

Overview

TG02 + carfilzomib is an investigational combination therapy for multiple myeloma composed of **TG02**, a multi-kinase inhibitor targeting kinases including cyclin-dependent kinase 9 (CDK9), and **carfilzomib**, a second-generation proteasome inhibitor approved for use in relapsed/refractory multiple myeloma. TG02 is known to decrease expression of Mcl-1 protein mainly via translational regulation, while carfilzomib inhibits proteasome function leading to increased expression of the pro-apoptotic protein NOXA and indirectly inhibiting the anti-apoptotic protein Mcl-1. The dual action aims for enhanced apoptosis in myeloma cells by 'dual inhibition' of Mcl-1 and promising additive or synergistic therapeutic effects. This combination has shown additive efficacy in preclinical myeloma models and patient samples, with ongoing research to elucidate full mechanisms and therapeutic potential[1][3][5].

02

Targets

26S proteasomeCDK9 (Cyclin-dependent kinase 9)JAK2 (Janus kinase 2)FLT3 (Fms related receptor tyrosine kinase 3)

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