Drug intelligence / Profile preview

TG02 citrate + carfilzomib + dexamethasone

Development stage
Unknown
Lead developer
Cothera Bioscience
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is an **investigational combination therapy** consisting of **TG02 citrate (zotiraciclib)**, **carfilzomib**, and **dexamethasone**. TG02 citrate (zotiraciclib) is an orally active, spectrum-selective kinase inhibitor targeting cyclin-dependent kinases (notably CDK9), JAK2, and FLT3, developed to deplete Myc and block key cancer cell signaling pathways. Carfilzomib is a second-generation epoxyketone-based proteasome inhibitor. Dexamethasone is a synthetic glucocorticoid with broad anti-inflammatory and immunosuppressive effects. The combination has been studied primarily in early-phase clinical trials for relapsed/refractory multiple myeloma, including heavily pretreated and carfilzomib-refractory populations. Zotiraciclib is under investigation and has received orphan drug status for certain cancers, but the triple combination is not approved for use.

Brand names
Kyprolis + dexamethasone (for the approved combination of carfilzomib + dexamethasone)
Other names
zotiraciclib citrate + carfilzomib + dexamethasoneTG-02 citrate + carfilzomib + dexamethasone
02

Targets

JAK2 (Janus kinase 2)GR (Glucocorticoid receptor)PSMB8 (Immunoproteasome)PSMB5 (Proteasome subunit beta Type-5)CDK9 (Cyclin-dependent kinase 9)FLT3 (Fms related receptor tyrosine kinase 3)

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