- Guide to PHARMACOLOGY
Synonyms: compound 26h [PMID: 22148278] | SB-1317 | SB1317 | TG-02 | TG02
Compound class: Synthetic organic
Comment: Zotiraciclib (TG02) is an orally active multi-kinase inhibitor, with a unique activity profile against CDKs, JAK2 and FLT3 [4-5]. Like pacritinib it is a small molecule macrocycle. TG02 was rationally designed to simultaneously inhibit several key signalling pathways, with the aim of maximising anti-cancer efficacy. It is being investigated for its anti-leukemic potential [2-3].
The compound is administered as the citrate salt.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|No information available.|
|Summary of Clinical Use|
|TG02 is being evaluated in Phase 1 clinical trials for chronic lymphocytic leukemia or small lymphocytic lymphoma (NCT01699152; dose ranging study) and advanced hematological malignancies (NCT01204164; dose-escalation study with arms investigating TG02 as a monotherapy, in combination with carfilzomib and dexamethasone in multiple myeloma patients and in combination with carfilzomib and dexamethasone in carfilzomib refractory multiple myeloma patients).|
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT01204164||Phase 1 Study of TG02 Citrate in Patients With Advanced Hematological Malignancies||Phase 1 Interventional||Tragara Pharmaceuticals, Inc.|
|NCT01699152||Phase 1 Study of TG02 Citrate in Patients With Chronic Lymphocytic Leukemia and Small Lymphocytic Lymphoma||Phase 1 Interventional||Tragara Pharmaceuticals, Inc.|