Drugs in Clinical Pipeline: TGR-1202 | Orphan Drug | Kinase Inhibitor | Phosphoinositide 3-kinase delta (PI3Kδ) Inhibitors | Cancer Drug

TGR-1202 [(S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one] is a potent, orally available, small molecule selective phosphoinositide 3-kinase (PI3K) delta (PI3Kδ;  IC₅₀ = 22.23 nM) kinase inhibitor with high selectivity over all other PI3K isoforms (48 – 10000 times) as well that for a 441-kinase panel. The selectivity and activity of TGR-1202 is credited to its design with a unique backbone compared to other PI3K inhibitors in development [1, 2].

TGR-1202 : 2D and 3D Structure

TGR-1202 is currently under clinical development for patients with relapsed and refractory hematological malignancies.

On Aug 24, 2016 TG Therapeutics, Inc. announced that the U.S. Food and Drug Administration (FDA) has granted orphan drug designation for the oral, next generation PI3K-delta (PI3Kδ) inhibitor, TGR-1202, in the treatment of patients with Chronic Lymphocytic Leukemia (CLL).