Umbralisib

Umbralisib
Clinical data
Other names	RP5264; TGR 1202
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name 2-[(1S)-1-[4-Amino-3-(3-fluoro-4-propan-2-yloxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-6-fluoro-3-(3-fluorophenyl)chromen-4-one;
CAS Number	1532533-67-7;
PubChem CID	72950888;
Chemical and physical data
Formula	C31H24F3N5O3
Molar mass	571.560 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@@H](C1=C(C(=O)C2=C(O1)C=CC(=C2)F)C3=CC(=CC=C3)F)N4C5=NC=NC(=C5C(=N4)C6=CC(=C(C=C6)OC(C)C)F)N;

Umbralisib (development codes RP5264 and TGR 1202) is an experimental oral PI3K delta inhibitor.[1] It also inhibits CK1 epsilon.[2]

It has undergone clinical studies for chronic lymphocytic leukemia (CLL).[3][4] Three year data (including follicular lymphoma and DLBCL) was announced June 2016.[5] It is in combination trials for various leukemias and lymphomas, such as mantle cell lymphoma (MCL)[6][7] and other lymphomas.[8]

The drug has been granted the FDA's breakthrough therapy status for use in patients with marginal zone lymphoma (MZL), a type of cancer with no specifically approved therapies.[9]

References

Clinical trial number NCT01767766 for "Evaluate the Safety and Efficacy of TGR 1202 in Patients With Relapsed or Refractory Hematologic Malignancies" at ClinicalTrials.gov
Umbralisib Shows Early Promise in CLL and Lymphoma. Feb 2018
Novel BTK, PI3K Inhibitors on Horizon for Relapsed CLL. March 2016
Therapy Focus –- TG Could Benefit From Zydelig Setback. March 2016
TG Therapeutics Inc.: TG Therapeutics, Inc. Announces First Patient Enrolled in the Registration-Directed UNITY-DLBCL Phase 2b Trial. June 2016
Clinical trial number NCT02268851 for "A Phase I/Ib Safety and Efficacy Study of the PI3K-delta Inhibitor TGR-1202 and Ibrutinib in Patients With CLL or MCL" at ClinicalTrials.gov
Follow-Up Data for Combination of TGR-1202 (umbralisib) plus Ibrutinib in Patients with Relapsed or Refractory CLL and MCL. Globenewswire.com 2017
Clinical trial number NCT02793583 for "Study to Assess the Efficacy and Safety of Ublituximab + TGR-1202 With or Without Bendamustine and TGR-1202 Alone in Patients With Previously Treated Non-Hodgkin's Lymphoma (UNITY-NHL)" at ClinicalTrials.gov
FDA Grants Umbralisib Breakthrough Designation for Marginal Zone Lymphoma'. Onclive.com. January 2019