Drugs / Umbralisib
Umbralisib
also known as
TGR-1202 · RP-5264 · RP-5307 · TGR-1202 (4-METHYLBENZENESULFONATE) · TGR-1202 base · TGR-1202 FREE BASE · Ukoniq · UMBRALISIB TOSYLATE
Small molecule targets ABL1, CSNK1E, PIK3CD via inhibition
Regulatory milestones approvals, filings & regulatory actions · 1 recorded
| Milestone | Jurisdiction | Brand | Indication | Date | Sentence it was read from |
|---|---|---|---|---|---|
| Approved | US (FDA) | UKONIQ | — | 2021-02-05 | fda.gov ↗ |
Trials 32
News releases announcing trial results or a regulatory action · 2
| Date | Issuer | Release |
|---|---|---|
| 2021-02-08 | Alembic Pharmaceuticals Ltd. | Regulatory Press Release - Rhizen - Umbralisib-UNKONIQ Approval alembicpharmaceuticals.com ↗
Accelerated approval was granted for these indications , under a priority review (MZL), based on the results of the Phase 2 UNITY-NHL Trial (NCT02793583) ; in MZL, an ORR of 49% with 16% complete responses and in FL an ORR of 43% with 3% complete responses were achieved, respectively. |
| 2015-04-20 | Ligand Pharmaceuticals | Results Ligand Partner TG Therapeutics Presents Positive Pre-clinical Data on IRAK4 Compounds at the American Association for Cancer Research (AACR) Annual Meeting ligand.com ↗
Compounds demonstrated marked synergy when combined with the novel targeted kinase inhibitors TGR-1202, TG Therapeutics’ proprietary PI3K delta inhibitor, and the BTK inhibitor, ibrutinib. |
All press releases naming this drug 2 releases
| Date | Issuer | Release |
|---|---|---|
| 2021-02-08 | Alembic Pharmaceuticals Ltd. | Press Release - Rhizen - Umbralisib-UNKONIQ Approval alembicpharmaceuticals.com ↗ |
| 2015-04-20 | Ligand Pharmaceuticals | Ligand Partner TG Therapeutics Presents Positive Pre-clinical Data on IRAK4 Compounds at the American Association for Cancer Research (AACR) Annual Meeting ligand.com ↗ |
Evidence & citations 15 cited values
Every value below carries the sentence it was read from. 34 sources stand behind the page.
| Field | Value | Cited text |
|---|---|---|
| Known as | Umbralisib | “Umbralisib (TGR-1202) is a novel next-generation inhibitor of phosphatidylinositol 3-kinase (PI3K) isoform p110δ (PI3Kδ), which is structurally distinct from other PI3Kδ...” PMID 29475723 ↗ Feb 2018 |
| Known as | RP-5264 | ChEMBL registry synonym — accepted as the source's own label CHEMBL3948730 ↗ |
| Known as | RP-5307 | ChEMBL registry synonym — accepted as the source's own label CHEMBL3948730 ↗ |
| Known as | TGR-1202 | “This research study will evaluate the safety and efficacy of a study drug called Umbralisib (also known as TGR-1202) alone as a possible treatment for Waldenstrom's...” NCT03364231 ↗14“Umbralisib (TGR-1202) is a novel next-generation inhibitor of phosphatidylinositol 3-kinase (PI3K) isoform p110δ (PI3Kδ), which is structurally distinct from other PI3Kδ...” PMID 29475723 ↗ Feb 2018 “A Phase I Study Evaluating the Safety and Efficacy of TGR 1202 Alone and in Combination With Either Nab-paclitaxel + Gemcitabine or With FOLFOX in Patients With Select Relapsed...” NCT02574663 ↗ “receive ublituximab (TG-1101) treatment in combination with umbralisib (TGR-1202)” NCT02656303 ↗ |
| Known as | TGR-1202 (4-METHYLBENZENESULFONATE) | ChEMBL registry synonym — accepted as the source's own label CHEMBL3948730 ↗ |
| Known as | TGR-1202 base | ChEMBL registry synonym — accepted as the source's own label CHEMBL3948730 ↗ |
| Known as | TGR-1202 FREE BASE | ChEMBL registry synonym — accepted as the source's own label CHEMBL3948730 ↗ |
| Known as | Ukoniq | ChEMBL registry synonym — accepted as the source's own label CHEMBL3948730 ↗ |
| Known as | UMBRALISIB TOSYLATE | ChEMBL registry synonym — accepted as the source's own label CHEMBL3948730 ↗ |
| Action | Inhibit | “Umbralisib also uniquely inhibits casein kinase-1ε, a major regulator of protein translation.” PMID 29475723 ↗ Feb 20183“PI3-kinase p110-delta subunit inhibitor” CHEMBL3948730 ↗ “Tyrosine-protein kinase ABL inhibitor” CHEMBL3948730 ↗ “Casein kinase I epsilon inhibitor” CHEMBL3948730 ↗ |
| Modality | Small molecule | “Umbralisib is a highly-specific and orally available dual inhibitor of phosphoinositide-3-kinase (PI3K) delta (δ) and casein kinase 1 epsilon (CK1ε)” NCT04692155 ↗ |
| Route | Oral | “Patients self-administered an umbralisib oral tablet once per day in 28-day cycles” PMID 29475723 ↗ Feb 2018 |
| Target | ABL1 | “Tyrosine-protein kinase ABL inhibitor” CHEMBL3948730 ↗ |
| Target | CSNK1E | “Casein kinase I epsilon inhibitor” CHEMBL3948730 ↗ |
| Target | PIK3CD | “PI3-kinase p110-delta subunit inhibitor” CHEMBL3948730 ↗ |