umbralisib
Trade name: Ukoniq
Small moleculeapprovedOrphan Drug FDABreakthrough Therapy FDA
Approved
Feb 5, 2021
Umbralisib, sold under the brand name Ukoniq, is an anti-cancer medication for the treatment of marginal zone lymphoma (MZL) and follicular lymphoma (FL). It is taken by mouth. — Wikipedia
Clinical trial activity
35 trials · 26 clinical orgs · 1 marketing orgs
Phase 1
16
Phase 2
23
Phase 3
2
Phase 4
0
Earliest trial started Jan 1, 2013 (NCT01767766)
Timeline
2010s
- Jan 1, 2013
TG Therapeutics, Inc. — Earliest Phase 1 Sponsor(trial)
- Jan 1, 2016
TG Therapeutics, Inc. — Earliest Phase 2 Sponsor(trial)
- Jan 1, 2016
TG Therapeutics, Inc. — Earliest Phase 3 Sponsor(trial)
- Apr 11, 2019
Orphan Drug Designation
2020s
- Feb 5, 2021
TG Therapeutics, Inc. — Earliest FDA Approval
- Feb 5, 2021
TG Therapeutics, Inc. — Marketing Organization
- Feb 5, 2021
TG Therapeutics, Inc. — NDA Secondary Org
- Feb 5, 2021
TG Therapeutics, Inc. — NDA Organization
Indications
Studied for
- Colorectal Neoplasms · Phase 1
- Esophageal Neoplasms · Phase 1
- Hodgkin Disease · Phase 2
- Intestinal Neoplasms · Phase 1
- Leukemia, Lymphocytic, Chronic, B-Cell · Phase 3
- Lymphoma · Phase 2
- Lymphoma, B-Cell, Marginal Zone · Phase 2/Phase 3
- Lymphoma, Follicular · Phase 2/Phase 3
- Lymphoma, Large B-Cell, Diffuse · Phase 2/Phase 3
- Lymphoma, Mantle-Cell · Phase 2/Phase 3
- Lymphoma, Non-Hodgkin · Phase 2
- Lymphoma, T-Cell, Peripheral · Phase 1
- Pancreatic Neoplasms · Phase 1
- Polycythemia Vera · Phase 1
- Primary Myelofibrosis · Phase 1
- Rectal Neoplasms · Phase 1
- Stomach Neoplasms · Phase 1
- Waldenstrom Macroglobulinemia · Phase 2
Mechanism of action
- PI3-kinase p110-delta subunitINHIBITOR
PIK3CD inhibitor
- Casein kinase I epsilonINHIBITOR
Casein kinase I epsilon inhibitor
- Tyrosine-protein kinase ABLINHIBITOR
Tyrosine-protein kinase ABL inhibitor
Approval history
- approvedPriority reviewAcceleratedBreakthroughFeb 5, 2021
Chemistry & pharmacology
Loading structure…
SMILES
CC(C)Oc1ccc(-c2nn([C@@H](C)c3oc4ccc(F)cc4c(=O)c3-c3cccc(F)c3)c3ncnc(N)c23)cc1F- Mol. weight
- 571.56 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Discontinued
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL3948730 ↗
- WikipediaUmbralisib ↗
- ChEMBLCHEMBL3989869 ↗
- ChEMBLCHEMBL3545267 ↗
Also known as
- tgr-1202
- tgr-1202
- tgr-1202
- umbralisib
- umbralisib
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05152459 | Phase 1/Phase 2 (Phase 2) | Dec 30, 2021 | City of Hope National Medical Center, National Cancer Institute (NCI) |
| NCT04970901 | Phase 1 | Dec 30, 2021 | ADC Therapeutics SARL |
| NCT04692155 | Phase 1/Phase 2 (Phase 2) | Jun 30, 2021 | University of Alabama, Birmingham |
| NCT04624633 | Phase 2 | Apr 30, 2021 | AstraZeneca, Harvard University, TG Therapeutics, Inc. |
| NCT04783415 | Phase 2 | Mar 26, 2021 | City of Hope National Medical Center, National Cancer Institute (NCI) |
| NCT04635683 | Phase 1 | Jan 1, 2021 | Ohio State University |
| NCT04508647 | Phase 2 | Dec 31, 2020 | University of Colorado, Denver |
| NCT04149821 | Phase 2 | Nov 30, 2019 | Cornell University, TG Therapeutics, Inc. |
| NCT04163718 | Phase 2 | Nov 12, 2019 | TG Therapeutics, Inc., University of South Florida |
| NCT04016805 | Phase 2 | Jul 31, 2019 | TG Therapeutics, Inc. |
| NCT03776864 | Phase 2 | Jul 15, 2019 | TG Therapeutics, Inc., University of Washington |
| NCT03828448 | Phase 2 | Jun 30, 2019 | TG Therapeutics, Inc. |
| NCT03801525 | Phase 2 | May 31, 2019 | TG Therapeutics, Inc. |
| NCT03919175 | Phase 2 | May 1, 2019 | Harvard University, TG Therapeutics, Inc. |
| NCT03671590 | Phase 1 | Sep 10, 2018 | St. Vincents Hospital, TG Therapeutics, Inc. |
| NCT03379051 | Phase 1/Phase 2 (Phase 2) | Apr 9, 2018 | New York University, TG Therapeutics, Inc., University of Rochester |
| NCT03283137 | Phase 1 | Jan 23, 2018 | University of Chicago |
| NCT03364231 | Phase 2 | Nov 30, 2017 | Georgetown University, TG Therapeutics, Inc. |
| NCT03269669 | Phase 2 | Aug 10, 2017 | National Cancer Institute (NCI), Southwest Oncology Group |
| NCT03178201 | Phase 2 | Jul 5, 2017 | Columbia University, TG Therapeutics, Inc. |
Showing 20 of 35 trials
Page 1 / 2
Organizations
Research & Development (26)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| TG Therapeutics, Inc. | For profit | 24 | 17 | 3 | 2013 |
| National Cancer Institute (NCI) | Government | 4 | 1 | 1 | 2016 |
| Columbia University | Academic/Hospital | 3 | 2 | 2 | 2016 |
| Harvard University | Academic/Hospital | 3 | 3 | 2 | 2014 |
| City of Hope National Medical Center | Academic/Hospital | 2 | 2 | 1 | 2021 |
| SCRI Development Innovations | For profit | 2 | 0 | 1 | 2013 |
| University of Pennsylvania | Academic/Hospital | 2 | 0 | 1 | 2015 |
| ADC Therapeutics SARL | For profit | 1 | 1 | 1 | 2021 |
| AstraZeneca | For profit | 1 | 0 | 1 | 2021 |
| Cornell University | Academic/Hospital | 1 | 1 | 1 | 2019 |
| Georgetown University | Academic/Hospital | 1 | 0 | 1 | 2017 |
| New York University | Academic/Hospital | 1 | 0 | 1 | 2018 |
| Ohio State University | Academic/Hospital | 1 | 1 | 1 | 2021 |
| Southwest Oncology Group | Academic/Hospital | 1 | 0 | 1 | 2017 |
| St. Vincents Hospital | Academic/Hospital | 1 | 0 | 1 | 2018 |
| The Leukemia and Lymphoma Society | Academic/Hospital | 1 | 0 | 1 | 2014 |
| University of Alabama, Birmingham | Academic/Hospital | 1 | 1 | 1 | 2021 |
| University of California, Irvine | Academic/Hospital | 1 | 0 | 1 | 2013 |
| University of Chicago | Academic/Hospital | 1 | 1 | 1 | 2018 |
| University of Colorado, Denver | Academic/Hospital | 1 | 1 | 1 | 2020 |
26 organizations
Page 1 / 2
Marketing (3)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| TG Therapeutics, Inc. | For profit | MKTG | Feb 5, 2021 |
| TG Therapeutics, Inc. | For profit | NDA2 | Feb 5, 2021 |
| TG Therapeutics, Inc. | For profit | NDA | Feb 5, 2021 |