fedratinib
Trade name: Inrebic
Approved
Aug 16, 2019
Fedratinib (SAR-302503, TG-101348) is a selective small-molecule inhibitor of Janus kinase-2. Fedratinib demonstrated therapeutic efficacy in a murine model of myeloproliferative disease. Sanofi was developing Fedratinib for the treatment of myeloproliferative diseases and solid tumors. The clinical development of fedratinib was terminated after reports of Wernicke's encephalopathy in myelofibrosis patients. — NCATS
Clinical trial activity
33 trials · 17 clinical orgs · 3 marketing orgs
Earliest trial started Jan 1, 2008 (NCT00631462)
Timeline
2000s
- Jan 1, 2008
Earliest Phase 1 Sponsor(trial)
- May 18, 2009
Orphan Drug Designation
2010s
- Jan 1, 2011
Earliest Phase 2 Sponsor(trial)
- Jan 1, 2011
Earliest Phase 3 Sponsor(trial)
- Aug 16, 2019
Celgene — Earliest FDA Approval
- Aug 16, 2019
Impact Therapeutics, Inc. — Marketing Organization
- Aug 16, 2019
Celgene — NDA Organization
- Aug 16, 2019
Impact Therapeutics, Inc. — NDA Secondary Org
- Aug 16, 2019
Bristol-Myers — Marketing Organization
Indications
Approved for
Studied for
- Arthritis, Rheumatoid · Phase 3
- Dermatitis · Phase 2
- Dermatomyositis · Phase 4
- Healthy Volunteers · Phase 1
- Hematologic Neoplasms · Phase 3
- Kidney Failure, Chronic · Phase 1
- Leukemia, Myeloid, Acute · Phase 2
- Leukemia, Neutrophilic, Chronic · Phase 2
- Liver Diseases · Phase 1
- Mutation · Phase 1
- Myelodysplastic Syndromes · Phase 2
- Myeloproliferative Disorders · Phase 2
- Neoplasms · Phase 1
- Polycythemia Vera · Phase 3
- Primary Myelofibrosis · Phase 3
- Thrombocythemia, Essential · Phase 2
Mechanism of action
- Tyrosine-protein kinase JAK2INHIBITOR
JAK2 inhibitor
Potent inhibitor of BRD4 (PMID: 24584101).
FLT3 inhibitor
Potent inhibitor of BRD4 (PMID: 24584101).
Approval history
- approvedPriority reviewAug 16, 2019
Chemistry & pharmacology
SMILES
CC1=CN=C(NC2=CC=C(OCCN3CCCC3)C=C2)N=C1NC4=CC=CC(=C4)S(=O)(=O)NC(C)(C)C- Mol. weight
- 524.678 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaFedratinib ↗
- NCATS6L1XP550I6 ↗
- ChEMBLCHEMBL4297216 ↗
- ChEMBLCHEMBL1287853 ↗
Also known as
- fedratinib
- fedratinib
- fedratinib
- fedratinib
- n-tert-butyl-3-(5-methyl-2-(4-(2-(pyrrolidin-1-yl)ethoxy)phenylamino) pyrimidin-4-ylamino)benzenesulfonamide
- sar302503
- sar302503
- sar302503
- sar-302503
- sar-302503
- tg101348
- tg101348
- tg101348
- tg101348
- tg-101348
- tg-101348
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07228624 | Phase 2 | May 1, 2026 | Incyte, University of Washington |
| NCT06715982 | Phase 2 | Dec 31, 2024 | Chinese Academy of Medical Sciences |
| NCT06301373 | N/A | Apr 1, 2024 | Sun Yat-Sen University |
| NCT05524857 | Phase 1 | Sep 30, 2022 | Bristol-Myers Squibb, Columbia University |
| NCT05379322 | Phase 3 | Jul 31, 2022 | Abu Dhabi Stem Cells Center |
| NCT05393674 | Phase 2 | Jun 14, 2022 | Celgene, IKF Klinische Krebsforschung GmbH am Krankenhaus Nordwest, Institut für Klinische Krebsforschung IKF GmbH, University of Greifswald |
| NCT05177211 | Phase 2 | Mar 1, 2022 | Bristol-Myers Squibb, University of South Florida |
| NCT05127174 | Phase 1/Phase 2 (Phase 2) | Nov 9, 2021 | Bristol-Myers Squibb, University of South Florida |
| NCT04955938 | Phase 1 | Oct 29, 2021 | University of Chicago |
| NCT05051553 | Phase 1 | Sep 21, 2021 | Bristol-Myers Squibb |
| NCT04817007 | Phase 1 | Mar 23, 2021 | Bristol-Myers Squibb |
| NCT04702464 | Phase 1 | Jan 12, 2021 | Bristol-Myers Squibb, Celgene |
| NCT04446650 | Phase 1/Phase 2 (Phase 2) | Jun 30, 2020 | Celgene |
| NCT04370301 | Phase 2 | Jun 1, 2020 | University of Washington |
| NCT04966884 | Phase 4 | Apr 2, 2020 | Jiao Tong University |
| NCT04282187 | Phase 2 | Mar 19, 2020 | University of Washington |
| NCT04231435 | Phase 1 | Dec 18, 2019 | Celgene |
| NCT03983239 | Phase 1 | Dec 15, 2019 | Celgene |
| NCT03983161 | Phase 1 | Dec 15, 2019 | Celgene |
| NCT03952039 | Phase 3 | Aug 23, 2019 | Celgene |
Organizations
Research & Development (17)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Sanofi | For profit | 10 | 10 | 3 | 2008 |
| Celgene | For profit | 9 | 8 | 4 | 2019 |
| Bristol-Myers Squibb | For profit | 6 | 2 | 2 | 2021 |
| University of Washington | Academic/Hospital | 3 | 3 | 1 | 2020 |
| Mayo Clinic | Academic/Hospital | 2 | 0 | 2 | 2008 |
| University of South Florida | Academic/Hospital | 2 | 2 | 1 | 2021 |
| Abu Dhabi Stem Cells Center | Academic/Hospital | 1 | 1 | 1 | 2022 |
| Chinese Academy of Medical Sciences | Academic/Hospital | 1 | 1 | 1 | 2024 |
| Columbia University | Academic/Hospital | 1 | 1 | 1 | 2022 |
| IKF Klinische Krebsforschung GmbH am Krankenhaus Nordwest | Academic/Hospital | 1 | 1 | 1 | 2022 |
| Incyte | For profit | 1 | 0 | 1 | 2026 |
| Institut für Klinische Krebsforschung IKF GmbH | Academic/Hospital | 1 | 0 | 1 | 2022 |
| Jiao Tong University | Academic/Hospital | 1 | 1 | 1 | 2020 |
| Sun Yat-Sen University | Academic/Hospital | 1 | 1 | 1 | 2024 |
| TargeGen | For profit | 1 | 1 | 1 | 2008 |
| University of Chicago | Academic/Hospital | 1 | 1 | 1 | 2021 |
| University of Greifswald | Academic/Hospital | 1 | 0 | 1 | 2022 |
Marketing (4)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Bristol-Myers | For profit | MKTG | Aug 16, 2019 |
| Celgene | For profit | NDA | Aug 16, 2019 |
| Impact Therapeutics, Inc. | For profit | MKTG | Aug 16, 2019 |
| Impact Therapeutics, Inc. | For profit | NDA2 | Aug 16, 2019 |