pemigatinib
Trade name: Pemazyre
Approved
Apr 17, 2020
Pemigatinib, sold under the brand name Pemazyre, is an anti-cancer medication used for the treatment of bile duct cancer (cholangiocarcinoma). Pemigatinib works by blocking FGFR2 in tumor cells to prevent them from growing and spreading. — Wikipedia
Clinical trial activity
45 trials · 42 clinical orgs · 2 marketing orgs
Earliest trial started Jan 1, 2015 (NCT02393248)
Timeline
2010s
Indications
Approved for
Studied for
- Biliary Tract Neoplasms · Phase 2
- Breast Neoplasms · Phase 2
- Carcinoma · Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 2
- Carcinoma, Transitional Cell · Phase 2
- Cholangiocarcinoma · Phase 3
- Colitis, Ulcerative · Phase 1/Phase 2
- Colorectal Neoplasms · Phase 2
- Digestive System Neoplasms · Phase 2
- Drug Therapy · Phase 1/Phase 2
- Endometrial Neoplasms · Phase 2
- Fibroblast Growth Factor 1 · Phase 2
- Gastrointestinal Neoplasms · Phase 2
- Glioblastoma · Phase 2
- Glioma · Phase 2
- Immune Checkpoint Inhibitors · Phase 2
- Leukemia, Myeloid, Acute · Phase 1
- Liposarcoma · Phase 2
- Lung Neoplasms · Phase 2
- Lymphoma · Phase 2
- Lymphoma, Non-Hodgkin · Phase 2
- Multiple Myeloma · Phase 1/Phase 2
- Mutation · Phase 2
- Myeloproliferative Disorders · Phase 2
- Neoplasm Metastasis · Phase 3
- Neoplasms · Phase 2
- Pancreatic Neoplasms · Phase 2
- Receptors, Fibroblast Growth Factor · Phase 2
- Sarcoma · Phase 2
- Stomach Neoplasms · Phase 2
- Urinary Bladder Neoplasms · Phase 2
Mechanism of action
- Fibroblast growth factor receptor 2ANTAGONIST
FGFR2 antagonist
- Fibroblast growth factor receptor 1INHIBITOR
Fibroblast growth factor receptor 1 inhibitor
Inhibits FGFR1/2/3-dependent phosphorylation and signaling in cells that have activating FGFR amplifications/fusions and decreases cancer cell viability.
IC50s for FGFR1/2/3 < 2 nM. The IC50 for FGFR4 is 100x higher in vitro. Indicated for cancers with FGFR2 fusions or other rearrangements as detected by an FDA-approved test.
- Fibroblast growth factor receptor 2INHIBITOR
Fibroblast growth factor receptor 2 inhibitor
Inhibits FGFR1/2/3-dependent phosphorylation and signaling in cells that have activating FGFR amplifications/fusions and decreases cancer cell viability.
IC50s for FGFR1/2/3 < 2 nM. The IC50 for FGFR4 is 100x higher in vitro. Indicated for cancers with FGFR2 fusions or other rearrangements as detected by an FDA-approved test.
- Fibroblast growth factor receptor 3INHIBITOR
Fibroblast growth factor receptor 3 inhibitor
Inhibits FGFR1/2/3-dependent phosphorylation and signaling in cells that have activating FGFR amplifications/fusions and decreases cancer cell viability.
IC50s for FGFR1/2/3 < 2 nM. The IC50 for FGFR4 is 100x higher in vitro. Indicated for cancers with FGFR2 fusions or other rearrangements as detected by an FDA-approved test.
Approval history
- approvedPriority reviewAcceleratedBreakthroughApr 17, 2020
Chemistry & pharmacology
SMILES
CCN1C(=O)N(c2c(F)c(OC)cc(OC)c2F)Cc2cnc3[nH]c(CN4CCOCC4)cc3c21- Mol. weight
- 487.51 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaPemigatinib ↗
- ChEMBLCHEMBL4297522 ↗
Also known as
- incb054828
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06906562 | Phase 2 | Aug 26, 2025 | Incyte, Ohio State University |
| NCT06728410 | Phase 2 | Jan 31, 2025 | AstraZeneca, Hoosier Cancer Research Network, Incyte, University of Alabama, Birmingham |
| NCT06653777 | Phase 2 | Dec 15, 2024 | Curie Institute, National Cancer Institute, France, UNICANCER |
| NCT06300528 | Phase 2 | Nov 30, 2024 | Incyte, University of Utah |
| NCT06439485 | Phase 2 | Nov 29, 2024 | Genentech, Incyte, University of Texas at Houston |
| NCT06551896 | Phase 2 | Aug 15, 2024 | Sun Yat-Sen University |
| NCT06530823 | Phase 2 | Aug 1, 2024 | Eastern Hepatobiliary Surgery Hospital |
| NCT06302621 | Phase 1 | Jul 1, 2024 | Boehringer Ingelheim, Harvard University, Incyte |
| NCT06389799 | Phase 2 | Jun 20, 2024 | Lund University |
| NCT05997459 | Phase 2 | Aug 25, 2023 | Sun Yat-Sen University |
| NCT05913661 | Phase 2 | Jul 31, 2023 | Jinan University, Shenzhen University, Sun Yat-Sen University |
| NCT06022289 | Phase 2 | May 1, 2023 | Tianjin Medical University |
| NCT05651672 | Phase 2 | Dec 2, 2022 | Tianjin Medical University |
| NCT05565794 | Phase 2 | Nov 30, 2022 | IKF Klinische Krebsforschung GmbH am Krankenhaus Nordwest, Incyte |
| NCT05560334 | Phase 2 | Sep 8, 2022 | Tianjin Medical University |
| NCT05559775 | Phase 2 | Aug 10, 2022 | Chinese Academy of Medical Sciences |
| NCT05216120 | Phase 2 | Jun 14, 2022 | HonorHealth Research Institute, Incyte |
| NCT05267106 | Phase 2 | May 20, 2022 | Incyte |
| NCT05253807 | Phase 2 | Apr 29, 2022 | Incyte |
| NCT05287386 | Phase 2 | Jan 21, 2022 | Xiamen University |