Belzutifan
Trade name: Welireg
Small moleculeapprovedOrphan Drug FDA
Approved
Aug 13, 2021
Clinical trial activity
31 trials · 11 clinical orgs · 1 marketing orgs
Phase 1
15
Phase 2
20
Phase 3
6
Phase 4
0
Earliest trial started Dec 1, 2016 (NCT02974738)
Timeline
2010s
Indications
Studied for
- Adenocarcinoma · Phase 1
- Biliary Tract Neoplasms · Phase 2
- Breast Neoplasms · Phase 2
- Carcinoma, Hepatocellular · Phase 2
- Carcinoma, Renal Cell · Phase 3
- Colorectal Neoplasms · Phase 2
- Endometrial Neoplasms · Phase 2
- Esophageal Neoplasms · Phase 2
- Genital Neoplasms, Female · Phase 2
- Glioblastoma · Phase 1
- Glioma · Phase 2
- Healthy Volunteers · Phase 1
- Intestinal Neoplasms · Phase 2
- Kidney · Phase 2
- Kidney Failure, Chronic · Phase 1
- Kidney Neoplasms · Phase 2
- Liver Diseases · Phase 1
- Mutation · Phase 2
- Neoplasms · Phase 2
- Neuroectodermal Tumors, Primitive · Phase 2
- Ovarian Neoplasms · Phase 2
- Pancreatic Neoplasms · Phase 2
- Retinal Diseases · Phase 2
- Uterine Cervical Neoplasms · Phase 2
- Uterine Neoplasms · Phase 2
- Vaginal Neoplasms · Phase 2
- von Hippel-Lindau Disease · Phase 2
- Vulvar Neoplasms · Phase 2
- Watchful Waiting · Phase 2
Mechanism of action
Hypoxia inducible factors; HIF-1-alpha, HIF-2-alpha antagonist
Endothelial PAS domain-containing protein 1 inhibitor
Approval history
- approvedPriority reviewAug 13, 2021
Chemistry & pharmacology
Loading structure…
SMILES
CS(=O)(=O)c1ccc(Oc2cc(F)cc(C#N)c2)c2c1[C@H](O)[C@H](F)[C@@H]2F- Mol. weight
- 383.35 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Black box warningFirst in class
Sources
- ChEMBLCHEMBL4585668 ↗
Also known as
- pt2977
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07187778 | Phase 2 | Feb 28, 2026 | Merck, University of Texas at Houston |
| NCT07227402 | Phase 3 | Dec 29, 2025 | Exelixis, Merck |
| NCT07023432 | Phase 2 | Dec 3, 2025 | University of Texas at Houston |
| NCT07179770 | Phase 1 | Sep 15, 2025 | National Cancer Institute (NCI), New York University |
| NCT07121959 | Phase 1 | Aug 18, 2025 | Merck |
| NCT07049926 | Phase 1/Phase 2 (Phase 2) | Jul 20, 2025 | Exelixis, Merck |
| NCT06903715 | Phase 1 | Mar 28, 2025 | Merck |
| NCT06677190 | Phase 2 | Jan 1, 2025 | Harvard University, Merck |
| NCT06428396 | Phase 2 | Oct 30, 2024 | Merck |
| NCT06234605 | Phase 1 | Apr 29, 2024 | HiberCell, Inc., Merck |
| NCT07167329 | Phase 2 | Jan 1, 2024 | Hospital A.C. Camargo |
| NCT05468697 | Phase 1/Phase 2 (Phase 2) | Aug 10, 2022 | Merck |
| NCT05899049 | Phase 3 | Jul 27, 2022 | Eisai, Merck |
| NCT05239728 | Phase 3 | Mar 15, 2022 | Merck |
| NCT04995484 | Phase 1 | Dec 10, 2021 | Merck |
| NCT04994522 | Phase 1 | Dec 10, 2021 | Merck |
| NCT05030506 | Phase 1 | Oct 13, 2021 | Merck |
| NCT04976634 | Phase 2 | Aug 18, 2021 | Merck |
| NCT04924075 | Phase 2 | Aug 12, 2021 | Merck |
| NCT04846920 | Phase 1 | Jun 14, 2021 | Merck |
Showing 20 of 31 trials
Page 1 / 2
Organizations
Research & Development (11)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Merck | For profit | 23 | 20 | 3 | 2019 |
| Peloton Therapeutics, Inc. | For profit | 4 | 4 | 2 | 2016 |
| Eisai | For profit | 3 | 0 | 1 | 2020 |
| Exelixis | For profit | 2 | 0 | 2 | 2025 |
| Harvard University | Academic/Hospital | 2 | 2 | 2 | 2021 |
| University of Texas at Houston | Academic/Hospital | 2 | 2 | 1 | 2025 |
| Eli Lilly | For profit | 1 | 0 | 1 | 2021 |
| HiberCell, Inc. | For profit | 1 | 1 | 1 | 2024 |
| Hospital A.C. Camargo | Academic/Hospital | 1 | 1 | 1 | 2024 |
| National Cancer Institute (NCI) | Government | 1 | 0 | 1 | 2025 |
| New York University | Academic/Hospital | 1 | 1 | 1 | 2025 |
11 organizations
Page 1 / 1