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belzutifan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 5469 | 1672668-24-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Belzutifan is an inhibitor of hypoxia-inducible factor 2 alpha (HIF-2alpha), with potential antineoplastic activity. HIF-2alpha is a transcription factor that plays a role in oxygen sensing by regulating genes that promote adaptation to hypoxia. Under normal oxygen levels, HIF-2alpha is targeted for ubiquitin-proteasomal degradation by VHL protein. Lack of functional VHL protein results in stabilization and accumulation of HIF-2alpha. Upon stabilization, HIF-2alpha translocates into the nucleus and interacts with hypoxia-inducible factor 1 beta (HIF-1beta) to form a transcriptional complex that induces expression of downstream genes, including genes associated with cellular proliferation, angiogenesis, and tumor growth. Belzutifan binds to HIF-2alpha, and in conditions of hypoxia or impairment of VHL protein function, belzutifan blocks the HIF-2alpha-HIF-1beta interaction, leading to reduced transcription and expression of HIF-2alpha target genes. In vivo, belzutifan demonstrated anti-tumor activity in mouse xenograft models of renal cell carcinoma.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,EIF2AK3,GRK2,PDK1,PDK2,PDK4,PIK3CG,PRKDC | 8 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 13, 2021 | FDA | MERCK SHARP DOHME |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Anaemia | 220.81 | 43.06 | 79 | 427 | 352723 | 90275218 |
| Hypoxia | 136.49 | 43.06 | 38 | 468 | 72361 | 90555580 |
| Malignant neoplasm progression | 62.09 | 43.06 | 23 | 483 | 106847 | 90521094 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Malignant neoplasm progression | 240.36 | 43.26 | 88 | 805 | 108312 | 42512130 |
| Hypoxia | 204.97 | 43.26 | 70 | 823 | 69716 | 42550726 |
| Anaemia | 171.34 | 43.26 | 92 | 801 | 280186 | 42340256 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Anaemia | 360.45 | 44.67 | 159 | 1193 | 546927 | 110041020 |
| Malignant neoplasm progression | 282.66 | 44.67 | 98 | 1254 | 174469 | 110413478 |
| Hypoxia | 278.17 | 44.67 | 90 | 1262 | 129425 | 110458522 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01XX74 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents |
| MeSH PA | D000970 | Antineoplastic Agents |
| FDA MoA | N0000185506 | Cytochrome P450 3A4 Inducers |
| FDA MoA | N0000193998 | Hypoxia-inducible Factor 2 alpha Inhibitors |
| FDA EPC | N0000193999 | Hypoxia-inducible Factor Inhibitor |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Related Drugs by ATC class:
L01XX Other antineoplastic agents 33 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Von Hippel-Lindau (VHL) disease | indication | 46659004 | DOID:14175 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 40MG | WELIREG | MERCK SHARP DOHME | N215383 | Aug. 13, 2021 | RX | TABLET | ORAL | 9908845 | Sept. 5, 2034 | TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER WITH LOCALLY ADVANCED, UNRESECTABLE, OR METASTATIC PHEOCHROMOCYTOMA OR PARAGANGLIOMA (PPGL) |
| 40MG | WELIREG | MERCK SHARP DOHME | N215383 | Aug. 13, 2021 | RX | TABLET | ORAL | 9908845 | Sept. 5, 2034 | TREATMENT OF ADULT PATIENTS WITH ADVANCED RENAL CELL CARCINOMA WITH A CLEAR CELL COMPONENT FOLLOWING A PROGRAMMED DEATH RECEPTOR-I OR PROGRAMMED DEATH-LIGAND 1 INHIBITOR AND A VASCULAR ENDOTHELIAL GROWTH FACTOR TYROSINE KINASE INHIBITOR |
| 40MG | WELIREG | MERCK SHARP DOHME | N215383 | Aug. 13, 2021 | RX | TABLET | ORAL | 9908845 | Sept. 5, 2034 | TREATMENT OF ADULT PATIENTS WITH VON HIPPEL-LINDAU DISEASE WHO REQUIRE THERAPY FOR ASSOCIATED RENAL CELL CARCINOMA, CENTRAL NERVOUS SYSTEM HEMANGIOBLASTOMAS, OR PANCREATIC NEUROENDOCRINE TUMORS, NOT REQUIRING IMMEDIATE SURGERY |
| 40MG | WELIREG | MERCK SHARP DOHME | N215383 | Aug. 13, 2021 | RX | TABLET | ORAL | RE49948 | Sept. 5, 2034 | TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER WITH LOCALLY ADVANCED, UNRESECTABLE, OR METASTATIC PHEOCHROMOCYTOMA OR PARAGANGLIOMA (PPGL) |
| 40MG | WELIREG | MERCK SHARP DOHME | N215383 | Aug. 13, 2021 | RX | TABLET | ORAL | RE49948 | Sept. 5, 2034 | TREATMENT OF ADULT PATIENTS WITH ADVANCED RENAL CELL CARCINOMA WITH A CLEAR CELL COMPONENT FOLLOWING A PROGRAMMED DEATH RECEPTOR-I OR PROGRAMMED DEATH-LIGAND 1 INHIBITOR AND A VASCULAR ENDOTHELIAL GROWTH FACTOR TYROSINE KINASE INHIBITOR |
| 40MG | WELIREG | MERCK SHARP DOHME | N215383 | Aug. 13, 2021 | RX | TABLET | ORAL | RE49948 | Sept. 5, 2034 | TREATMENT OF ADULT PATIENTS WITH VON HIPPEL-LINDAU DISEASE WHO REQUIRE THERAPY FOR ASSOCIATED RENAL CELL CARCINOMA, CENTRAL NERVOUS SYSTEM HEMANGIOBLASTOMAS, OR PANCREATIC NEUROENDOCRINE TUMORS, NOT REQUIRING IMMEDIATE SURGERY |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 40MG | WELIREG | MERCK SHARP DOHME | N215383 | Aug. 13, 2021 | RX | TABLET | ORAL | Aug. 13, 2026 | NEW CHEMICAL ENTITY |
| 40MG | WELIREG | MERCK SHARP DOHME | N215383 | Aug. 13, 2021 | RX | TABLET | ORAL | Dec. 14, 2026 | TREATMENT OF ADULT PATIENTS WITH ADVANCED RENAL CELL CARCINOMA FOLLOWING A PROGRAMMED DEATH RECEPTOR-1 OR PROGRAMMED DEATH-LIGAND 1 INHIBITOR AND A VASCULAR ENDOTHELIAL GROWTH FACTOR TYROSINE KINASE INHIBITOR |
| 40MG | WELIREG | MERCK SHARP DOHME | N215383 | Aug. 13, 2021 | RX | TABLET | ORAL | May 14, 2028 | TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER WITH LOCALLY ADVANCED, UNRESECTABLE, OR METASTATIC PHEOCHROMOCYTOMA OR PARAGANGLIOMA (PPGL) |
| 40MG | WELIREG | MERCK SHARP DOHME | N215383 | Aug. 13, 2021 | RX | TABLET | ORAL | Aug. 13, 2028 | TREATMENT OF ADULT PATIENTS WITH VON HIPPEL-LINDAU (VHL) DISEASE WHO REQUIRE THERAPY FOR ASSOCIATED RENAL CELL CARCINOMA (RCC), CENTRAL NERVOUS SYSTEM (CNS) HEMANGIOBLASTOMAS, OR PANCREATIC NEUROENDOCRINE TUMORS (PNET), NOT REQUIRING IMMEDIATE SURGERY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Endothelial PAS domain-containing protein 1 | Transcription factor | INHIBITOR | IC50 | 8 | DRUG LABEL | DRUG LABEL | |||
| Vascular endothelial growth factor A | Secreted | EC50 | 7.75 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 7K28NB895L | UNII |
| C5418188 | UMLSCUI |
| CHEBI:757730 | CHEBI |
| 72Q | PDB_CHEM_ID |
| CHEMBL4585668 | ChEMBL_ID |
| D11954 | KEGG_DRUG |
| 117947097 | PUBCHEM_CID |
| DB15463 | DRUGBANK_ID |
| 11196 | INN_ID |
| C000720612 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11251 | IUPHAR_LIGAND_ID |
| 41129411000001102 | SNOMEDCT_US |
| 4040773 | VANDF |
| 349651 | MMSL |
| 39823 | MMSL |
| d09792 | MMSL |
| 018835 | NDDF |
| 2567226 | RXNORM |
| 7K28NB895L | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| WELIREG | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-5331 | TABLET, FILM COATED | 40 mg | ORAL | NDA | 33 sections |