Belzutifan
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2021
- First approval year
- 2021
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Belzutifan
- Molecular weight
- 383.35
- Structure (SMILES)
- CS(=O)(=O)c1ccc(Oc2cc(F)cc(C#N)c2)c2c1[C@H](O)[C@H](F)[C@@H]2F
- welireg
- Welireg
- belzutifan
- Belzutifan
- belzutifan [INN]
- Belzutifan [MI]
- BELZUTIFAN [ORANGE BOOK]
- BELZUTIFAN [USAN]
- Belzutifan [WHO-DD]
- Belzutifan 120mg
- belzutifan inn
- belzutifan mi
- belzutifan orange book
- belzutifan usan
- belzutifan who dd
- mk 6482
- Mk-6482
- MK-6482
- mk6482
- MK6482
- pt 2977
- Pt 2977
- PT-2977
- pt2977
- Pt2977
- PT2977
- ATC classification codes
- L01XX74
Sources for recorded values
- CAS registry numbers
- 1672668-24-4
- ChEMBL ID
- CHEMBL4585668
- InChIKey
- LOMMPXLFBTZENJ-ZACQAIPSSA-N
- PubChem compound IDs
- 117947097
- RxNorm IDs (RxCUI)
- 2567226
- FDA ingredient codes (UNII)
- 7K28NB895L
- Applicant
- MERCK SHARP DOHME
- Approval date
- 13 Aug 2021
- Application number
- NDA215383
- Status
- Authorised
- Status date
- 12 Feb 2025
- Authorisation date
- 12 Feb 2025
- Approved indications
- Renal cell carcinoma (RCC) Welireg is indicated as monotherapy for the treatment of adult patients with advanced clear cell renal cell carcinoma that progressed following two or more lines of therapy that included a PD-(L)1 inhibitor and at least two VEGF-targeted therapies. von Hippel-Lindau (VHL) disease-associated tumours Welireg is indicated as monotherapy for the treatment of adult patients with von Hippel-Lindau disease who require therapy for associated, localised renal cell carcinoma (RCC), central nervous system (CNS) haemangioblastomas, or pancreatic neuroendocrine tumours (pNET), and for whom localised procedures are unsuitable.
- Product number
- EMEA/H/C/005636
- Authorisation holder
- Merck Sharp & Dohme B.V.
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- Yes
- Additional monitoring
- Yes
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Carcinoma, Renal Cell
- von Hippel-Lindau Disease
European medicines record
- Patents
- 3
- Designations
- 5
- Earliest recorded loss of exclusivity
- 30 Jun 2042
- First in class
- Yes
- Fast track
- No
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- Pharmacology name
- belzutifan
- Type
- Synthetic organic
- Drug name stem
- -ifan
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Binding
- Action type
- Binding
- Target
- endothelial PAS domain protein 1
- Gene symbol
- EPAS1
- Protein identifier
- Q99814
- Median affinity
- 8.05
- Affinity units
- pIC50
- Mechanism
- Endothelial PAS domain-containing protein 1 inhibitor
- Action type
- Inhibitor
- Target
- Endothelial PAS domain-containing protein 1
- Protein identifier
- Q99814
Open Targets mechanisms
- Mechanism
- Endothelial PAS domain-containing protein 1 inhibitor
- Action type
- Inhibitor
- Target
- Endothelial PAS domain-containing protein 1
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000349
- Subject identifier
- D002292
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000681
- Subject identifier
- D002292
- Condition
- Liver Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001421
- Subject identifier
- D008107
- Condition
- Renal Insufficiency, Chronic
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003884
- Subject identifier
- D051436
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 4
- Condition identifier
- EFO:0005708
- Subject identifier
- D002292
- Condition
- Neuroendocrine Tumors
- Highest recorded phase
- 4
- Condition identifier
- EFO:1000045
- Subject identifier
- D018358
- Condition
- von Hippel-Lindau Disease
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0008667
- Subject identifier
- D006623
- Condition
- Hemangioblastoma
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0016748
- Subject identifier
- D018325
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000681
- Condition identifier
- EFO_0001421
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003884
- Highest recorded phase
- 1
- Condition identifier
- EFO_0005708
- Highest recorded phase
- 1
- Condition identifier
- EFO_1000045
- Condition identifier
- MONDO_0000448
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0000548
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0003060
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005005
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005086
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005184
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005549
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005575
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005580
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0007254
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0007256
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0008233
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0008315
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0008667
- Condition identifier
- MONDO_0008667
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0009831
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0011962
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0016748
And 3 more, listed on the interactive page.
- Warning
- Black Box Warning
- Effect
- cardiotoxicity
- Warning
- Black Box Warning
- Effect
- teratogenicity
- Warning
- Black Box Warning
- Effect
- cardiotoxicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- teratogenicity
- Country
- United States
- NCT03634540
- NCT04627064
- NCT04195750
- NCT04489771
- NCT04586231
- NCT04626479
- NCT04626518
- NCT04736706
- NCT04846920
- NCT05030506
- NCT05239728
- NCT05468697
- NCT05899049
- NCT04994522
- NCT04995484
- NCT06234605
- Dose
- 120 mg
- Route
- Oral
- How often
- Once daily
- Do not chew, crush, or split
- Swallow tablets whole
- Take with or without food
- Hydrogen bond acceptors
- 5
- Hydrogen bond donors
- 1
- Polar surface area
- 87.39
- Calculated partition coefficient (ALogP)
- 3.29
- Calculated partition coefficient (XLogP)
- 2
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 3
- Heavy atoms
- 26
- Molecular formula
- C17H12F3NO4S
- Monoisotopic mass
- 383.04391352
- Natural product
- No
- 0006-5331
- Recorded assays
- 360
- Active assays
- 16
Active assay types
- Confirmatory
- Antineoplastic Agents
Distribution coefficient (LogD)
- Median
- 1.2
- Mean
- 1.2
- Minimum
- 1.2
- Maximum
- 1.2
- Unit
- unitless
- Assays
- 2
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- LogD
Related records
Trials (37)
- A Clinical Study of Belzutifan (MK-6482) Alone or With Phenytoin in Healthy Participants (CA46602/MK-6482-035)
- A Clinical Study of Belzutifan (MK-6482) and Zanzalintinib in People With Renal Cell Carcinoma (RCC) (LITESPARK-034/LS-034/MK-6482-034)
- A Clinical Study of Belzutifan and Zanzalintinib in People With Recurrent Kidney Cancer Following Adjuvant Therapy (MK-6482-033)
- A Food Effect Study in Healthy Volunteers With Belzutifan (PT2977, MK-6482) Tablets
- A Phase 2 Study of Belzutifan (PT2977, MK-6482) for the Treatment of Von Hippel Lindau (VHL) Disease-Associated Renal Cell Carcinoma (RCC) (MK-6482-004)
- A Study of Belzutifan (MK-6482) and Metformin in Healthy Adult Participants (MK-6482-039)
- A Study of Belzutifan (MK-6482) as Monotherapy and in Combination With Lenvatinib (E7080/MK-7902) With or Without Pembrolizumab (MK-3475) in China Participants With Advanced Renal Cell Carcinoma (MK-6482-010)
- A Study of Belzutifan (MK-6482) in Combination With Lenvatinib Versus Cabozantinib for Treatment of Renal Cell Carcinoma (MK-6482-011)
- A Study of Belzutifan (MK-6482) in Combination With Palbociclib Versus Belzutifan Monotherapy in Participants With Advanced Renal Cell Carcinoma (MK-6482-024/LITESPARK-024)
- A Study of Belzutifan (MK-6482) in Participants With Advanced Clear Cell Renal Cell Carcinoma (MK-6482-018)
- A Study of Belzutifan (MK-6482) in Participants With Advanced Renal Cell Carcinoma (MK-6482-013)
- A Study of Belzutifan (MK-6482) in Participants With Hepatic Impairment (MK-6482-020)
- A Study of Belzutifan (MK-6482) in Participants With Renal Impairment (MK-6482-021)
- A Study of Belzutifan (MK-6482) Plus Pembrolizumab (MK-3475) Versus Placebo Plus Pembrolizumab in Participants With Clear Cell Renal Cell Carcinoma Post Nephrectomy (MK-6482-022)
- A Study of Belzutifan (MK-6482) Versus Everolimus in Participants With Advanced Renal Cell Carcinoma (MK-6482-005)
- A Study of Belzutifan in Adolescent Participants With Solid Tumors (MK-9999-01E/LIGHTBEAM-U01)
- A Study of HC-7366 in Combination With Belzutifan (WELIREG™) in Patients With Renal Cell Carcinoma
- A Study of Pembrolizumab (MK-3475) in Combination With Belzutifan (MK-6482) and Lenvatinib (MK-7902), or Pembrolizumab/Quavonlimab (MK-1308A) in Combination With Lenvatinib, Versus Pembrolizumab and Lenvatinib, for Treatment of Advanced Clear Cell Renal Cell Carcinoma (MK-6482-012)
- A Study of Pembrolizumab (MK-3475) in Combination With Belzutifan (MK-6482) and Lenvatinib (MK-7902), or Pembrolizumab/Quavonlimab (MK-1308A) in Combination With Lenvatinib, vs Pembrolizumab and Lenvatinib, for Treatment of Advanced Clear Cell Renal Cell Carcinoma (MK-6482-012)-China Extension Study
- A Trial of Belzutifan (PT2977, MK-6482) in Combination With Cabozantinib in Patients With Clear Cell Renal Cell Carcinoma (ccRCC) (MK-6482-003)
Approved for (7)
- Clear cell renal carcinoma
- Hemangioblastoma
- Neoplasm
- Pancreatic neuroendocrine tumor
- Renal cell adenocarcinoma
- Renal cell carcinoma
- Von Hippel-Lindau disease
In development for (2)
- Chronic kidney disease Phase 1
- Liver disorder Phase 1
Targets (1)
- EPAS1 Endothelial PAS domain-containing protein 1 inhibitor