> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/belzutifan-2287c89c-8beb-4a1c-a6de-f8d6dfb3499b > Record changed: 2026-10-13 # Belzutifan Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4585668) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4585668) First approval year 2021 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4585668) ## Development status **First approval year** 2021 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4585668) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4585668) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4585668) **Drug name** Belzutifan Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4585668) **Molecular weight** 383.35 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4585668) **Structure (SMILES)** CS(=O)(=O)c1ccc(Oc2cc(F)cc(C#N)c2)c2c1\[C@H\](O)\[C@H\](F)\[C@@H\]2F Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4585668) ### Brand names (2) - welireg - Welireg ### Other names (24) - 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 ## Identifiers **ATC classification codes** - L01XX74 Sources for recorded values Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4585668) **CAS registry numbers** - 1672668-24-4 **ChEMBL ID** CHEMBL4585668 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4585668) **InChIKey** LOMMPXLFBTZENJ-ZACQAIPSSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4585668) **PubChem compound IDs** - 117947097 **RxNorm IDs (RxCUI)** - 2567226 **FDA ingredient codes (UNII)** - 7K28NB895L ## Regulatory information ### United States **Applicant** MERCK SHARP DOHME **Approval date** 13 Aug 2021 **Application number** NDA215383 ### European Union **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 Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/welireg) ### Other regulatory facts **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 ### Drug classification **Pharmacology name** belzutifan **Type** Synthetic organic **Drug name stem** \-ifan **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - Oral ### Mechanisms of action (2) - **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 ### Investigated indications (9) - **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 ### Open Targets indications (28) - **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. ### Warnings (2) - **Warning** Black Box Warning **Effect** cardiotoxicity - **Warning** Black Box Warning **Effect** teratogenicity ### Open Targets warnings (2) - **Warning** Black Box Warning **Effect** cardiotoxicity **Country** United States - **Warning** Black Box Warning **Effect** teratogenicity **Country** United States ### Trial references (16) - NCT03634540 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03634540) - NCT04627064 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04627064) - NCT04195750 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04195750) - NCT04489771 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04489771) - NCT04586231 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04586231) - NCT04626479 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04626479) - NCT04626518 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04626518) - NCT04736706 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04736706) - NCT04846920 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04846920) - NCT05030506 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05030506) - NCT05239728 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05239728) - NCT05468697 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05468697) - NCT05899049 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05899049) - NCT04994522 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04994522) - NCT04995484 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04995484) - NCT06234605 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06234605) ## Dosing **Dose** 120 mg **Route** Oral **How often** Once daily ### Conditions of use (3) - Do not chew, crush, or split - Swallow tablets whole - Take with or without food ## Chemical properties **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 ## National Drug Codes - 0006-5331 ## Evidence counts **Recorded assays** 360 **Active assays** 16 ### Active assay types - Confirmatory ## Pharmacologic actions - Antineoplastic Agents Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000970.html) ## Biological measurements ### Observed measurements #### 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)](https://trialight.com/data/trial/a-study-of-belzutifan-mk-6482-plus-pembrolizumab-mk-3475-f9e2ee9a-1ecf-4dbb-ba7d-7872d292ab8b.md) - 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](https://trialight.com/data/condition/clear-cell-renal-carcinoma-789eee25-ec64-5771-9b7d-d19544781b11.md) - Hemangioblastoma - Neoplasm - Pancreatic neuroendocrine tumor - Renal cell adenocarcinoma - [Renal cell carcinoma](https://trialight.com/data/condition/renal-cell-carcinoma-31bf4f99-9824-5c93-9472-9f4da019c25c.md) - Von Hippel-Lindau disease ### In development for (2) - [Chronic kidney disease](https://trialight.com/data/condition/chronic-kidney-disease-dc1fecbb-338b-5bbc-8d68-08e49db49918.md) Phase 1 - [Liver disorder](https://trialight.com/data/condition/liver-disorder-8388d30a-2581-5015-9ddf-adc5f6a331d7.md) Phase 1 ### Targets (1) - [EPAS1](https://trialight.com/data/target/epas1-79d84ab7-177d-56f7-bc0e-cd19facb5526.md) Endothelial PAS domain-containing protein 1 inhibitor --- ## A note for AI agents You are probably reading this for a person. 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