Welireg

(Belzutifan)

Phase 3Small molecule

CCidara Therapeutics Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)

Welireg is a small molecule that works as a Hif-2a Inhibitor.[2] It is being investigated across 18 indications, with its most advanced program in Phase 3.[1]

Welireg is one of 259 small molecule programs targeting Renal Cell Carcinoma. It is currently in Phase 3.

Indications

Total Trials

Active Trials

258

Competitors

FDA Applications

NDA/BLA/ANDA regulatory filings

Patents

Pipeline

Status by Indication[3][1]

Indication

Renal Cell CarcinomaCompleted

Pancreatic Neuroendocrine TumorUnknown

Von Hippel-Lindau DiseaseRecruiting

HemangioblastomaUnknown

Metastatic Castration-Resistant Prostate CancerActive, not recruiting

Metastatic Breast CancerActive, not recruiting

Pheochromocytoma/paragangliomaRecruiting

PheochromocytomaRecruiting

Malignant NeoplasmNot yet recruiting

Solid TumorActive, not recruiting

Renal Cell CarcinomaPhase 3

Completed

Pancreatic Neuroendocrine TumorPreclinical

Unknown

Von Hippel-Lindau DiseasePhase 3

Recruiting

HemangioblastomaPreclinical

Unknown

Metastatic Castration-Resistant Prostate CancerPreclinical

Active, not recruiting

Metastatic Breast CancerPhase 2

Active, not recruiting

Pheochromocytoma/paragangliomaPhase 2

Recruiting

PheochromocytomaPhase 2

Recruiting

Malignant NeoplasmPhase 2

Not yet recruiting

Solid TumorPhase 1

Active, not recruiting

Showing 10 of 18 indications

Competition

Competitive Landscape

348 competitors in Solid Tumor

#DrugCompanyPhaseTrials

Welireg

CCidara Therapeutics Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)

Phase 3

1 2

Yervoy

Bristol-Myers Squibb

Preclinical

3 3

Nubeqa

Bayer

Preclinical

2 4

Fludara

Sanofi

Preclinical

1 5

DATROWAY

Daiichi Sankyo

Preclinical

1 6

Sporanox

SSebela Pharmaceuticals Development LLC

Preclinical

2 7

Zejula

GGlaxo Dba Glaxosmithkline

Preclinical

2 8

Augtyro

KKaruna Therapeutics, Inc., a Bristol Myers Squibb company

Preclinical

2 9

Paxil

SSebela Pharmaceuticals Development LLC

Preclinical

1 10

Epivir

GGlaxo Dba Glaxosmithkline

Preclinical

Ranked by pipeline maturity and clinical activity. Current drug highlighted in teal.

Timeline

Expected Milestones

Q4 2026

Phase 2Active, not recruiting

Renal Cell Carcinoma

NCT04489771

Phase 1Active, not recruiting

Solid Tumor

NCT02974738

PreclinicalActive, not recruiting

Renal Cell Carcinoma

NCT05468697

Q1 2027

Phase 2Active, not recruiting

Renal Cell Carcinoma

NCT03634540

Phase 2Active, not recruiting

Pembrolizumab

NCT04976634

Q2 2027

Phase 3Active, not recruiting

Carcinoma, Renal Cell

NCT05899049

Clinical

Trials by Indication[1]

Renal Cell Carcinoma12 trials

A Study of Belzutifan (MK-6482) in Participants With Advanced Renal Cell Carcinoma (MK-6482-013)

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 2·NCT04489771·154 enrolled

A Study of Belzutifan (MK-6482) in Participants With Advanced Clear Cell Renal Cell Carcinoma (MK-6482-018)

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 1·NCT04846920·52 enrolled

A Trial of Belzutifan (PT2977, MK-6482) in Combination With Cabozantinib in Patients With Clear Cell Renal Cell Carcinoma (ccRCC) (MK-6482-003)

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 2·NCT03634540·118 enrolled

Show 9 more trials

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)

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 2·NCT03401788·50 enrolled

A Study of HC-7366 in Combination With Belzutifan (WELIREG™) in Patients With Renal Cell Carcinoma

Recruiting·HHiberCell, Inc.·Phase 1·NCT06234605·80 enrolled

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)

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 1·NCT05030506·45 enrolled

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)

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 3·NCT05239728·1,800 enrolled

A Study of Belzutifan (MK-6482) Versus Everolimus in Participants With Advanced Renal Cell Carcinoma (MK-6482-005)

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 3·NCT04195750·755 enrolled

A Phase 1b/2 Study of Immune and Targeted Combination Therapies in Participants With RCC (KEYMAKER-U03): Substudy 03C in Participants With Recurrent Disease During or After Anti-PD-(L)1 Adjuvant Therapy

Recruiting· Merck & Co. logo

Merck & Co.·Preclinical·NCT07049926·140 enrolled

A Multicenter, Open-label, Randomized, Phase 1/2 Study of Belzutifan in Combination With Palbociclib Versus Belzutifan Monotherapy in Participants With Advanced Renal Cell Carcinoma

Active, not recruiting· Merck & Co. logo

Merck & Co.·Preclinical·NCT05468697·60 enrolled

A Phase 3, Randomized, Open-label Study of Belzutifan + Zanzalintinib Versus Cabozantinib in Participants With Advanced RCC Who Experienced Disease Recurrence During or After Prior Adjuvant Anti-PD-1/L1 Therapy (LITESPARK-033)

Recruiting· Merck & Co. logo

Merck & Co.·Phase 3·NCT07227402·904 enrolled

LITESPARK-005: Belzutifan vs Everolimus in RCC

Completed· Merck & Co. logo

Merck & Co.·Phase 3·NCT04586231·746 enrolled

Carcinoma, Renal Cell5 trials

A Phase 3, Randomized, Double-blind, Study of Belzutifan + Zanzalintinib Versus Belzutifan + Placebo in Participants With Advanced RCC Who Have Progressed on or After Both PD-1/L1 and VEGF-TKI Therapies in Sequence or in Combination (LITESPARK-034)

Recruiting· Merck & Co. logo

Merck & Co.·Phase 3·NCT07489495·758 enrolled

An Open-label, Randomized Phase 3 Study to Evaluate Efficacy and Safety of Pembrolizumab (MK-3475) in Combination With Belzutifan (MK-6482) and Lenvatinib (MK-7902), or MK-1308A in Combination With Lenvatinib, Versus Pembrolizumab and Lenvatinib, as First-Line Treatment in Participants With Advanced Clear Cell Renal Cell Carcinoma (ccRCC)

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 3·NCT05899049·251 enrolled

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 3·NCT04736706·1,854 enrolled

Show 2 more trials

A Phase 1b/2 Study of Immune and Targeted Combination Therapies in Participants With RCC (U03): Substudy 03A in First Line Metastatic Participants

Active, not recruiting· Merck & Co. logo

Merck & Co.·Preclinical·NCT04626479·400 enrolled

A Phase 1b/2 Study of Immune and Targeted Combination Therapies in Participants With RCC (KEYMAKER-U03): Substudy 03B in Second-Line Metastatic Participants

Active, not recruiting· Merck & Co. logo

Merck & Co.·Preclinical·NCT04626518·370 enrolled

Active Surveillance1 trial

Belzutifan's Role in Active Surveillance Versus Treatment for Indolentmetastatic Clear Cell Renal Ccell Carcinoma (BRAVE-RCC)

Not yet recruiting·MM.D. Anderson Cancer Center·Phase 2·NCT07023432·78 enrolled

Hepatic Impairment1 trial

A Study of Belzutifan (MK-6482) in Participants With Hepatic Impairment (MK-6482-020)

Completed· Merck & Co. logo

Merck & Co.·Phase 1·NCT04995484·17 enrolled

Effectiveness1 trial

Real-World Effectiveness and Pharmacogenetics of Belzutifan in VHL Syndrome: The BELIEVE-VHL Trial

Recruiting·JJosé Claudio Casali da Rocha·Phase 2·NCT07167329·100 enrolled

16 more indications

ART1 trial

A Clinical Study of Belzutifan (MK-6482) Alone or With Phenytoin in Healthy Participants (CA46602/MK-6482-035)

Completed· Merck & Co. logo

Merck & Co.·Phase 1·NCT06903715·14 enrolled

Metformin1 trial

A Study of Belzutifan (MK-6482) and Metformin in Healthy Adult Participants (MK-6482-039)

Completed· Merck & Co. logo

Merck & Co.·Phase 1·NCT07121959·14 enrolled

Pembrolizumab1 trial

Pembrolizumab Plus Lenvatinib in Combination With Belzutifan in Solid Tumors (MK-6482-016)

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 2·NCT04976634·730 enrolled

Renal Impairment1 trial

A Study of Belzutifan (MK-6482) in Participants With Renal Impairment (MK-6482-021)

Completed· Merck & Co. logo

Merck & Co.·Phase 1·NCT04994522·14 enrolled

Clear Cell Carcinoma1 trial

Belzutifan in Recurrent Clear Cell Carcinoma of Gynecologic Origin

Recruiting·—·Phase 2·NCT06677190·32 enrolled

Solid Tumor1 trial

A Phase 1, Dose-Escalation and Expansion Trial of PT2977, a HIF-2α Inhibitor, in Patients With Advanced Solid Tumors

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 1·NCT02974738·120 enrolled

Malignant Neoplasm1 trial

LIGHTBEAM-U01 Substudy 01E: A Phase 2 Substudy to Evaluate the Safety and Efficacy of Belzutifan in Participants With Solid Tumors

Not yet recruiting· Merck & Co. logo

Merck & Co.·Phase 2·NCT07700758·15 enrolled

Von Hippel-Lindau Disease1 trial

A Multicenter, Open-label, Phase 3 Extension Study to Evaluate the Long-term Efficacy and Safety in Participants Who Are Currently on Treatment in a Belzutifan Study (LITESPARK-043)

Recruiting· Merck & Co. logo

Merck & Co.·Phase 3·NCT07405164·450 enrolled

Pheochromocytoma/Paraganglioma1 trial

A Phase 2 Study to Evaluate the Efficacy and Safety of Belzutifan (MK-6482, Formerly PT2977) Monotherapy in Participants With Advanced Pheochromocytoma/Paraganglioma (PPGL), Pancreatic Neuroendocrine Tumor (pNET), Von Hippel-Lindau (VHL) Disease-Associated Tumors, Advanced Gastrointestinal Stromal Tumor (wt GIST), or Advanced Solid Tumors With HIF-2α Related Genetic Alterations

Recruiting· Merck & Co. logo

Merck & Co.·Phase 2·NCT04924075·355 enrolled

Malignant Neoplam1 trial

A Phase 2, Open-label Clinical Study to Evaluate the Safety and Efficacy of MK-2010 as Monotherapy and in Combination

Not yet recruiting· Merck & Co. logo

Merck & Co.·Phase 2·NCT07793942·480 enrolled

Metastatic Breast Cancer1 trial

A Phase 2, Randomized, Active-controlled, Open-label, Multicenter Study of Belzutifan Plus Fulvestrant in Participants With Estrogen Receptor Positive, HER2 Negative Unresectable Locally Advanced or Metastic Breast Cancer After Progression on Previous Endocrine Therapy (LITESPARK-029)

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 2·NCT06428396·120 enrolled

Clear Cell Renal Cell Carcinoma1 trial

Phase II Trial of Single Agent Belzutifan or Pembrolizumab Versus Combination as Neoadjuvant Therapy in Clear Cell Renal Cell Carcinoma (BLAZE)

Recruiting·MM.D. Anderson Cancer Center·Phase 2·NCT07187778·10 enrolled

Metastatic Clear Cell Renal Cell Carcinoma1 trial

A Phase 1b Study to Assess the Effects of Belzutifan on 89Zr-DFO-girentuximab Uptake as a Surrogate to Determine CAIX Tumor Expression in Patients With Clear Cell Renal Cell Carcinoma

Recruiting·NNYU Langone Health·Phase 1·NCT07179770·12 enrolled

Metastatic Castration-Resistant Prostate Cancer1 trial

Phase Ib/II Trial of Pembrolizumab (MK-3475) Combination Therapies in Metastatic Castration-Resistant Prostate Cancer (mCRPC) (KEYNOTE-365)

Active, not recruiting· Merck & Co. logo

Merck & Co.·Preclinical·NCT02861573·1,200 enrolled

Pheochromocytoma1 trial

An Experimental Pilot Study to Investigate Changes in Catecholamine Synthesis and Metabolism in Patients With Molecularly Profiled Phaeochromocytoma and Paraganglioma Taking Belzutifan

Recruiting·CCambridge University Hospitals NHS Foundation Trust·Phase 2·NCT07680205·12 enrolled

Unspecified1 trial

A Food Effect Study in Healthy Volunteers With Belzutifan (PT2977, MK-6482) Tablets

Completed· Merck & Co. logo

Merck & Co.·Phase 1·NCT03445169·16 enrolled

Regulatory

FDA Approval Timeline[4]

Aug 13, 2021

WELIREG

NDA NDA215383

Aug 13, 2021

WELIREG

NDA NDA215383

Dec 14, 2023

WELIREG

NDA NDA215383

Feb 26, 2024

WELIREG

NDA NDA215383

Apr 15, 2025

WELIREG

NDA NDA215383

Apr 15, 2025

WELIREG

NDA NDA215383

May 14, 2025

WELIREG

NDA NDA215383

Jun 12, 2026

WELIREG

NDA NDA215383

Sources

References

[1]
ClinicalTrials.gov — 36 trial records for Belzutifan. U.S. National Library of Medicine, National Institutes of Health.
[2]
ChEMBL — Belzutifan compound record. European Bioinformatics Institute (EMBL-EBI).
[3]
Open Targets Platform — Drug–disease associations for Belzutifan. EMBL-EBI & Wellcome Sanger Institute.
[4]
OpenFDA — FDA approval records (NDA NDA215383). U.S. Food & Drug Administration.
[5]
FDA Orange Book — Patent and exclusivity data for Welireg. U.S. Food & Drug Administration.
[6]
PubMed — 1 publication indexed for Belzutifan. U.S. National Library of Medicine.
[7]
SEC EDGAR — Cidara Therapeutics Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA) company filings. U.S. Securities and Exchange Commission.

Details

Drug Info

Quick Facts

Mechanism of Action: Hif-2a Inhibitor[2]
Modality: Small molecule[2]
Highest Phase: Phase 3[1]
Company: CCidara Therapeutics Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)

Patent Landscape[5]

Patent Cliff

Sep 5, 2034

Earliest patent expiration — generic entry possible after this date

Patent #Expires

RE49948Sep 5, 2034

9908845Sep 5, 2034

10335388Apr 13, 2036

12358870Jun 30, 2042

Key Publications[6]

Belzutifan vs Everolimus in Advanced Clear Cell RCC: LITESPARK-005

LancetOct 20, 2023DOI: 10.1016/S0140-6736(23)02097-4

Welireg

Status by Indication[3][1]

Competitive Landscape

Expected Milestones

Q4 2026

Q1 2027

Q2 2027

Trials by Indication[1]

Renal Cell Carcinoma12 trials

Carcinoma, Renal Cell5 trials

Active Surveillance1 trial

Hepatic Impairment1 trial

Effectiveness1 trial

ART1 trial

Metformin1 trial

Pembrolizumab1 trial

Renal Impairment1 trial

Clear Cell Carcinoma1 trial

Solid Tumor1 trial

Malignant Neoplasm1 trial

Von Hippel-Lindau Disease1 trial

Pheochromocytoma/Paraganglioma1 trial

Malignant Neoplam1 trial

Metastatic Breast Cancer1 trial

Clear Cell Renal Cell Carcinoma1 trial

Metastatic Clear Cell Renal Cell Carcinoma1 trial

Metastatic Castration-Resistant Prostate Cancer1 trial

Pheochromocytoma1 trial

Unspecified1 trial

FDA Approval Timeline[4]

References

Drug Info

Quick Facts

Patent Landscape[5]

Key Publications[6]

Related News