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 16 indications, with its most advanced program in Phase 3.[1]

Welireg is one of 307 small molecule programs targeting Kidney Cancer. It is currently in Phase 3.

Indications

Total Trials

Active Trials

306

Competitors

FDA Application

NDA/BLA/ANDA regulatory filings

Patents

Pipeline

Status by Indication[3][1]

Indication

Kidney CancerActive, not recruiting

Pancreatic Neuroendocrine TumorUnknown

Von Hippel-Lindau DiseaseRecruiting

HemangioblastomaUnknown

Liver DiseaseActive, not recruiting

Breast CancerActive, not recruiting

Pancreatic CancerRecruiting

Prostate CancerActive, not recruiting

Renal Cell CarcinomaActive, not recruiting

Chronic Kidney DiseaseActive, not recruiting

Kidney CancerPhase 3

Active, not recruiting

Pancreatic Neuroendocrine TumorPreclinical

Unknown

Von Hippel-Lindau DiseasePhase 3

Recruiting

HemangioblastomaPreclinical

Unknown

Liver DiseasePhase 1

Active, not recruiting

Breast CancerPhase 2

Active, not recruiting

Pancreatic CancerPhase 2

Recruiting

Prostate CancerPhase 1/Phase 2

Active, not recruiting

Renal Cell CarcinomaPhase 3

Active, not recruiting

Chronic Kidney DiseasePhase 1

Active, not recruiting

Showing 10 of 16 indications

Competition

Competitive Landscape

2828 competitors in Breast Cancer

#DrugCompanyPhaseTrials

Welireg

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

Phase 3

34 2

Cymbalta

Alnylam Pharmaceuticals

Preclinical

3 3

Chirocaine

PPurdue Pharma LP

Preclinical

1 4

Vfend

PPrism Pharmaceuticals

Preclinical

—5

QS21

MMemorial Sloan Kettering Cancer Center

Preclinical

3 6

Vit D

PPost Graduate Institute of Medical Education and Research, Chandigarh

Preclinical

1 7

Ablavar

LLantheus Medical Imaging

Preclinical

2 8

Sertraline ODT

PPfizer's Upjohn has merged with Mylan to form Viatris Inc.

Preclinical

1 9

Combination NRT

UUniversity of Alabama at Birmingham

Preclinical

1 10

Fluoroestradiol (18f)

AAssistance Publique - Hôpitaux de Paris

Preclinical

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

Timeline

Expected Milestones

Q3 2026

Phase 1/2Active, not recruiting

Renal Cell Carcinoma

NCT05468697

Phase 1Active, not recruiting

Renal Cell Carcinoma

NCT04846920

Phase 3Active, not recruiting

Renal Cell Carcinoma

NCT04195750

Q4 2026

Phase 2Active, not recruiting

Renal Cell Carcinoma

NCT04489771

Phase 3Active, not recruiting

Renal Cell Carcinoma

NCT04736706

Q1 2027

Phase 2Active, not recruiting

Renal Cell Carcinoma

NCT03634540

Clinical

Trials by Indication[1]

Renal Cell Carcinoma18 trials

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)

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 3·NCT04736706·1,653 enrolled

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) 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

Show 15 more trials

Substudy 03A: A Study of Immune and Targeted Combination Therapies in Participants With First Line (1L) Renal Cell Carcinoma (MK-3475-03A)

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 1/2·NCT04626479·400 enrolled

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

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

Substudy 03B: A Study of Immune and Targeted Combination Therapies in Participants With Second Line Plus (2L+) Renal Cell Carcinoma (MK-3475-03B/KEYMAKER-U03)

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 1/2·NCT04626518·370 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 Study of Belzutifan (MK-6482) in Combination With Palbociclib Versus Belzutifan Monotherapy in Participants With Advanced Renal Cell Carcinoma (MK-6482-024/LITESPARK-024)

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 1/2·NCT05468697·60 enrolled

Effects of Belzutifan on 89Zr-DFO-girentuximab PET Uptake in Patients With Renal Cell Carcinoma (RCC)

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

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

Active, not recruiting· Merck & Co. logo

Merck & Co.·Phase 3·NCT05899049·249 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

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 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

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

LITESPARK-005: Belzutifan vs Everolimus in RCC

Completed· Merck & Co. logo

Merck & Co.·Phase 3·NCT04586231·746 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

Clear Cell Carcinoma1 trial

Belzutifan in Recurrent Clear Cell Carcinoma of Gynecologic Origin

Recruiting·—·Phase 2·NCT06677190·32 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

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

12 more indications

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

Patients With Advanced Solid Tumors1 trial

A Trial of Belzutifan (PT2977, MK-6482) Tablets In Patients With Advanced Solid Tumors (MK-6482-001)

Active, not recruiting· Merck & Co. logo

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

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

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

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

Carcinoma, Renal Cell1 trial

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

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

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

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

Sources

References

[1]
ClinicalTrials.gov — 34 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

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

Q3 2026

Q4 2026

Q1 2027

Trials by Indication[1]

Renal Cell Carcinoma18 trials

Active Surveillance1 trial

Clear Cell Carcinoma1 trial

Hepatic Impairment1 trial

Renal Impairment1 trial

Effectiveness1 trial

Patients With Advanced Solid Tumors1 trial

ART1 trial

Metformin1 trial

Pembrolizumab1 trial

Metastatic Castration-Resistant Prostate Cancer1 trial

Von Hippel-Lindau Disease1 trial

Carcinoma, Renal Cell1 trial

Metastatic Breast Cancer1 trial

Pheochromocytoma/Paraganglioma1 trial

Pheochromocytoma1 trial

Unspecified1 trial

FDA Approval Timeline[4]

References

Drug Info

Quick Facts

Patent Landscape[5]

Key Publications[6]

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