Belzutifan versus Everolimus for Advanced Renal-Cell Carcinoma.

Belzutifan, a hypoxia-inducible factor 2α inhibitor, showed clinical activity in clear-cell renal-cell carcinoma in early-phase studies.

In a phase 3, multicenter, open-label, active-controlled trial, we enrolled participants with advanced clear-cell renal-cell carcinoma who had previously received immune checkpoint and antiangiogenic therapies and randomly assigned them, in a 1:1 ratio, to receive 120 mg of belzutifan or 10 mg of everolimus orally once daily until disease progression or unacceptable toxic effects occurred.

The dual primary end points were progression-free survival and overall survival. The key secondary end point was the occurrence of an objective response (a confirmed complete or partial response).

A total of 374 participants were assigned to belzutifan, and 372 to everolimus. At the first interim analysis (median follow-up, 18.4 months), the median progression-free survival was 5.6 months in both groups; at 18 months, 24.0% of the participants in the belzutifan group and 8.3% in the everolimus group were alive and free of progression (two-sided P = 0.002, which met the prespecified significance criterion). A confirmed objective response occurred in 21.9% of the participants (95% confidence interval [CI], 17.8 to 26.5) in the belzutifan group and in 3.5% (95% CI, 1.9 to 5.9) in the everolimus group (P<0.001, which met the prespecified significance criterion). At the second interim analysis (median follow-up, 25.7 months), the median overall survival was 21.4 months in the belzutifan group and 18.1 months in the everolimus group; at 18 months, 55.2% and 50.6% of the participants, respectively, were alive (hazard ratio for death, 0.88; 95% CI, 0.73 to 1.07; two-sided P = 0.20, which did not meet the prespecified significance criterion). Grade 3 or higher adverse events of any cause occurred in 61.8% of the participants in the belzutifan group (grade 5 in 3.5%) and in 62.5% in the everolimus group (grade 5 in 5.3%). Adverse events led to discontinuation of treatment in 5.9% and 14.7% of the participants, respectively.

Belzutifan showed a significant benefit over everolimus with respect to progression-free survival and objective response in participants with advanced clear-cell renal-cell carcinoma who had previously received immune checkpoint and antiangiogenic therapies. Belzutifan was associated with no new safety signals. (Funded by Merck Sharp and Dohme, a subsidiary of Merck; LITESPARK-005 ClinicalTrials.gov number, NCT04195750.).

The New England journal of medicine. 2024 Aug 22 [Epub]

Toni K Choueiri, Thomas Powles, Katriina Peltola, Guillermo de Velasco, Mauricio Burotto, Cristina Suarez, Pooja Ghatalia, Roberto Iacovelli, Elaine T Lam, Elena Verzoni, Mahmut Gümüş, Walter M Stadler, Christian Kollmannsberger, Bohuslav Melichar, Balaji Venugopal, Marine Gross-Goupil, Alexandr Poprach, Maria De Santis, Fabio A Schutz, Se Hoon Park, Dmitry A Nosov, Camillo Porta, Jae Lyun Lee, Xavier Garcia-Del-Muro, Elisa Biscaldi, Ray Manneh Kopp, Mototsugu Oya, Li He, Aobo Wang, Rodolfo F Perini, Donna Vickery, Laurence Albiges, Brian Rini, LITESPARK-005 Investigators

From Dana-Farber Cancer Institute, Boston (T.K.C.); Barts Cancer Centre, Queen Mary University of London BRC, Royal Free NHS Trust, London (T.P.), and Beatson West of Scotland Cancer Centre and the University of Glasgow, Glasgow (B.V.) - all in the United Kingdom; HUS Helsinki University Hospital, Comprehensive Cancer Center, Helsinki (K.P.); University Hospital 12 de Octubre, Instituto de Investigación Sanitaria Hospital 12 de Octubre (imas12), Madrid (G.V.), and Medical Oncology, Vall d´Hebron Institute of Oncology (VHIO), Hospital Universitari Vall d´Hebron, Vall d´Hebron Barcelona Hospital Campus (C.S.), and Institute Catalan of Oncology-ICO-IDIBELL University of Barcelona (X.G.-M.), Barcelona - all in Spain; Bradford Hill Clinical Research Center, Santiago, Chile (M.B.); Fox Chase Cancer Center, Philadelphia (P.G.); Fondazione Policlinico Universitario A. Gemelli IRCCS, Rome (R.I.), Fondazione IRCCS Istituto Nazionale dei Tumori, Milan (E.V.), the University of Bari "A. Moro" and Azienda Ospedaliera Policlinico di Bari, Bari (C.P.), and Fondazione Salvatore Maugeri clinica del lavoro, Pavia (E.B.) - all in Italy; the University of Colorado Cancer Center, Aurora (E.T.L.); Istanbul Medeniyet University, Prof. Dr. Suleyman Yalcin City Hospital, Istanbul, Turkey (M.G.); the University of Chicago Medical Center, Chicago (W.M.S.); BC Cancer-Vancouver Center, Vancouver, BC, Canada (C.K.); the Department of Oncology, Palacký University and University Hospital, Olomouc (B.M.), and the Department of Comprehensive Cancer Care and Faculty of Medicine, Masaryk Memorial Cancer Institute and Masaryk University, Brno (A.P.) - both in the Czech Republic; University Hospital Bordeaux-Hôpital Saint-André, Bordeaux (M.G.-G.), and Département de Médecine Oncologique, Gustave Roussy, Université Paris Saclay, Villejuif (L.A.) - both in France; Charité Universitaetsmedizin Berlin, Department of Urology, Berlin (M.D.S.); the Department of Urology, Medical University of Vienna, Vienna (M.D.S.); BP-A Beneficencia Portuguesa de São Paulo, Sao Paulo (F.A.S.); Samsung Medical Center, Sungkyunkwan University School of Medicine (S.H.P.), and Asan Medical Center, University of Ulsan College of Medicine (J.L.L.) - both in Seoul, South Korea; Central Clinical Hospital with Polyclinic, Moscow (D.A.N.); Sociedad de Oncología y Hematología del Cesar, Valledupar, Colombia (R.M.K.); Keio University Hospital, Tokyo (M.O.); Merck, Rahway, NJ (L.H., A.W., R.F.P., D.V.); and Vanderbilt Ingram Cancer Center, Nashville (B.R.).