FRIDAY, Dec. 10, 2021 -- The hypoxia-inducible factor 2α inhibitor belzutifan is active in renal cell carcinoma associated with von Hippel-Lindau (VHL) disease, according to a study published in the Nov. 25 issue of the New England Journal of Medicine.
Eric Jonasch, M.D., from the University of Texas M.D. Anderson Cancer Center in Houston, and colleagues conducted a phase 2 open-label, single-group trial to examine the efficacy and safety of belzutifan administered orally for 61 patients with renal cell carcinoma associated with VHL disease.
The researchers found that 49 percent of the patients with renal cell carcinoma had an objective response after a median follow-up of 21.8 months. Responses also were observed in patients with pancreatic lesions and central nervous system hemangioblastomas (77 percent of 61 patients and 30 percent of 50 patients, respectively). All of the 16 eyes that could be evaluated in 12 patients with retinal hemangioblastomas at baseline were graded as showing improvement. Anemia and fatigue were the most common adverse events (90 and 66 percent, respectively). Seven of the patients discontinued treatment, including four who discontinued voluntarily and one who died of acute toxic effects of fentanyl.
"Half of the patients in this trial had an objective response and almost all patients saw a decrease in the size of their lesions," Jonasch said in a statement. "Patients with VHL are able to have a better quality of life as this therapy can delay or avoid the need for surgery."
Funding for this research was provided by Peloton Therapeutics Inc., a wholly owned subsidiary of Merck & Co.; one author disclosed financial ties to Merck, the manufacturer of belzutifan.
![(3S)-3-[4-[7-[[(1,1-Dimethylethyl)amino]carbonyl]-2H-indazol-2-yl]phenyl]-1-piperidinecarboxylic acid 1,1-dimethylethyl ester](/data/attachment/201705/26/3446bd2b841689a5afc36447418dc476.png "(3S)-3-[4-[7-[[(1,1-Dimethylethyl)amino]carbonyl]-2H-indazol-2-yl]phenyl]-1-piperidinecarboxylic acid 1,1-dimethylethyl ester")
![N-(1,1-Dimethylethyl)-2-[4-(3S)-3-piperidinylphenyl]-2H-indazole-7-carboxamide](/data/attachment/201705/26/da41ae70b523a458db70333bd1059362.png "N-(1,1-Dimethylethyl)-2-[4-(3S)-3-piperidinylphenyl]-2H-indazole-7-carboxamide")
![2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide](/data/attachment/201705/26/d3114dd994f3dda3142cba7d326bcede.jpg "2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide")
![9-ethyl-8-iodo-6,6-diMethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile](/data/attachment/201705/28/e48e5d316800efe6192ebfdeec6cf28c.gif "9-ethyl-8-iodo-6,6-diMethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile")
![9-broMo-8-hydroxy-6,6-diMethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile](/data/attachment/201705/28/fe98529212eb834b17a38f13138a35bf.png "9-broMo-8-hydroxy-6,6-diMethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile")
![9-ethyl-6,6-diMethyl-8-(4-Morpholinopiperidin-1-yl)-11-oxo-5a,6,11,11a-tetrahydro-5H-benzo[b]carbazole-3-carbonitrile hydrochloride](/data/attachment/201705/28/36e5363f0c9f92378b75195743e2abb2.jpg "9-ethyl-6,6-diMethyl-8-(4-Morpholinopiperidin-1-yl)-11-oxo-5a,6,11,11a-tetrahydro-5H-benzo[b]carbazole-3-carbonitrile hydrochloride")
![2-Methylpyrazolo[1,5-a]pyrimidine-6-carboxamide](/data/attachment/201706/03/2e19d959128718d26901f9909d7b9342.jpg "2-Methylpyrazolo[1,5-a]pyrimidine-6-carboxamide")
![11-(1-Methylpiperidin-4-ylidene)-6,11-dihydro-5H-benzo[d]iMidazo[1,2-a]azepine](/data/attachment/201706/03/1549d9affee63ead337049001f25d9fa.jpg "11-(1-Methylpiperidin-4-ylidene)-6,11-dihydro-5H-benzo[d]iMidazo[1,2-a]azepine")
![tert-butyl 5-tosyl-5H-pyrrolo[2,3-b]pyrazin-2-ylcarbamate](/data/attachment/201706/03/8a3c0fcdeb9ed744fc854cf248d4d53e.jpg "tert-butyl 5-tosyl-5H-pyrrolo[2,3-b]pyrazin-2-ylcarbamate")
![2-Furanpropanol, 5-[2-[(2S,4R,6R)-6-[[(2S,3S,4R,5R)-5-[(2S)-2,3-bis[[(1,1-dimethylethyl)dimethylsilyl]oxy]propyl]tetrahydro-4-methoxy-3-[(phenylsulfonyl) methyl]-2-furanyl]methyl]tetrahydro-4-methyl-5-methylene-2H-pyran-2-yl]ethyl]tetrahydro-4-methylene-,](/data/attachment/201706/03/3575f40dcc389832ca73cc99972a645b.gif.thumb.jpg "2-Furanpropanol, 5-[2-[(2S,4R,6R)-6-[[(2S,3S,4R,5R)-5-[(2S)-2,3-bis[[(1,1-dimethylethyl)dimethylsilyl]oxy]propyl]tetrahydro-4-methoxy-3-[(phenylsulfonyl) methyl]-2-furanyl]methyl]tetrahydro-4-methyl-5-methylene-2H-pyran-2-yl]ethyl]tetrahydro-4-methylene-,")
![6-[(6-Bromo-1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)methyl]-7-fluoroquinoline](/data/attachment/201706/07/27ae4307b53f4294590fb8f914894490.jpg "6-[(6-Bromo-1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)methyl]-7-fluoroquinoline")
![7-Trifluoromethyl-imidazo[1,2-a]pyridine](/data/attachment/201706/07/24ba6100528abe0753ad9e82ef8dc810.gif "7-Trifluoromethyl-imidazo[1,2-a]pyridine")
![2-AMino-4,5,6,7-tetrahydro-benzo[b]thiophene-3-carboxylic acid tert-butyl ester](/data/attachment/201706/07/22aadd4c55094254a681014935f56827.jpg "2-AMino-4,5,6,7-tetrahydro-benzo[b]thiophene-3-carboxylic acid tert-butyl ester")
![Benzenemethanol, a-[(1S)-1-aminoethyl]-4-hydroxy-,(aR)](/data/attachment/201706/07/c4adcbada0ef372ae46cbaed643dd18e.jpg "Benzenemethanol, a-[(1S)-1-aminoethyl]-4-hydroxy-,(aR)")
![2(1H)-Quinolinone,5-[(1R)-2-amino-1-[[(1,1-dimethylethyl)dimethylsilyl]oxy]ethyl]-8-hydroxy](/data/attachment/201706/07/e0e9b5769a45af836d70be4140043125.gif.thumb.jpg "2(1H)-Quinolinone,5-[(1R)-2-amino-1-[[(1,1-dimethylethyl)dimethylsilyl]oxy]ethyl]-8-hydroxy")
![2-{[3-(4-Fluorophenyl)-4-oxo-3,4,6,7-tetrahydrothieno[3,2-d]pyrim idin-2-yl]sulfanyl}-N-(6-methyl-1,3-benzothiazol-2-yl)acetamide](/data/attachment/201706/07/5754ee36bdfbf4148f45632422f563b9.jpg "2-{[3-(4-Fluorophenyl)-4-oxo-3,4,6,7-tetrahydrothieno[3,2-d]pyrim idin-2-yl]sulfanyl}-N-(6-methyl-1,3-benzothiazol-2-yl)acetamide")
![2-((3-(2-methoxyphenyl)-4-oxo-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)-N-(6-methylbenzo[d]thiazol-2-yl)acetamide](/data/attachment/201706/08/47a8b3c98aef0b9ba378c4b7c6cef435.jpg "2-((3-(2-methoxyphenyl)-4-oxo-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)-N-(6-methylbenzo[d]thiazol-2-yl)acetamide")
![N-(6-Methyl-2-benzothiazolyl)-2-[(3,4,6,7-tetrahydro-4-oxo-3-phenylthieno[3,2-d]pyrimidin-2-yl)thio]-acetamide](/data/attachment/201706/08/beda6f8f4655aa74d3646cfc7621fb20.jpg "N-(6-Methyl-2-benzothiazolyl)-2-[(3,4,6,7-tetrahydro-4-oxo-3-phenylthieno[3,2-d]pyrimidin-2-yl)thio]-acetamide")
![4(3H)-Quinazolinone,7-bromo-6-chloro-3-[3-(3-hydroxy-2-piperidinyl)-2-oxopropyl]](/data/attachment/201706/09/b600ffca12695094db2c5f6045cb6685.jpg "4(3H)-Quinazolinone,7-bromo-6-chloro-3-[3-(3-hydroxy-2-piperidinyl)-2-oxopropyl]")
![9-OXO-1,2,3,9-TETRAHYDRO-PYRROLO[2,1-B]QUINAZOLINE-6-CARBOXYLIC ACID](/data/attachment/201706/09/d6b395bbfb23e628be7d536d9cc2b512.gif "9-OXO-1,2,3,9-TETRAHYDRO-PYRROLO[2,1-B]QUINAZOLINE-6-CARBOXYLIC ACID")
![2-Butenoic acid, 2-hydroxy-4-[5-(1-Methylethyl)-2,4-bis(phenylMethoxy)phenyl]-4-oxo-, ethyl ester](/data/attachment/201706/09/11c6e17ba89840528c5461ae5350df33.gif "2-Butenoic acid, 2-hydroxy-4-[5-(1-Methylethyl)-2,4-bis(phenylMethoxy)phenyl]-4-oxo-, ethyl ester")
methanone](/data/attachment/201706/09/ca947be16560699c92609cd96b352c02.png.thumb.jpg "[4-amino-2-(ethylsulfanyl)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone")
![Benzenesulfonamide, 2-[(5-bromo-2-chloro-4-pyrimidinyl)amino]-N-methyl](/data/attachment/201706/10/ce0d621896c03bdb67e3b184103e84ff.png.thumb.jpg "Benzenesulfonamide, 2-[(5-bromo-2-chloro-4-pyrimidinyl)amino]-N-methyl")
![1,2,3,4-Tetrahydro-benzo[b]azepin-5-one 1127-74-8](/data/attachment/201901/28/b183df1e648eca4396ad0d319a1254bc.jpg "1,2,3,4-Tetrahydro-benzo[b]azepin-5-one 1127-74-8")
1127-74-8,1,2,3,4-Tetrahydro-benzo[b]azepin-5-one
Read More
4038-14-6,(3,4-dimethoxyphenyl)-phenylmethanone
Read More
![3-Ethynylimidazo[1,2-a]pyridine 943320-53-4](/data/attachment/201901/28/d6294d1dabcee85ee04792b0c0e255c0.jpg "3-Ethynylimidazo[1,2-a]pyridine 943320-53-4")
![2-[3-(trifluoromethyl)phenyl]acetonitrile 2338-76-3](/data/attachment/201901/29/22b99245cb0bbcd2d86f238725d9fb9d.jpg "2-[3-(trifluoromethyl)phenyl]acetonitrile 2338-76-3")
2338-76-3,2-[3-(trifluoromethyl)phenyl]acetonitrile
Read More![2-[3-(trifluoromethyl)phenyl]acetic acid 351-35-9](/data/attachment/201901/29/7dbc74a276a4c124b9460222442fd80f.jpg "2-[3-(trifluoromethyl)phenyl]acetic acid 351-35-9")
351-35-9,2-[3-(trifluoromethyl)phenyl]acetic acid
Read More
2997-92-4,2,2'-Azobis(2-methylpropionamidine) dihydrochloride
Read More
95585-78-7,L-Phenylalanine, 1-methylethyl ester, hydrochloride
Read More
20324-87-2,Disodium 7,7'-(carbonyldiimino)bis(4-hydroxynaphthalene-2-sulphonate)
Read More
182498-32-4,1-(2-bromophenyl)-3-(2-hydroxy-4-nitrophenyl)urea
Read More
![(4-nitrophenyl) 4-[bis(1,3-benzodioxol-5-yl)-hydroxymethyl]piperidine-1-carboxylate 1101854-58-3](/data/attachment/201903/22/9e81dae7e0bdec56ac6052b1872d9626.jpg "(4-nitrophenyl) 4-[bis(1,3-benzodioxol-5-yl)-hydroxymethyl]piperidine-1-carboxylate 1101854-58-3")
1101854-58-3,(4-nitrophenyl) 4-[bis(1,3-benzodioxol-5-yl)-hydroxymethyl]piperidine-1-carboxylate
Read More
170565-89-6,N,N-dimethyl-2-oxo-1,3-dihydroindole-5-sulfonamide
Read More![5,6,11,12-tetrahydrodibenzo[1,2-b:1,2-g][8]annulene 1460-59-9](/data/attachment/201903/23/50930df6d55412ac8f4da0724b497aaf.jpg "5,6,11,12-tetrahydrodibenzo[1,2-b:1,2-g][8]annulene 1460-59-9")
1460-59-9,5,6,11,12-tetrahydrodibenzo[1,2-b:1',2'-g][8]annulene
Read More
![2-chloro-6-[(2R)-2-hydroxy-3-[(2-methyl-1-naphthalen-2-ylpropan-2-yl)amino]propoxy]benzonitrile 284035-33-2](/data/attachment/201903/23/7e63bafe6c4b7e146e00c57dfca99672.jpg "2-chloro-6-[(2R)-2-hydroxy-3-[(2-methyl-1-naphthalen-2-ylpropan-2-yl)amino]propoxy]benzonitrile 284035-33-2")
284035-33-2,2-chloro-6-[(2R)-2-hydroxy-3-[(2-methyl-1-naphthalen-2-ylpropan-2-yl)amino]propoxy]benzonitrile
Read More
![N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-2-methyl-1-oxo-1,2-dihydroisoquinoline-4-carboxamide 440662-09-9](/data/attachment/201903/23/e26baac537719657acd9f1f55568401d.jpg "N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-2-methyl-1-oxo-1,2-dihydroisoquinoline-4-carboxamide 440662-09-9")
440662-09-9,N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-2-methyl-1-oxo-1,2-dihydroisoquinoline-4-carboxamide
Read More![N-[2-[2-(4-chlorophenyl)-1,3-thiazol-4-yl]ethyl]butanamide 932986-18-0](/data/attachment/201903/23/7d2bbd100c8322ae16168937617e1bb2.jpg "N-[2-[2-(4-chlorophenyl)-1,3-thiazol-4-yl]ethyl]butanamide 932986-18-0")
932986-18-0,N-[2-[2-(4-chlorophenyl)-1,3-thiazol-4-yl]ethyl]butanamide
Read More
1234015-52-1,5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2-carbonitrile
Read More![3-Methyl-3-[(1E)-2-phenylethenyl]-3,2:5,2:5,3-quaterpyridine 1651890-44-6](/data/attachment/201903/23/07bf6fd99e81033df0c83039ccdde036.jpg "3-Methyl-3-[(1E)-2-phenylethenyl]-3,2:5,2:5,3-quaterpyridine 1651890-44-6")
1651890-44-6,3'-Methyl-3''-[(1E)-2-phenylethenyl]-3,2':5',2'':5'',3'''-quaterpyridine
Read More![3-[4-(Dimethylamino)-3-biphenylyl]-1,1-dimethylure 1469924-27-3](/data/attachment/201903/23/f69ad7342d131146640e0c88f73e9a25.jpg "3-[4-(Dimethylamino)-3-biphenylyl]-1,1-dimethylure 1469924-27-3")
1469924-27-3,3-[4'-(Dimethylamino)-3-biphenylyl]-1,1-dimethylure
Read More
3897-94-7,8-Methoxy-N,N-dipropyl-1,2,3,4-tetrahydro-2-naphthalenamine
Read More![4-{4-[(4-{[3-(Acryloylamino)phenyl]amino}-5-fluoro-2-pyrimidinyl) amino]phenoxy}-N-methyl-2-pyridinecarboxamide 1202759-32-7](/data/attachment/201903/23/bb4110673d0676f81860d708092eb660.jpg "4-{4-[(4-{[3-(Acryloylamino)phenyl]amino}-5-fluoro-2-pyrimidinyl) amino]phenoxy}-N-methyl-2-pyridinecarboxamide 1202759-32-7")
1202759-32-7,4-{4-[(4-{[3-(Acryloylamino)phenyl]amino}-5-fluoro-2-pyrimidinyl) amino]phenoxy}-N-methyl-2-pyridinecarboxamide
Read More
71145-03-4,1,4-Dihydro-2,6-dimethyl-3-nitro-4-(2-trifluoromethylphenyl)-pyridine-5-carboxylic acid methyl ester
Read More![2-[[3-[[2-(dimethylamino)phenyl]methyl]-2-pyridin-4-yl-1,3-diazinan-1-yl]methyl]-N,N-dimethylaniline 500579-04-4](/data/attachment/201903/23/b396a2326dddb511aae497b01fbd4c77.jpg "2-[[3-[[2-(dimethylamino)phenyl]methyl]-2-pyridin-4-yl-1,3-diazinan-1-yl]methyl]-N,N-dimethylaniline 500579-04-4")
500579-04-4,2-[[3-[[2-(dimethylamino)phenyl]methyl]-2-pyridin-4-yl-1,3-diazinan-1-yl]methyl]-N,N-dimethylaniline
Read More
1443437-74-8,N-(4-chlorophenyl)-1-(3-(furan-2-yl)benzoyl)piperidine-3-carboxamide
Read More
1125-29-7 1,3,5-Trimethyl-1H-pyrazole-4-carboxylic acid
Read More
![[2-(aminocarbonyl)phenyl]acetic acid 23362-56-3](/data/attachment/202211/10/9756043560e11c17cf958f3ed54d541a.png.thumb.jpg "[2-(aminocarbonyl)phenyl]acetic acid 23362-56-3")
23362-56-3 [2-(aminocarbonyl)phenyl]acetic acid
Read More
103788-65-4 2-(5-Methyl-2-phenyl-1,3-oxazol-4-yl)ethan-1-ol
Read More
120503-69-7 2-Amino-6-cyclopropylamino-9H-purine
Read More
Deutsche
Español
français
italiano
português
日本語
한국어
العربية
русский
bahasa Indonesia
Tiếng Việt
Send Email
Skype
3391543003
+86 15195055733
