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Donafenib is a Chinese redesign of sorafenib that lived longer than the original in a head-to-head liver cancer trial and is approved in China as a first-line option.
Zelgen's donafenib was approved by the NMPA in June 2021 for first-line unresectable hepatocellular carcinoma on the ZGDH3 trial (668 patients: median overall survival 12.1 versus 10.3 months with sorafenib, hazard ratio 0.83; Journal of Clinical Oncology 2021), the first drug to beat sorafenib on survival in this setting. Radioiodine-refractory differentiated thyroid cancer followed in 2022. A modest gain, but a first for a Chinese company and a model of incremental chemistry (deuteration) turned into an approval.
Deuterium-substituted analogue of sorafenib inhibiting RAF kinases and VEGFR/PDGFR; deuteration slows metabolism and raises exposure. Connects to VEGF / VEGFR and BRAF.
1.Donafenib slips into a pocket on VEGF / VEGFR.
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| Region | Year | Indication |
|---|---|---|
| China | 2021 | First-line unresectable hepatocellular carcinoma (ZGDH3) |
| China | 2022 | Radioiodine-refractory differentiated thyroid cancer |
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Query for this drug: (TITLE:"Donafenib" OR ABSTRACT:"Donafenib" OR TITLE:"Zepsun" OR ABSTRACT:"Zepsun" OR TITLE:"CM4307" OR ABSTRACT:"CM4307") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Donafenib, not a curated reading list.
Shares Shukui Qin, Hepatocellular carcinoma (KEGG map), VEGF angiogenesis, VEGF / VEGFR and the tag china.
Shares Anti-angiogenic therapy, Small-molecule kinase inhibitors and the tag china.
Shares Anti-angiogenic therapy, Hepatocellular carcinoma and the tag china.
Shares RAS / RAF / MEK / ERK (MAPK), Small-molecule kinase inhibitors and the tag china.
Shares VEGF angiogenesis, VEGF / VEGFR, Thyroid cancer, Anti-angiogenic therapy and the tag china.
Shares RAS / RAF / MEK / ERK (MAPK), Small-molecule kinase inhibitors and the tag china.
Shares RAS / RAF / MEK / ERK (MAPK), Small-molecule kinase inhibitors and the tag china.
Shares RAS / RAF / MEK / ERK (MAPK), Small-molecule kinase inhibitors and the tag china.