DONAFENIB

Donafenib
Clinical data
Trade names	Zepsun
Other names	CM-4307
Legal status
Legal status	Rx in China;
Identifiers
	IUPAC name 4-[4-[[4-Chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-(trideuteriomethyl)pyridine-2-carboxamide;
CAS Number	1130115-44-4;
PubChem CID	25191001;
DrugBank	DB15414;
ChemSpider	23937167;
UNII	41XGO0VS1U;
ChEMBL	ChEMBL4297490;
CompTox Dashboard ( EPA)	DTXSID90648995 ;
Chemical and physical data
Formula	C21H16ClF3N4O3
Molar mass	464.83 g·mol−1
3D model ( JSmol)	Interactive image;
	SMILES [2H]C([2H])([2H])NC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F;
	InChI InChI=1S/C21H16ClF3N4O3/c1-26-19(30)18-11-15(8-9-27-18)32-14-5-2-12(3-6-14)28-20(31)29-13-4-7-17(22)16(10-13)21(23,24)25/h2-11H,1H3,(H,26,30)(H2,28,29,31)/i1D3; Key:MLDQJTXFUGDVEO-FIBGUPNXSA-N;

Donafenib, sold under the brand name Zepsun, is a pharmaceutical drug for the treatment of cancer.

In China, donafenib is approved for the treatment of unresectable hepatocellular carcinoma in patients who have not previously received systemic treatment.^[1]^[2]

Donafenib is a kinase inhibitor that targets Raf kinase and various receptor tyrosine kinases.^[3] It is a deuterated derivative of sorafenib with improved pharmacokinetic properties.^[4]^[5]

References

^ Keam SJ, Duggan S (November 2021). "Donafenib: First Approval". Drugs. 81 (16): 1915–1920. doi: 10.1007/s40265-021-01603-0. PMID 34591285.
^ Chen R, Ielasi L, di Carlo A, Tovoli F (February 2023). "Donafenib in hepatocellular carcinoma". Drugs of Today. 59 (2): 83–90. doi: 10.1358/dot.2023.59.2.3507751. PMID 36811408.
^ "Donafenib". NCI Cancer Dictionary. National Cancer Institute, National Institutes of Health.
^ Qin S, Bi F, Gu S, Bai Y, Chen Z, Wang Z, et al. (September 2021). "Donafenib Versus Sorafenib in First-Line Treatment of Unresectable or Metastatic Hepatocellular Carcinoma: A Randomized, Open-Label, Parallel-Controlled Phase II-III Trial". Journal of Clinical Oncology. 39 (27): 3002–3011. doi: 10.1200/JCO.21.00163. PMC 8445562. PMID 34185551.
^ Qin S, Bi F, Xu J, Du C, Fan Q, Zhang L, et al. (2020). "P-86 Comparison of the pharmacokinetics of donafenib and sorafenib in patients with advanced hepatocellular carcinoma: An open-label, randomized, parallel-controlled, multicentre phase II/III trial". Annals of Oncology. 31: S117–S118. doi: 10.1016/j.annonc.2020.04.168.

[1] Keam SJ, Duggan S (November 2021). "Donafenib: First Approval". Drugs. 81 (16): 1915–1920. doi: 10.1007/s40265-021-01603-0. PMID 34591285.

[2] Chen R, Ielasi L, di Carlo A, Tovoli F (February 2023). "Donafenib in hepatocellular carcinoma". Drugs of Today. 59 (2): 83–90. doi: 10.1358/dot.2023.59.2.3507751. PMID 36811408.

[3] "Donafenib". NCI Cancer Dictionary. National Cancer Institute, National Institutes of Health.

[4] Qin S, Bi F, Gu S, Bai Y, Chen Z, Wang Z, et al. (September 2021). "Donafenib Versus Sorafenib in First-Line Treatment of Unresectable or Metastatic Hepatocellular Carcinoma: A Randomized, Open-Label, Parallel-Controlled Phase II-III Trial". Journal of Clinical Oncology. 39 (27): 3002–3011. doi: 10.1200/JCO.21.00163. PMC 8445562. PMID 34185551.

[5] Qin S, Bi F, Xu J, Du C, Fan Q, Zhang L, et al. (2020). "P-86 Comparison of the pharmacokinetics of donafenib and sorafenib in patients with advanced hepatocellular carcinoma: An open-label, randomized, parallel-controlled, multicentre phase II/III trial". Annals of Oncology. 31: S117–S118. doi: 10.1016/j.annonc.2020.04.168.

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