Regorafenib

Regorafenib
Clinical data
Trade names	Stivarga, Regonix
Other names	BAY 73-4506
AHFS/Drugs.com	Monograph
MedlinePlus	a613004
License data	US DailyMed: Regorafenib;
Pregnancy; category	AU: D; ;
Routes of; administration	By mouth
ATC code	L01EX05 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; UK: POM (Prescription only); US: WARNINGRx-only; EU: Rx-only;
Pharmacokinetic data
Bioavailability	69-83%
Protein binding	99.5%
Metabolism	Liver (UGT1A9-mediated)
Elimination half-life	20-30 hours
Excretion	Feces (71%), urine (19%)
Identifiers
	IUPAC name 4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide hydrate;
CAS Number	755037-03-7;
PubChem CID	11167602;
DrugBank	DB08896;
ChemSpider	9342697;
UNII	24T2A1DOYB;
KEGG	D10138;
ChEBI	CHEBI:68647;
ChEMBL	ChEMBL1946170;
CompTox Dashboard (EPA)	DTXSID60226441 ;
ECHA InfoCard	100.248.939
Chemical and physical data
Formula	C21H15ClF4N4O3
Molar mass	482.82 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CNC(=O)c1cc(ccn1)Oc2ccc(c(c2)F)NC(=O)Nc3ccc(c(c3)C(F)(F)F)Cl;
	InChI InChI=1S/C21H15ClF4N4O3/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26/h2-10H,1H3,(H,27,31)(H2,29,30,32); Key:FNHKPVJBJVTLMP-UHFFFAOYSA-N;

Regorafenib, sold under the brand name Stivarga among others, is an oral multi-kinase inhibitor developed by Bayer which targets angiogenic, stromal and oncogenic receptor tyrosine kinase (RTK). Regorafenib shows anti-angiogenic activity due to its dual targeted VEGFR2-TIE2 tyrosine kinase inhibition. Since 2009 it was studied as a potential treatment option in multiple tumor types.^[3] By 2015 it had two US approvals for advanced cancers.

^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved October 22, 2023.
^ "Stivarga EPAR". European Medicines Agency (EMA). August 26, 2013. Archived from the original on March 6, 2021. Retrieved August 30, 2024.
^ "Bayer Announces New Data on Oncology Portfolio To Be Presented at the ECCO-ESMO Congress 2009". Archived from the original on July 11, 2010. Retrieved September 19, 2009.

[FDA-AllBoxedWarnings-1] "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved October 22, 2023.

[Stivarga_EPAR-2] "Stivarga EPAR". European Medicines Agency (EMA). August 26, 2013. Archived from the original on March 6, 2021. Retrieved August 30, 2024.

[3] "Bayer Announces New Data on Oncology Portfolio To Be Presented at the ECCO-ESMO Congress 2009". Archived from the original on July 11, 2010. Retrieved September 19, 2009.

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