Regorafenib

Regorafenib

Clinical data
Trade names	Stivarga
Synonyms	BAY 73-4506
[[Regulation of therapeutic goods |Template:Engvar data]]	US FDA: Regorafenib
Pregnancy category	US: D (Evidence of risk)
Routes of administration	Oral
Legal status
Legal status	US: ℞-only
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
ChemSpider	28295228
KEGG	D10138
ChEMBL	ChEMBL1946170
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C21H17ClF4N4O4
Molar mass	482.82 g mol
3D model (JSmol)	Interactive image
SMILES CNC(=O)c1cc(ccn1)Oc2ccc(c(c2)F)NC(=O)Nc3ccc(c(c3)C(F)(F)F)Cl.O
InChI InChI=1S/C21H15ClF4N4O3.H2O/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);1H2 Key:ZOPOQLDXFHBOIH-UHFFFAOYSA-N

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Evidence Based Medicine
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Clinical Trials
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Definitions
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Continuing Medical Education (CME)
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International
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Experimental / Informatics
List of terms related to Regorafenib

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Regorafenib (BAY 73-4506, commercial name Stivarga) 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. It is currently being studied as a potential treatment option in multiple tumor types.

Regorafenib demonstrated to increase the overall survival of patients with metastatic colorectal cancer and has been approved by the Food and Drug Administration on September 27, 2012.

Stivarga is being approved with a Boxed Warning alerting patients and health care professionals that severe and fatal liver toxicity occurred in patients treated with Stivarga during clinical studies. The most common side effects reported in patients treated with Stivarga include weakness or fatigue, loss of appetite, hand-foot syndrome (also called palmar-plantar erythrodysesthesia), diarrhea, mouth sores (mucositis), weight loss, infection, high blood pressure, and changes in voice volume or quality (dysphonia).