Drug · Small Molecule

Regorafenib

CI-DRUG-00000512Explore in graph →NCIt C184955 CHEMBL1946170 CIViC Approved

Regulatory

Approvals (7)

Each record names the authority, jurisdiction, indication text and status. A drug approved in one jurisdiction for one indication is not 'approved' in general.

emaRegulatory1 approval record · authority, jurisdiction and indication text as published.

Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
EU EMA	—	Stivarga is indicated as monotherapy for the treatment of adult patients with: metastatic colorectal cancer (CRC) who have been previously treated with, or are not considered candidates for, available therapies - these include fluoropyrimidine-based chemotherapy, an anti-VEGF therapy and an anti-EGFR therapy; unresectable or metastatic gastrointestinal stromal tumors (GIST) who progressed on or are intolerant to prior treatment with imatinib and sunitinib; hepatocellular carcinoma (HCC) who have been previously treated with sorafenib.

Derived

Development pipeline

Most advanced stage across all cancers, then per top-level cancer reached through trial conditions or approval indications. Approval in any ingested jurisdiction outranks trial phase; counts are interventional studies.

Scope	Stage	Max phase	Active	Recruiting	Phase 3	Trials	Approvals	Jurisdictions	First approval	First trial
All cancers	Approved	Phase 4	56	28	30	215	7	CA, EU, US	Sep 27, 2012	Apr 30, 2008
Malignant Liver Neoplasm	Approved	Phase 3	10	4	3	24	1	US	Sep 27, 2012	May 14, 2013
Malignant Central Nervous System Neoplasm	Phase3	Phase 3	3	3	1	6	0	—	—	2015-11
Malignant Lung Neoplasm	Phase2	Phase 2	2	1	0	4

Curated evidence

Clinical evidence (19)

CIViC items in which this therapy appears, grouped by cancer context, then molecular profile. 50 items per page.

civicCuratedShowing 1–19 of 19 evidence items · levels, directions and significance as curated at the source; each row links to its CIViC record.

Therapy	Cancer	Type	Level	Direction · significance	Rating (1–5)	Status	Evidence	Source
BRAF Kinase Domain Duplication1
Regorafenib

Clinical trials

Trials with this intervention (244)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 1–50 of 244 studies · status and phase as posted by the registrant; each row links to the study record.

NCT	Title	Status	Phase	Enrollment (n)	Sponsor	Countries	Last update	Source
NCT06047379	Safety and Efficacy of NEO212 in Patients With Astrocytoma IDH-mutant, Glioblastoma IDH-wildtype or Brain Metastasis	recruiting	Phase 1 / Phase 2	134	Neonc Technologies, Inc.INDUSTRY	1	Sep 24, 2026	clinicaltrials
NCT06246643	A Study of Continued Treatment With Regorafenib in Participants With Solid Tumors Who Have Participated in Other Bayer Studies	active not recruiting

Molecule

Record

Kind: Small Molecule
Mechanism: Tyrosine-protein kinase ABL inhibitor; Serine/threonine-protein kinase RAF inhibitor; Stem cell growth factor receptor inhibitor; Fibroblast growth factor receptor 1 inhibitor; MAP kinase p38 beta inhibitor; Fibroblast growth factor receptor 2 inhibitor; Tyrosine-protein kinase FRK inhibitor; Discoidin domain-containing receptor 2 inhibitor; Serine/threonine-protein kinase B-raf inhibitor; Tyrosine-protein kinase TIE-2 inhibitor; Platelet-derived growth factor receptor inhibitor; Vascular endothelial growth factor receptor inhibitor; Tyrosine-protein kinase receptor RET inhibitor; Ephrin type-A receptor 2 inhibitor; Nerve growth factor receptor Trk-A inhibitor
Targets: 18 genes
UNII: MGN125FS9D
Aliases: 2-Pyridinecarboxamide, 4-(4-((((4-Chloro-3-(Trifluoromethyl)Phenyl)Amino)Carbonyl)Amino)-3-Fluorophenoxy)-N-Methyl-, Hydrate (1:1), 4-(4-(((4-chloro-3-(trifluoromethyl)phenyl)carbamoyl)amino)-3-fluorophenoxy)-N-methylpyridine-2-carboxamide, BAY 73-4506, BAY-734506, BAY 73-4506 monohydrate, BAY 73-4506 Monohydrate, BAY-734506 MONOHYDRATE, Regorafenib, REGORAFENIB, Regorafenib anhydrous, Regorafenib hydrate, Regorafenib Monohydrate, Stivarga, STIVARGA

Data updated 21 hours agoSource updated unknown

Identifiers

Codes (4)

Upstream identifiers kept as first-class codes; each links to its registry where a stable public URL exists.

System	Code	Label
ATC (WHO)

KIT A502_Y503dup1
Imatinib + Ponatinib + RegorafenibSubstitutes	Gastrointestinal Stromal Tumor	Predictive	D	Does Not Support Sensitivity Response	3	accepted	EID4630 In an in vitro study, an IL-3-independent Ba/F3 cell line expressing the KIT exon 9 A502_Y503dup primary activating mutation demonstrated reduced sensitivity to regorafenib (IC50: 138 nmol/L), imatini… (full text at CIViC) PMID 25239608 · Garner et al., 2014 · Open in CIViC	civic

KIT A502_Y503dup1

Imatinib + Ponatinib + RegorafenibSubstitutes

Gastrointestinal Stromal Tumor

Predictive

Does Not Support Sensitivity Response

accepted

EID4630

In an in vitro study, an IL-3-independent Ba/F3 cell line expressing the KIT exon 9 A502_Y503dup primary activating mutation demonstrated reduced sensitivity to regorafenib (IC50: 138 nmol/L), imatini… (full text at CIViC)

PMID 25239608 · Garner et al., 2014 · Open in CIViC