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 201–244 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
NCT02106845	Effect of Regorafenib on Digoxin and Rosuvastatin in Patients With Advanced Solid Malignant Tumors.	completed	Phase 1	42	BayerINDUSTRY	2	Jun 7, 2019	clinicaltrials
NCT01538680	Regorafenib in Subjects With Metastatic Colorectal Cancer (CRC) Who Have Progressed After Standard Therapy(CONSIGN)	no longer available

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 19 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