Regorafenib

Overview

Regorafenib is an orally-administered inhibitor of multiple kinases. It is used for the treatment of metastatic colorectal cancer, advanced gastrointestinal stromal tumours, and hepatocellular carcinoma. FDA approved on September 27, 2012. Approved use of Regorafenib was expanded to treat Hepatocellular Carcinoma in April 2017.

Indication

Regorafenib is indicated for the treatment of patients with metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy. Regorafenib is also indicated for the treatment of patients with locally advanced, unresectable or metastatic gastrointestinal stromal tumour (GIST) who have been previously treated with imatinib mesylate and sunitinib malate. Regorafenib is also indicated for the treatment of patients with hepatocellular carcinoma (HCC) previously treated with sorafenib.

Associated Conditions

Hepatocellular Carcinoma
Metastatic Colorectal Cancer (CRC)
Metastatic Gastrointestinal Stromal Tumor (GIST)
Locally advanced Gastrointestinal stromal tumor
Unresectable Gastrointestinal stromal tumor

Clinical Trials

Title	Posted	Study ID	Phase	Status	Sponsor
The Study of JMT101 Combined With Irinotecan as a ≥3rd-Line Treatment in Metastatic Colorectal Cancer	2025/08/21	NCT07134205	Not Applicable	Not yet recruiting	Shanghai JMT-Bio Inc.
Tauroursodeoxycholic Acid (TUDCA) Plus Camrelizumab and Regorafenib in Hepatocellular Carcinoma Previously Treated With Anti-PD1/PD-L1 and Bevacizumab	2025/08/03	NCT07100392	Not Applicable	Recruiting	Fudan University
Comparing the Combination of Trastuzumab and Regorafenib With Regorafenib Monotherapy for Advanced Hepatocellular Carcinoma After First-line Treatment	2025/07/22	NCT07078305	Not Applicable	Not yet recruiting	Tianjin Medical University Cancer Institute and Hospital
Efficacy And Safety Of Hydroxychloroquine Combined With Methotrexate, Capecitabine And Bevacizumab Vs. Regorafenib In Participants With Refractory Metastatic Colorectal Cancer With Mutations In RAS Genes	2025/04/29	NCT06949982	Phase 2	Recruiting	Sergey Orlov, MD
Regorafenib and Yttrium-90 Radioembolization for Unresectable Hepatocellular Carcinoma	2025/03/30	NCT06902246	Phase 2	Not yet recruiting	University of Miami
5-Fluorouracil/Leucovorin (5FU/LV) in Combination With Regorafenib in Patients With Metastatic Colorectal Cancer	2025/03/20	NCT06887218	Phase 2	Recruiting	The Methodist Hospital Research Institute
"Thymalfasin Immunotherapy Study with Triple Regimen in Advanced MSS/pMMR Colorectal Cancer"	2025/02/17	NCT06829355	Phase 2	Recruiting	Beijing Friendship Hospital
Testing a New Combination of Anti-cancer Drugs in Patients Newly Diagnosed With Ewing Sarcoma Who Have Cancer That Has Spread to Other Parts of the Body	2025/02/11	NCT06820957	Phase 2	Not yet recruiting	Children's Oncology Group
Safety and Efficacy of SYHA1813 Single Agent or in Combination With Different Regimens in Unresectable Locally Advanced or Metastatic Solid Tumors.	2024/11/11	NCT06682611	Phase 1	Not yet recruiting	Shanghai Runshi Pharmaceutical Technology Co., Ltd
Botensilimab, Balstilimab and Regorafenib or Botensilimab and Balstilimab for the Treatment of Advanced or Metastatic Microsatellite Stable Colorectal Cancer	2024/08/28	NCT06575725	Phase 2	Withdrawn	City of Hope Medical Center

FDA Drug Approvals

Approved Product	Manufacturer	NDC Code	Route	Strength	Effective Date
Stivarga	Bayer HealthCare Pharmaceuticals Inc.	50419-171	ORAL	40 mg in 1 1	12/9/2020

EMA Drug Approvals

Approved Product	Authorization Holder	Status	Issued Date
Stivarga	Bayer Pharma AG,13342 Berlin,Germany	Authorised	8/26/2013

HSA Drug Approvals

Approved Product	Manufacturer	Approval Number	Dosage Form	Strength	Approval Date
Stivarga Tablet 40mg	Bayer AG, Leverkusen	SIN14360P	TABLET, FILM COATED	40.00mg	6/7/2013

NMPA Drug Approvals

Approved Product	Company	Approval Number	Drug Type	Dosage Form	Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product	Registration No.	Company	Licence No.	Strength	Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

Approved Product	ARTG ID	Sponsor	Registration Type	Status	Registration Date
STIVARGA regorafenib 40 mg tablet bottle	200553	Bayer Australia Ltd	Medicine	A	11/29/2013

Health Canada Drug Approvals

Approved Product	Company	DIN	Dosage Form	Strength	Market Date
STIVARGA	Bayer Inc	02403390	Tablet - Oral	40 MG	4/2/2013

CIMA AEMPS Drug Approvals

Approved Product	Company	Registration Number	Pharmaceutical Form	Prescription Type	Status
STIVARGA 40 MG COMPRIMIDOS RECUBIERTOS CON PELICULA	Bayer Ag	113858002	COMPRIMIDO RECUBIERTO CON PELÍCULA	Diagnóstico Hospitalario	Commercialized

Philippines FDA Drug Approvals

Approved Product	Company	License Number	Dosage Form	Strength	Approval Date
No Philippines FDA approvals found for this drug.

Saudi SFDA Drug Approvals

Approved Product	Company	License Number	Dosage Form	Strength	Approval Date
No Saudi SFDA approvals found for this drug.

Malaysia NPRA Drug Approvals

Approved Product	Company	Registration Number	Dosage Form	Strength	Approval Date
No Malaysia NPRA approvals found for this drug.

UK EMC Drug Information

Medicine Name	MA Holder	MA Number	Pharmaceutical Form	Active Ingredient	Authorization Date
No UK EMC drug information found for this drug.

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