regorafenib (stivarga) Report issue

Small molecule Orphan Drug FDA Approved FDA Fast Track FDA Priority Review FDA
AACT ChEMBL DrugBank Drug Central Drugs@FDA KEGG MeSH PubChem repoDB

Active Ingredient History

NOW
  • Now
Regorafenib (trade name Stivarga) is an orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. Regorafenib binds to and inhibits vascular endothelial growth factor receptors (VEGFRs) 2 and 3, and Ret, Kit, PDGFR and Raf kinases, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. VEGFRs are receptor tyrosine kinases that play important roles in tumor angiogenesis; the receptor tyrosine kinases RET, KIT, and PDGFR, and the serine/threonine-specific Raf kinase are involved in tumor cell signaling. In in vivo models, regorafenib demonstrated anti-angiogenic activity in a rat tumor model, and inhibition of tumor growth as well as anti-metastatic activity in several mouse xenograft models including some for human colorectal carcinoma. Since 2009 it was studied as a potential treatment option in multiple tumor types. Stivarga is approved by FDA to treat two different tumor types: metastatic colorectal cancer in patients 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 (approved in 2012) and to treat patients with locally advanced, unresectable or metastatic gastrointestinal stromal tumor who have been previously treated with imatinib mesylate and sunitinib malate (approved in 2013).   NCATS

Chemistry

  • SMILES: CNC(=O)C1=CC(OC2=CC=C(NC(=O)NC3=CC=C(Cl)C(=C3)C(F)(F)F)C(F)=C2)=CC=N1
  • InChIKey: FNHKPVJBJVTLMP-UHFFFAOYSA-N
  • Mol. Mass: 482.815
  • ALogP: 5.69
  • ChEMBL Molecule:
    regorafenib  
More Chemistry

Pharmacology

Alternative names

4-(4-(((4-chloro-3-(trifluoromethyl)phenyl)carbamoyl)amino)-3-fluorophenoxy)-n-methylpyridine-2-carboxamide | anhydrous regorafenib | bay 73-4506 | bay-73-4506 | bay73-4506 | bay-734506 monohydrate | regorafenib | régorafénib | regorafenib hydrate | regorafenib monohydrate | regorafenibum | stivarga

Organizations (174)

Research & Development (174)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (1)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (84)

Approved Indications (2)


 

Colorectal Neoplasms (approved 2012)

Gastrointestinal Neoplasms (approved 2012)

Experimental Indications - Clinical Trial Phases 1-4 (83)


 

Adenocarcinoma (Phase 2)

Angiogenesis Modulating Agents (Phase 2)

Bile Duct Neoplasms (Phase 2)

Biliary Tract Neoplasms (Phase 2)

Biomarkers (Phase 2)

Bone Neoplasms (Phase 1)

Brain Neoplasms (Phase 2)

Breast Neoplasms (Phase 2)

Carcinoma (Phase 1/Phase 2)

Carcinoma, Adenoid Cystic (Phase 2)

Carcinoma, Hepatocellular (Phase 3)

Carcinoma, Islet Cell (Phase 2)

Carcinoma, Merkel Cell (Phase 1/Phase 2)

Carcinoma, Non-Small-Cell Lung (Phase 2)

Carcinoma, Renal Cell (Phase 2)

Carcinoma, Squamous Cell (Phase 1/Phase 2)

Carcinoma, Transitional Cell (Phase 2)

CCR5 Receptor Antagonists (Phase 2)

Cholangiocarcinoma (Phase 2)

Chondroma (Phase 2)

Chondrosarcoma (Phase 2)

Chondrosarcoma, Mesenchymal (Phase 2)

Colonic Neoplasms (Phase 3)

Colorectal Neoplasms (Phase 4)

Dietary Fats (Phase 1)

Digestive System Neoplasms (Phase 2)

DNA Mismatch Repair (Phase 2)

Drug-Related Side Effects and Adverse Reactions (Phase 4)

Drugs, Investigational (Phase 3)

Education (Phase 4)

Esophageal Neoplasms (Phase 3)

Esophageal Squamous Cell Carcinoma (Phase 1/Phase 2)

Fallopian Tube Neoplasms (Phase 2)

Fatigue (Phase 2)

Gastrinoma (Phase 2)

Gastrointestinal Stromal Tumors (Phase 4)

Glioblastoma (Phase 2/Phase 3)

Glucagonoma (Phase 2)

Hamartoma (Phase 2)

Immune Checkpoint Inhibitors (Phase 2)

Immunotherapy (Phase 2)

Insulinoma (Phase 2)

Intestinal Neoplasms (Phase 2)

Leukemia, Myeloid, Acute (Phase 1)

Liposarcoma (Phase 2)

Liver Neoplasms (Phase 3)

Lung Neoplasms (Phase 2)

Lymphoma, Non-Hodgkin (Phase 2)

Macular Degeneration (Phase 2)

Melanoma (Phase 2)

Mesothelioma (Phase 1/Phase 2)

Mesothelioma, Malignant (Phase 2)

Microsatellite Instability (Phase 2)

Multiple Myeloma (Phase 2)

Mutation (Phase 2)

Neoplasm Metastasis (Phase 2)

Neoplasms ()

Neuroendocrine Tumors (Phase 2)

Oncogene Proteins (Phase 2)

Oncogenes (Phase 2)

Osteosarcoma (Phase 2)

Ovarian Neoplasms (Phase 2)

Palliative Care (Phase 2)

Palliative Medicine (Phase 2)

Pancreatic Neoplasms (Phase 2)

Pharmacokinetics (Phase 1)

Prostatic Neoplasms (Phase 2)

Prostatic Neoplasms, Castration-Resistant (Phase 2)

Proto-Oncogene Proteins B-raf (Phase 2)

Proto-Oncogene Proteins c-met (Phase 2)

ras Proteins (Phase 2)

Rectal Neoplasms (Phase 2)

Rhabdomyosarcoma (Phase 2)

Sarcoma (Phase 2)

Sarcoma, Ewing (Phase 2)

Small Cell Lung Carcinoma (Phase 2)

Somatostatinoma (Phase 2)

Squamous Cell Carcinoma of Head and Neck (Phase 1/Phase 2)

Stomach Neoplasms (Phase 2)

Thymoma (Phase 2)

Thyroid Neoplasms (Phase 2)

Triple Negative Breast Neoplasms (Phase 1/Phase 2)

Uterine Cervical Neoplasms (Phase 1/Phase 2)

Overview

  • Highest Phase: Phase 4
  • # of Trials: 224
  • # of Trial Organizations: 174

Trials by Phase

Trial Phase Start Date Organizations Indications

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