Regorafenib for cancer

Expert Opinion on Investigational Drugs
Dirk Strumberg, Beate Schultheis

Abstract

Regorafenib (BAY 73-4506) is a novel, orally active, diphenylurea multikinase inhibitor of VEGFR1-3, c-KIT, TIE-2, PDGFR-β, FGFR-1, RET, RAF-1, BRAF and p38 MAP kinase. This review covers the preclinical development of regorafenib as well as the pivotal Phase I studies. The safety profile of regorafenib is discussed in context with other oral multikinase inhibitors bearing a similar target profile. Current clinical developments, especially in colorectal cancer (CRC) and gastrointestinal stromal tumor (GIST), are addressed. Open questions on clinically useful biomarkers predicting response with regard to a personalized therapy strategy are also being discussed. Regorafenib (BAY 73-4506) is a novel, orally active multikinase inhibitor that is well tolerated in preclinical mouse models as well as clinically according to Phase I - III trials performed. The toxicity profile is comparable with other oral multikinase inhibitors with similar molecular targets. Regorafenib has promising antineoplastic activity in various tumor types. Two large, randomized Phase III pivotal registration studies in patients with GIST and CRC, respectively, already completed enrolment, with final results being awaited. Further extensive clinical developmen...Continue Reading

References

Jan 12, 2007·The New England Journal of Medicine·Bernard EscudierUNKNOWN TARGET Study Group
May 15, 2007·Oncogene·A S DhillonW Kolch
May 20, 2008·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Mathias BoughanimPhilippe Morice
Jul 25, 2008·The New England Journal of Medicine·Josep M LlovetUNKNOWN SHARP Investigators Study Group
Jan 20, 2009·Annals of Oncology : Official Journal of the European Society for Medical Oncology·H IzzedineJ P Spano
Apr 1, 2009·The American Journal of Medicine·Faina Gurevich, Mark A Perazella
Apr 1, 2009·Nature Reviews. Clinical Oncology·Francesco TorinoGiampietro Gasparini
Nov 18, 2009·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Merrill S KiesVassiliki Papadimitrakopoulou
Dec 17, 2009·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·Hassane IzzedineJean Charles Soria
Apr 20, 2010·Critical Reviews in Oncology/hematology·Joaquim BellmuntDavid Quinn
Oct 6, 2010·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Patrick J RobertsMark A Socinski
May 18, 2011·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Thomas J George, Helen Leather
Nov 8, 2011·Clinical Colorectal Cancer·Edward Chu
Jan 24, 2012·Expert Opinion on Pharmacotherapy·Dirk Strumberg
Feb 15, 2012·Nature Reviews. Clinical Oncology·James P B O'ConnorGordon C Jayson
Apr 5, 2012·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Axel Grothey, Heinz-Josef Lenz
May 10, 2012·British Journal of Cancer·D StrumbergK Mross

❮ Previous
Next ❯

Citations

May 24, 2013·Investigational New Drugs·Viswanath Reddy BelumMario E Lacouture
May 7, 2013·Targeted Oncology·Hans PrenenEric Van Cutsem
Feb 26, 2013·BioDrugs : Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy·Giuseppe AprileFrancesco Giuliani
Apr 11, 2013·Journal of Interferon & Cytokine Research : the Official Journal of the International Society for Interferon and Cytokine Research·Serge Y Fuchs
Jul 10, 2012·The Oncologist·Sabine TejparMassimiliano Mazzone
Dec 7, 2013·World Journal of Gastroenterology : WJG·Inês MarquesRamon Andrade de Mello
Oct 24, 2013·European Journal of Clinical Pharmacology·Zexing WangXiaoxiang Guan
Aug 21, 2013·Cancer Chemotherapy and Pharmacology·Rosalba D'AlessandroBrian I Carr
Jun 19, 2013·Expert Opinion on Drug Discovery·Joshua C Curtin
Jun 26, 2015·Expert Opinion on Investigational Drugs·Oliver Waidmann, Jörg Trojan
Jun 5, 2014·Expert Opinion on Drug Discovery·Koh MiuraTsuneaki Fujiya
Oct 18, 2015·Neoplasia : an International Journal for Oncology Research·Li-Ching FanKuen-Feng Chen
Apr 6, 2016·Acta Crystallographica. Section C, Structural Chemistry·Meng Ying SunXiu Rong Hu
Dec 7, 2013·Cancer Biology & Therapy·Paul Dent
Mar 19, 2014·Bioorganic & Medicinal Chemistry·Hong X DingChristopher J O'Donnell
Jun 12, 2016·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·Cristina MirantesXavier Dolcet
Jun 6, 2017·Expert Review of Anticancer Therapy·Lorenza RimassaArmando Santoro
Jan 10, 2018·British Journal of Clinical Pharmacology·Torsten ZimmermannFrank Donath
May 31, 2016·Therapeutic Advances in Medical Oncology·Helena VerdaguerTeresa Macarulla
Aug 12, 2014·World Journal of Gastroenterology : WJG·Valentina GrossiCristiano Simone
Oct 15, 2019·Expert Opinion on Biological Therapy·Teresa MacarullaJosep Tabernero
Nov 16, 2017·Oncotarget·Bin Zhao, Hong Zhao
Nov 25, 2016·Frontiers in Pharmacology·Massimiliano BerrettaRaffaele Di Francia
Apr 10, 2019·Experimental Biology and Medicine·Ajaikumar B KunnumakkaraBharat B Aggarwal
Aug 5, 2020·Chemical Communications : Chem Comm·Patrick RoserMalte Drescher
Apr 26, 2014·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Dongshi ChenLin Zhang
Apr 20, 2014·Molecular Cancer Therapeutics·Annett MadererMarkus Moehler
Sep 25, 2014·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Wei-Tien TaiKuen-Feng Chen
Mar 8, 2013·Cancer Research·Damien GeraldLaura E Benjamin
Dec 31, 2020·Expert Opinion on Investigational Drugs·Ibrahim Halil SahinRichard Kim
Feb 14, 2020·International Journal of Radiation Biology·Meghna MehtaAnupama Munshi
Dec 7, 2015·Cardio-Oncology·Yishay WasserstrumZaza Iakobishvili

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.