Products Cabozantinib is commercially available in the form of film-coated tablets (Cabometyx). It was approved in the United States in 2012, in the EU in 2013, and in many countries in 2017. In some countries, Cometriq capsules are additionally on the market for the treatment of medullary thyroid carcinoma. This article relates to renal cell … Cabozantinib
Products Pazopanib is commercially available in the form of film-coated tablets (Votrient). It was approved in the EU and many countries in 2010. Structure and properties Pazopanib (C21H23N7O2S, Mr = 437.52 g/mol) exists in drugs as pazopanib hydrochloride, a white to yellowish solid that is sparingly soluble in water at pH 1 and practically insoluble … Pazopanib
Products Nilotinib is commercially available in capsule form (Tasigna). It has been approved in many countries since 2007. Structure and properties Nilotinib (C28H22F3N7O, Mr = 529.5 g/mol) is present in the drug product as nilotinib hydrochloride monohydrate, a white to slightly yellowish or greenish-yellow powder. The aminopyrimidine is structurally closely related to its precursor imatinib … Nilotinib
Products Tofacitinib was approved in the United States in November 2012, in many countries in 2013, and in the EU in 2017 in film-coated tablet form (Xeljanz). The European Medicines Agency initially rejected the approval in April 2013. However, baricitinib was approved. In the United States, additional sustained-release film-coated tablets are available that are taken … Tofacitinib
Products Vandetanib is commercially available in the form of film-coated tablets (Caprelsa). It was approved in the EU in 2011. It was registered in many countries in May 2012. Structure and properties Vandetanib (C22H24BrFN4O2, Mr = 475.4 g/mol) is a quinazolinamine and piperidine derivative that is practically insoluble in water. Effects Vandetanib (ATC L01XE12) is … Vandetanib
Products Vatalanib is in the development phase and is not yet commercially available. Structure and properties Vatalanib (C20H15ClN4, Mr = 346.8 g/mol) is a chlorinated pyridine and aminophthalazine derivative. In pharmaceuticals, it is present as vatalanib succinate. Effects Vatalanib has antiangiogenic, antitumor, and antiproliferative properties. The effects are based on inhibition of all known VEGF … Vatalanib
Products Gilteritinib was approved in the form of film-coated tablets in the United States in 2018, in the EU in 2019, and in many countries in 2020 (Xospata). Structure and properties Gilteritinib (C29H44N8O3, Mr = 552.7 g/mol) is present in the drug as gilteritinib fumarate, a light yellow to yellow powder or crystals that are … Gilteritinib
Products Dacomitinib was approved in the US in 2018 and in the EU and many countries in 2019 in film-coated tablet form (Vizimpro). Structure and properties Dacomitinib (C24H25ClFN5O2, Mr = 469.9 g/mol) is present in the drug product as dacomitinib monohydrate, a white to pale yellow powder. Effects Dacomitinib (ATC L01XE47) has antitumor and antiproliferative … Dacomitinib
Products Regorafenib is commercially available in the form of film-coated tablets (Stivarga). It was approved in many countries in February 2013. Structure and properties Regorafenib (C21H15ClF4N4O3, Mr = 482.8 g/mol) is present in drugs as regorafenib monohydrate, which is practically insoluble in water. Effects Regorafenib (ATC L01XE21) has antitumor and antiangiogenic properties. The effects are … Regorafenib
Products Janus kinase inhibitors are commercially available in the form of tablets and capsules with different galenics. Structure and properties The structure of Janus kinase inhibitors is characterized by nitrogen heterocycles, which are often condensed. Effects The agents have selective immunosuppressive, anti-inflammatory, and antiproliferative properties. The effects are based on inhibition of Janus kinases (JAK). … Janus Kinase Inhibitors
Products Neratinib was approved in the form of film-coated tablets in the United States in 2017, in the EU in 2018, and in many countries in 2020 (Nerlynx). Structure and properties Neratinib (C30H29ClN6O3, Mr = 557.1 g/mol) is present in the drug as neratinib maleate, a white to yellow powder that is water soluble, especially … Neratinib
Products Baricitinib was approved in many countries and in the EU in 2017 and in the United States in 2018 in film-coated tablet form (Olumiant). Structure and properties Baricitinib (C16H17N7O2S, Mr = 371.4 g/mol) is structurally related to adenosine triphosphate and interacts with the ATP-binding site of kinases. It is sparingly soluble in water. Effects … Baricitinib
