Fedratinib

Products Fedratinib was approved in the United States in 2019 in capsule form (Inrebic). Structure and properties Fedratinib is present in the drug as dihydrochloride and monohydrate (fedratinib dihydrochloride monohydrate). Effects Fedratinib has antiproliferative properties. The effects are due to selective inhibition of Janus kinases 2 (JAK2). These are intracellular enzymes that belong to the … Fedratinib

Cabozantinib

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

Pazopanib

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

Nilotinib

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

Vandetanib

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

Vatalanib

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

Tofacitinib

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

Lenvatinib

Products Lenvatinib was approved in many countries in 2015 in capsule form (Lenvima). In 2017, Kisplyx capsules were also approved. Structure and properties Lenvatinib (C21H19ClN4O4, Mr = 426.9 g/mol) is present in the drug as lenvatinib mesilate, a white to pale reddish-yellow powder that is sparingly soluble in water. It is a quinoline and carboxamide … Lenvatinib

Pancreatic Cancer Causes and Treatment

Symptoms Symptoms of pancreatic cancer include: Jaundice, light-colored stools, dark urine, and itching due to narrowing of the bile duct (cholestasis) Upper abdominal pain, tumor pain Indigestion, lack of appetite, weight loss, muscle wasting, feeling full, nausea, vomiting, diarrhea. Fatigue, weakness Inflammation of the pancreas, dysglycemia. Thrombosis In addition, there are the adverse effects of … Pancreatic Cancer Causes and Treatment

Kinase Inhibitors

Background Kinases (phosphotransferases) are a large family of enzymes involved in the transduction and amplification of signals on and in cells. They exert their effects by phosphorylating their substrates, that is, by adding a phosphate group to the molecules (Figure). Kinases have complicated names that are usually abbreviated: ALK, AXL, BCR-ABL, c-Kit, c-Met, ERBB, EGFR, … Kinase Inhibitors

Gilteritinib

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

Dacomitinib

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