Products Upadacitinib was approved in the US and EU in 2019 and in many countries in 2020 in extended-release tablet form (Rinvoq sustained-release tablets). Structure and properties Upadacitinib (C17H19F3N6O, Mr = 380.4 g/mol) exists in the drug as a hemihydrate. Effects Upadacitinib has selective immunosuppressive and anti-inflammatory properties. The effects are due to selective and … Upadacitinib
Products Nintedanib was approved in many countries in 2015 in soft capsule form (Ofev). Structure and properties Nintedanib (C31H33N5O4, Mr = 539.6 g/mol) is present in the drug as nintedanibesilate, a light yellow powder. Effects Nintedanib (ATC L01XE31) has antiproliferative and antitumor properties. It inhibits intracellular signaling pathways responsible for fibroblast proliferation, migration, and transformation. … Nintedanib
Products Vemurafenib was approved in 2011 in film-coated tablet form (Zelboraf). Structure and properties Vemurafenib (C23H18ClF2N3O3S, Mr = 489.9 g/mol) is a white, crystalline substance that is practically insoluble in water. Effects Vemurafenib (ATC L01XE15) has antitumor and antiproliferative properties. It reduces mortality and increases survival. The properties are based on inhibition of the mutant … Vemurafenib
Products Palbociclib was approved in capsule form in the United States in 2015, in the EU in 2016, and in many countries in 2017 (Ibrance). Structure and properties Palbociclib (C24H29N7O2, Mr = 447.5 g/mol) is a pyridopyrimidine and exists as a yellow to orange powder. Effects Palbociclib (ATC L01XE33) has antitumor and antiproliferative properties. The … Palbociclib
Products Entrectinib was approved in capsule form in the United States in 2019 and in the EU and Switzerland in 2020 (Rozlytrek). Structure and properties Entrectinib (C31H34F2N6O2, Mr = 560.6 g/mol) exists as a white to faint pink powder. Effects Entrectinib (ATC L01XE56) has antitumor, antiproliferative, and proapoptotic properties. The effects are due to inhibition … Entrectinib
Products Lorlatinib 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 (Lorviqua, or Lorbrena in the United States). Structure and properties Lorlatinib (C21H19FN6O2, Mr = 406.4 g/mol) exists as a white powder. Effects Lorlatinib (ATC L01XE44) has antitumor and … Lorlatinib
Products Ruxolitinib was approved in tablet form in the United States in 2011 and in the EU and Switzerland in 2012 (Jakavi). Structure and properties Ruxolitinib (C17H21N6O4P, Mr = 404.4 g/mol) is present in drugs as ruxolitinib phosphate, a white to light pink powder that is soluble in water. It is a pyrrolopyrimidine pyrazole derivative … Ruxolitinib
Products Bosutinib is commercially available in the form of film-coated tablets (Bosulif). The drug was approved in many countries in 2014. Structure and properties Bosutinib (C26H29Cl2N5O3, Mr = 530.4 g/mol) is a quinoline and piperazine derivative. It is present in drugs as bosutinib monohydrate, a white to yellowish powder that is sparingly soluble in water. … Bosutinib
Products Dabrafenib was approved in the US and EU in 2013 and in many countries in 2014 in hard capsule form (Tafinlar). Structure and properties Dabrafenib (C23H20F3N5O2S2, Mr = 519.6 g/mol) is present in drugs as dabrafenib mesilate, a white to slightly colored powder that is practically insoluble in water. It is a thiazole and … Dabrafenib
Products Midostaurin was approved in many countries, in the EU and in the US in 2017 in the form of soft capsules (Rydapt). Structure and properties Midostaurin (C35H30N4O4, Mr = 570.6 g/mol) is a -benzoyl derivative of staurosporine, an alkaloid isolated from the bacterium. The two active metabolites CGP62221 and CGP52421 are involved in the … Midostaurin
Products Erlotinib is commercially available in the form of film-coated tablets (Tarceva). It has been approved in many countries since 2005. Generic versions were registered in 2018. Structure and properties Erlotinib (C22H23N3O4, Mr = 393.4 g/mol) is present in drugs as erlotinib hydrochloride, a white powder that is sparingly soluble in water. Solubility increases with … Erlotinib
Products Ceritinib is commercially available in capsule form (Zykadia). It was approved in the United States in 2014 and in the EU and many countries in 2015. In 2020, film-coated tablets were registered. Structure and properties Ceritinib (C28H36N5O3ClS, Mr = 558.14 g/mol) exists as a white to slightly yellow or slightly brown powder. Effects Ceritinib … Ceritinib
