Products Lapatinib is commercially available in the form of film-coated tablets (Tyverb). It has been approved in many countries since 2007. Structure and properties Lapatinib (C29H26ClFN4O4S, Mr = 581.1 g/mol) is present in drugs as lapatinibditosylate monohydrate. It is a 4-aniline quinazoline that exists as a yellow powder that is sparingly soluble in water. Effects … Lapatinib
Products Larotrectinib has been approved in the United States since 2018, in the EU since 2019, and in many countries since 2020 in capsule and oral solution form (Vitrakvi). Structure and properties Larotrectinib (C21H22F2N6O2, Mr = 428.4 g/mol) is present in the drug as larotrectinib sulfate. Effects Larotrectinib (ATC L01XE53) has antitumor and antiproliferative properties. … Larotrectinib
Products Idelalisib was approved in many countries in 2015 in film-coated tablet form (Zydelig). Structure and properties Idelalisib (C22H18FN7O, Mr = 415.4 g/mol) exists as a white powder that is soluble in acidic environments. Effects Idelalisib (ATC L01XX47) has antiproliferative, selective cytotoxic, and antitumor properties. The effects are due to inhibition of phosphatidylinositol 3-kinase p110δ. … Idelalisib
Products Ribociclib was approved in the United States, the EU, and many countries in 2017 in film-coated tablet form (Kisqali). Structure and properties Ribociclib (C23H30N8O, Mr = 434.5 g/mol) is present in the drug as ribociclibsuccinate, a pale yellow to yellow-brown crystalline powder. Effects Ribociclib (ATC L01XE42) has antitumor and antiproliferative properties. The effects are … Ribociclib
Products Binimetinib was approved in the EU and US in 2018 and in many countries in 2019 in film-coated tablet form (Mektovi). Structure and properties Binimetinib (C17H15BrF2N4O3, Mr = 441.2 g/mol) exists as a light yellow powder that is practically insoluble in water. Effects Binimetinib (ATC L01XE41) has antitumor and antiproliferative properties. The effects are … Binimetinib
Products Ibrutinib is commercially available in capsule form (Imbruvica). It has been approved in many countries since 2014. Film-coated tablets were registered in 2019. Structure and properties Ibrutinib (C25H24N6O2, Mr = 440.5 g/mol) exists as a white substance that is practically insoluble in water. Effects Ibrutinib (ATC L01XE27) is a noncompetitive (irreversible) inhibitor of Bruton’s … Ibrutinib
Products Osimertinib was approved in the United States in 2015 and in the EU and Switzerland in 2016 in film-coated tablet form (Tagrisso). Structure and properties Osimertinib exists in the drug product as osimertinib mesilate (C28H33N7O2 – CH4O3S, Mr = 596 g/mol). It is a methylindole, aniline and pyrimidine derivative. Effects Osimertinib (ATC L01XE35) has … Osimertinib
Products Tucatinib was approved in the United States and many countries in 2020 in film-coated tablet form (Tukysa). Structure and properties Tucatinib (C26H24N8O2, Mr = 480.5 g/mol) Effects Tucatinib has antitumor and antiproliferative properties. The effects are due to inhibition of HER2 tyrosine kinase. The half-life is approximately 8.5 hours. Indications In combination with trastuzumab … Tucatinib
Products Ponatinib is commercially available in film-coated tablet form (Iclusig). It was approved in the EU in 2013 and in many countries in 2014. Structure and properties Ponatinib (C29H27F3N6O, Mr = 532.6 g/mol) is present in the drug as ponatinib hydrochloride, a white to yellow powder whose water solubility decreases with increasing pH. It is … Ponatinib
Products Alpelisib was approved in the United States in 2019 and in many countries in 2020 in film-coated tablet form (Piqray). Structure and properties Alpelisib (C19H22F3N5O2S, Mr = 441.5 g/mol) exists as a white powder. Effects Alpelisib (ATC L01XX65) has antiproliferative and antitumor properties. The effects are due to inhibition of the α-subunit of phosphatidylinositol … Alpelisib
Products Imatinib is commercially available in the form of film-coated tablets (Gleevec, Gleevec GIST, generic). It has been approved in many countries since 2001. Generics came on the market in 2016. They were not approved for the treatment of gastrointestinal stromal tumors (GIST) because this indication was still protected by a patent. In 2017, imatinib … Imatinib
Products Afatinib was approved in the US and EU in 2013 and in many countries in 2014 in film-coated tablet form (Giotrif). Structure and properties Afatinib (C24H25ClFN5O3, Mr = 485.9 g/mol) is a 4-aniline quinazoline derivative that is present in drugs as afatinib dimaleate, a white to brownish-yellow powder that is soluble in water. It … Afatinib
