Tucatinib

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

Pomalidomide

Products Pomalidomide is commercially available in the form of hard capsules (Imnovid). It has been approved in many countries since 2014. It has been registered in the EU and the United States since 2013. Structure and properties Pomalidomide (C13H11N3O4, Mr = 273.2 g/mol) is an amino derivative of thalidomide and a racemate. It is also … Pomalidomide

Ponatinib

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

Imatinib

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

Alpelisib

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

Aromatase Inhibitors

Products Aromatase inhibitors are commercially available in the form of film-coated tablets and coated tablets. The first third-generation agent to be approved in many countries was anastrozole in 1996 (Arimidex, USA 1995). Other drugs are available today. The active ingredients available today all belong to the third generation. Earlier agents such as aminoglutethimide and formestane … Aromatase Inhibitors

Afatinib

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

Sacubitril

Products The fixed combination of the neprilysin inhibitor sacubitril with valsartan was approved in the United States, the EU, and many countries in 2015 in the form of film-coated tablets (Entresto). The combination is also referred to as LCZ696. Structure and properties Sacubitril (C24H29NO5, Mr = 411.5 g/mol) is an ester prodrug that is hydrolyzed … Sacubitril