Axitinib

Products Axitinib was approved in many countries in 2012 in film-coated tablet form (Inlyta). Structure and properties Axitinib (C22H18N4OS, Mr = 386.5 g/mol) is a benzamide and benzindazole derivative. It exists as a white to slightly yellow powder. Effects Axitinib (ATC L01XE17) has antitumor properties. The effects are due to inhibition of VEGFR-1, -2, and … Axitinib

Oclacitinib

Products Oclacitinib is commercially available in the form of film-coated tablets for dogs (Apoquel). It has been approved in many countries since 2014. Structure and properties Oclacitinib (C15H23N5O2S, Mr = 337.4 g/mol) is present in the drug as oclacitinib maleate. Effects Oclacitinib (ATCvet QD11AH90) has anti-inflammatory, antiallergic, and antipruritic properties. The effects are due to … Oclacitinib

Sunitinib

Products Sunitinib is commercially available in capsule form (Sutent). It has been approved in many countries since 2006. Structure and properties Sunitinib (C22H27FN4O2, Mr = 398.5 g/mol) is present in the drug as sunitinibmalate, a yellow to orange powder that is soluble in water. It is an indolin-2-one and pyrrole derivative. It has an active … Sunitinib

Abemaciclib

Products Abemaciclib 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 2019 (Verzenios). Structure and properties Abemaciclib (C27H32F2N8, Mr = 506.6 g/mol) exists as a white to yellow powder. Effects Abemaciclib (ATC L01XE50) has antitumor and antiproliferative properties. The effects … Abemaciclib

Crizotinib

Products Crizotinib has been approved in many countries since 2012 in capsule form (Xalkori). Structure and properties Crizotinib (C21H22Cl2FN5O, Mr = 450.3 g/mol) is an aminopyridine. It exists as a white to yellowish powder that is soluble in acidic solution to 10 mg/mL. Effects Crizotinib (ATC L01XE16) has antitumor and antiproliferative properties. The effects are … Crizotinib

Trametinib

Products Trametinib was approved in the form of film-coated tablets in the United States in 2013, in the EU in 2014, and in many countries in 2016 (Mekinist). Structure and properties Trametinib (C26H23FIN5O4, Mr = 615.4 g/mol) is a pyridine and a pyrimidine derivative. It is present in the drug product as trametinib dimethyl sulfoxide, … Trametinib

Dasatinib

Products Dasatinib is commercially available in the form of film-coated tablets (Sprycel). It has been approved in many countries since 2007. Generic versions were registered in 2020. Structure and properties Dasatinib (C22H26ClN7O2S, Mr = 488.0 g/mol) exists as a white powder that is insoluble in water. It is an aminopyrimidine derivative. Effects Dasatinib (ATC L01XE06) … Dasatinib

Alectinib

Products Alectinib was approved in capsule form in Japan in 2014, in the United States in 2015, and in many countries in 2017 (Alecensa). Structure and properties Alectinib (C30H34N4O2, Mr = 482.6 g/mol) is present in the drug product as alectinib hydrochloride, a white to yellow-white powder. It has an active metabolite (M4). Effects Alectinib … Alectinib

Gefitinib

Products Gefitinib is commercially available in the form of film-coated tablets (Iressa). It was approved in many countries in 2011. Structure Gefitinib (C22H24ClFN4O3, Mr = 446.9 g/mol) is a morpholine and aniline quinazoline derivative. It exists as a white powder that is sparingly soluble in water, especially at high pH. Effects Gefitinib (ATC L01XE02) is … Gefitinib

Cobimetinib

Products Cobimetinib is commercially available in the form of film-coated tablets (Cotellic). It was approved in many countries in 2015. Structure and properties Cobimetinib (C21H21F3IN3O2, Mr = 531.3 g/mol) is present in the drug as cobimetinib hemifumarate, a white crystalline substance whose solubility is pH-dependent. Effects Cobimetinib (ATC L01XE38) has antitumor and antiproliferative properties. The … Cobimetinib

Encorafenib

Products Encorafenib was approved in capsule form in the United States and EU in 2018 and in many countries in 2019 (Braftovi). Structure and properties Encorafenib (C22H27ClFN7O4S, Mr = 540.0 g/mol) exists as a white powder that is somewhat soluble in water only at low pH. Effects Encorafenib (ATC L01XE46) has antitumor and antiproliferative properties. … Encorafenib

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