Eribulin

Products Eribulin is commercially available as a solution for injection (Halaven). It was approved in many countries and in the EU in 2011. In the United States, it has been registered since 2010. Structure and properties Eribulin is present in drugs as eribulin mesilate (C40H59NO11 – CH4O3S, Mr = 826.0 g/mol), a white crystalline powder … Eribulin

Regorafenib

Products Regorafenib is commercially available in the form of film-coated tablets (Stivarga). It was approved in many countries in February 2013. Structure and properties Regorafenib (C21H15ClF4N4O3, Mr = 482.8 g/mol) is present in drugs as regorafenib monohydrate, which is practically insoluble in water. Effects Regorafenib (ATC L01XE21) has antitumor and antiangiogenic properties. The effects are … Regorafenib

Apixaban

Products Apixaban has been approved in many countries since 2011 in the form of film-coated tablets (Eliquis). Structure and properties Apixaban (C25H25N5O4, Mr = 460.0 g/mol) was developed starting from razaxaban. It is an oxopiperidine and pyrazole derivative. Effects Apixaban (ATC B01AF02) has antithrombotic properties. It is an oral, direct, potent, selective, and reversible inhibitor … Apixaban

Velpatasvir

Products Velpatasvir was approved in 2016 in fixed combination with the HCV polymerase inhibitor sofosbuvir in film-coated tablet form (Epclusa, Gilead). Another fixed combination is Vosevi with sofosbuvir and voxilaprevir. Structure and properties Velpatasvir (C49H54N8O8, Mr = 883.0 g/mol) Effects Velpatasvir has antiviral properties. The effects are due to binding to the viral protein NS5A … Velpatasvir

Venetoclax

Products Venetoclax was approved in the US and EU in 2016 and in many countries in 2018 in film-coated tablet form (Venclyxto, Venclexta). Structure and properties Venetoclax (C45H50ClN7O7S, Mr = 868.4 g/mol) exists as a light to dark yellow powder that is sparingly soluble in water. Effects Venetoclax (ATC L01XX52) has antitumor and cytotoxic properties. … Venetoclax

Daclatasvir

Products Daclatasvir was approved in the EU in 2014 and in many countries in 2015 in film-coated tablet form (Daklinza, Bristol-Myers Squibb). Structure and properties Daclatasvir (C40H50N8O6, Mr = 738.9 g/mol) is present in the drug product as daclatasvir dihydrochloride. Effects Daclatasvir (ATC J05AX14) has antiviral properties. The effects are due to binding to the … Daclatasvir

P-Glycoprotein

P-glycoprotein P-glycoprotein (P-gp, MDR1) is a primary active efflux transporter with a molecular weight of 170 kDa, belonging to the ABC superfamily and consisting of 1280 amino acids. P-gp is the product of the -gene (formerly: ). P is for , ABC is for . Occurrence P-glycoprotein is found on various tissues of the human … P-Glycoprotein