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 Lasmiditan was approved in the United States in 2019 in film-coated tablet form (Reyvow). Structure and properties Lasmiditan (C19H18F3N3O2, Mr = 377.4 g/mol) is present in the drug as lasmiditanhemisuccinate, a white crystalline powder that is sparingly soluble in water. It is a piperidine and pyridine derivative and has no indole structure. Effects Lasmiditan … Lasmiditan
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 Ledipasvir is approved as a fixed combination with sofosbuvir in the form of film-coated tablets (Harvoni). It was released in many countries in 2014. The high price of the drug is controversial (see Sofosbuvir). Cheaper generics are available in India: MyHep LVIR. Structure and properties Ledipasvir (C49H54F2N8O6, Mr = 888.9 g/mol) is practically insoluble … Ledipasvir
Products Ubrogepant was approved in the United States in 2019 in tablet form (Ubrelvy). Structure and properties Ubrogepant (C29H26F3N5O3, Mr = 549.6 g/mol) exists as a white powder that is practically insoluble in water. Effects Ubrogepant has analgesic properties and is effective against other symptoms of migraine such as photophobia (sensitivity to light), phonophobia (sensitivity … Ubrogepant
Products Rolapitant was approved in the form of film-coated tablets in the United States in 2015, in the EU in 2017, and in many countries in 2018 (Varuby). Structure and properties Rolapitant (C25H26F6N2O2, Mr = 500.5 g/mol) is present in the drug as rolapitane hydrochloride, a white powder that is more soluble in water at … Rolapitant
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 Fostemsavir was approved in the United States in 2020 in sustained-release (ER) tablet form (Rukobia). Fostemsavir is the first agent in this drug class. Structure and properties Fostemsavir (C25H26N7O8P, Mr = 583.5 g/mol) is a prodrug. It is present in the drug as fostemsavirtromethamine, which is biotransformed in the body to the active metabolite … Fostemsavir
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 Simeprevir was approved in capsule form in the United States in 2013, in the EU in 2014, and in many countries in 2015 (Olysio). Structure and properties Simeprevir (C38H47N5O7S2, Mr = 749.9 g/mol) is present in the drug product as simeprevir sodium. The macrocyclic molecule contains a sulfonamide moiety, which may cause adverse effects … Simeprevir
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
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
