Introduction Breast cancer resistance protein (BCRP or ABCG2) is an efflux transporter that belongs to the ABC superfamily (ATP-binding cassette). It is encoded by the gene first isolated from breast cancer cells in 1998. BCRP consists of 655 amino acids and has a molecular weight of 72 kDa. BCRP mediates resistance to structurally and pharmacologically … BCRP
Products Tipranavir is commercially available in capsule form (Aptivus). It has been approved in many countries since 2005. Structure and properties Tipranavir (C31H33F3N2O5S, Mr = 602.7 g/mol) exists as a white to slightly yellowish substance that is insoluble in an aqueous buffer at pH 7.5. Tipranavir has a nonpeptidic structure. Effects Tipranavir (ATC J05AE09) has … Tipranavir
Products Triazolam is commercially available in tablet form (Halcion). It has been approved in many countries since 1978. Structure and properties Triazolam (C17H12Cl2N4, Mr = 343.2 g/mol) exists as a white crystalline powder that is poorly soluble in water. It is a triazole derivative (triazol-am). Effects Triazolam (ATC N05CD05) has sedative, antianxiety, anticonvulsant, amnesic, and … Triazolam
Products Lopinavir is commercially available as film-coated tablets and as a syrup as a fixed combination with ritonavir (Kaletra). It has been approved in many countries since 2000. Structure and properties Lopinavir (C37H48N4O5, Mr = 628.8 g/mol) exists as a white to yellowish white powder that is practically insoluble in water. Effects Lopinavir (ATC J05AE06) … Lopinavir
Products Pitavastatin is commercially available in the form of film-coated tablets (Livazo). It was first approved in many countries in July 2012. In Japan, it has been on the market since 2003, and it is also available in other countries such as the United States and Germany. Structure and properties Pitavastatin (C25H24FNO4, Mr = 421.5 … Pitavastatin
Products Ranolazine is commercially available in the form of sustained-release tablets (Ranexa). It was approved in the United States as early as 2006, in the EU in July 2008, and in many countries in April 2010. Structure and properties Ranolazine or ()–(2, 6-dimethylphenyl)-4(2-hydroxy-3-(2-methoxyphenoxy)-propyl)-1-piperazine acetamide (C24H33N3O4, Mr = 427.54 g/mol) is a piperazine derivative and a … Ranolazine
Products Most HIV protease inhibitors are commercially available in tablet or capsule form. In addition, a few liquid dosage forms are available for ingestion. Saquinavir (Invirase) was the first to be lanicized in 1995. Structure and properties The first HIV protease inhibitors were modeled on the natural peptide substrate of the HIV protease. The protease … HIV Protease Inhibitor
Products Midazolam is commercially available as film-coated tablets and as a solution for injection (Dormicum, generic). It has been approved in many countries since 1982. Midazolam nasal spray has not yet been registered in many countries and must be prepared in a pharmacy as an extemporaneous formulation or imported. In 2012, a solution for use … Midazolam
Products Rifabutin is commercially available in capsule form (mycobutin). It has been approved in many countries since 1994. Structure and properties Rifabutin (C46H62N4O11, Mr = 847 g/mol ) is a semisynthetic ansamycin antibiotic. It exists as a reddish purple amorphous powder that is sparingly soluble in water. Effects Rifabutin (ATC J04AB04) has antibacterial properties against … Rifabutin
Products Atazanavir is commercially available in capsule form (Reyataz). It has been approved in many countries since 2004. Generic versions were registered in 2017. Structure and properties Atazanavir (C38H52N6O7, Mr = 704.9 g/mol) is present in drugs as atazanavir sulfate, a white to slightly yellow crystalline powder that is sparingly soluble in water. Effects Atazanavir … Atazanavir
Background The human organism has several mechanisms to metabolize endogenous and foreign substances. One of these mechanisms is glucuronidation, which occurs primarily in the liver. In this process, enzymes from the superfamily of UDP-glucuronosyltransferases (UGT) transfer a molecule of glucuronic acid from UDP-glucuronic acid to the substrate. Using acetaminophen as an example, alcohols, phenols, carboxylic … Meulengracht’s Disease
Products Fosamprenavir is commercially available in the form of film-coated tablets (Telzir). It has been approved in many countries since 2005. Structure and properties Fosamprenavir (C25H36N3O9PS, Mr = 585.6 g/mol) is present in drugs as fosamprenavir calcium. It is a prodrug that is rapidly biotransformed in the intestinal mucosa to the active metabolite amprenavir. Amprenavir … Fosamprenavir
