Products Rivaroxaban is commercially available in the form of film-coated tablets (Xarelto, Xarelto vascular). It was approved in 2008 as the first agent in the direct factor Xa inhibitor group. Low-dose Xarelto vascular, 2.5 mg, was registered in many countries in 2019. Structure and properties Rivaroxaban (C19H18ClN3O5S, Mr = 435.9 g/mol) is a pure -enantiomer … Rivaroxaban
Products Most statins are commercially available in the form of film-coated tablets, and some are also available as capsules. The first active ingredient to be marketed was lovastatin from Merck in the United States in 1987. In many countries, simvastatin (Zocor) and, shortly thereafter, pravastatin (Selipran) were the first agents to be approved in 1990. … Statins
Products Sofosbuvir is commercially available in the form of film-coated tablets (Sovaldi). It was approved in the United States and EU in 2013 and in many countries in 2014. The very high price of the drug has been a source of debate. Sofosbuvir is also combined fixed with ledipasvir (Harvoni). Cheaper generics are available in … Sofosbuvir
Products Carfilzomib was approved in many countries in 2015 as a powder for the preparation of an infusion solution (Kyprolis). Structure and properties Carfilzomib (C40H57N5O7, Mr = 719.9 g/mol) exists as a crystalline substance that is practically insoluble in water. It is a peptide derivative, a tetrapeptide epoxyketone. Epoxyketones are derivatives of epoxomicin, a natural … Carfilzomib
Products Darolutamide was approved in the US in 2019 and in the EU and Switzerland in 2020 in film-coated tablet form (Nubeqa). Structure and properties Darolutamide (C19H19ClN6O2, Mr = 398.8 g/mol) exists as a white to grayish or yellowish-white crystalline powder and is practically insoluble in water. The drug has a nonsteroidal structure and is … Darolutamide
Products Empagliflozin is commercially available in the form of film-coated tablets. It was approved in the EU, the United States, and many countries in 2014 (Jardiance). Empagliflozin is also combined fixed with metformin (Jardiance Met) as well as with linagliptin (Glyxambi). Trijardy XR is a fixed combination of empagliflozin, linagliptin, and metformin. Structure and properties … Empagliflozin
Products Topotecan is commercially available in capsule form and as a lyophilizate (Hycamtin, generic). It has been approved in many countries since 1996. Structure and properties Topotecan (C23H23N3O5, Mr = 421.4 g/mol) is present in the drug as topotecan hydrochloride. It is a semisynthetic derivative of camptothecin, a plant alkaloid derived from the tree. Effects … Topotecan
Definition When two or more drugs are combined, they may affect each other. This is especially true with regard to their pharmacokinetics (ADME) and effects and adverse effects (pharmacodynamics). This phenomenon is called interaction and drug-drug interaction. Interactions are usually undesirable because they can lead to, for example, loss of efficacy, side effects, poisoning, hospitalization, … Interactions
Products Lenvatinib was approved in many countries in 2015 in capsule form (Lenvima). In 2017, Kisplyx capsules were also approved. Structure and properties Lenvatinib (C21H19ClN4O4, Mr = 426.9 g/mol) is present in the drug as lenvatinib mesilate, a white to pale reddish-yellow powder that is sparingly soluble in water. It is a quinoline and carboxamide … Lenvatinib
Products Glecaprevir was approved in the United States, many countries, and the EU in 2017 as a fixed-dose combination with pibrentasvir in film-coated tablet form (Maviret). Structure and properties Glecaprevir (C38H46F4N6O9S, Mr = 838.9 g/mol) exists as a white crystalline powder. Effects Glecaprevir has antiviral properties. The effects are due to inhibition of the viral … Glecaprevir
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
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
