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
Symptoms Rheumatoid arthritis is a chronic, inflammatory and systemic joint disease. It manifests as pain, symmetrically tense, achy, warm, and swollen joints, swelling, and morning stiffness that lasts for more than an hour. Initially, the hands, wrists, and feet are most affected, but later numerous other joints are also affected. Over time, deformities and rheumatoid … Rheumatoid Arthritis Causes and Treatment
Symptoms Symptoms of Covid-19 include (selection): Fever Cough (irritating cough or with sputum) Respiratory disorders, shortness of breath, shortness of breath. Feeling sick, fatigue Cold symptoms: runny nose, stuffy nose, sore throat. Pain in the limbs, muscle and joint pain. Gastrointestinal complaints: Diarrhea, nausea, vomiting, abdominal pain. Nervous system: impairment of the sense of smell … COVID-19
Products TNF-α inhibitors are commercially available as injectable and infusion preparations. Infliximab (Remicade) was the first agent from this group to be approved in 1998, and in many countries in 1999. Biosimilars of some representatives are now available. Others will follow in the next few years. This article refers to biologics. Small molecules can also … TNF-Α Inhibitors
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
Products Tofacitinib was approved in the United States in November 2012, in many countries in 2013, and in the EU in 2017 in film-coated tablet form (Xeljanz). The European Medicines Agency initially rejected the approval in April 2013. However, baricitinib was approved. In the United States, additional sustained-release film-coated tablets are available that are taken … Tofacitinib
Background Kinases (phosphotransferases) are a large family of enzymes involved in the transduction and amplification of signals on and in cells. They exert their effects by phosphorylating their substrates, that is, by adding a phosphate group to the molecules (Figure). Kinases have complicated names that are usually abbreviated: ALK, AXL, BCR-ABL, c-Kit, c-Met, ERBB, EGFR, … Kinase Inhibitors
Products Janus kinase inhibitors are commercially available in the form of tablets and capsules with different galenics. Structure and properties The structure of Janus kinase inhibitors is characterized by nitrogen heterocycles, which are often condensed. Effects The agents have selective immunosuppressive, anti-inflammatory, and antiproliferative properties. The effects are based on inhibition of Janus kinases (JAK). … Janus Kinase Inhibitors
Products Baricitinib was approved in many countries and in the EU in 2017 and in the United States in 2018 in film-coated tablet form (Olumiant). Structure and properties Baricitinib (C16H17N7O2S, Mr = 371.4 g/mol) is structurally related to adenosine triphosphate and interacts with the ATP-binding site of kinases. It is sparingly soluble in water. Effects … Baricitinib
Products Upadacitinib was approved in the US and EU in 2019 and in many countries in 2020 in extended-release tablet form (Rinvoq sustained-release tablets). Structure and properties Upadacitinib (C17H19F3N6O, Mr = 380.4 g/mol) exists in the drug as a hemihydrate. Effects Upadacitinib has selective immunosuppressive and anti-inflammatory properties. The effects are due to selective and … Upadacitinib
Products Ruxolitinib was approved in tablet form in the United States in 2011 and in the EU and Switzerland in 2012 (Jakavi). Structure and properties Ruxolitinib (C17H21N6O4P, Mr = 404.4 g/mol) is present in drugs as ruxolitinib phosphate, a white to light pink powder that is soluble in water. It is a pyrrolopyrimidine pyrazole derivative … Ruxolitinib
Products Immunosuppressants are commercially available in numerous dosage forms, for example, as creams, ointments, tablets, capsules, solutions, eye drops, and injectables. Structure and properties Within immunosuppressants, several groups can be identified. These include steroids such as the glucocorticoids, substances of microbiological origin such as ciclosporin and mycophenolate mofetil, derivatives of nucleic acids and their components … Immunosuppressants
