Maraviroc

• (S) -4,4- Difluorcyclohexan carboxylic acid - { (1R, 3S, 5S) -3 - [ 3 - (3 -isopropyl- 5-methyl- [1,2,4] triazol- 4-yl) -8 - azabicyclo [3.2.1 ] oct -8-yl ]-1- phenyl-propyl } -amide
• Latin: Maravirocum

J05AX09

Entry inhibitor

CR5 co-receptor antagonist

Template: Infobox chemical / molecular formula search available

Maraviroc (trade name: Celsentri ®, manufactured by Pfizer) is a complex chemical compound that is used as a drug for the treatment of HIV infection and its consequences. It belongs to the group of entry inhibitors ( co-receptor antagonists).

Pharmacology

Maraviroc is an entry inhibitor of the human chemokine receptor CCR5 is a selective inhibitor blocked and thus the docking of HIV viruses to human cells, particularly macrophages prevented. The cell is not infected. Its effect is limited to -use CCR5 (R5 ) HIV viruses. It is now possible with the help of bioinformatic methods to distinguish CCR5 -use HIV viruses of CXCR4-using HIV viruses with very high accuracy.

Pharmacokinetics

Maraviroc is absorbed from the gastrointestinal tract. The recommended dose is 150 twice daily, 300 or 600 mg, depending on the rest of HAART, which influences the behavior through interaction of maraviroc more or less. Bioavailability is 23 to 33 %. The ingestion of the drug may occur with or without food. The active ingredient is bound to 76 % bound to plasma proteins, the volume of distribution was calculated to be 2.8 ± 0.9 l / kg.

Maraviroc is metabolized by cytochrome P450 monooxygenases. A relevant induktorischer or inhibitory effect was not detected. The main metabolite is a desalkylierter on the nitrogen metabolite. The substance is excreted mainly in the faeces (approximately 25% unchanged); 8 % of a dose of 300 mg appear unchanged in the urine. Following intravenous administration, the elimination half-life is approximately 13 hours.

In patients with congenital or drug-induced renal failure on circumstances, a dose adjustment is required ( including other HAART drugs). In mild or moderate hepatic impairment, blood levels are increased by approximately 25 to 46 %. For this group of patients are not yet sufficient data before. Studies in children and elderly patients have not been conducted.

Side effects

Cough, pyrexia, upper respiratory tract infections, rash, complaints of the musculoskeletal system, abdominal pain and dizziness are the most common adverse events reported continued diarrhea, edema, influenza, esophogeal candidiasis, sleep disorders, rhinitis, parasomnias and Harnwegsabnormalitäten were recorded.