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The primary mechanism of action of thalidomide and its analogs in both their anti-cancer and teratogenic effects is now known to be as cereblon E3 ligase modulators. [ 25 ] [ 27 ] [ 28 ] [ 29 ] Thalidomide also binds to and acts as an antagonist of the androgen receptor and hence is a nonsteroidal antiandrogen of some capacity. [ 30 ]
The thalidomide molecule is a synthetic derivative of glutamic acid and consists of a glutarimide ring and a phthaloyl ring (Figure 5). [15] [16] Its IUPAC name is 2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione and it has one chiral center [15] After thalidomide's selective inhibition of TNF-α had been reported, a renewed effort was put in thalidomide's clinical development.
Adverse effects by frequency: [1] [2] ... For information regarding birth defects, see thalidomide. Very common (may affect more than 1 in 10 people)
Thalidomide is a classical example highlighting the alleged role of chirality in drug toxicity. Thalidomide was a racemic therapeutic and prescribed to pregnant women to control nausea and vomiting. The drug was withdrawn from world market when it became evident that the use in pregnancy causes phocomelia (clinical conditions where babies are ...
A TNF inhibitor is a pharmaceutical drug that suppresses the physiologic response to tumor necrosis factor (TNF), which is part of the inflammatory response.TNF is involved in autoimmune and immune-mediated disorders such as rheumatoid arthritis, ankylosing spondylitis, inflammatory bowel disease, psoriasis, hidradenitis suppurativa and refractory asthma, so TNF inhibitors may be used in their ...
Thalidomide brought on changes in the way drugs are tested, what type of drugs are used during pregnancy, and increased the awareness of potential side effects of drugs. According to Canadian news magazine programme W5 , most, but not all, victims of thalidomide receive annual benefits as compensation from the Government of Canada .
Severe side effects include low blood platelets, low white blood cells, and blood clots. [8] The dose may need to be adjusted in people with kidney problems. [8] Lenalidomide is closely related to thalidomide, which is known to cause severe birth defects, so its use during pregnancy is very likely to harm the fetus. [8]
Thalidomide is a drug whose two enantiomers cause distinctly different effects from one another. The unforeseen teratogenicity of the (R)-(+)-isomer caused it to become an important case study of stereochemistry in medicine.
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