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Immunomodulatory drug
Thalidomide
2D structure of thalidomide
Synonyms None
ATC code L04AX
MeSH

None

Drugs.com

Other immunosuppressants

Def. properties
Property Details
Chem. 2,3-dihydro-1H-isoindole
Pharm. Inhibition of cereblon, angiogenesis, inflammation and immunomodulatory effects


Immunomodulatory drugs are drugs that are analogues of thalidomide and possess similar immunologic properties, including:[1][2][3]

along with several non-immunologic effects such as:[1]

(S)-thalidomide bound to murine cereblon

Mouse cereblon bound by (S)-thalidomide

Labelled structure of (S)-lenalidomide bound to human cereblon

Human cereblon bound by (S)-lenalidomide



IMiDs can be broken down into two major classes or "generations" based on their tolerability and therapeutic effects.
First-generation IMiD:

Second-generation IMiDs:

Sometimes an additional generation, namely third-generation of IMiDs are classed as IMiDs. I do not consider them IMiDs as while they are structurally related to thalidomide (usually distantly) they lack many of the pharmacologic properties characteristic of thalidomide like cereblon binding; the only such example that has yet received regulatory approval is apremilast.

External linksEdit

Reference listEdit

  1. 1.0 1.1 Vallet, S; Witzens-Harig, M; Jaeger, D; Podar, K (March 2012). "Update on immunomodulatory drugs (IMiDs) in hematologic and solid malignancies.". Expert Opinion on Pharmacotherapy 13 (4): 473–94. PMID 22324734. doi:10.1517/14656566.2012.656091. 
  2. Castelli, R; Cannavò, A; Conforti, F; Grava, G; Cortelezzi, A (October 2012). "Immunomodulatory drugs in multiple myeloma: from molecular mechanisms of action to clinical practice.". Immunopharmacology and Immunotoxicology 34 (5): 740–53. PMID 22401643. doi:10.3109/08923973.2012.658921. 
  3. Pan, B; Lentzsch, S (October 2012). "The application and biology of immunomodulatory drugs (IMiDs) in cancer.". Pharmacology & Therapeutics 136 (1): 56–68. PMID 22796518. doi:10.1016/j.pharmthera.2012.07.004. 
  4. Chang, XB; Stewart, AK (2011). "What is the functional role of the thalidomide binding protein cereblon?". International Journal of Biochemistry and Molecular Biology 2 (3): 287–94. PMC 3193296. PMID 22003441. 

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