Cereblon modulator
Cereblon E3 ligase modulator
- Redirects the cereblon E3 ubiquitin ligase → tags selected proteins for degradation
- Degrades Ikaros/Aiolos → anti-myeloma and immunomodulatory effects
- Degradation of developmental transcription factors → teratogenicity
- Thromboembolism risk
Drugs with this mechanism (2)
- Lenalidomide — Cereblon modulator for myeloma; thalidomide analog with the same teratogenicity.
- Thalidomide — Immunomodulator used for myeloma and erythema nodosum leprosum; extreme teratogenicity, neuropathy, and thrombosis risks.
Self-check
- Which proteins are degraded for the anti-myeloma effect of cereblon modulation?
Ikaros and Aiolos. - Why can cereblon modulation be teratogenic?
Degrades developmental transcription factors.
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