RAR agonist
Retinoic acid receptor agonist
- ↑ transcription of differentiation genes
- Drives promyelocytes to mature in acute promyelocytic leukemia
- Curative in acute promyelocytic leukemia
- Normalizes keratinocyte turnover → ↓ acne, psoriasis
- Strongly teratogenic
- Mucocutaneous dryness and irritation
Drugs with this mechanism (4)
- Acitretin — Systemic retinoid for severe psoriasis; alcohol converts it to long-lived etretinate.
- Alitretinoin — Pan-retinoid agonist (both RAR and RXR).
- Tazarotene — Receptor-selective topical retinoid for psoriasis and acne; contraindicated in pregnancy.
- Tretinoin — All-trans retinoic acid; topical acne drug and systemic differentiation therapy for APL.
Self-check
- What does RAR activation make malignant promyelocytes do?
Mature. - What major fetal risk accompanies RAR agonism?
Strong teratogenicity.
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