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The Meconopsis plants (Chinese: ), belonging to the family Papaveraceae, have been used as traditional Tibetan medicine (TTM) for thousands of years. Meconopsis has the effects of clearing heat, reducing swelling, and easing pain, and is mainly prescribed for heat syndromes, hepatitis, pneumonia, and pain in joints. Phytochemical studies have revealed the presence of major isoquinoline alkaloids and flavonoids. Modern pharmacological research has demonstrated its antitumor, hepatoprotective, analgestic, antimicrobial, anti-oxidant, antitussive, and anti-inflammatory activities. However, resource availability, in-depth in vivo pharmacological study and qualitative and quantitative analysis are still insufficient and deserve further efforts. This paper provides a comprehensive advance on the ethnopharmacological, phytochemical, and pharmacological studies of the genus, in hopes of promoting a better understanding of their medicinal values.