It has in vitro and in vivo activities against mouse models of polycystic kidney disease[2] and pancreatic cancer, but its physical properties[3] and severe toxicity[4] limit its therapeutic potential.

[3][5] Triptolide is a component of ContraPest, a contraceptive pest control liquid used to reduce rat populations in the United States.

[10] The level of resistance conferred by the C342T mutation is about 100-fold higher than the most triptolide-resistant mutants previously identified.

[15] Glutriptolide, a glucose conjugate of triptolide with better solubility and lower toxicity, did not inhibit XPB activity in vitro, but exhibited tumor control in vivo, which is likely due to sustained stepwise release of active triptolide within cancer cells.

[16] A second generation glutriptolide has been recently reported for targeting hypoxic cancer cells with increased glucose transporter expression.