Table 2 Clinical evaluation of triptolide derivatives

PG490-88

Advanced solid tumors

0.5–18 mg/m², infusion for 2 times every 3 weeks (days 1 and 8)

Anaemia, fatigue, nausea, vomiting, diarrhoea and constipation; two cases of death at the dose of 12 and 18 mg/m²

Phase I: suspended

[116]

Refractory or relapsing acute leukemia

0.15–13 mg/m², infusion for 5 consecutive days every 15 days

Dose-limited cerebellar toxicity

Phase I: completed

[128]

LLDT-8

Rheumatoid arthritis

0.25–1.0 mg/day, 24 weeks

Reversible leukopenia, hematologic toxicity, and upper respiratory tract infection

Phase II: completed

[129]

HIV-associated chronic immune activation

N/A

N/A

Phase I: ongoing

[113]

Minnelide

Pancreatic cancer

0.67 mg/m², infusion for 21 consecutive days every 28 days

Reversible leukopenia, neutropenia, and cerebellar toxicities

Phase II: completed

[130]

Advanced solid tumors

Minnelide™ Capsules, oral administration for 21 consecutive days every 28 days

N/A

Phase I: ongoing

[131]