From: Targeting tumorigenesis: development and use of mTOR inhibitors in cancer therapy
mTOR Inhibitor | T1/2 (h) | Primary Metabolite | Dose and Schedule | MTD | DLTs (all grade 3) | Suggested Phase II Dose |
---|---|---|---|---|---|---|
Ridaforolimus [22] | 56-74 | Not sirolimus pro-drug | 3-28 mg/d IV × 5 d q 2 wk | 18.75 mg | Mouth sores | 12.5 mg IV × 5 d q 2 wk |
~30 | Not sirolimus pro-drug | Oral daily: 5-10 mg/d Oral weekly: 5-70 mg/wk | NR | Daily: hyperglycemia, stomatitis Weekly: stomatitis, fatigue, neutropenia, hyperglycemia | Daily: 10 mg Weekly: 50-70 mg | |
Temsirolimus [26] | 13-22 | Sirolimus | 7.5-220 mg/m2/wk | Formal definition of MTD not met | Neutropenia, thrombocytopenia, hypophosphatemia; asthenia, diarrhea; manic-depressive syndrome, stomatitis; ALT elevation | 25, 75, and 250 mg (flat dose) wkly |