Table 3.
Phase I studies of TAS‐102 orally given in patients with solid tumors to determine toxicity and efficacy profiles
| Study (reference) | Treatment | Evaluation | |||
|---|---|---|---|---|---|
| Dose (mg/m2 per day) | Schedule | No. patients | Toxicity | Efficacy (best response) | |
| Hong et al.( 75 ) | 100 | q1d×14 | 2 | °3/4 bone marrow suppression (2/2) # | ND |
| 50 | q1d×14 | 6 | °3/4 toxicities (0/6) | SD (2/6), PD (4/6) ## | |
| 60 | q1d×14 | 6 | °3/4 granulocytopenia (3/6) | SD (2/6), PD (4/6) | |
| Dwivedy et al.( 76 ) | 50 | q1d×5 | 3 | °3/4 toxicities (0/3) | ND |
| 70 | q1d×5 | 6 | °4 granulocytopenia (1/6), °3 toxicities (0/6) | SD (1/6), NE (5/6) | |
| 80 | q1d×5 | NK | NK | NK | |
| Thomas et al.( 77 ) | 120 | q1d×5 | NK | °4 granulocytopenia (NK) | NK |
| Wolff et al. (unpublished) | 60 | TID×5 | 3 | °3 neutropenia (3/3) | SD (9/15)* |
| 70 | TID×5 | 6 | °3 neutropenia (5/6) | ||
| 80 | TID×5 | 6 | °3/4 neutropenia (6/6), °3 thrombocytopenia (1/6) | ||
| Green et al.( 78 ) | 80 | BID×5 | 3 | °3/4 granulocytopenia (2/3) | SD (7/19)* |
| 90 | BID×5 | 16 | °3/4 granulocytopenia (9/16), °4 thrombocytopenia (1/16) | ||
Dose not specified, median duration of SD was >4 months;
# number of patients with toxicity/number of patients enrolled.
number of patients/number of patients enrolled; BID×5: twice per day for 5 days followed by 2 days rest for 2 weeks, repeated every 4 weeks; ND, not determined; NE, not evaluable; NK, not known; PD, progressive disease. q1d×14, once per day for 14 days, repeated every 3 weeks; q1d×5, once per day for 5 days followed by 2 days rest for 2 weeks, repeated every 4 weeks (Dwivedy et al. 76 ) or for 1 week, repeated every 3 weeks (Thomas et al. 77 ); SD, stable disease; TID×5, three times per day for 5 days followed by 2 days rest for 2 weeks, repeated every 4 weeks.