Table 3.
Experimental Brain Metastasis Preventive Activity of Compounds in the 231-BR Model.
| Drug: | Dose andSchedule2: | Expt3: | Median4 Number Large Metastases: | %Reduction: | P: | Ref.: | |
|---|---|---|---|---|---|---|---|
| Vehicle | Drug | ||||||
| Capecitabine | 400 D PO | 1 | 6.2 | 4.8 | −23 | 0.40 | |
| 2 | 2.7 | 1.7 | −37 | 0.59 | |||
| 3 | 3.0 | 1.9 | −37 | 1.0 | |||
| Carboplatin | 50 W IV | 1 | 6.2 | 3.6 | −42 | 0.32 | |
| 2 | 3.0 | 3.0 | 0 | 1.0 | |||
| Doxorubicin | 5 W IV | 1 | 6.2 | 5.4 | −13 | 0.04 | |
| Gemcitabine | 50 2xW IV | 1 | 2.7 | 0 | −100 | 0.008 | |
| 2 | 2.0 | 0 | −100 | <0.0001 | |||
| Irinotecan | 4×7 IV | 1 | 2.0 | 1.0 | −50 | 0.090 | |
| 2 | 3.8 | 1.8 | −53 | 0.010 | |||
| Paclitaxel | 6 W IV | 1 | 8.5 | 7.4 | −13 | 1.0 | |
| 2 | 3.9 | 4.8 | +23 | 0.75 | |||
| 3 | 6.2 | 4.0 | −35 | 0.65 | |||
| Lapatinib5 | 100 Dx2 PO | P | 6.8 | 3.4 | −50 | 0.0001 | (109) |
| Vorinostat | 150 D IP | P | 7.7* | 2.9* | −62 | <0.0001 | (110) |
| Pazopanib5 | 100 Dx2 PO | P | 3.9 | 1.1 | −73 | <0.0001 | (111) |
| TPI-287 | 18 3×4 IV | P | 4.3* | 1.9* | −55 | 0.025 | (112) |
Includes previously published and unpublished results, the latter without references and conducted in the Steeg laboratory.
Dose in mg/kg. D, Daily; Dx2, Twice daily; M-F, Daily- Monday through Friday; W, Weekly; 2xW, Twice weekly; 4×7, Every fourth day for 7 treatments; 4×5–2, Two doses of 5 mg/kg, reduced to 2 mg/kg thereafter for toxicity; 3×4, Three treatments-every fourth day; IV, Intravenously; PO, Oral; IP, Intraperitoneally.
P, Pooled data from multiple experiments as published.
Data published as means indicated by *
Tested on a HER2 transfectant of 231-BR.