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. 2021 Jun 22;20(9):1499–1507. doi: 10.1158/1535-7163.MCT-21-0221

Figure 3.

Figure 3. Evaluation of efficacy of TPX-0131 in CDX models in SCID/beige mice administered TPX-0131 via oral gavage twice daily for seven consecutive days. A, Antitumor effect of TPX-0131 on Ba/F3 cell–derived xenograft model with an EML4-ALK G1202R fusion. B, Antitumor effect of TPX-0131 on Ba/F3 cell-derived xenograft model with an EML4-ALK G1202R/L1198F fusion. C, Antitumor effect of TPX-0131 on Ba/F3 cell-derived xenograft model with an EML4-ALK G1202R/L1196M fusion. Waterfall plots for each model represents the degree of xenograft response for each mouse. BID, twice daily. It should be noted that 5 mg/kg dosing of TPX-0131 and lorlatinib in mouse models result in different unbound exposures (e.g., 12 hours postdose TPX-0131, 8 nmol/L; lorlatinib, 358 nmol/L).

Evaluation of efficacy of TPX-0131 in CDX models in SCID/beige mice administered TPX-0131 via oral gavage twice daily for seven consecutive days. A, Antitumor effect of TPX-0131 on Ba/F3 cell–derived xenograft model with an EML4-ALK G1202R fusion. B, Antitumor effect of TPX-0131 on Ba/F3 cell-derived xenograft model with an EML4-ALK G1202R/L1198F fusion. C, Antitumor effect of TPX-0131 on Ba/F3 cell-derived xenograft model with an EML4-ALK G1202R/L1196M fusion. Waterfall plots for each model represents the degree of xenograft response for each mouse. BID, twice daily. It should be noted that 5 mg/kg dosing of TPX-0131 and lorlatinib in mouse models result in different unbound exposures (e.g., 12 hours postdose TPX-0131, 8 nmol/L; lorlatinib, 358 nmol/L).