Antitumor activity of motesanib alone and in combination with cisplatin or docetaxel in multiple human non–small-cell lung cancer xenograft models

Table 1 Mutational status of NSCLC xenograft tumor models and associated motesanib antitumor activity

Xenograft tumor model	Tumor volume at initiation of therapy (mm³)	Motesanib monotherapy dose (mg/kg BID)	% Tumor growth inhibition*	Confirmed mutations^†
A549	153	75	107	KRAS, STK11
Calu-6	336	75	66	KRAS, TP53
NCI-H358	202	75	127	KRAS, TP53 ^§
NCI-H1299	141	75	72	NRAS, TP53 ^§
NCI-H1650	179	75^‡	78	EGFR, BRAF, TP53 ^¶

BID, twice daily.
*Data from a single experiment.
^†By DNA sequencing (see Methods, Cell Lines and Reagents).
^‡Based on once daily administration.
^§NCI-H358 and NCI-H1299 cells are TP53 null per previously published literature[52, 53].
^¶The functional significance of the BRAF mutation (heterozygous deletion of exon 2) is unknown. NCI-H1650 cells have been reported to carry mutations in CDKN2A, EGFR, and TP53[50, 51].

ISSN: 1476-4598