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Association details:
| Biomarker: | KIF5B-RET fusion |
|---|---|
| Cancer: | Non Small Cell Lung Cancer |
| Drug: | agerafenib (RXDX-105) (BRAF inhibitor, RET inhibitor, CS-1 inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
A Phase I/Ib Trial of the VEGFR-Sparing Multikinase RET Inhibitor RXDX-105
Published date:
11/30/2019
Excerpt:
A waterfall plot of the best objective response to RXDX-105 in 27 evaluable patients with RET tyrosine kinase inhibitor-naïve RET fusion-positive non-small cell lung cancers is shown. Cases are grouped by upstream partner: KIF5B-RET, non-KIF5B-RET, and unknown (FISH-positive)...The patient with a KIF5B-RET fusion-positive NSCLC who had a >50% reduction in target lesions had a best response of progressive disease due to the presence of new non-target lesions on follow-up imaging....the objective response rates and/or median progression-free survival (when available) in KIF5B-RET-containing tumors were lower than in non-KIF5B-RET-containing tumors.
DOI:
10.1158/2159-8290.CD-18-0839
Trial ID:
Source:
Title:
Novel human-derived RET fusion NSCLC cell lines have heterogeneous responses to RET inhibitors and differential regulation of downstream signaling
Published date:
04/01/2021
Excerpt:
...three novel RET-positive(RET+) patient-derived cancer cell lines, CUTO22(KIF5B-RET+), CUTO32(KIF5B-RET+) and CUTO42(EML4-RET+)...CUTO22 and CUTO42 cell lines were sensitive to the selective RET inhibitors RXDX-105 and BLU-667...CUTO22 and CUTO42 cell lines had <50nM IC50 values for RXDX-105 and BLU-667...
DOI:
10.1124/molpharm.120.000207
Source:
Title:
Antitumor Activity of RXDX-105 in Multiple Cancer Types with RET Rearrangements or Mutations
Excerpt:
...NSCLC PDX models CTG-0838 and CTG-1048, available at Champions Oncology, both of which contain the KIF5B-RET fusion, the most common RET gene rearrangement observed in lung cancer. Treatment of CTG-0838 with RXDX-105 at 30 mg/kg BID resulted in significant tumor growth inhibition...
DOI:
10.1158/1078-0432.CCR-16-1887
