^
Association details:
Biomarker:HER-2 amplification
Cancer:Breast Cancer
Drug:Tukysa (tucatinib) (HER2 inhibitor)
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: C2 – Inclusion Criteria
Title:

Basket Study of Tucatinib and Trastuzumab in Solid Tumors With HER2 Alterations

Excerpt:
...- Disease demonstrating HER2 alterations (overexpression/amplification or HER2 activating mutations), as determined by local or central testing processed in a Clinical Laboratory Improvement Amendments (CLIA)- or International Organization for Standardization (ISO) accredited laboratory, according to one of the following:...
Trial ID:
Evidence Level:
Sensitive: C2 – Inclusion Criteria
Title:

A Study of Tucatinib Given Before Surgery to People With HER2+ Cancers That Have Spread to the Brain

Excerpt:
...- Patients with HER2 overexpressed/amplified/mutant metastatic breast/lung/esophagogastric/colorectal cancer (IHC, fluorescent in situ hybridation or sequencing-confirmed primary, brain, or other metastatic site) and one or more brain tumor(s) planned for neurosurgical resection....
Trial ID:
More C2 evidence
Evidence Level:
Sensitive: C2 – Inclusion Criteria
Title:

A Study of ARRY-380 in Patients With Advanced HER2+ Cancer

Excerpt:
...Assess amplification/expression of HER2 in archival and tumor tissues....
Trial ID:
Less C2 evidence
Evidence Level:
Sensitive: D – Preclinical
Title:

Tucatinib has Selective Activity in HER2-Positive Cancers and Significant Combined Activity with Approved and Novel Breast Cancer-Targeted Therapies

Published date:
05/04/2022
Excerpt:
In this preclinical study, we explore single-agent and combined activity of tucatinib, a novel HER2-selective small-molecule inhibitor. Tucatinib demonstrated potent, selective activity in a panel of 456 human cancer cell lines, with activity restricted to cell lines (breast and non-breast) with HER2-amplification, including models of acquired resistance to trastuzumab.
DOI:
10.1158/1535-7163.MCT-21-0847
Evidence Level:
Sensitive: D – Preclinical
Title:

Tucatinib has Selective Activity in HER2-Positive Cancers and Significant Combined Activity with Approved and Novel Breast Cancer-Targeted Therapies

Published date:
04/13/2022
Excerpt:
Tucatinib demonstrated potent, selective activity in a panel of 456 human cancer cell lines, with activity restricted to cell lines (breast and non-breast) with HER2-amplification, including models of acquired resistance to trastuzumab.
DOI:
10.1158/1535-7163.MCT-21-0847
Evidence Level:
Sensitive: D – Preclinical
Title:

Comparative analysis of drug response and gene profiling of HER2-targeted tyrosine kinase inhibitors

Published date:
01/21/2021
Excerpt:
In this study, the anti-proliferative effects of the three TKIs were directly compared using a 115 cancer cell line panel….All three TKIs were effective against HER2-amplified breast cancer models; neratinib showing the most potent activity, followed by tucatinib then lapatinib.
DOI:
10.1038/s41416-020-01257-x
Evidence Level:
Sensitive: D – Preclinical
Title:

Preclinical Activity of HER2-Selective Tyrosine Kinase Inhibitor Tucatinib as a Single Agent or in Combination with Trastuzumab or Docetaxel in Solid Tumor Models

Published date:
04/04/2020
Excerpt:
The selectivity of tucatinib for HER2 is further supported by the data showing that the cytotoxic activity of tucatinib correlated with HER2 expression levels in a panel of breast cancer cell lines; only HER2-amplified cell lines showed a high degree of sensitivity to tucatinib.
DOI:
10.1158/1535-7163.MCT-19-0873