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Small pills that block HER2 from inside the cell, complementing antibody drugs; tucatinib is notable for working against brain metastases.
Lapatinib (2007), neratinib (2017) and tucatinib (2020) are oral kinase inhibitors of HER2, with lapatinib and neratinib also hitting EGFR. Tucatinib, more selective and so less prone to diarrhoea and rash, improved survival with trastuzumab and capecitabine in the HER2CLIMB trial including patients with brain metastases, and gained a colorectal cancer indication in 2023. Neratinib is used as extended adjuvant therapy after trastuzumab.
ATP-competitive inhibitors bind the intracellular kinase domain of HER2, blocking downstream signalling even when antibodies cannot reach the tumour, such as behind the blood-brain barrier.
Lapatinib was the first HER2-blocking pill (2007) and is now mostly a comparator arm and a late-line option, displaced by tucatinib and ADCs.
A pill taken for a year after trastuzumab to further reduce recurrence in HER2-positive, hormone-positive breast cancer, limited by severe diarrhoea.
Poziotinib was a tablet designed to fit the awkward shape of HER2 and EGFR exon 20 mutations in lung cancer. It shrank tumours in some patients but caused severe rash and diarrhoea, and the FDA declined to approve it in 2022.
A HER2-selective pill that works in the brain, for HER2-positive breast cancer with brain metastases.
Query for this technology: (TITLE:"HER2 tyrosine kinase inhibitors" OR ABSTRACT:"HER2 tyrosine kinase inhibitors") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about HER2 tyrosine kinase inhibitors, not a curated reading list.
Shares HER2CLIMB-02, HER2CLIMB-05, NALA, Neratinib.
Shares Tucatinib+Trastuzumab+Eribulin in HER2+ MBC, Clinical Trial of Alpelisb and Tucatinib in Patients With PIK3CA-Mutant HER2+ Metastatic Breast Cancer., HER2-positive breast cancer, Colorectal cancer.
Shares MOUNTAINEER, Tucatinib, HER2-amplified colorectal cancer, HER2.
Shares HER2CLIMB, Tucatinib, HER2, HER2-positive breast cancer.
Shares Poziotinib, HER2-amplified colorectal cancer, Colorectal cancer.
Shares MOUNTAINEER, HER2-amplified colorectal cancer, HER2, Colorectal cancer.
Shares Neratinib, HER2CLIMB, Tucatinib, HER2-positive breast cancer.
Shares NALA, Neratinib, HER2-positive breast cancer.