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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.
Lapatinib is a reversible, ATP-competitive dual inhibitor of the EGFR and HER2 kinases, and was the first HER2-blocking pill (2007). It is approved with capecitabine for HER2-positive advanced breast cancer after trastuzumab (EGF100151: time to progression 8.4 versus 4.4 months) and with letrozole in hormone receptor-positive, HER2-positive disease. The adjuvant ALTTO trial was negative and neoadjuvant NeoALTTO raised pathological complete response but not survival, so it never established a role in early disease. Diarrhoea and rash are the main toxicities, with a hepatotoxicity warning. It has been displaced by tucatinib and by antibody-drug conjugates and now serves mainly as the control arm in ACE-Breast-02 and other Chinese ADC trials. For a newcomer, lapatinib is the original HER2 pill, now mostly a comparator and a late-line option.
1.Lapatinib slips into a pocket on HER2.
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance: how tumours escape each drug class · Lines of therapy.
Oral, self-administered, so it is a Part D drug: covered through a stand-alone Part D plan or Medicare Advantage drug benefit, usually on the specialty tier with 25 to 33% coinsurance until the annual cap ($2,000 in 2025, $2,100 in 2026). Generic lapatinib is available.
Multi-source generic on low-cost tiers; usually no prior authorisation. Cash prices without insurance are modest. Prior authorisation is uncommon for the generic.
Sources: Medicare.gov: Drug coverage (Part D) · Medicare.gov: Costs for Medicare drug coverage (annual out-of-pocket cap). Not medical or financial advice; verify with your plan.
Sources: NICE TA257. Funding decisions are indication-specific and change monthly; verify with NICE and your treating team.
In combination with letrozole for post-menopausal women with HR-positive metastatic breast cancer that overexpresses the HER2 receptor for whom hormonal therapy is indicated
Accelerated approval on a surrogate endpoint, with a confirmatory trial required.
In combination with letrozole for post-menopausal women with HR-positive metastatic breast cancer that overexpresses the HER2 receptor for whom hormonal therapy is indicated
Confirmed: the accelerated approval of 2010 converted to traditional approval 8.9 years after it was granted.
| Region | Year | Indication |
|---|---|---|
| US | 2007 | HER2+ advanced breast cancer with capecitabine after trastuzumab |
| US | 2010 | HR+/HER2+ metastatic breast cancer with letrozole |
| Adverse event | Any grade | Grade 3+ |
|---|---|---|
| Diarrhoea | 65% | 13% |
| Palmar-plantar erythrodysaesthesia (with capecitabine) | 53% | - |
| Rash | 28% | - |
Events listed without rates were not read from a primary source; see the label. Blank cells mean the figure was not sourced, not that it is zero.
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The first demonstration that HER2 is actionable in colorectal cancer, and the trial that defined the colorectal-specific HER2 scoring criteria every later trial has used.
It is where HER2-directed colorectal therapy came from: the xenopatient result led directly to HERACLES and therefore to every HER2 regimen now used in the disease.
Query for this drug: (TITLE:"Lapatinib" OR ABSTRACT:"Lapatinib" OR TITLE:"Tykerb" OR ABSTRACT:"Tykerb") 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 Lapatinib, not a curated reading list.
Shares NALA, HER2 tyrosine kinase inhibitors, HER2-positive breast cancer with brain metastases, Breast cancer (KEGG map).
Shares A molecularly annotated platform of patient-derived xenografts identifies HER2 as an effective therapeutic target in cetuximab-resistant colorectal cancer, Dual-targeted therapy with trastuzumab and lapatinib in treatment-refractory, KRAS codon 12/13 wild-type, HER2-positive metastatic colorectal cancer (HERACLES), EGFR, HER2.
Shares ACE-Breast-02, HER2, HER2-positive breast cancer.
Shares HER2 tyrosine kinase inhibitors, HER2-positive breast cancer with brain metastases, HER2-positive breast cancer, Small-molecule kinase inhibitors.
Shares HER2 tyrosine kinase inhibitors, HER2-positive breast cancer with brain metastases, HER2-positive breast cancer, Small-molecule kinase inhibitors.
Shares HERACLES, Dual-targeted therapy with trastuzumab and lapatinib in treatment-refractory, KRAS codon 12/13 wild-type, HER2-positive metastatic colorectal cancer (HERACLES), Colorectal cancer.
Shares ACE-Breast-02, HER2, HER2-positive breast cancer.
Shares HERACLES, Dual-targeted therapy with trastuzumab and lapatinib in treatment-refractory, KRAS codon 12/13 wild-type, HER2-positive metastatic colorectal cancer (HERACLES), Colorectal cancer.