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A HER2-selective pill that works in the brain, for HER2-positive breast cancer with brain metastases.
Tucatinib is a HER2-selective reversible tyrosine kinase inhibitor that spares EGFR, so it causes less rash and diarrhoea than lapatinib or neratinib, and it penetrates the central nervous system. Taken as 300 mg twice daily, it was approved in 2020 with trastuzumab and capecitabine for HER2-positive metastatic breast cancer after HER2CLIMB, which showed an overall survival benefit that held in patients with active brain metastases, a group usually excluded from trials. In 2023 it was approved with trastuzumab for HER2-positive, RAS-wild-type metastatic colorectal cancer after MOUNTAINEER. Pfizer (via Seagen) markets it. Its place after trastuzumab deruxtecan, which also has brain activity, is the current sequencing question. For a newcomer: the HER2 pill chosen when the cancer has reached the brain.
Highly HER2-selective reversible TKI sparing EGFR. Connects to HER2.
1.Oral drug is absorbed and reaches the tumour
Source: www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications. Doses are for orientation; the current label governs.
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).
Covered for FDA-labelled and NCCN-listed uses, but almost always behind prior authorisation confirming diagnosis, biomarker and line of therapy; dispensed through a specialty pharmacy.
Part D out-of-pocket capped at $2,000 (2025) / $2,100 (2026). Medicare patients cannot use manufacturer co-pay cards; charity funds (PAN, HealthWell, CancerCare) and the Extra Help subsidy are the routes.
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 TA786 · SMC advice: tucatinib. Funding decisions are indication-specific and change monthly; verify with NICE and your treating team.
| Date | Deal | Type | Upfront | Total | Source |
|---|---|---|---|---|---|
| 2023-03-13 | Seagen to Pfizer (incl. Seagen) Padcev, Tivdak, Adcetris, Tukysa and the vedotin ADC platform | Acquisition | not disclosed | $43bn | source |
HER2+ metastatic breast cancer including brain metastases, with trastuzumab and capecitabine (HER2CLIMB) source
In combination with trastuzumab for the treatment of adult patients with RAS wild-type, HER2-positive, unresectable or metastatic colorectal cancer that has progressed following treatment with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy
HER2+ RAS wild-type metastatic colorectal cancer with trastuzumab (MOUNTAINEER, accelerated) The confirmatory requirement was still open 3.7 years later, when the FDA's table was read. source
| Region | Year | Indication |
|---|---|---|
| US | 2020 | HER2+ metastatic breast cancer including brain metastases, with trastuzumab and capecitabine |
| US | 2023 | HER2+ RAS-wild-type mCRC with trastuzumab |
| US | 2023 | HER2-positive, RAS wild-type unresectable or metastatic colorectal cancer that has progressed after fluoropyrimidine, oxaliplatin and irinotecan, with trastuzumab · Accelerated approval on 19 January 2023 on the MOUNTAINEER cohorts; MOUNTAINEER-03 is the confirmatory trial. No NICE recommendation for colorectal cancer at September 2026. |
| Adverse event |
|---|
| Diarrhoea |
| Palmar-plantar erythrodysaesthesia |
| Nausea |
| Fatigue |
| Hepatotoxicity |
| Stomatitis |
HER2CLIMB: 81% any grade, 13% grade 3. 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.
| Country | Reimbursement | List price | Assistance |
|---|---|---|---|
| United States | Medicare Part D (oral); commercial plans per formulary, often with prior authorisation | not disclosed | pfizeroncologytogether.com |
| United Kingdom | NICE: recommended with trastuzumab and capecitabine for HER2+ breast cancer after ≥2 anti-HER2 regimens (TA786) | not disclosed | - |
List prices are manufacturer or Medicare figures where publicly disclosed; net prices after rebates are usually lower. Reimbursement changes; check the payer.
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The first United States approval of a HER2-directed regimen in colorectal cancer, and the basis for MOUNTAINEER-03, which is testing the combination with chemotherapy in the first line.
This analysis is the evidence base for treating active HER2-positive brain metastases with a systemic regimen, sometimes deferring radiotherapy, and for tucatinib's brain-specific labelling.
Tucatinib-based therapy is the standard for HER2-positive disease with active brain metastases and a standard later-line option overall; it was the first trial to enrol progressing brain metastases and show a systemic drug helps them.
It fixes the population size for HER2-directed therapy, shows the enrichment in wild-type disease that makes reflex HER2 testing worthwhile there, and establishes that HER2 is not itself prognostic in this cancer.
It is the threshold behind the colorectal HER2 approvals: the more-than-50% rule, rather than the 10% used in gastric cancer, is what a pathologist applies when a bowel cancer is called HER2-positive.
Query for this drug: (TITLE:"Tucatinib" OR ABSTRACT:"Tucatinib" OR TITLE:"Tukysa" OR ABSTRACT:"Tukysa") 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 Tucatinib, not a curated reading list.
Shares HER2-positive brain metastases, HER2 tyrosine kinase inhibitors, HER2-positive breast cancer with brain metastases, HER2 IHC 3+ (HER2-positive by immunohistochemistry).
Shares Systemic-first management of HER2-positive brain metastases, HER2-positive brain metastases, HER2-positive breast cancer with brain metastases, Brain metastases (secondary brain tumours).
Shares Tucatinib + trastuzumab + capecitabine for brain metastases, HER2CLIMB brain metastases analysis: intracranial efficacy and survival with tucatinib, HER2CLIMB: tucatinib with trastuzumab and capecitabine for HER2-positive metastatic breast cancer, including brain metastases, A Study of Tucatinib and Trastuzumab in People With Rectal Cancer.
Shares HER2 overexpression and amplification as a potential therapeutic target in colorectal cancer: analysis of 3256 patients enrolled in the QUASAR, FOCUS and PICCOLO colorectal cancer trials, Assessment of a HER2 scoring system for colorectal cancer: results from a validation study, Tucatinib plus trastuzumab for chemotherapy-refractory, HER2-positive, RAS wild-type unresectable or metastatic colorectal cancer (MOUNTAINEER), HER2 IHC 3+ (HER2-positive by immunohistochemistry).
Shares Study of Patritumab Deruxtecan With Other Anticancer Agents in Participants With HER2 Positive Breast Cancer That Has Spread and Cannot Be Surgically Removed (MK-1022-009), A Phase 1b/2 Study of T-DXd Combinations in HER2-positive Metastatic Breast Cancer, HER2CLIMB-05, HER2-positive breast cancer with brain metastases.
Shares HER2 tyrosine kinase inhibitors, HER2-positive breast cancer with brain metastases, Breast cancer (KEGG map), HER2.
Shares MOUNTAINEER-03, Assessment of a HER2 scoring system for colorectal cancer: results from a validation study, HER2-amplified colorectal cancer, HER2.
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.