Therapy Detail
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| Therapy Name | Tucatinib |
| Synonyms | |
| Therapy Description |
Tucatinib (ARRY-380) selectivity inhibits ERBB2 (HER2), resulting in decreased proliferation and increased apoptosis in ERBB2 (HER2) expressing tumor cells (PMID: 28053022). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Tucatinib | Tukysa | ONT-380|ARRY-380|irbinitinib | HER2 Inhibitor 23 | Tukysa (tucatinib) selectivity inhibits ERBB2 (HER2), resulting in decreased proliferation and increased apoptosis in ERBB2 (HER2) expressing tumor cells (PMID: 28053022). Tukysa (tucatinib) in combination with Herceptin (trastuzumab) and Xeloda (capecitabine) is FDA approved for use in patients with advanced unresectable or metastatic ERBB2 (HER2)-positive breast cancer, including patients with brain metastasis, who have received prior anti-HER2 therapies (FDA.gov). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| ERBB2 G776delinsVC ERBB2 C805S | Advanced Solid Tumor | resistant | Tucatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC and an acquired ERBB2 (HER2) C805S were resistant to Tucatinib (ARRY-380) in culture (PMID: 30527195). | 30527195 |
| ERBB2 over exp | stomach cancer | sensitive | Tucatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Tukysa (tucatinib) inhibited proliferation of an ERBB2 (HER2) over expressing gastric cancer cell line in culture (Cancer Res April 15, 2010 70:3610). | detail... |
| ERBB2 positive | Her2-receptor positive breast cancer | sensitive | Tucatinib | Phase I | Actionable | In a Phase I trial, treatment with Tukysa (tucatinib) resulted in a response rate of 14% (3/22; all partial responses (PR)) and a clinical benefit rate (PR plus stable disease for greater than or equal to 24 weeks) of 27% (6/22) in Erbb2 (Her2)-positive breast cancer patients (PMID: 28053022). | 28053022 |
| ERBB2 Y772_A775dup | Advanced Solid Tumor | resistant | Tucatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) were resistant to Tukysa (tucatinib) in culture (PMID: 30527195). | 30527195 |
| ERBB2 G778_P780dup | Advanced Solid Tumor | decreased response | Tucatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) G778_P780dup (reported as P780_Y781insGSP) demonstrated decreased response to Tukysa (tucatinib) compared to Poziotinib (HM781-36B) in culture (PMID: 30527195). | 30527195 |
| ERBB2 G776delinsVC | Advanced Solid Tumor | resistant | Tucatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Tukysa (tucatinib) in culture (PMID: 30527195). | 30527195 |
| ERBB2 Y772_A775dup ERBB2 C805S | Advanced Solid Tumor | resistant | Tucatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) and an acquired ERBB2 (HER2) C805S were resistant to Tukysa (tucatinib) in culture (PMID: 30527195). | 30527195 |
| ERBB2 positive | stomach carcinoma | sensitive | Tucatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Tukysa (tucatinib) inhibited tumor growth in a ERBB2 (HER2)-positive gastric carcinoma cell line xenograft model (Cancer Res April 15, 2012 72:852). | detail... |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status |
|---|---|---|---|---|
| NCT03043313 | Phase II | Trastuzumab + Tucatinib Tucatinib | Tucatinib Plus Trastuzumab in Patients With HER2+ Colorectal Cancer | Recruiting |
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