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Therapy Name | Lapatinib |
Synonyms | |
Therapy Description |
Tykerb (lapatinib) reversibly inhibits ERBB2 (HER2) and EGFR, resulting in decreased downstream signaling and potentially leading to reduced tumor growth (PMID: 22477724). Tykerb (lapatinib) is FDA approved for ERBB2 (HER2)-positive (overexpressing) breast cancer (FDA.gov). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Lapatinib | Tykerb | Lapatinib Ditosylate | EGFR Inhibitor (Pan) 61 HER2 Inhibitor 41 | Tykerb (lapatinib) reversibly inhibits ERBB2 (HER2) and EGFR, resulting in decreased downstream signaling and potentially leading to reduced tumor growth (PMID: 22477724). Tykerb (lapatinib) is FDA approved for ERBB2 (HER2)-positive (overexpressing) breast cancer (FDA.gov). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
ERBB4 E452K | melanoma | sensitive | Lapatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited growth and induced apoptosis in melanoma cells harboring ERBB4 E452K in culture (PMID: 19718025). | 19718025 |
ERBB3 Q809R | Advanced Solid Tumor | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited proliferation and colony formation in transformed cell lines expressing ERBB3 (HER3) Q809R (PMID: 23680147). | 23680147 |
ERBB3 P262H | Advanced Solid Tumor | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited proliferation and colony formation in transformed cell lines expressing ERBB3 (HER3) P262H (PMID: 23680147). | 23680147 |
ERBB4 R393W | melanoma | sensitive | Lapatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival of melanoma cells harboring ERBB4 R393W in culture (PMID: 19718025). | 19718025 |
ERBB4 A17V | hematologic cancer | sensitive | Lapatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB4 A17V demonstrated sensitivity to Tykerb (lapatinib) similar to wild-type Erbb4 in culture, resulting in decreased cell viability (PMID: 33323455). | 33323455 |
PIK3CA E545K | breast cancer | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). | 26627007 |
ERBB3 act mut | Advanced Solid Tumor | sensitive | Lapatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited proliferation and colony formation in transformed cell lines expressing ERBB3 (HER3) activating mutations (PMID: 23680147). | 23680147 |
PIK3CA Q546K | breast cancer | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). | 26627007 |
ERBB4 E317K | melanoma | sensitive | Lapatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited growth and induced apoptosis in melanoma cells harboring ERBB4 E317K in culture (PMID: 19718025). | 19718025 |
PIK3CA E542K | breast cancer | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E542K in culture (PMID: 26627007). | 26627007 |
ERBB4 R544W | melanoma | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) induced apoptosis in melanoma cells harboring ERBB4 R544W in culture (PMID: 19718025). | 19718025 |
ERBB4 E563K | melanoma | sensitive | Lapatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival and induced apoptosis in melanoma cells harboring ERBB4 E563K in culture (PMID: 19718025). | 19718025 |
ERBB3 V714M | Advanced Solid Tumor | sensitive | Lapatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited cell proliferation in transformed cell lines expressing ERBB3 (HER3) V714M in culture (PMID: 23680147). | 23680147 |
ERBB3 V104M | Advanced Solid Tumor | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited proliferation and colony formation in transformed cell lines expressing ERBB3 (HER3) V104M (PMID: 23680147). | 23680147 |
PIK3CA G1049R | breast cancer | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). | 26627007 |
ERBB4 G936R | Advanced Solid Tumor | sensitive | Lapatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB4 G936R demonstrated sensitivity to Tykerb (lapatinib) similar to wild-type Erbb4 in culture, resulting in decreased cell viability (PMID: 33323455). | 33323455 |
ERBB3 A232V | Advanced Solid Tumor | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited proliferation and colony formation in transformed cell lines expressing ERBB3 (HER3) A232V (PMID: 23680147). | 23680147 |
ERBB3 G284R | Advanced Solid Tumor | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited proliferation and colony formation in transformed cell lines expressing ERBB3 (HER3) G284R (PMID: 23680147). | 23680147 |
PIK3CA N345K | breast cancer | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). | 26627007 |
ERBB3 T355I | estrogen-receptor positive breast cancer | no benefit | Lapatinib | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with Tykerb (lapatinib) did not significantly reduce the proliferation of estrogen-receptor positive breast cancer cells expressing ERBB3 (HER3) T355I in culture relative to control and combination treatments (PMID: 29963236). | 29963236 |
ERBB3 D297H | head and neck squamous cell carcinoma | sensitive | Lapatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Tykerb (lapatinib) treatment inhibited viability of a hypopharyngeal squamous cell carcinoma cell line harboring ERBB3 (HER3) D297H in culture (PMID: 33473169). | 33473169 |
PIK3CA H1047L | breast cancer | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). | 26627007 |
ERBB3 T389K | Advanced Solid Tumor | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited proliferation and colony formation in transformed cell lines expressing ERBB3 (HER3) T389K (PMID: 23680147). | 23680147 |
ERBB3 M91I | bladder carcinoma | resistant | Lapatinib | Preclinical - Cell culture | Actionable | In a preclinical study, a bladder carcinoma cell line harboring ERBB3 (HER3) M91I was resistant to Tykerb (lapatinib) in culture (PMID: 33473169). | 33473169 |
PIK3CA H1047R | breast cancer | sensitive | Lapatinib | Preclinical | Actionable | In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). | 26627007 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT01306045 | Phase II | Erlotinib Lapatinib MK2206 Sunitinib Selumetinib | Molecular Profiling and Targeted Therapy for Advanced Non-Small Cell Lung Cancer, Small Cell Lung Cancer, and Thymic Malignancies | Active, not recruiting | USA | 0 |
NCT00939523 | Phase II | Lapatinib | Targeted Therapy With Lapatinib in Patients With Recurrent Pituitary Tumors Resistant to Standard Therapy | Completed | USA | 0 |
NCT02788201 | Phase II | Erlotinib Thiotepa Imatinib Dacarbazine Arsenic trioxide Idarubicin Mitomycin C Thioguanine Mercaptopurine Methotrexate Cladribine Epirubicin Gemcitabine Doxorubicin Bleomycin Etoposide Gefitinib Daunorubicin Lomustine Sorafenib Sunitinib Ifosfamide Asparaginase Ixabepilone Abiraterone Azacitidine Ruxolitinib Decitabine Axitinib Estramustine Floxuridine Lapatinib Carmustine Fludarabine Nilotinib Cisplatin Vismodegib Vandetanib Melphalan Busulfan Carboplatin Toremifene Crizotinib Dactinomycin Temsirolimus Vorinostat Romidepsin Fluorouracil Irinotecan Bortezomib Tamoxifen Topotecan Chlorambucil Pentostatin Eribulin Carfilzomib Vemurafenib Hydroxyurea Exemestane Vincristine Sulfate Dasatinib Mitoxantrone Vinblastine Cytarabine Tretinoin Clofarabine Teniposide Docetaxel Pazopanib Oxaliplatin Streptozocin Paclitaxel Bendamustine Mechlorethamine Mitotane | Genomic Based Assignment of Therapy in Advanced Urothelial Carcinoma | Completed | USA | 0 |
NCT01622868 | Phase II | Lapatinib | Whole-Brain Radiation Therapy or Stereotactic Radiosurgery With or Without Lapatinib Ditosylate in Treating Patients With Brain Metastasis From HER2-Positive Breast Cancer | Completed | USA | CAN | 1 |
NCT04591431 | Phase II | Everolimus Nivolumab Itacitinib Erlotinib Ponatinib Pemigatinib Ipatasertib Ipilimumab Cobimetinib Atezolizumab Palbociclib Entrectinib Vemurafenib Lapatinib Trastuzumab Brigatinib Alectinib Ado-trastuzumab emtansine Pertuzumab Vismodegib | The Rome Trial From Histology to Target: the Road to Personalize Target Therapy and Immunotherapy (ROME) | Active, not recruiting | ITA | 0 |
NCT01160211 | Phase III | Lapatinib + Trastuzumab Letrozole Anastrozole Lapatinib Trastuzumab Exemestane | A Study to Compare the Safety and Efficacy of an Aromatase Inhibitor in Combination With Lapatinib, Trastuzumab or Both for the Treatment of Hormone Receptor Positive, HER2+ Metastatic Breast Cancer | Completed | USA | ITA | GBR | FRA | ESP | DEU | CAN | BEL | AUS | 29 |
NCT03784014 | Phase III | Ceritinib Dabrafenib + Trametinib Capmatinib Durvalumab + Olaparib Nilotinib Futibatinib Trametinib Palbociclib Glasdegib Lapatinib | Molecular Profiling of Advanced Soft-tissue Sarcomas (MULTISARC) | Active, not recruiting | FRA | 0 |
NCT01868503 | Phase II | Lapatinib | Lapatinib Ditosylate and Radiation Therapy in Treating Patients With Locally Advanced or Locally Recurrent Breast Cancer | Terminated | USA | 0 |
NCT01427322 | Phase I | Lapatinib | Randomized RT +/- Lapatinib for Advanced Solid Tumor Cancer Patients Receiving Radiation Therapy for Metastatic Disease | Terminated | USA | 0 |
NCT00863122 | Phase I | Lapatinib | Concentration and Activity of Lapatinib in Vestibular Schwannomas | Completed | USA | 0 |
NCT02551718 | Phase I | Bosutinib Irinotecan Romidepsin Busulfan Melphalan Nilotinib Crizotinib Cytarabine Mitoxantrone Dasatinib Pazopanib Paclitaxel Clofarabine Hydroxyurea Tretinoin Carfilzomib Nelarabine Bexarotene Pentostatin Everolimus Cabozantinib Mercaptopurine Methotrexate Cladribine Thioguanine Daunorubicin Ponatinib Etoposide Afatinib Gefitinib Gemcitabine Regorafenib Arsenic trioxide Trametinib Imatinib Erlotinib Dabrafenib Decitabine Axitinib Azacitidine Ruxolitinib Fludarabine Lapatinib Ceritinib Sirolimus Sorafenib Lomustine Sunitinib Cabazitaxel Temsirolimus Topotecan Bortezomib Pralatrexate | High Throughput Drug Sensitivity Assay and Genomics- Guided Treatment of Patients With Relapsed or Refractory Acute Leukemia | Completed | USA | 0 |
NCT00790816 | Phase I | Lapatinib + Paclitaxel Lapatinib Lapatinib + Trastuzumab Capecitabine + Lapatinib Lapatinib + Letrozole Capecitabine + Lapatinib + Oxaliplatin Gemcitabine + Lapatinib Docetaxel + Lapatinib Fluorouracil + Lapatinib + Leucovorin + Oxaliplatin Fluorouracil + Irinotecan + Lapatinib + Leucovorin | Continuation Study of Lapatinib Monotherapy or Lapatinib in Combination With Other Anti-cancer Agents | Completed | USA | NLD | ESP | CAN | 1 |
NCT02559778 | Phase I | Bortezomib Crizotinib Lapatinib Vorinostat Eflornithine Sorafenib Dasatinib | Pediatric Precision Laboratory Advanced Neuroblastoma Therapy (PEDS-PLAN) | Recruiting | USA | CAN | 0 |
NCT02101905 | Phase I | Lapatinib | Lapatinib Ditosylate Before Surgery in Treating Patients With Recurrent High-Grade Glioma | Active, not recruiting | USA | 0 |
NCT00759642 | Phase II | Lapatinib | Lapatinib in Women With Metastatic Breast Cancer Who Have Failed Prior Antihormone Therapy | Terminated | USA | 0 |