Therapy Detail

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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).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Lapatinib Tykerb Lapatinib Ditosylate EGFR Inhibitor (Pan) 55 HER2 Inhibitor 36 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).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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
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
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
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
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
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 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
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 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
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
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
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 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
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 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
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
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 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
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
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
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
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
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

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
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 | ESP | CAN 2
NCT02559778 Phase I Bortezomib Crizotinib Lapatinib Vorinostat Eflornithine Sorafenib Dasatinib Pediatric Precision Laboratory Advanced Neuroblastoma Therapy Recruiting USA 0
NCT01868503 Phase II Lapatinib Lapatinib Ditosylate and Radiation Therapy in Treating Patients With Locally Advanced or Locally Recurrent Breast Cancer Terminated USA 0
NCT00939523 Phase II Lapatinib Targeted Therapy With Lapatinib in Patients With Recurrent Pituitary Tumors Resistant to Standard Therapy Completed USA 0
NCT02101905 Phase I Lapatinib Lapatinib Ditosylate Before Surgery in Treating Patients With Recurrent High-Grade Glioma Active, not recruiting 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
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
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) Recruiting ITA 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
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 | FRA | ESP | DEU | CAN | BEL 31
NCT03784014 Phase III Ceritinib Dabrafenib + Trametinib Capmatinib Durvalumab + Olaparib Nilotinib Futibatinib Trametinib Palbociclib Glasdegib Lapatinib Molecular Profiling of Advanced Soft-tissue Sarcomas (MULTISARC) Recruiting FRA 0
NCT00759642 Phase II Lapatinib Lapatinib in Women With Metastatic Breast Cancer Who Have Failed Prior Antihormone Therapy Terminated USA 0
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
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


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