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Table 2 Examples of drugs targeting downstream effectors of tyrosine kinase receptors that are in clinical development

From: Receptor tyrosine kinases and downstream pathways as druggable targets for cancer treatment: the current arsenal of inhibitors

TARGET DRUG DISEASE TRIAL PHASE STATUS CLINICAL TRIAL NUMBER
BRAF;CRAF/RTK Sorafenib + Vinorelbine Breast Cancer I/II Completed NCT00828074
BRAF;CRAF/Microtubule/DNA replication Sorafenib + Paclitaxel + Carboplatin Ovarian Cancer II Completed NCT00390611
Pan RAF LY3009120 Advanced or Metastatic Cancer I Active NCT02014116
Pan RAF PLX8394 Advanced Cancers I/II Terminated NCT02012231
Pan RAF PLX8394 Advanced Unresectable Solid Tumors I/II Recruiting NCT02428712
MEK1/2 Trametinib Oral Cavity Squamous Cell Cancer II Completed NCT01553851
MEK1/2 Trametinib Cancer II Active NCT01072175
MEK1/2 Dabrafenib Papillary Thyroid Carcinoma Unknown Completed NCT01534897
MEK1/2/BRAF/BRAF Binimetinib + Encorafenib + Vemurafenib Melanoma III Active NCT01909453
MEK1/2/BRAF/EGFR Binimetinib + Encorafenib + Cetuximab Metastatic Colorectal Cancer III Recruiting NCT02928224
MEK1/2/CDK4/6 Binimetinib + Palbociclib NSCLC I/II Recruiting NCT03170206
BRAF/EGFR Encorafenib + Cetuximab Metastatic Colorectal Cancer I/II Active NCT01719380
BRAF Encorafenib Melanoma and Metastatic Colorectal Cancer I Active NCT01436656
BRAF + PD-1/PD-L1 axis Vemurafenib + Pembrolizumab Melanoma I Recruiting NCT02818023
BRAF + PD-1/PD-L1 axis Vemurafenib + Atezolizumab Melanoma   Active NCT01656642
PI3K/Estrogen Receptor Buparsilib (BKM120) + Fulvestrant Metastatic Breast Cancer III Active NCT01633060
PI3K/EGFR, HER2neu Buparsilib (BKM120) + Lapatinib Breast Cancer I/II Suspended (data analysis) NCT01589861
PI3K Alpelisib + Fulvestrant Breast Cancer III Recruiting NCT02437318
PI3K Alpesilib + Fulvestrant Breast Cancer II Not yet recruiting NCT03386162
PI3K/Aromatase Alpelisib + Fulvestrant + Letrozole Breast Cancer II Recruiting NCT03056755
PI3K/mTOR/Aromatase Alpelisib + Everolimus + Exemestane Breast Cancer, Kidney Cancer, Pancreatic Neuroendocrine Cancer I Active NCT02077933
PI3K Taselisib + Fulvestrant Breast Cancer III Active NCT02340221
PI3K/Aromatase Taselisib + Letrozole Breast Cancer II Completed NCT02273973
PI3K Taselisib Recurrent Squamous Cell Lung Carcinoma, Stage IV Squamous Cell Lung Carcinoma II Active NCT02785913
PI3K Copanlisib (BAY80-6946) Non-Hodgkin Lymphoma III Active NCT02369016
PI3K/CD20 Copanlisib (BAY80-6946) + Rituximab Non-Hodgkin Lymphoma III Recruiting NCT02367040
PI3K Copanlisib (BAY80-6946) Diffuse Large B-cell Lymphoma (DLBCL) II Active NCT02391116
AKT/Androgen Receptor AZD5363 + Enzalutamide Adenocarcinoma of the Prostate II Recruiting NCT02525068
AKT/Microtubule AZD5363 + Paclitaxel Advanced Gastric Cancer II Recruiting NCT02451956
AKT AZD5363 Metastatic Castrate-Resistant Prostate Cancer (mCRPC) I Completed NCT01692262
  1. NSCLC Non-Small Cell Lung Cancer, RTK receptor tyrosine kinase