Targeted Cancer Therapies Guide

The table below lists all targeted cancer therapies with regulatory approval as of July 2017, grouped by their respective mechanisms of action.

Main Group Mechanism of Action Substances (Targets)
Anti-Hormone Therapies Estrogen Receptor Modulators Diethylstilbestrol, Fulvestrant, Tamoxifen, Toremifen
Aromatase Inhibitors Anastrozole, Exemestane, Letrozole
Androgen Receptor Inhibitors Bicalutamide, Enzalutamide, Flutamide
GnRH Receptor Modulators Abarelix, Degarelix, Leuprorelin, Triptorelin
(Growth-) Receptor Inhibitors Intracellular Tyrosine Kinase Inhibitors Afatinib (EGFR), Brigatinib (ALK, EGFR), Erlotinib (EGFR, HER1R), Gefitinib (EGFR), Lapatinib (EGFR, HER2), Lenvatinib (VEGFR1-3, FGFR1-4, PDGFRα, KIT, RET), Neratinib (EGFR, HER2), Osimertinib (EGFR T790M), Sunitinib (PDGF, VEGF, KIT, FLT, RET)
Extracellular Receptor Inhibitors Bevacizumab (VEGF), Cetuximab (EGFR), Dinutuximab (GD2), Necitumumab (EGFR), Olaratumab (PDGFRα), Panitumumab (EGFR), Pertuzumab (HER2), Trastuzumab (HER2)
Protein Inhibitors ALK Inhibitors Alectinib, Ceritinib, Crizotinib (ALK, MET, ROS1)
B-Raf Inhibitors Dabrafenib, Encorafenib, Vemurafenib
BCR-ABL Inhibitors Dasatinib (BCR-ABL, SRC), Imatinib (BCR-ABL), Nilotinib (BCR-ABL)
MEK Inhibitors Binimetinib, Cobimetinib, Trametinib
mTOR Inhibitors Everolimus, Temsirolimus
Immunotherapy Immune-Checkpoint Inhibitors Atezolizumab (PD-L1), Avelumab (PD-L1), Durvalumab (PD-L1), Ipilimumab (CTLA-4), Nivolumab (PD-1), Pembrolizumab (PD-1)
Off-label Use: The Drug Rediscovery Protocol (DRUP Trial)