Table 1:
Solid tumors: Fusion target | |||||
Drug | Disease Indication | Line of Therapy | Aberrant gene | Number of studies** | Response Rate (%)** |
Alectinib | NSCLC | 2+ | ALK | 1 | 79% |
Brigatinib | NSCLC | 2+ | ALK | 1 | 53% |
Ceritinib | NSCLC | 2+ | ALK | 1 | 73% |
Crizotinib | NSCLC | 1 | ALK/ROS1 | 2 | 56% |
Entrectinib | Solid tumors | 1+ | NTRK/ROS1/ALK | 1 | 78% |
Larotrectinib | Solid tumors | 1+ | NTRK | 1 | 75% |
Solid tumor: Non-fusion target | |||||
Drug | Disease Indication | Line of Therapy | Aberrant gene | Number of studies** | Response Rate (%) |
Afatinib | NSCLC | 1+ | EGFR | 1 | 50% |
Dabrafenib | Melanoma | 1+ | BRAF | 1 | 54% |
Dacomitinib | NSCLC | 1+ | EGFR | 1 | 75% |
Erlotinib | NSCLC | 1+ | EGFR | 1 | 65% |
Gefitinib | NSCLC | 1 | EGFR | 1 | 70% |
Imatinib | GIST | 1 | KIT | 1 | 51% |
Olaparib | Ovarian | 4+ | BRCA | 1 | 34% |
Osimertinib | NSCLC | 1+ | EGFR | 1 | 51% |
Rucaparib | Ovarian | 3+ | BRCA | 1 | 54% |
Talazoparib | Breast | 2+ | BRCA | 1 | 50% |
TDM-1 | Breast | 2+ | HER2 | 1 | 44% |
Trastuzumab | Breast | 2+ | HER2 | 1 | 14% |
Vemurafenib | Melanoma | 1+ | BRAF | 1 | 48% |
Hematologic malignancies: Fusion Target | |||||
Drug | Disease Indication | Line of Therapy | Aberrant gene | Number of studies** | Response Rate (%) |
All trans-retinoic acid | APL | 1+ | PML-RARA | 1 | 72% |
Bosutinib | CML | 2+ | BCR-ABL | 2 | 31% |
Dasatinib | CML | 1+ | BCR-ABL | 2 | 63% |
Imatinib | CML | 1 | BCR-ABL | 1 | 73% |
Nilotinib | CML | 1+ | BCR-ABL | 1 | 84% |
Ponatinib | CML | 2+ | BCR-ABL | 1 | 46% |
Hematologic malignancies: Target non-fusion | |||||
Drug | Disease Indication | Line of Therapy | Aberrant gene | Number of studies** | Response Rate (%) |
Enasidenib | AML | 2+ | IDH2 | 1 | 23% |
Gilteritinib | AML | 2+ | FLT3 | 1 | 21% |
Ivosidenib | AML | 2+ | IDH1 | 1 | 33% |
Vemurafenib | ECD | 1+ | BRAF | 1 | 55% |
Approved by the Food and Drug Administration (FDA)
Refers to number of studies provided in FDA package insert; Response rate is per package insert. If more than one study listed, the mean is given
Abbreviations: AML=acute myelogenous leukemia; CML=chronic myelogenous leukemia; ECD=Erdheim-Chester disease; NHL=non-Hodgkin’s lymphoma; NSCLC=non-small cell lung cancer