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Therapy Name | Afatinib |
Synonyms | |
Therapy Description |
Gilotrif (afatinib) is a second-generation pan-Egfr inhibitor with activity against EGFR T790M and EGFR exon 19 and 21 deletions, and also inhibits ERBB2 (HER2), ERBB3 (HER3), ERBB4 (HER4) (PMID: 24435321, PMID: 25505694). Gilotrif (afatinib) is FDA approved for use in non-small cell lung cancer patients harboring non-resistant EGFR mutations, including exon 19 deletions, L858R, S768I, G719X, and L861Q, and for patients with metastatic squamous NSCLC (FDA.gov). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Afatinib | Gilotrif | BIBW 2992|Giotrif | EGFR Inhibitor (Pan) 61 EGFR Inhibitor 2nd gen 5 HER inhibitor (Pan) 6 | Gilotrif (afatinib) is a second-generation pan-Egfr inhibitor with activity against EGFR T790M and EGFR exon 19 and 21 deletions, and also inhibits ERBB2 (HER2), ERBB3 (HER3), ERBB4 (HER4) (PMID: 24435321, PMID: 25505694). Gilotrif (afatinib) is FDA approved for use in non-small cell lung cancer patients harboring non-resistant EGFR mutations, including exon 19 deletions, L858R, S768I, G719X, and L861Q, and for patients with metastatic squamous NSCLC (FDA.gov). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
ERBB3 V104L | Her2-receptor positive breast cancer | sensitive | Afatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gilotrif (afatinib) treatment inhibited activation of Erbb2 (Her2) and decreased viability and proliferation in an ERBB2 (HER2)-positive breast cancer cell line expressing ERBB3 (HER3) V104L in culture (PMID: 38751013). | 38751013 |
ERBB4 R687K | Advanced Solid Tumor | sensitive | Afatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gilotrif (afatinib) inhibited growth of a transformed cell line expressing ERBB4 R687K in culture (PMID: 36860695). | 36860695 |
ERBB4 mutant | lung squamous cell carcinoma | predicted - sensitive | Afatinib | Phase III | Actionable | In a Phase III trial (LUX-Lung 8), secondary analysis demonstrated favorable outcomes with Gilotrif (afatinib) treatment compared to Tarceva (erlotinib) in lung squamous cell carcinoma patients with ERBB (HER) family mutations, and ERBB4 (HER4) mutations predicted an OS (HR=0.22) and PFS (HR=0.21) benefit for Gilotrif (afatinib) over Tarceva (erlotinib) treatment (PMID: 29902295; NCT01523587). | 29902295 |
ERBB4 G741R | Advanced Solid Tumor | sensitive | Afatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gilotrif (afatinib) inhibited growth of a transformed cell line expressing ERBB4 G741R in culture (PMID: 36860695). | 36860695 |
ERBB4 G1109C | head and neck squamous cell carcinoma | sensitive | Afatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Gilotrif (afatinib) treatment induced apoptosis in head and neck squamous cell carcinoma cells harboring ERBB4 (HER4) G1109C in culture and inhibited tumor growth in cell line xenograft models (PMID: 27207775). | 27207775 |
ERBB3 V104M | urinary bladder cancer | predicted - sensitive | Afatinib | Case Reports/Case Series | Actionable | In a Phase II clinical trial, a patient with ERBB3 V104M mutant urothelial carcinoma had improved progression free survival when treated with Gilotrif (afatinib), and median PFS was 6.6 months for patients with ERBB2 or ERBB3 alterations relative to 1.4 months for patients lacking alterations (PMID: 27044931). | 27044931 |
ERBB3 G284R | transitional cell carcinoma | sensitive | Afatinib | Case Reports/Case Series | Actionable | In a Phase II trial, a patient with urothelial carcinioma harboring ERBB3 G284R demonstrated stable disease for 7 months when treated with Gilotrif (afatinib) (J Clin Oncol 33, 2015 (suppl 7; abstr 312)). | detail... |
ERBB4 G936R | Advanced Solid Tumor | sensitive | Afatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB4 G936R demonstrated sensitivity to Gilotrif (afatinib) similar to wild-type Erbb2 in culture, resulting in decreased cell viability (PMID: 33323455). | 33323455 |
ERBB4 A17V | hematologic cancer | sensitive | Afatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB4 A17V demonstrated sensitivity to Gilotrif (afatinib) similar to wild-type Erbb4 in culture, resulting in decreased cell viability (PMID: 33323455). | 33323455 |
ROS1 rearrange | lung non-small cell carcinoma | no benefit | Afatinib | Guideline | Actionable | EGFR tyrosine kinase inhibitors including Tarceva (erlotinib), Iressa (gefitinib), Gilotrif (afatinib), and Tagrisso (osimertinib) are not indicated for use as subsequent therapy in ROS1 rearranged non-small cell lung cancer patients who relapsed on Alecensa (alectinib), Xalkori (crizotinib), or Zykadia (ceritinib) (NCCN.org). | detail... |
BRAF G469V | lung adenocarcinoma | sensitive | Afatinib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, Gilotrif (afatinib) treatment inhibited viability of cells derived from a patient-derived xenograft (PDX) model of lung adenocarcinoma harboring BRAF G469V in culture and led to inhibition of tumor growth in a patient-derived xenograft (PDX) model (PMID: 34648945). | 34648945 |
ALK rearrange | lung non-small cell carcinoma | no benefit | Afatinib | Guideline | Actionable | EGFR tyrosine kinase inhibitors including Tarceva (erlotinib), Iressa (gefitinib), Gilotrif (afatinib), and Tagrisso (osimertinib) are not indicated for use as subsequent therapy in ALK rearranged non-small cell lung cancer patients who relapsed on Alecensa (alectinib), Xalkori (crizotinib), or Zykadia (ceritinib) (NCCN.org). | detail... |
ERBB3 G284R | urinary bladder cancer | sensitive | Afatinib | Case Reports/Case Series | Actionable | In a Phase II clinical trial, a patient with ERBB3 G284R mutant urothelial carcinoma had improved progression free survival when treated with Gilotrif (afatinib), and median PFS was 6.6 months for patients with ERBB2 or ERBB3 alterations relative to 1.4 months for patients lacking alterations (PMID: 27044931). | 27044931 |
ERBB4 E715K | Advanced Solid Tumor | sensitive | Afatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gilotrif (afatinib) inhibited growth of a transformed cell line expressing ERBB4 E715K in culture (PMID: 36860695). | 36860695 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT01553942 | Phase II | Afatinib Cisplatin Pemetrexed Disodium | Afatinib With CT and RT for EGFR-Mutant NSCLC | Active, not recruiting | USA | 0 |
NCT03878524 | Phase I | Oxaliplatin Palbociclib Vemurafenib Sirolimus Tretinoin Celecoxib Ipilimumab Ruxolitinib Dasatinib Abiraterone Idelalisib Trametinib Imatinib Erlotinib Carboplatin Olaparib Panobinostat Bortezomib Afatinib Fluorouracil Vorinostat Pembrolizumab Leucovorin Enzalutamide Ponatinib Nivolumab Everolimus Sunitinib Cabazitaxel Cabozantinib Lenvatinib Pertuzumab Sorafenib Venetoclax Bevacizumab | A Personalized Medicine Study for Patients With Advanced Cancer of the Breast, Prostate, Pancreas or Those With Refractory Acute Myelogenous Leukemia (SMMART) | Terminated | USA | 0 |
NCT01649284 | Phase I | Afatinib | Afatinib Expanded Access Program | Approved for marketing | USA | 0 |
NCT02115048 | Phase II | Afatinib Letrozole | Clinical Study for the Treatment of Breast Cancer the Patient Will Receive Afatinib Plus Letrozole or Letrozole Alone | Terminated | USA | ESP | 2 |
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 |
NCT02372006 | Phase Ib/II | Afatinib | Trial of Afatinib in Pediatric Tumours | Completed | USA | NLD | ITA | GBR | FRA | ESP | DEU | CAN | AUT | AUS | 2 |
NCT01824823 | Phase II | Afatinib | Afatinib After Chemoradiation and Surgery in Treating Patients With Stage III-IV Squamous Cell Carcinoma of the Head and Neck at High-Risk of Recurrence | Terminated | USA | 0 |
NCT02451553 | Phase I | Afatinib Capecitabine | Afatinib Dimaleate and Capecitabine in Treating Patients With Advanced Refractory Solid Tumors, Pancreatic Cancer or Biliary Cancer | Completed | USA | 0 |
NCT02695290 | Phase III | Afatinib | Afatinib in EGFR+NSCLC (Recurrent or Stage IV) - Patients With Poor Performance Status (ECOG 2 or 3) | Terminated | USA | 0 |
NCT02491099 | Phase II | Afatinib | A Phase II Evaluation of Afatinibin Patients With Persistent or Recurrent HER2-positive Uterine Serous Carcinoma (Afatinib) | Recruiting | USA | 0 |
NCT01647711 | Phase I | Afatinib | A Study of Intermittent, High-dose Afatinib to Determine the Maximal Tolerated Dose and Assess Activity of This Dose Against Non-small Cell Lung Cancer With T790M Mutations | Completed | USA | 0 |
NCT01783587 | Phase I | Afatinib Docetaxel | Safety Study of Afatinib and Postoperative Radiation Therapy to Treat Head and Neck Cancer | Completed | USA | 0 |
NCT05432518 | Phase I | Olaparib Palbociclib Afatinib Everolimus Dasatinib | GBM Personalized Trial | Recruiting | CAN | 0 |
NCT02423525 | Phase I | Afatinib | Safety Study of Afatinib for Brain Cancer | Completed | USA | 0 |
NCT02271906 | Phase II | Afatinib | The ATTAIN Study: A Therapeutic Trial of Afatinib In the Neoadjuvant Setting | Terminated | USA | 0 |
NCT02122172 | Phase II | Afatinib | Afatinib in Advanced Refractory Urothelial Cancer | Terminated | USA | 0 |
NCT05070403 | Phase II | Afatinib | Study of Afatinib in Advanced Cutaneous Squamous Cell Carcinoma | Recruiting | USA | 0 |
NCT04410653 | Phase II | Afatinib | Afatinib in Advanced NRG1-Rearranged Malignancies | Completed | DEU | 0 |
NCT02768337 | Phase Ib/II | Afatinib | Cambridge Brain Mets Trial 1 (CamBMT1) | Terminated | GBR | 0 |
NCT02541903 | Phase II | Afatinib | Trial Using Gilotrif for Advanced Penile Squamous Cell Carcinoma | Terminated | USA | 0 |
NCT01746251 | Phase II | Afatinib | Adjuvant Afatinib in Stage I-III NSCLC With EGFR Mutation | Unknown status | USA | 0 |
NCT03297606 | Phase II | Bosutinib Palbociclib Vismodegib Ipilimumab + Nivolumab Cobimetinib + Vemurafenib Temsirolimus Olaparib Erlotinib Crizotinib Sunitinib Afatinib Dasatinib Pertuzumab + Trastuzumab Axitinib | Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR) (CAPTUR) | Recruiting | CAN | 0 |
NCT02506517 | Phase II | Afatinib | A Study of Afatinib in Patients With Advanced Cancer With Changes in the HER Gene | Completed | CAN | 0 |
NCT03088059 | Phase II | Niraparib Durvalumab + Monalizumab Methotrexate Carboplatin Rogaratinib Mitomycin C Docetaxel Afatinib Paclitaxel Durvalumab Monalizumab Palbociclib Bleomycin Gemcitabine Fluorouracil | Biomarker-based Study in R/M SCCHN (UPSTREAM) | Active, not recruiting | ITA | GBR | FRA | ESP | BEL | 0 |
NCT02438722 | Phase II | Afatinib Afatinib + Cetuximab | S1403, Afatinib Dimaleate With or Without Cetuximab in Treating Patients With Newly Diagnosed Stage IV or Recurrent, EGFR Mutation Positive Non-small Cell Lung Cancer | Active, not recruiting | USA | 0 |
NCT02183883 | Phase II | Afatinib | Deciphering Afatinib Response and Resistance With INtratumour Heterogeneity (DARWIN1) | Completed | GBR | 0 |
NCT03083678 | Phase II | Afatinib | Afatinib in Locally Advanced and Metastatic Chordoma | Unknown status | NLD | ITA | GBR | 0 |
NCT05298176 | Phase II | Afatinib Afatinib + Carboplatin + Pemetrexed Disodium Carboplatin + Osimertinib + Pemetrexed Disodium Osimertinib | Combining Afatinib and Concurrent Chemotherapy, Followed by Osimertinib and Concurrent Chemotherapy, in Untreated EGFR Positive NSCLC Tumors (COMBINATION) | Recruiting | NLD | 0 |
NCT02514174 | FDA approved | Afatinib | Afatinib Treatment for Patients With EGFR Mutation Positive NSCLC Who Are Age 70 or Older | Completed | USA | 0 |
NCT02795156 | Phase II | Cabozantinib Afatinib Regorafenib | Study Assessing Activity of Molecularly Matched Targeted Therapies in Select Tumor Types Based on Genomic Alterations | Completed | USA | 0 |
NCT01345669 | Phase III | Afatinib | LUX-Head&Neck 2: A Phase III Trial of Afatinib (BIBW 2992) Versus Placebo for the Treatment of Head and Neck Squamous Cell Cancer After Treatment With Chemo-radiotherapy | Terminated | USA | NLD | ITA | GBR | FRA | ESP | DEU | CAN | BEL | AUT | AUS | 18 |
NCT02693535 | Phase II | Cobimetinib + Vemurafenib Atezolizumab + Talazoparib Regorafenib Larotrectinib Trastuzumab + Tucatinib Ipilimumab + Nivolumab Palbociclib Afatinib Entrectinib Talazoparib Pembrolizumab Temsirolimus Pertuzumab + Trastuzumab Atezolizumab + Pertuzumab/trastuzumab/hyaluronidase-zzxf Crizotinib Abemaciclib Sunitinib Olaparib | TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer (TAPUR) | Recruiting | USA | 0 |