Therapy Detail
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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). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Afatinib | Gilotrif | BIBW 2992|Giotrif | EGFR Inhibitor (Pan) 63 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). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| 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 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 |
| 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 |
| 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 |
| 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 |
| 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 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 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 |
| 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 |
| 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 |
| 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 |
| 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 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| 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 |
| 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 |
| NCT01746251 | Phase II | Afatinib | Adjuvant Afatinib in Stage I-III NSCLC With EGFR Mutation | Unknown status | USA | 0 |
| NCT02768337 | Phase Ib/II | Afatinib | Cambridge Brain Mets Trial 1 (CamBMT1) | Terminated | 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) | Completed | NLD | 0 |
| NCT02271906 | Phase II | Afatinib | The ATTAIN Study: A Therapeutic Trial of Afatinib In the Neoadjuvant Setting | Terminated | USA | 0 |
| NCT02465060 | Phase II | Erdafitinib Trametinib Crizotinib Sapanisertib Fexagratinib Dasatinib Osimertinib Palbociclib Capivasertib Larotrectinib Ulixertinib Nivolumab + Relatlimab Copanlisib Sunitinib Nivolumab Pertuzumab + Trastuzumab Ipatasertib Dabrafenib + Trametinib Binimetinib Adavosertib Afatinib Defactinib GSK2636771 Vismodegib Ado-trastuzumab emtansine Taselisib | Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) | Active, not recruiting | USA | 2 |
| NCT01553942 | Phase II | Afatinib Cisplatin Pemetrexed Disodium | Afatinib With CT and RT for EGFR-Mutant NSCLC | Active, not recruiting | USA | 0 |
| NCT02514174 | FDA approved | Afatinib | Afatinib Treatment for Patients With EGFR Mutation Positive NSCLC Who Are Age 70 or Older | Completed | USA | 0 |
| 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 |
| NCT06486142 | Phase III | Osimertinib Afatinib Dacomitinib | EGFR-mutated Lung Cancer in Randomized Investigator-Initiated Study (ERIS) | Recruiting | SWE | 0 |
| NCT02122172 | Phase II | Afatinib | Afatinib in Advanced Refractory Urothelial Cancer | Terminated | USA | 0 |
| NCT01783587 | Phase I | Afatinib Docetaxel | Safety Study of Afatinib and Postoperative Radiation Therapy to Treat Head and Neck Cancer | Completed | USA | 0 |
| NCT02183883 | Phase II | Afatinib | Deciphering Afatinib Response and Resistance With INtratumour Heterogeneity (DARWIN1) | Completed | GBR | 0 |
| NCT05432518 | Phase I | Olaparib Palbociclib Afatinib Everolimus Dasatinib | GBM Personalized Trial | Recruiting | CAN | 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 | ROU | ESP | 1 |
| NCT02423525 | Phase I | Afatinib | Safety Study of Afatinib for Brain Cancer | Completed | USA | 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 |
| NCT03083678 | Phase II | Afatinib | Afatinib in Locally Advanced and Metastatic Chordoma | Completed | NLD | ITA | GBR | 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 | Expanded access | Afatinib | Afatinib Expanded Access Program | Approved for marketing | 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 |
| 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 |
| 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 |
| 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 | SWE | NLD | ITA | ISR | HUN | GRC | GBR | FRA | FIN | ESP | DNK | DEU | CZE | CHE | CAN | BRA | BEL | AUT | AUS | ARG | 8 |
| NCT04410653 | Phase II | Afatinib | Afatinib in Advanced NRG1-Rearranged Malignancies | Completed | DEU | 0 |
| NCT02541903 | Phase II | Afatinib | Trial Using Gilotrif for Advanced Penile Squamous Cell Carcinoma | Terminated | USA | 0 |
| NCT02506517 | Phase II | Afatinib | A Study of Afatinib in Patients With Advanced Cancer With Changes in the HER Gene | Completed | CAN | 0 |
| NCT05070403 | Phase II | Afatinib | Study of Afatinib in Advanced Cutaneous Squamous Cell Carcinoma | Recruiting | USA | 0 |
| NCT06648096 | Phase Ib/II | Afatinib | Afatinib in Patients with Fanconi Anemia (FA) and Advanced Head and Neck Squamous Cell Carcinoma (HNSCC) (AFAN) | Recruiting | ESP | DEU | 0 |
| NCT02491099 | Phase II | Afatinib | A Phase II Evaluation of Afatinib in Patients With Persistent or Recurrent HER2-positive Uterine Serous Carcinoma (Afatinib) | Recruiting | USA | 0 |
| NCT02372006 | Phase Ib/II | Afatinib | Trial of Afatinib in Pediatric Tumours | Completed | USA | NLD | ITA | GBR | FRA | ESP | DNK | DEU | CAN | AUT | AUS | 1 |
| 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 |
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