EGFR tyrosine kinase inhibitor (third-generation)
This page covers all EGFR tyrosine kinase inhibitor (third-generation) drugs tracked by Drug Landscape: marketed products and active clinical-stage compounds, targeting EGFR (Epidermal Growth Factor Receptor), EGFR; thymidylate synthase and folate-dependent enzymes, HER2, EGFR.
Targets
EGFR (Epidermal Growth Factor Receptor) · EGFR; thymidylate synthase and folate-dependent enzymes · HER2, EGFR · EGFR · EGFR (epidermal growth factor receptor) · EGFR exon 20 insertion mutations · EGFR (epidermal growth factor receptor) and c-MET (mesenchymal-epithelial transition factor) · EGFR (erlotinib); DNA alkylation (temozolomide) · EGFR (gefitinib); thymidylate synthase, dihydrofolate reductase (pemetrexed); DNA (platinum agents) · EGFR (Epidermal Growth Factor Receptor), particularly mutant forms including T790M
Marketed (7)
- Osimertinib (Osi) · AbbVie · Oncology
Osimertinib is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to and inhibits mutant EGFR, including T790M resistance mutations, blocking downstream signaling in cancer cells. - Erlotinib, Pemetrexed · Hunan Province Tumor Hospital · Oncology
This combination uses erlotinib to inhibit EGFR signaling and pemetrexed to disrupt folate-dependent nucleotide synthesis, together targeting non-small cell lung cancer through dual pathways. - placebo matching lapatinib · GlaxoSmithKline · Oncology
Lapatinib is a small-molecule tyrosine kinase inhibitor that blocks HER2 and EGFR signaling to inhibit cancer cell growth. - Sequential and maintenance icotinib · Betta Pharmaceuticals Co., Ltd. · Oncology
Icotinib is a small-molecule tyrosine kinase inhibitor that selectively blocks epidermal growth factor receptor (EGFR) signaling to inhibit tumor cell proliferation. - Maintenance icotinib · Betta Pharmaceuticals Co., Ltd. · Oncology
Icotinib is a small-molecule tyrosine kinase inhibitor that selectively blocks epidermal growth factor receptor (EGFR) signaling to inhibit tumor cell proliferation. - Sequential Icotinib Plus Chemotherapy · Betta Pharmaceuticals Co., Ltd. · Oncology
Icotinib is an EGFR tyrosine kinase inhibitor that blocks epidermal growth factor receptor signaling, used sequentially with chemotherapy to treat EGFR-mutant lung cancer. - Icotinib plus WBRT · Betta Pharmaceuticals Co., Ltd. · Oncology
Icotinib is an EGFR tyrosine kinase inhibitor that blocks epidermal growth factor receptor signaling in cancer cells, combined with whole-brain radiotherapy (WBRT) to treat brain metastases.
Phase 3 pipeline (31)
- ZD1839 (Gefitinib) · AstraZeneca · Oncology
ZD1839 (Gefitinib) is a small molecule that inhibits the epidermal growth factor receptor (EGFR) tyrosine kinase. - TAK-788 · Millennium Pharmaceuticals, Inc. · Oncology
TAK-788 is a selective inhibitor of epidermal growth factor receptor (EGFR) exon 20 insertion mutations. - ASKC202+ Limertinib · Jiangsu Aosaikang Pharmaceutical Co., Ltd. · Oncology
ASKC202 is a bispecific antibody targeting EGFR and c-MET, combined with limertinib, a third-generation EGFR tyrosine kinase inhibitor, to overcome resistance in EGFR-mutant lung cancer. - Firmonertinib Mesilate Tablets · Allist Pharmaceuticals, Inc. · Oncology
Firmonertinib mesilate is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to and inhibits mutant EGFR, including T790M resistance mutations. - erlotinib HCl · Genentech, Inc. · Oncology
Erlotinib is a small-molecule tyrosine kinase inhibitor that blocks the epidermal growth factor receptor (EGFR), preventing cancer cell proliferation and survival. - HS-10241+ Almonertinib · Jiangsu Hansoh Pharmaceutical Co., Ltd. · Oncology
HS-10241 is a third-generation EGFR tyrosine kinase inhibitor designed to target EGFR mutations including common and uncommon variants, often combined with almonertinib (a third-generation EGFR-TKI) to enhance efficacy against resistant lung cancers. - Furmonertinib Mesilate Tablets · Allist Pharmaceuticals, Inc. · Oncology
Furmonertinib is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to and inhibits mutant EGFR, including T790M resistance mutations. - Erlotinib, Temozolomide · Tel-Aviv Sourasky Medical Center · Oncology
This combination uses erlotinib to inhibit EGFR signaling and temozolomide to alkylate DNA, together targeting cancer cell growth and survival. - Placebo Gefitinib Tablets · Hangzhou ACEA Pharmaceutical Research Co., Ltd. · Oncology
Gefitinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. - EGFR-TK Inhibitor · Xinqiao Hospital of Chongqing · Oncology
This drug inhibits tyrosine kinase activity of the epidermal growth factor receptor (EGFR), blocking downstream signaling that drives cancer cell proliferation. - Active Comparator (erlotinib) · Pfizer · Oncology
Erlotinib is a tyrosine kinase inhibitor that blocks epidermal growth factor receptor (EGFR) signaling to inhibit cancer cell proliferation. - Aumolertinib Oral Tablet · Shanghai Cancer Hospital, China · Oncology
Aumolertinib is a third-generation EGFR tyrosine kinase inhibitor that selectively targets EGFR mutations, including T790M resistance mutations, to inhibit tumor cell proliferation. - Almonertinib plus carboplatin and pemetrexed · Cancer Institute and Hospital, Chinese Academy of Medical Sciences · Oncology
Almonertinib inhibits EGFR tyrosine kinase while carboplatin and pemetrexed provide platinum-based chemotherapy and antimetabolite activity, respectively, to target non-small cell lung cancer. - Gefitinib and Pemetrexed/platinum · Sun Yat-sen University · Oncology
This combination uses gefitinib to inhibit EGFR signaling in lung cancer cells while pemetrexed/platinum chemotherapy provides additional cytotoxic activity through multiple mechanisms. - Erlotinib /Gefitinib · Zhejiang Cancer Hospital · Oncology
Erlotinib and gefitinib are tyrosine kinase inhibitors that block epidermal growth factor receptor (EGFR) signaling to inhibit cancer cell proliferation. - Gefitinib mono-therapy · Sun Yat-sen University · Oncology
Gefitinib is a tyrosine kinase inhibitor that selectively blocks epidermal growth factor receptor (EGFR) signaling to inhibit cancer cell proliferation. - Cross-over to Osimertinib · AstraZeneca · Oncology
Osimertinib is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to and inhibits mutant EGFR, blocking downstream signaling in EGFR-mutant lung cancers. - Tarceva (erlotinib HCl) · Genentech, Inc. · Oncology
Tarceva (erlotinib HCl) works by inhibiting the epidermal growth factor receptor (EGFR) tyrosine kinase. - ZD1839 · University of Chicago · Oncology
ZD1839 is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that blocks EGFR signaling to inhibit cancer cell proliferation. - Osimertinib tablet · Shanghai JMT-Bio Inc. · Oncology
Osimertinib is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to and inhibits mutant EGFR, including T790M resistance mutations, blocking downstream signaling in cancer cells. - SHR-A2009 ; Aumolertinib · Suzhou Suncadia Biopharmaceuticals Co., Ltd. · Oncology
Aumolertinib is a third-generation EGFR tyrosine kinase inhibitor that selectively targets EGFR mutations, including T790M resistance mutations, to inhibit tumor cell proliferation. - AZD9291 Dosing · AstraZeneca · Oncology
AZD9291 is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to and inhibits mutant EGFR, including T790M resistance mutations, while sparing wild-type EGFR. - Combination PD-1/PD-L1 ICI + VEGFR-TKI · University Hospital, Bordeaux · Oncology
This combination blocks PD-1/PD-L1 immune checkpoints to enhance T-cell anti-tumor activity while simultaneously inhibiting VEGFR tyrosine kinases to suppress tumor angiogenesis and promote anti-angiogenic immune effects. - EGFR-TKI · Sichuan Cancer Hospital and Research Institute · Oncology
EGFR-TKI inhibits epidermal growth factor receptor tyrosine kinase activity to block cancer cell proliferation and survival signaling. - lapatinib (GW572016) · GlaxoSmithKline · Oncology
Lapatinib is a small-molecule tyrosine kinase inhibitor that blocks HER2 and EGFR signaling to inhibit cancer cell growth. - Erlotinib chlorhydrate · Grupo de Investigación Clínica en Oncología Radioterapia · Oncology
Erlotinib is a small-molecule tyrosine kinase inhibitor that blocks epidermal growth factor receptor (EGFR) signaling to inhibit cancer cell proliferation. - ICP-488 Tablets · Beijing InnoCare Pharma Tech Co., Ltd. · Oncology
ICP-488 is a tyrosine kinase inhibitor that targets mutant EGFR and other kinases involved in cancer cell proliferation. - AZD9291 · Soroka University Medical Center · Oncology
AZD9291 is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to mutant EGFR while sparing wild-type EGFR, overcoming resistance from the T790M mutation. - Gefitinib or Docetaxel · AstraZeneca · Oncology
Gefitinib is an EGFR tyrosine kinase inhibitor that blocks epidermal growth factor receptor signaling to inhibit cancer cell proliferation, while Docetaxel is a microtubule-stabilizing taxane that prevents cell division. - Osimertinib Mesylate Tablets · Sun Yat-sen University · Oncology
Osimertinib is a third-generation, irreversible tyrosine kinase inhibitor that selectively targets EGFR mutations, including the T790M resistance mutation, in non-small cell lung cancer. - Abivertinib Maleate Capsules · Hangzhou ACEA Pharmaceutical Research Co., Ltd. · Oncology
Abivertinib is a tyrosine kinase inhibitor that targets mutant EGFR and other kinases involved in cancer cell proliferation.
Phase 2 pipeline (6)
- Administration of Vorolanib · Li-kun Chen · Oncology
Vorolanib is a tyrosine kinase inhibitor that targets vascular endothelial growth factor receptors (VEGFR) to inhibit angiogenesis and tumor growth. - BKM120 and Erlotinib · SCRI Development Innovations, LLC · Oncology
BKM120 is a PI3K inhibitor, and Erlotinib is a tyrosine kinase inhibitor targeting EGFR. - Icotinib with concurrent radiotherapy · Betta Pharmaceuticals Co., Ltd. · Oncology
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor - Gefitinib, Cisplatin and Radiotherapy · AstraZeneca · Oncology
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor - Erlotinib, standard dose · Hoffmann-La Roche · Oncology
Erlotinib is a tyrosine kinase inhibitor that targets the epidermal growth factor receptor (EGFR) tyrosine kinase. - Alomnertinib Mesilate · Shanghai Hengrui Pharmaceutical Co., Ltd. · Oncology
Alomnertinib mesilate is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to and inhibits mutant EGFR, including T790M resistance mutations.
Patent intelligence
- egfr tyrosine kinase inhibitor patent landscape — aggregated cliff calendar, attackable patents, originator estates