GEFITINIB
Gefitinib is a tyrosine kinase inhibitor indicated for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors harbor epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations, as detected by an FDA-approved test. Its efficacy has not been established in patients with EGFR mutations outside of these specific markers.
How GEFITINIB Works
Gefitinib is a reversible inhibitor of the EGFR tyrosine kinase. It binds to the intracellular catalytic domain of the receptor, preventing the autophosphorylation of tyrosine residues. This action blocks downstream signaling pathways that drive tumor cell proliferation, survival, and metastasis. Gefitinib demonstrates a higher binding affinity for EGFR exon 19 deletions and exon 21 (L858R) mutations compared to wild-type EGFR. It also inhibits IGF and PDGF-mediated signaling at clinically relevant concentrations.
Details
- Status
- Prescription
- First Approved
- 2022-09-23
- Routes
- ORAL
- Dosage Forms
- TABLET
GEFITINIB Approval History
What GEFITINIB Treats
1 indicationsGEFITINIB is approved for 1 conditions since its original approval in 2022. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Non-Small Cell Lung Cancer
GEFITINIB Target & Pathway
ProTarget
A receptor that triggers cell growth, proliferation, and survival when activated. Mutations or overexpression of EGFR drive many cancers, particularly lung cancer. Blocking EGFR stops the growth signals that fuel tumor progression.
GEFITINIB Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
Direct competitors
Same target(s) AND same indication — head-to-head.
MoA expansion candidates
Same target(s), different indications — where else is this mechanism being explored?
Indication competitors
Same indication, different mechanism — what else might this patient receive?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
What's emerging in GEFITINIB's indications
See all emerging drugs →Phase 3 candidates targeting molecules with no FDA-approved drug, in indications GEFITINIB treats. First-in-class if their pivotal trials read out positive.
Drugs Similar to GEFITINIB
3 of 20FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Clinical Trial Registry
50 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT03758287 | PCD-DCT053-16-001 | Ph 1, Ph 2 | completed | Ningetinib (CT053PTSA) Plus Gefitinib in Stage IIIB or IV NSCLC Patients With EGFR Mutation and T790M Negative |
| NCT03122717 | 16-627 | Ph 1, Ph 2 | active not recruiting | Osimertinib and Gefitinib in EGFR Inhibitor naïve Advanced EGFR Mutant Lung Cancer |
| NCT03040973 | CINC280A2X02B 2024-510948-31-00 | Ph 2 | active not recruiting | Study to Allow Patients Previously Participating in a Novartis Sponsored Trial to Continue Receiving Capmatinib Treatment as Single Agent or in Combination With Other Treatments or the Combination Treatment Alone |
| NCT07477457 | 25-257 | Ph 2 | recruiting | A Study of Gefitinib, Trametinib, Disulfiram, and Sunitinib in Addition to Standard Chemotherapy in People With Osteosarcoma |
| NCT03333343 | CEGF816X2102 2024-511757-21-00 | Ph 1 | active not recruiting | Study of EGF816 in Combination With Selected Targeted Agents in EGFR-mutant NSCLC |
| NCT02411448 RELAY results posted | 15540 I4T-MC-JVCY, 2014-004824-22 | Ph 3 | active not recruiting | A Study of Ramucirumab (LY3009806) in Combination With Erlotinib in Previously Untreated Participants With EGFR Mutation-Positive Metastatic NSCLC (RELAY) |
| NCT02856893 APPLE results posted | EORTC-1613 ESR-15-11406 | Ph 2 | active not recruiting | Osimertinib Treatment on EGFR T790M Plasma Positive NSCLC Patients (APPLE) |
| NCT03653546 BM | AZD3759-003 | Ph 2, Ph 3 | completed | First Line Treatment in EGFR Mutation Positive Advanced NSCLC Patients With Central Nervous System (CNS) Metastases |
| NCT03292133 results posted | 17-291 | Ph 2 | terminated | A Study of EGF816 and Gefitinib in TKI-naïve EGFR-mutant Non-Small Cell Lung Cancer |
| NCT03944772 ORCHARD | D6186C00001 2023-504624-25-00, 2018-003974-29 | Ph 2 | active not recruiting | Phase 2 Platform Study in Patients With Advanced Non-Small Lung Cancer Who Progressed on First-Line Osimertinib Therapy (ORCHARD) |
| NCT02588261 SOLAR results posted | 8273-CL-0302 2015-002894-39 | Ph 3 | terminated | A Study of ASP8273 vs. Erlotinib or Gefitinib in First-line Treatment of Patients With Stage IIIB/IV Non-small Cell Lung Cancer Tumors With EGFR Activating Mutations |
| NCT03866499 | BPI-7711301 | Ph 3 | active not recruiting | A Study of BPI-7711 Capsule in Non-small Cell Lung Cancer Patients |
| NCT01513174 GOAL results posted | GECP10-03_GOAL 2010-024178-21 | Ph 1, Ph 2 | completed | Study With Gefitinib in Combination With Olaparib (AZD2281) Versus Gefitinib Alone |
| NCT04143607 | ASK-LC-120067-F-III | Ph 3 | active not recruiting | ASK120067 Versus Gefitinib as First-line Treatment for EGFRm Locally Advanced or Metastatic NSCLC |
| NCT01485809 SIIS | SVH-1 | Ph 2 | completed | Efficacy and Safety Study of Gefitinib in Squamous NSCLC Patients Who Failed First-Line Chemotherapy |
| NCT01774721 results posted | A7471050 DP312804 | Ph 3 | completed | ARCHER1050: A Study of Dacomitinib vs. Gefitinib in 1st-Line Treatment Of Advanced NSCLC. |
| NCT01833572 | ISSIRES0081 FUSCC1301 | Ph 2 | completed | Preoperative Gefitinib for EGFR Mutant II-IIIa NSCLC (ECTOP-1001) |
| NCT03599518 results posted | DS1205-A-J102 184026 | Ph 1 | terminated | DS-1205c With Gefitinib for Metastatic or Unresectable Epidermal Growth Factor Receptor (EGFR)-Mutant Non-Small Cell Lung Cancer |
| NCT02039674 results posted | 3475-021 MK-3475-021, KEYNOTE-021 | Ph 1, Ph 2 | completed | A Study of Pembrolizumab (MK-3475) in Combination With Chemotherapy or Immunotherapy in Participants With Non-small Cell Lung Cancer (MK-3475-021/KEYNOTE-021) |
| NCT01982955 results posted | EMR 200095-006 2016-001604-28 | Ph 1, Ph 2 | completed | Tepotinib With Gefitinib in Participants With Locally Advanced or Metastatic NSCLC (INSIGHT) |
| NCT02447419 | 2014-10-029 | Ph 2 | completed | Study to Evaluate the Safety and Efficacy of Gefitinib, in Subjects With EFGR Amplification Refractory Solid Tumors |
| NCT03170180 | 2016-12-058 | Ph 2 | completed | Exploratory Study of Drug Sensitivity Prediction Software (IRCR-DReSS) With Patient-derived Tumor Cells of Metastatic Gastric Cancer |
| NCT02088112 | D791PC00001 | Ph 1 | completed | MEDI4736 (Anti PD-L1) Combined With Gefitinib in Subjects With Non-Small Cell Lung Cancer(NSCLC). |
| NCT02804776 PROGRESS | ECRU-LUNG-2013 | Ph 2 | completed | PRe-Operative Gefitinib in Resectable EGFR Mutation Positive Lung Cancer With Sector Sequencing for Biomarker Discovery |
| NCT01610336 results posted | CINC280X2202 2011-002569-39 | Ph 2 | completed | A Safety and Efficacy Study of INC280 and Gefitinib in Patients With EGFR Mutated, c-MET-amplified NSCLC Who Have Progressed After EGFRi Treatment |
| NCT01556191 LADIE | IFCT-1003 | Ph 2 | completed | Lung Cancer in Women Treated With Anti-oestrogens anD Inhibitors of EGFR |
| NCT01544179 IMPRESS results posted | D791LC00001 | Ph 3 | completed | A Study of IRESSA Treatment Beyond Progression in Addition to Chemotherapy Versus Chemotherapy Alone |
| NCT02374645 | D5080C00001 | Ph 1 | completed | A Phase I Study of Safety and Pharmacokinetics of Volitinib in Combination With Gefitinib in EGFR(+) NSCLC |
| NCT01466660 results posted | 1200.123 2011-001814-33 | Ph 2 | completed | LUX-Lung 7: A Phase IIb Trial of Afatinib(BIBW2992) Versus Gefitinib for the Treatment of 1st Line EGFR Mutation Positive Adenocarcinoma of the Lung |
| NCT01933347 | CTONG1304 | Ph 2 | completed | Third-line Treatment of Gefitinib in NSCLC Patients |
| NCT02976116 | 2016-013-00CH1 | Ph 2 | completed | A Phase II Study of Fruquintinib in Combination With Gefitinib in Patients With Advanced Non-small Cell Lung Cancer |
| NCT01469000 results posted | 14034 H3E-CR-JMIT | Ph 2 | completed | A Study of Pemetrexed and Gefitinib Versus Gefitinib in Non-Small Cell Lung Cancer (NSCLC) |
| NCT02179671 results posted | D4191C00011 | Ph 2 | completed | Immune-Modulated Study of Selected Small Molecules (Gefitinib, AZD9291, or Selumetinib + Docetaxel) or a 1st Immune-Mediated Therapy (IMT; Tremelimumab) With a Sequential Switch to a 2nd IMT (MEDI4736) in Patients With Locally Advanced or Metastatic Non-Small-Cell Lung Cancer |
| NCT02326285 NeoIntercal | AIO-TRK-0214 2014-005595-28, IISR ESR-14-10598 | Ph 2, Ph 3 | terminated | Induction Therapy With Intercalated Tyrosine Kinase Inhibitor (TKI) and Chemotherapy in NSCLC With Activating Epidermal Growth Factor Receptor (EGFR) Mutation in Stages II-IIIB |
| NCT02299765 | ISSIRES0109 | Ph 4 | terminated | Intercalating and Maintenance Gefitinib in Combination With Chemotherapy for Advanced EGFR-mutant NSCLC |
| NCT01310855 results posted | CDR0000696313 UCL-10/0035, ZENECA-ISSRECE00002 | Ph 2 | terminated | Cediranib Maleate With or Without Gefitinib in Treating Patients With Recurrent or Progressive Glioblastoma |
| NCT01024413 | C-TONG0901 | Ph 3 | completed | Phase III Trial to Evaluate the Elortinib vs Gefitinib in Advanced NSCLC With EGFR Exon 19 or 21 Mutations |
| NCT01404260 ISCAN results posted | CTONG 1102 | Ph 3 | completed | Intercalating and Maintenance Use of Iressa Versus Chemotherapy in Selected Advanced Non Small Cell Lung Cancer |
| NCT01203917 IFUM results posted | D791AC00014 | Ph 4 | completed | Efficacy, Safety, Tolerability of Gefitinib as 1st Line in Caucasian Patients With EGFR Mutation Positive Advanced NSCLC |
| NCT01405846 TIDAL1 | P01425 2010-023355-29, 11/H0304/8 | Ph 2 | terminated | Feasibility Study to Estimate Number of Patients With Precancerous Areas in Their Airways and the Response to Gefitinib |
| NCT02040064 GEFTREM | 2013-003015-21 2013/2028 | Ph 1 | completed | Tolerability and Efficacy of Tremelimumab in Combination With Gefitinib in NSCLC Patients |
| NCT01783834 | 2008-GIRBA-1739 | Ph 2 | completed | Gefitinib Versus Pemetrexed for Previously Treated NSCLC Patients |
| NCT00770588 INFORM results posted | D7913L00071 | Ph 4 | completed | Assess the Efficacy, Safety and Tolerability of Gefitinib (Iressa® 250mg) as Maintenance Therapy in Locally Advanced or Metastatic (Stage IIIB/IV) Non Small Cell Lung Cancer (NSCLC) |
| NCT00986284 | TMU-CIH-LCC-001 | Ph 2 | suspended | Epidermal Growth Factor Receptor (EGFR) Status Based Gefitinib Neoadjuvant Therapy in Non Small Cell Lung Cancer (NSCLC) |
| NCT01017874 results posted | 13021 H3E-CR-S131 | Ph 3 | completed | A Study of Alimta/Cisplatin/Gefitinib for Asian Non-smoking Participants With Non Small Cell Lung Cancer |
| NCT01602289 | 14637 I4C-JE-JTBD | Ph 1 | completed | A Study of LY2875358 in Japanese Participants With Advanced Cancer |
| NCT01039948 | P06162 | Ph 1, Ph 2 | completed | A Phase 1b/2 Study in Asian Subjects With Non-Small Cell Lung Cancer |
| NCT01498562 DATE | 4-2011-0662 | Ph 2 | completed | Phase II Study of Gefitinib Plus Nimotuzumab Versus Gefitinib in Non-small Cell Lung Cancer |
| NCT01040780 ICOGEN results posted | BPI-2009 | Ph 3 | completed | Safety and Efficacy Study of Icotinb in Non-small Cell Lung Cancer (NSCLC) Patients |
| NCT00807066 RANGE | ONC-2008-001 | Ph 3 | completed | Randomized Gefitinib Trial |
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
GEFITINIB FDA Label Details
Indications & Usage
GEFITINIB is indicated for the treatment of Non-Small Cell Lung Cancer.
Looking for the branded version?
IRESSA
Full clinical data, patents, trials, and competitive landscape for gefitinib.
Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.