Osimertinib
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Also known as Azd-9291AZD-9291 FREE BASEAZD9291MereletinibTagrissoOsimertinibOsimerlinib
Summary
Osimertinib (CHEMBL3353410) is an approved small-molecule antineoplastic agent (ATC L01EB04) targeting EGFR; indicated across 12 conditions including neoplasm and non-small cell lung carcinoma; with CIViC clinical evidence for 53 variant-indication associations (e.g. EGFR T790M in lung non-small cell carcinoma).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EB04
- Targets: 1 (EGFR)
- Indications: 12 conditions
- Clinical trials: 232
- Precision-oncology evidence (CIViC): 53 variant–indication associations
- Chemistry: 499.6 Da · C28H33N7O2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL3353410 |
| Name | Osimertinib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 71496458 |
| ChEBI | CHEBI:90943 |
| ATC | L01EB04 |
| Molecular formula | C28H33N7O2 |
| Molecular weight | 499.6 |
| InChIKey | DUYJMQONPNNFPI-UHFFFAOYSA-N |
SMILES: CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC
IUPAC name: N-[2-[2-(dimethylamino)ethyl-methylamino]-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]prop-2-enamide
ChEBI definition: A member of the class of aminopyrimidines that is 4-(1-methylindol-3-yl)pyrimidin-2-amine in which one of the amino hydrogens is replaced by a 2-methoxy-4-2-(dimethylamino)ethylamino-5-acrylamidophenyl group. Used (as the mesylate salt) for treatment of EGFR T790M mutation positive non-small cell lung cancer.
Pharmacological roles (ChEBI): antineoplastic agent, epidermal growth factor receptor antagonist.
Also known as: Azd-9291, AZD-9291, AZD-9291 FREE BASE, AZD9291, Mereletinib, Osimertinib, Tagrisso, OSIMERTINIB, osimertinib, Osimertinib; Tagrisso, Osimerlinib
Parent form; salt/anhydrous children: CHEMBL3545063, CHEMBL4472934, CHEMBL4741340, CHEMBL4754013, CHEMBL4784911, CHEMBL6068008
Patent coverage: 3,993 distinct patent families (8,898 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 8,509 (96%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| EGFR | epidermal growth factor receptor | Inhibition | 6.31 | 17.5% | P00533 |
Broader ChEMBL bioactivity targets: 41 (assay-derived). Sample: Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma, Receptor tyrosine-protein kinase erbB-2, 5-hydroxytryptamine receptor 2B, Cholecystokinin receptor type A, Alpha-2C adrenergic receptor, Insulin receptor, Epidermal growth factor receptor, D(1A) dopamine receptor, Muscarinic acetylcholine receptor M2, 5-hydroxytryptamine receptor 1A.
Bioactivity
ChEMBL activities: 322 potent at pChembl ≥ 5 of 339 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| EGFR | 10.7 | IC50 | 0.02 | nM | CHEMBL_ACT_22408226 |
| EGFR | 10.3 | IC50 | 0.05 | nM | CHEMBL_ACT_25098087 |
| EGFR | 10.24 | IC50 | 0.06 | nM | CHEMBL_ACT_24976287 |
| EGFR | 10.22 | IC50 | 0.06 | nM | CHEMBL_ACT_22408234 |
| EGFR | 9.8 | IC50 | 0.16 | nM | CHEMBL_ACT_25891717 |
| EGFR | 9.7 | IC50 | 0.2 | nM | CHEMBL_ACT_22408242 |
| EGFR | 9.7 | IC50 | 0.2 | nM | CHEMBL_ACT_22844195 |
| EGFR | 9.6 | IC50 | 0.25 | nM | CHEMBL_ACT_24976298 |
| EGFR | 9.47 | IC50 | 0.34 | nM | CHEMBL_ACT_26025788 |
| EGFR | 9.43 | IC50 | 0.37 | nM | CHEMBL_ACT_26009419 |
| EGFR | 9.38 | IC50 | 0.42 | nM | CHEMBL_ACT_19310371 |
| EGFR | 9.38 | IC50 | 0.41 | nM | CHEMBL_ACT_24413820 |
| EGFR | 9.37 | IC50 | 0.43 | nM | CHEMBL_ACT_22921882 |
| EGFR | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_22844219 |
| EGFR | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_24823398 |
| EGFR | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_24871173 |
| EGFR | 9.29 | IC50 | 0.51 | nM | CHEMBL_ACT_25891714 |
| EGFR | 9.26 | IC50 | 0.55 | nM | CHEMBL_ACT_22814393 |
| EGFR | 9.26 | IC50 | 0.55 | nM | CHEMBL_ACT_26009379 |
| EGFR | 9.22 | IC50 | 0.6 | nM | CHEMBL_ACT_22782715 |
| EGFR | 9.22 | IC50 | 0.6 | nM | CHEMBL_ACT_22968057 |
| EGFR | 9.21 | IC50 | 0.62 | nM | CHEMBL_ACT_23250045 |
| EGFR | 9.15 | IC50 | 0.7 | nM | CHEMBL_ACT_25094732 |
| EGFR | 9.1 | IC50 | 0.8 | nM | CHEMBL_ACT_24871227 |
| EGFR | 9.1 | IC50 | 0.8 | nM | CHEMBL_ACT_25700936 |
| EGFR | 9.05 | IC50 | 0.9 | nM | CHEMBL_ACT_18299295 |
| EGFR | 9.05 | IC50 | 0.9 | nM | CHEMBL_ACT_18539745 |
| EGFR | 9.05 | IC50 | 0.9 | nM | CHEMBL_ACT_25533425 |
| EGFR | 9.02 | IC50 | 0.95 | nM | CHEMBL_ACT_19310359 |
| EGFR | 9 | IC50 | 1 | nM | CHEMBL_ACT_18189839 |
Target pathways
Aggregated over 1 target gene(s): EGFR.
Top Reactome pathways
37 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signaling by ERBB2 | 1 | EGFR |
| Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants | 1 | EGFR |
| Signaling by ERBB4 | 1 | EGFR |
| SHC1 events in ERBB2 signaling | 1 | EGFR |
| PLCG1 events in ERBB2 signaling | 1 | EGFR |
| PIP3 activates AKT signaling | 1 | EGFR |
| Signaling by EGFR | 1 | EGFR |
| GRB2 events in EGFR signaling | 1 | EGFR |
| GAB1 signalosome | 1 | EGFR |
| SHC1 events in EGFR signaling | 1 | EGFR |
| EGFR downregulation | 1 | EGFR |
| GRB2 events in ERBB2 signaling | 1 | EGFR |
| PI3K events in ERBB2 signaling | 1 | EGFR |
| EGFR interacts with phospholipase C-gamma | 1 | EGFR |
| EGFR Transactivation by Gastrin | 1 | EGFR |
| Constitutive Signaling by Aberrant PI3K in Cancer | 1 | EGFR |
| Signal transduction by L1 | 1 | EGFR |
| Constitutive Signaling by EGFRvIII | 1 | EGFR |
| Inhibition of Signaling by Overexpressed EGFR | 1 | EGFR |
| RAF/MAP kinase cascade | 1 | EGFR |
| ERBB2 Regulates Cell Motility | 1 | EGFR |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 1 | EGFR |
| ERBB2 Activates PTK6 Signaling | 1 | EGFR |
| Cargo recognition for clathrin-mediated endocytosis | 1 | EGFR |
| Clathrin-mediated endocytosis | 1 | EGFR |
| PTK6 promotes HIF1A stabilization | 1 | EGFR |
| Downregulation of ERBB2 signaling | 1 | EGFR |
| TFAP2 (AP-2) family regulates transcription of growth factors and their receptors | 1 | EGFR |
| Extra-nuclear estrogen signaling | 1 | EGFR |
| NOTCH3 Activation and Transmission of Signal to the Nucleus | 1 | EGFR |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| cell morphogenesis | 1 |
| ossification | 1 |
| embryonic placenta development | 1 |
| positive regulation of protein phosphorylation | 1 |
| hair follicle development | 1 |
| ubiquitin-dependent protein catabolic process | 1 |
| signal transduction | 1 |
| cell surface receptor signaling pathway | 1 |
| epidermal growth factor receptor signaling pathway | 1 |
| salivary gland morphogenesis | 1 |
| learning or memory | 1 |
| positive regulation of cell population proliferation | 1 |
| gene expression | 1 |
| protein ubiquitination | 1 |
| cerebral cortex cell migration | 1 |
Indications & clinical
Indications
12 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| non-small cell lung carcinoma | 3 | MONDO:0005233 | EFO:0003060 |
| lung neoplasm | 3 | MONDO:0021117 | MONDO:0008903 |
| adenocarcinoma | 2 | MONDO:0004970 | EFO:0000228 |
| squamous cell carcinoma | 2 | MONDO:0005096 | EFO:0000707 |
| carcinoma | 2 | MONDO:0004993 | EFO:0000313 |
| glioblastoma | 2 | MONDO:0018177 | EFO:0000519 |
| colorectal neoplasm | 2 | MONDO:0005335 | MONDO:0005575 |
| brain neoplasm | 1 | MONDO:0021211 | EFO:0003833 |
3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 232.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 97 |
| PHASE1 | 43 |
| PHASE3 | 32 |
| PHASE1/PHASE2 | 28 |
| Not specified | 23 |
| PHASE4 | 4 |
| PHASE2/PHASE3 | 3 |
| EARLY_PHASE1 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT04413201 | PHASE4 | ACTIVE_NOT_RECRUITING | AFAMOSI: Efficacy and Safety of Afatinib Followed by Osimertinib Compared to Osimertinib in Patients with EGFRmutated/T790M Mutation Negative Nonsquamous NSCLC |
| NCT07279935 | PHASE4 | NOT_YET_RECRUITING | Osimertinib Combined With Chemotherapy in Patients Who Had Distant Recurrence After Adjuvant Osimertinib for EGFRm Resectable SIB-IIIA NSCLC. |
| NCT03853551 | PHASE4 | COMPLETED | Osimertinib Study in Indian Patients |
| NCT05785208 | PHASE4 | UNKNOWN | Efficacy Study of Osimertinib in Treatment-naïve Patients With EGFR Mutant NSCLC According to TP53 Mutational Status. |
| NCT02411448 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Ramucirumab (LY3009806) in Combination With Erlotinib in Previously Untreated Participants With EGFR Mutation-Positive Metastatic NSCLC (RELAY) |
| NCT02511106 | PHASE3 | ACTIVE_NOT_RECRUITING | AZD9291 Versus Placebo in Patients With Stage IB-IIIA Non-small Cell Lung Carcinoma, Following Complete Tumour Resection With or Without Adjuvant Chemotherapy. |
| NCT03521154 | PHASE3 | ACTIVE_NOT_RECRUITING | A Global Study to Assess the Effects of Osimertinib Following Chemoradiation in Patients With Stage III Unresectable Non-small Cell Lung Cancer (LAURA) |
| NCT04035486 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Osimertinib With or Without Chemotherapy as 1st Line Treatment in Patients With Mutated Epidermal Growth Factor Receptor Non-Small Cell Lung Cancer (FLAURA2) |
| NCT04181060 | PHASE3 | RECRUITING | Osimertinib With or Without Bevacizumab as Initial Treatment for Patients With EGFR-Mutant Lung Cancer |
| NCT04351555 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Osimertinib With or Without Chemotherapy Versus Chemotherapy Alone as Neoadjuvant Therapy for Patients With EGFRm Positive Resectable Non-Small Cell Lung Cancer |
| NCT04487080 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Amivantamab and Lazertinib Combination Therapy Versus Osimertinib in Locally Advanced or Metastatic Non-Small Cell Lung Cancer |
| NCT04695925 | PHASE3 | ACTIVE_NOT_RECRUITING | Osimertinib Monotherapy or Combination With Chemotherapy for Advanced NSCLC Concurrent EGFR and TP53 Mutations |
| NCT04765059 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Evaluate Chemotherapy Plus Osimertinib Against Chemotherapy Plus Placebo in Patients With Non-small Cell Lung Cancer (NSCLC) |
| NCT05020769 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | SI-B001 Combined With Osimertinib Mesylate Tablets in the Treatment of Recurrent Metastatic Non-small Cell Lung Cancer. |
| NCT05120349 | PHASE3 | ACTIVE_NOT_RECRUITING | A Global Study to Assess the Effects of Osimertinib in Participants With EGFRm Stage IA2-IA3 NSCLC Following Complete Tumour Resection |
| NCT05261399 | PHASE3 | ACTIVE_NOT_RECRUITING | Savolitinib Plus Osimertinib Versus Platinum-based Doublet Chemotherapy in Participants With Non-Small Cell Lung Cancer Who Have Progressed on Osimertinib Treatment |
| NCT05382728 | PHASE3 | RECRUITING | Phase III Study of TY-9591 in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer (FLETEO) |
| NCT05624996 | PHASE3 | RECRUITING | Testing the Addition of High Dose, Targeted Radiation to the Usual Treatment for Locally-Advanced Inoperable Non-Small Cell Lung Cancer |
| NCT05629234 | PHASE3 | ACTIVE_NOT_RECRUITING | Roll Over StudY for Patients Who Have Completed a Previous Oncology Study With Osimertinib (TAGRISSO) (ROSY-T) |
| NCT06323148 | PHASE3 | NOT_YET_RECRUITING | Adjuvant Target Therapy Guided by ctDNA-MRD in Patients With EGFR-mutant II-IIIA Non-small Cell Lung Cancer (ECTOP-1022) |
| NCT06350097 | PHASE3 | RECRUITING | Phase III, Open-label Study of First-line Osimertinib With or Without Datopotamab Deruxtecan for EGFRm Locally Advanced or Metastatic Non-small Cell Lung Cancer |
| NCT06380348 | PHASE3 | NOT_YET_RECRUITING | JMT101 in Combination With Osimertinib, Versus Cisplatin-pemetrexed in Participants With Locally Advanced or Metastatic Non-small Cell Lung Cancer (NSCLC) Characterized by Epithermal Growth Factor Receptor (EGFR) Exon 20ins Mutations |
| NCT06417814 | PHASE3 | RECRUITING | A Study to Investigate the Efficacy and Safety of Dato-DXd With or Without Osimertinib Compared With Platinum Based Doublet Chemotherapy in Participants With EGFR-Mutated Locally Advanced or Metastatic Non-Small Cell Lung Cancer |
| NCT06486142 | PHASE3 | RECRUITING | EGFR-mutated Lung Cancer in Randomized Investigator-Initiated Study |
| NCT06670196 | PHASE3 | RECRUITING | A Study of SKB264 in Combination With Osimertinib Versus Osimertinib in Patients With Epidermal Growth Factor Receptor (EGFR) Mutations, Locally Advanced or Metastatic Non-Squamous Non-Small Cell Lung Cancer |
| NCT06735391 | PHASE3 | RECRUITING | A Clinical Study of JMT101 in Combination With Osimertinib Versus Osimertinib Alone as First-Line Treatment for Patients With Locally Advanced or Metastatic Non-Squamous Non-Small Cell Lung Cancer (NSCLC) Harboring Epidermal Growth Factor Receptor (EGFR) Sensitive Mutations |
| NCT06838273 | PHASE3 | RECRUITING | A Study of BL-B01D1 in Combination With Osimertinib Versus Osimertinib as First-Line Treatment in Patients With EGFR-Mutated Locally Advanced or Metastatic Non-Small Cell Lung Cancer(PANKU-Lung04) |
| NCT07005102 | PHASE2/PHASE3 | RECRUITING | A Study to Assess Adverse Events, Change in Disease Activity of Intravenous Telisotuzumab Adizutecan in Combination With Osimertinib as First-Line Treatment in Adult Participants With Locally Advanced Unresectable or Metastatic EGFR-Mutated Non-Squamous Non-Small Cell Lung Cancer |
| NCT07376382 | PHASE3 | NOT_YET_RECRUITING | A Phase Ⅲ Clinical Study of SYS6010 in Combination With Osimertinib in Patients With Locally Advanced or Metastatic NSCLC |
| NCT02454933 | PHASE3 | COMPLETED | Study of AZD9291 Plus MEDI4736 Versus AZD9291 Monotherapy in NSCLC After Previous EGFR TKI Therapy in T790M Mutation Positive Tumours |
| NCT02474355 | PHASE3 | COMPLETED | Real World Treatment Study of AZD9291 for Advanced/Metastatic EGFR T790M Mutation NSCLC |
| NCT02959749 | PHASE2/PHASE3 | COMPLETED | Osimertinib or Docetaxel-bevacizumab as Third-line Treatment in EGFR T790M Mutated Non-Small Cell Lung Cancer |
| NCT02997501 | PHASE3 | COMPLETED | T790M Plasma Testing Methodology Comparison and Clinical Validation |
| NCT04816214 | PHASE3 | TERMINATED | Study Evaluating Efficacy and Safety of Capmatinib in Combination With Osimertinib in Adult Subjects With Non-small Cell Lung Cancers as Second Line Therapy |
| NCT04870190 | PHASE3 | UNKNOWN | Almonertinib Versus Osimertinib in the Patients With EGFR Mutations in Advanced NSCLC With Brain Metastases |
| NCT05015608 | PHASE3 | COMPLETED | Study on Savolitinib Combined With Osimertinib in Treatment of Advanced NSCLC With MET Amplification |
| NCT05104281 | PHASE3 | UNKNOWN | Osimertinib Combined With Bevacizumab in Patients With Brain Metastasis Epidermal Growth Factor Receptor (EGFR) Mutation Positive Metastatic Non-Small Cell Lung Cancer |
| NCT05493501 | PHASE3 | TERMINATED | Aumolertinib With Chemotherapy or Alone Compared With Osimertinib in Patients With Epidermal Growth Factor Receptor-Mutant Non-Small Cell Lung Cancer |
| NCT06093503 | PHASE3 | WITHDRAWN | Study of Intravenous Telisotuzumab Vedotin in Combination Osimertinib or Standard of Care Chemotherapy to Assess Change in Disease Activity in Adult Participants With Non-Small Cell Lung Cancer That Has a Mutation in the Epidermal Growth Factor Receptor Gene and That Overexpresses the c-Met Protein |
| NCT02465060 | PHASE2 | ACTIVE_NOT_RECRUITING | Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) |
Clinical evidence (CIViC)
Variant × indication × effect (53 predictive associations from 59 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| EGFR T790M | Lung Non-small Cell Carcinoma | Sensitivity/Response | Osimertinib | CIViC A | EID1592 +4 |
| EGFR L858R OR EGFR Exon 19 Deletion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Osimertinib | CIViC A | EID11219 +1 |
| EGFR L858R AND EGFR T790M | Lung Non-small Cell Carcinoma | Sensitivity/Response | Osimertinib | CIViC A | EID11599 |
| EGFR L858R OR EGFR Exon 19 Deletion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Chemotherapy + Osimertinib | CIViC A | EID12015 |
| EGFR T790M AND EGFR Exon 19 Deletion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Osimertinib | CIViC A | EID11598 |
| EGFR Exon 20 Insertion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Osimertinib | CIViC B | EID7610 |
| EGFR G719 | Lung Non-small Cell Carcinoma | Sensitivity/Response | Osimertinib | CIViC B | EID7857 |
| EGFR L861Q | Lung Non-small Cell Carcinoma | Sensitivity/Response | Osimertinib | CIViC B | EID7858 |
| EGFR S768I | Lung Non-small Cell Carcinoma | Sensitivity/Response | Osimertinib | CIViC B | EID7859 |
| ERBB2 Activating Mutation OR ERBB2 T790M | Cancer | Sensitivity/Response | Osimertinib | CIViC B | EID12026 |
| EGFR C797S | Lung Non-small Cell Carcinoma | Resistance | Osimertinib | CIViC B | EID964 |
| EGFR::RAD51 Fusion | Lung Adenocarcinoma | Sensitivity/Response | Osimertinib | CIViC C | EID11021 +1 |
| EGFR A763_Y764insFQEA | Lung Non-small Cell Carcinoma | Sensitivity/Response | Osimertinib | CIViC C | EID9225 |
| EGFR A767_V769dupASV | Lung Non-small Cell Carcinoma | Sensitivity/Response | Osimertinib | CIViC C | EID9220 |
| EGFR Amplification OR EGFR VIII | Malignant Glioma | Sensitivity/Response | Osimertinib | CIViC C | EID12694 |
| EGFR D770_N771insG | Lung Non-small Cell Carcinoma | Sensitivity/Response | Osimertinib | CIViC C | EID9223 |
| EGFR Exon 19 Deletion AND MET Y1003N | Lung Adenocarcinoma | Sensitivity/Response | Osimertinib + Capmatinib | CIViC C | EID11418 |
| EGFR L858R | Lung Adenocarcinoma | Sensitivity/Response | Osimertinib | CIViC C | EID8053 |
| EGFR L858R AND EGFR T790M AND VOPP1::EGFR Fusion | Lung Adenocarcinoma | Sensitivity/Response | Osimertinib | CIViC C | EID12549 |
| EGFR N771_P772insL | Lung Non-small Cell Carcinoma | Sensitivity/Response | Osimertinib | CIViC C | EID9221 |
| EGFR S768_D770dup | Lung Non-small Cell Carcinoma | Sensitivity/Response | Osimertinib | CIViC C | EID9224 |
| EGFR T790M | Lung Squamous Cell Carcinoma | Sensitivity/Response | Osimertinib | CIViC C | EID12066 |
| EGFR T790M | Lung Adenocarcinoma | Sensitivity/Response | Osimertinib | CIViC C | EID2157 |
| EGFR T790M | Pancreatic Adenocarcinoma | Sensitivity/Response | Osimertinib | CIViC C | EID6006 |
| EGFR T790M AND EGFR Exon 19 Deletion | Lung Adenocarcinoma | Sensitivity/Response | Osimertinib | CIViC C | EID1397 |
| EGFR T790M AND EGFR Exon 19 Deletion AND MET Splice Site (c.3027_3028+21delAGGTATATTTCAGTTTATTGTTC | Lung Adenocarcinoma | Sensitivity/Response | Capmatinib + Osimertinib | CIViC C | EID11693 |
| EGFR T790M AND EGFR Exon 19 del | Lung Adenocarcinoma | Sensitivity/Response | Osimertinib | CIViC C | EID12946 |
| EGFR::ERBB4 Fusion | Lung Adenocarcinoma | Sensitivity/Response | Osimertinib + Mobocertinib + Trastuzumab Deruxtecan + Tarloxotinib | CIViC C | EID12373 |
| EGFR::RAD51 Fusion | Lung Adenocarcinoma | Sensitivity/Response | Osimertinib + Erlotinib | CIViC C | EID12370 |
| ERBB2 L755P | Lung Non-small Cell Carcinoma | Sensitivity/Response | Osimertinib | CIViC C | EID12107 |
+23 more predictive associations (showing top 30 by level).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 13 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
156 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| AFATINIB | ChEMBL + PubChem | Phase 4 (approved) | EGFR |
| SELUMETINIB | ChEMBL + PubChem | Phase 4 (approved) | EGFR |
| ABEMACICLIB | ChEMBL | Phase 4 (approved) | EGFR |
| ACALABRUTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| AFATINIB DIMALEATE | ChEMBL | Phase 4 (approved) | EGFR |
| ALECTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | EGFR |
| AXITINIB | ChEMBL | Phase 4 (approved) | EGFR |
| BACITRACIN | ChEMBL | Phase 4 (approved) | EGFR |
| BITHIONOL | ChEMBL | Phase 4 (approved) | EGFR |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| CERITINIB | ChEMBL | Phase 4 (approved) | EGFR |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | EGFR |
| CHROMIC CHLORIDE | ChEMBL | Phase 4 (approved) | EGFR |
| CISPLATIN | ChEMBL | Phase 4 (approved) | EGFR |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | EGFR |
| COLISTIN | ChEMBL | Phase 4 (approved) | EGFR |
| CRIZOTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| DACOMITINIB | ChEMBL | Phase 4 (approved) | EGFR |
| DASATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| DOBUTAMINE | ChEMBL | Phase 4 (approved) | EGFR |
| DOCETAXEL | ChEMBL | Phase 4 (approved) | EGFR |
| EBASTINE | ChEMBL | Phase 4 (approved) | EGFR |
| ECONAZOLE | ChEMBL | Phase 4 (approved) | EGFR |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| FLUPHENAZINE | ChEMBL | Phase 4 (approved) | EGFR |
| GEFITINIB | ChEMBL | Phase 4 (approved) | EGFR |
| GENTIAN VIOLET | ChEMBL | Phase 4 (approved) | EGFR |
| GILTERITINIB | ChEMBL | Phase 4 (approved) | EGFR |
| HEXACHLOROPHENE | ChEMBL | Phase 4 (approved) | EGFR |
| IBRUTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| IMATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| LAPATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| LAPATINIB DITOSYLATE | ChEMBL | Phase 4 (approved) | EGFR |
| LAZERTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| LEVODOPA | ChEMBL | Phase 4 (approved) | EGFR |
| LORLATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| METHYLDOPA | ChEMBL | Phase 4 (approved) | EGFR |
| MICONAZOLE | ChEMBL | Phase 4 (approved) | EGFR |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | EGFR |
| MITOXANTRONE | ChEMBL | Phase 4 (approved) | EGFR |
| MOBOCERTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| MONTELUKAST | ChEMBL | Phase 4 (approved) | EGFR |
| NELFINAVIR | ChEMBL | Phase 4 (approved) | EGFR |
| NERATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| NICLOSAMIDE | ChEMBL | Phase 4 (approved) | EGFR |
| OLMUTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| PERHEXILINE | ChEMBL | Phase 4 (approved) | EGFR |
| PONATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| SORAFENIB | ChEMBL | Phase 4 (approved) | EGFR |
| SULOCTIDIL | ChEMBL | Phase 4 (approved) | EGFR |
| SUNITINIB | ChEMBL | Phase 4 (approved) | EGFR |
| TAMOXIFEN | ChEMBL | Phase 4 (approved) | EGFR |
| TERFENADINE | ChEMBL | Phase 4 (approved) | EGFR |
| THIORIDAZINE | ChEMBL | Phase 4 (approved) | EGFR |
| TRIBROMSALAN | ChEMBL | Phase 4 (approved) | EGFR |
| TUCATINIB | ChEMBL | Phase 4 (approved) | EGFR |
Related Atlas pages
- Genes: EGFR
- Diseases: neoplasm, non-small cell lung carcinoma, lung neoplasm, cancer, lung adenocarcinoma, malignant glioma, squamous cell lung carcinoma, pancreatic adenocarcinoma
- Drugs: Afatinib, Selumetinib, Abemaciclib, Acalabrutinib, Alectinib, Astemizole, Axitinib, Bacitracin, Bithionol, Bosutinib, Brigatinib, Cabozantinib, Ceritinib, Chlorpromazine, Chromic Chloride, Cisplatin, Clotrimazole, Colistin, Crizotinib, Dacomitinib, Dasatinib, Dobutamine, Docetaxel, Ebastine, Econazole, Erlotinib, Fedratinib, Fluphenazine, Gefitinib, Gilteritinib, Hexachlorophene, Ibrutinib, Imatinib, Lapatinib, Lazertinib, Levodopa, Lorlatinib, Methyldopa, Miconazole, Midostaurin, Mitoxantrone, Mobocertinib, Montelukast, Nelfinavir, Neratinib, Niclosamide, Olmutinib, Perhexiline, Ponatinib, Sorafenib, Suloctidil, Sunitinib, Tamoxifen, Terfenadine, Thioridazine, Tribromsalan, Tucatinib