Lorlatinib
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Also known as LorbrenaLorviquaPF-06463922NALORLATINIB_
Summary
Lorlatinib (CHEMBL3286830) is an approved small-molecule antineoplastic agent (ATC L01ED05) targeting ALK, ROS1, and FES; indicated across 10 conditions including non-small cell lung carcinoma and neoplasm; with CIViC clinical evidence for 25 variant-indication associations (e.g. ALK Fusion in lung non-small cell carcinoma).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01ED05
- Targets: 3 (ALK, ROS1, FES)
- Indications: 10 conditions
- Clinical trials: 60
- Precision-oncology evidence (CIViC): 25 variant–indication associations
- Chemistry: 406.4 Da · C21H19FN6O2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL3286830 |
| Name | Lorlatinib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 71731823 |
| ChEBI | CHEBI:143117 |
| ATC | L01ED05 |
| Molecular formula | C21H19FN6O2 |
| Molecular weight | 406.4 |
| InChIKey | IIXWYSCJSQVBQM-LLVKDONJSA-N |
SMILES: C[C@@H]1C2=C(C=CC(=C2)F)C(=O)N(CC3=NN(C(=C3C4=CC(=C(N=C4)N)O1)C#N)C)C
IUPAC name: (16R)-19-amino-13-fluoro-4,8,16-trimethyl-9-oxo-17-oxa-4,5,8,20-tetrazatetracyclo[16.3.1.02,6.010,15]docosa-1(22),2,5,10(15),11,13,18,20-octaene-3-carbonitrile
ChEBI definition: A cyclic ether that is 16,17-dihydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecin-15(10H)-one substituted by methyl groups at positions 2 and 10R, and by cyano, amino and fluoro groups at positions 3, 7 and 12 respectively. It is a small molecule inhibitor of ALK and ROS1 kinase developed by Pfizer for the treatment of ALK-positive non-small cell lung cancer.
Pharmacological roles (ChEBI): antineoplastic agent, EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor.
Also known as: Lorbrena, Lorlatinib, Lorviqua, PF-06463922, LORLATINIB, NA, LORLATINIB_, lorlatinib
Parent form; salt/anhydrous children: CHEMBL4539157, CHEMBL6068047
Patent coverage: 1,575 distinct patent families (3,598 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 3,106 (86%) 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 |
|---|---|---|---|---|---|
| ALK | ALK receptor tyrosine kinase | Inhibition | 9.15 | 0.8% | Q9UM73 |
| ROS1 | c-ros oncogene 1, receptor tyrosine kinase | Inhibition | 11.3 | 0.1% | P08922 |
| FES | FES proto-oncogene, tyrosine kinase | Inhibition | 8.22 | 0.2% | P07332 |
Broader ChEMBL bioactivity targets: 24 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Epidermal growth factor receptor, 5-hydroxytryptamine receptor 1A, Acetylcholinesterase, Adenosine receptor A3, Focal adhesion kinase 1, High affinity nerve growth factor receptor, 3’,5’-cyclic-AMP phosphodiesterase 4D, Tyrosine-protein kinase JAK2, Nuclear receptor subfamily 1 group I member 2.
Bioactivity
ChEMBL activities: 83 potent at pChembl ≥ 5 of 85 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| ROS1 | 10 | Ki | 0.1 | nM | CHEMBL_ACT_18761145 |
| ROS1 | 10 | Ki | 0.1 | nM | CHEMBL_ACT_22395851 |
| SLC34A2 | 9.72 | IC50 | 0.19 | nM | CHEMBL_ACT_22424896 |
| ALK | 9.7 | IC50 | 0.2 | nM | CHEMBL_ACT_14722505 |
| EML4 | 9.7 | IC50 | 0.2 | nM | CHEMBL_ACT_18761148 |
| CD74 | 9.64 | IC50 | 0.23 | nM | CHEMBL_ACT_22424892 |
| CD74 | 9.52 | IC50 | 0.3 | nM | CHEMBL_ACT_29238079 |
| SLC34A2 | 9.4 | IC50 | 0.4 | nM | CHEMBL_ACT_29238047 |
| ALK | 9.15 | Ki | 0.7 | nM | CHEMBL_ACT_14722369 |
| ALK | 9.15 | Ki | 0.7 | nM | CHEMBL_ACT_18285545 |
| ALK | 9.15 | Ki | 0.7 | nM | CHEMBL_ACT_18761156 |
| ALK | 9.15 | Ki | 0.7 | nM | CHEMBL_ACT_22424890 |
| ALK | 9.15 | Ki | 0.7 | nM | CHEMBL_ACT_25683778 |
| ALK | 8.89 | IC50 | 1.3 | nM | CHEMBL_ACT_14722560 |
| EML4 | 8.89 | IC50 | 1.3 | nM | CHEMBL_ACT_18761147 |
| ALK | 8.89 | IC50 | 1.3 | nM | CHEMBL_ACT_24953979 |
| ALK | 8.8 | IC50 | 1.6 | nM | CHEMBL_ACT_14722507 |
| EML4 | 8.8 | IC50 | 1.6 | nM | CHEMBL_ACT_18761149 |
| LTK | 8.57 | IC50 | 2.7 | nM | CHEMBL_ACT_14722558 |
| LTK | 8.57 | Ki | 2.7 | nM | CHEMBL_ACT_24958176 |
| FER | 8.48 | IC50 | 3.3 | nM | CHEMBL_ACT_14722519 |
| FER | 8.48 | Ki | 3.3 | nM | CHEMBL_ACT_24958172 |
| ALK | 8.38 | IC50 | 4.2 | nM | CHEMBL_ACT_14722511 |
| EML4 | 8.38 | IC50 | 4.2 | nM | CHEMBL_ACT_18761151 |
| ALK | 8.26 | IC50 | 5.5 | nM | CHEMBL_ACT_28859399 |
| ALK | 8.26 | IC50 | 5.5 | nM | CHEMBL_ACT_28859453 |
| ALK | 8.26 | IC50 | 5.5 | nM | CHEMBL_ACT_28859459 |
| ALK | 8.26 | IC50 | 5.5 | nM | CHEMBL_ACT_28859465 |
| ALK | 8.26 | IC50 | 5.5 | nM | CHEMBL_ACT_28859471 |
| ALK | 8.26 | IC50 | 5.5 | nM | CHEMBL_ACT_28859477 |
Target pathways
Aggregated over 3 target gene(s): ALK, ROS1, FES.
Top Reactome pathways
21 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signaling by SCF-KIT | 1 | FES |
| Signal Transduction | 1 | ALK |
| Disease | 1 | ALK |
| Signaling by ALK | 1 | ALK |
| Sema3A PAK dependent Axon repulsion | 1 | FES |
| SEMA3A-Plexin repulsion signaling by inhibiting Integrin adhesion | 1 | FES |
| CRMPs in Sema3A signaling | 1 | FES |
| Diseases of signal transduction by growth factor receptors and second messengers | 1 | ALK |
| Signaling by Receptor Tyrosine Kinases | 1 | ALK |
| Signaling by ALK in cancer | 1 | ALK |
| ALK mutants bind TKIs | 1 | ALK |
| Drug resistance of ALK mutants | 1 | ALK |
| ASP-3026-resistant ALK mutants | 1 | ALK |
| NVP-TAE684-resistant ALK mutants | 1 | ALK |
| alectinib-resistant ALK mutants | 1 | ALK |
| brigatinib-resistant ALK mutants | 1 | ALK |
| ceritinib-resistant ALK mutants | 1 | ALK |
| crizotinib-resistant ALK mutants | 1 | ALK |
| lorlatinib-resistant ALK mutants | 1 | ALK |
| Signaling by ALK fusions and activated point mutants | 1 | ALK |
| MDK and PTN in ALK signaling | 1 | ALK |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| protein phosphorylation | 3 |
| signal transduction | 2 |
| cell surface receptor protein tyrosine kinase signaling pathway | 2 |
| regulation of cell population proliferation | 2 |
| protein autophosphorylation | 2 |
| response to stress | 1 |
| phosphorylation | 1 |
| hippocampus development | 1 |
| adult behavior | 1 |
| swimming behavior | 1 |
| peptidyl-tyrosine autophosphorylation | 1 |
| regulation of apoptotic process | 1 |
| regulation of neuron differentiation | 1 |
| neuron development | 1 |
| negative regulation of lipid catabolic process | 1 |
Indications & clinical
Indications
10 indications (4 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 |
|---|---|---|---|
| non-small cell lung carcinoma | 4 | MONDO:0005233 | EFO:0003060 |
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| lymphoma | 4 | MONDO:0005062 | EFO:0000574 |
| neuroblastoma | 3 | MONDO:0005072 | EFO:0000621 |
| ganglioneuroblastoma | 3 | MONDO:0005035 | EFO:0000502 |
| anaplastic large cell lymphoma | 2 | MONDO:0020325 | EFO:0003032 |
| lung neoplasm | 2 | MONDO:0021117 | MONDO:0008903 |
| kidney disorder | 1 | MONDO:0005240 | EFO:0003086 |
| liver disorder | 1 | MONDO:0005154 | EFO:0001421 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 60.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 18 |
| Not specified | 18 |
| PHASE1 | 11 |
| PHASE4 | 5 |
| PHASE1/PHASE2 | 4 |
| PHASE3 | 3 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05144997 | PHASE4 | ACTIVE_NOT_RECRUITING | Lorlatinib Continuation Study |
| NCT06282874 | PHASE4 | ACTIVE_NOT_RECRUITING | Lorlatinib in Patients With ALK-Positive NSCLC With Brain or Leptomeningeal Metastases |
| NCT06893354 | PHASE4 | NOT_YET_RECRUITING | Explore the Mechanisms Underlying Disease Resistance and Potential Primary Resistance Mechanism of Induction Therapy Lorlatinib in Resectable Non-small Cell Lung Cancer (NSCLC) Harboring ALK Positive Mutation Revealed by Single-cell RNA Sequencing and Spatial Transcriptomics |
| NCT04362072 | PHASE4 | COMPLETED | Study of Lorlatinib In People With ALK-positive Non-small Cell Lung Cancer |
| NCT04541706 | PHASE4 | COMPLETED | Lorlatinib in ALK Inhibitor Treated Unresectable Advanced/Recurrent ALK-Positive Non Small Cell Lung Cancer Patients in India |
| NCT03052608 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study Of Lorlatinib Versus Crizotinib In First Line Treatment Of Patients With ALK-Positive NSCLC |
| NCT03126916 | PHASE3 | RECRUITING | Testing the Addition of 131I-MIBG or Lorlatinib to Intensive Therapy in People With High-Risk Neuroblastoma (NBL) |
| NCT06858410 | PHASE3 | NOT_YET_RECRUITING | Lorlatinib Compared with Concurrent/ Sequential Chemoradiotherapy in Stage III ALK Positive Lung Adenocarcinoma |
| NCT02925234 | PHASE2 | RECRUITING | The Drug Rediscovery Protocol (DRUP Trial) |
| NCT04127110 | PHASE2 | ACTIVE_NOT_RECRUITING | Activity of Lorlatinib Based on ALK Resistance Mutations Detected on Blood in ALK Positive NSCLC Patients |
| NCT04621188 | PHASE2 | ACTIVE_NOT_RECRUITING | Lorlatinib After Failure of First-line TKI in Patients With Advanced ROS1-positive NSCLC (ALBATROS) |
| NCT05297890 | PHASE2 | ACTIVE_NOT_RECRUITING | A Study of Lorlatinib in Subjects With ROS1-Positive Non-Small Cell Lung Cancer |
| NCT05740943 | PHASE2 | ACTIVE_NOT_RECRUITING | Induction Lorlatinib in Stage III Non-small Cell Lung Cancer |
| NCT06007937 | PHASE1/PHASE2 | RECRUITING | A Study of Lorlatinib in Combination With Ramucirumab in People With Lung Cancer |
| NCT06378892 | PHASE2 | RECRUITING | A Study to Evaluate the Combination of Platinum-pemetrexed Based Chemotherapy Plus Lorlatinib in ALK Positive Non-Small Cell Lung Cancer (NSCLC) With Exclusively Extracranial Disease Progression on Lorlatinib |
| NCT06682884 | PHASE2 | NOT_YET_RECRUITING | Lorlatinib as Neoadjuvant Treatment in Stage IB-IIIB ALK-rearranged Non-Small Cell Lung Cancer |
| NCT07083687 | PHASE2 | NOT_YET_RECRUITING | Lorlatinib in ROS1+ NSCLC With Brain Metastasis |
| NCT07415005 | PHASE2 | RECRUITING | Lorlatinib Plus Local Consolidation Therapy In ALK Positive Advanced Non-Small Cell Lung Cancer |
| NCT01970865 | PHASE1/PHASE2 | COMPLETED | A Study Of PF-06463922 An ALK/ROS1 Inhibitor In Patients With Advanced Non Small Cell Lung Cancer With Specific Molecular Alterations |
| NCT02584634 | PHASE1/PHASE2 | TERMINATED | Study to Evaluate Safety, Efficacy, Pharmacokinetics And Pharmacodynamics Of Avelumab In Combination With Either Crizotinib Or PF-06463922 In Patients With NSCLC. (Javelin Lung 101) |
| NCT02927340 | PHASE2 | UNKNOWN | A Study of Lorlatinib in Advanced ALK and ROS1 Rearranged Lung Cancer With CNS Metastasis in the Absence of Measurable Extracranial Lesions |
| NCT03439215 | PHASE2 | UNKNOWN | PF-06463922 for Crizotinib Pretreated ROS1 Positive Non-small-cell Lung Cancer |
| NCT03505554 | PHASE2 | UNKNOWN | A Study of Oral Lorlatinib in Patients With Relapsed ALK Positive Lymphoma |
| NCT03612154 | PHASE2 | UNKNOWN | Study of Lorlatinib in ROS1 Rearranged NSCLC |
| NCT03737994 | PHASE2 | TERMINATED | Targeted Treatment for ALK Positive Patients Who Have Previously Been Treated for Non-squamous Non-small Cell Lung Cancer |
| NCT03909971 | PHASE2 | COMPLETED | A Study of Lorlatinib in ALK Inhibitor-Treated ALK-Positive NSCLC in China |
| NCT04111705 | PHASE2 | COMPLETED | Lorlatinib After Failure of First-line Second-generation ALK Kinase Inhibitor in Patients With Advanced ALK-positive Non-small Cell Lung Cancer |
| NCT04292119 | PHASE1/PHASE2 | UNKNOWN | Lorlatinib Combinations in Lung Cancer |
| NCT05097599 | PHASE2 | TERMINATED | StrataPATH™ (Precision Indications for Approved Therapies) |
| NCT05948462 | PHASE2 | WITHDRAWN | Lorlatinib in Combination With Chemotherapy in Participants With Metastatic Anaplastic Lymphoma Kinase Positive (ALK+) Non-small Cell Lung Cancer (NSCLC) Who Progressed on Single-agent Lorlatinib |
| NCT02564562 | PHASE1 | COMPLETED | A Study To Investigate The Absorption, Distribution, Metabolism, And Excretion Of [14c]PF-06463922 In Healthy Male Volunteers |
| NCT02569554 | PHASE1 | COMPLETED | PPI And Food Effect Study For PF-06463922 In Healthy Volunteers |
| NCT02804399 | PHASE1 | COMPLETED | A Study To Evaluate The Effect Of Rifampin On Pharmacokinetics Of PF-06463922 In Healthy Volunteers |
| NCT02838264 | PHASE1 | COMPLETED | A Study To Evaluate The Effect Of Itraconazole On Pharmacokinetics Of PF-06463922 In Healthy Volunteers |
| NCT03107988 | PHASE1 | COMPLETED | NANT 2015-02: A Phase 1 Study of Lorlatinib (PF-06463922) |
| NCT03542305 | PHASE1 | COMPLETED | Lorlatinib Renal Impairment Study |
| NCT03726333 | PHASE1 | TERMINATED | Hepatic Impairment Study for Lorlatinib in Cancer Patients |
| NCT03878524 | PHASE1 | TERMINATED | Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial |
| NCT03961997 | PHASE1 | COMPLETED | Effect of Multiple Doses of Modafinil on the Pharmacokinetics of Single Dose Lorlatinib in Healthy Participants |
| NCT04800822 | PHASE1 | TERMINATED | PF-07284892 in Participants With Advanced Solid Tumors |
Clinical evidence (CIViC)
Variant × indication × effect (25 predictive associations from 28 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| ALK Fusion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Lorlatinib | CIViC A | EID11191 +3 |
| ALK Mutation | Lung Non-small Cell Carcinoma | Sensitivity/Response | Lorlatinib | CIViC A | EID11286 |
| ROS1 Fusion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Lorlatinib | CIViC B | EID11335 |
| ALK Fusion | Inflammatory Myofibroblastic Tumor | Sensitivity/Response | Lorlatinib | CIViC C | EID11294 |
| EML4::ALK Fusion AND ALK C1156Y | Lung Non-small Cell Carcinoma | Sensitivity/Response | Lorlatinib | CIViC C | EID842 |
| EML4::ALK Fusion AND ALK I1171N AND ALK L1196M | Malignant Pleural Mesothelioma | Sensitivity/Response | Lorlatinib | CIViC C | EID11113 |
| FN1::ALK Fusion | Inflammatory Myofibroblastic Tumor | Sensitivity/Response | Lorlatinib | CIViC C | EID11292 |
| ROS1 S1986Y/F | Lung Non-small Cell Carcinoma | Sensitivity/Response | Lorlatinib | CIViC C | EID7689 |
| TPM4::ALK Fusion | Inflammatory Myofibroblastic Tumor | Sensitivity/Response | Lorlatinib | CIViC C | EID11293 |
| EML4::ALK Fusion AND ALK G1202R AND ALK I1171N AND ALK L1196M | Malignant Pleural Mesothelioma | Resistance | Lorlatinib | CIViC C | EID11114 |
| EML4::ALK Fusion AND ALK G1202R AND ALK L1196M | Lung Non-small Cell Carcinoma | Resistance | Lorlatinib | CIViC C | EID7591 |
| EML4::ALK Fusion AND ALK L1198F AND ALK C1156Y | Lung Non-small Cell Carcinoma | Resistance | Lorlatinib | CIViC C | EID843 |
| ALK F1174L | Neuroblastoma | Sensitivity/Response | Lorlatinib | CIViC D | EID1329 |
| ALK F1245C | Neuroblastoma | Sensitivity/Response | Lorlatinib | CIViC D | EID1330 |
| ALK R1275Q | Neuroblastoma | Sensitivity/Response | Lorlatinib | CIViC D | EID1331 |
| EML4::ALK Fusion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Lorlatinib | CIViC D | EID1332 |
| EML4::ALK Fusion AND ALK G1202R | Cancer | Sensitivity/Response | Lorlatinib | CIViC D | EID7593 |
| EML4::ALK Fusion AND ALK L1196M | Cancer | Sensitivity/Response | Brigatinib + Lorlatinib + Alectinib + Ceritinib | CIViC D | EID7597 |
| GOPC::ROS1 e7::e35 | Glioblastoma | Sensitivity/Response | Lorlatinib | CIViC D | EID7483 |
| ROS1 G2032R AND v::ROS1 Fusion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Lorlatinib | CIViC D | EID1251 |
| ROS1 L2026M AND CD74::ROS1 Fusion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Lorlatinib | CIViC D | EID1253 |
| EML4::ALK Fusion AND ABCB1 Overexpression | Lung Adenocarcinoma | Resistance | Lorlatinib + Alectinib | CIViC D | EID10016 |
| EML4::ALK Fusion AND ALK C1156Y | Cancer | Resistance | Lorlatinib + Alectinib + Ceritinib + Brigatinib | CIViC D | EID7609 |
| EML4::ALK Fusion AND ALK G1202R AND ALK L1196M | Cancer | Resistance | Brigatinib + Crizotinib + Lorlatinib + Alectinib + Ceritinib | CIViC D | EID7592 |
| EML4::ALK Fusion AND ALK G1202R AND ALK L1198F | Cancer | Resistance | Alectinib + Lorlatinib + Brigatinib + Ceritinib | CIViC D | EID7595 |
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
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.
99 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| ALECTINIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, FES, ROS1 |
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, FES, ROS1 |
| ENTRECTINIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, FES, ROS1 |
| ERLOTINIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, FES, ROS1 |
| FEDRATINIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, FES, ROS1 |
| GILTERITINIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, FES, ROS1 |
| PAZOPANIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, FES, ROS1 |
| RUXOLITINIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, FES, ROS1 |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | ALK, FES, ROS1 |
| CERITINIB | ChEMBL | Phase 4 (approved) | ALK, FES, ROS1 |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | ALK, FES, ROS1 |
| LESTAURTINIB | ChEMBL | Phase 3 | ALK, FES, ROS1 |
| BMS-754807 | ChEMBL | Phase 2 | ALK, FES, ROS1 |
| FORETINIB | ChEMBL | Phase 2 | ALK, FES, ROS1 |
| R-406 | ChEMBL | Phase 2 | ALK, FES, ROS1 |
| TOZASERTIB | ChEMBL | Phase 2 | ALK, FES, ROS1 |
| Afatinib | PubChem | Approved | ALK, FES, ROS1 |
| Gefitinib | PubChem | Approved | ALK, FES, ROS1 |
| Idelalisib | PubChem | Approved | ALK, FES, ROS1 |
| Selumetinib | PubChem | Approved | ALK, FES, ROS1 |
| BOSUTINIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, FES |
| PALBOCICLIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, FES |
| REPOTRECTINIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, ROS1 |
| SUNITINIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, FES |
| VANDETANIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, FES |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | ALK, ROS1 |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | ALK, ROS1 |
| LINIFANIB | ChEMBL | Phase 3 | ALK, FES |
| ROCILETINIB | ChEMBL | Phase 3 | ALK, FES |
| BI-2536 | ChEMBL | Phase 2 | ALK, FES |
| CENISERTIB | ChEMBL | Phase 2 | ALK, ROS1 |
| ILORASERTIB | ChEMBL | Phase 2 | ALK, ROS1 |
| OSI-632 | ChEMBL | Phase 2 | ALK, ROS1 |
| PELITINIB | ChEMBL | Phase 2 | ALK, FES |
| REBASTINIB | ChEMBL | Phase 2 | FES, ROS1 |
| SELITRECTINIB | ChEMBL | Phase 2 | ALK, ROS1 |
| belumosudil | PubChem | Approved | ALK, ROS1 |
| Lapatinib | PubChem | Approved | FES, ROS1 |
| Momelotinib | PubChem | Approved | FES, ROS1 |
| Quizartinib | PubChem | Approved | FES, ROS1 |
| Sorafenib | PubChem | Approved | FES, ROS1 |
| AXITINIB | ChEMBL | Phase 4 (approved) | ROS1 |
| DASATINIB | ChEMBL | Phase 4 (approved) | FES |
| LAROTRECTINIB | ChEMBL | Phase 4 (approved) | ROS1 |
| MITOXANTRONE | ChEMBL | Phase 4 (approved) | ROS1 |
| NERATINIB | ChEMBL | Phase 4 (approved) | FES |
| OSIMERTINIB | ChEMBL | Phase 4 (approved) | ALK |
| UPADACITINIB | ChEMBL | Phase 4 (approved) | ALK |
| ALISERTIB | ChEMBL | Phase 3 | ROS1 |
| ALVOCIDIB | ChEMBL | Phase 3 | ALK |
| CANERTINIB | ChEMBL | Phase 3 | ALK |
| CEDIRANIB | ChEMBL | Phase 3 | ALK |
| DACTOLISIB | ChEMBL | Phase 3 | ALK |
| DOVITINIB | ChEMBL | Phase 3 | ALK |
| ENTOSPLETINIB | ChEMBL | Phase 3 | ROS1 |
| QUERCETIN | ChEMBL | Phase 3 | ALK |
| RUBOXISTAURIN | ChEMBL | Phase 3 | ROS1 |
| SEMAXANIB | ChEMBL | Phase 3 | ALK |
| BEMCENTINIB | ChEMBL | Phase 2 | ALK |
| CEP-11981 | ChEMBL | Phase 2 | ALK |
Related Atlas pages
- Genes: ALK, ROS1, FES
- Diseases: non-small cell lung carcinoma, neoplasm, lymphoma, neuroblastoma, ganglioneuroblastoma, inflammatory myofibroblastic tumor, malignant pleural mesothelioma, cancer, glioblastoma, lung adenocarcinoma
- Drugs: Alectinib, Crizotinib, Entrectinib, Erlotinib, Fedratinib, Gilteritinib, Pazopanib, Ruxolitinib, Brigatinib, Ceritinib, Nintedanib, Lestaurtinib, Afatinib, Gefitinib, Idelalisib, Selumetinib, Bosutinib, Palbociclib, Repotrectinib, Sunitinib, Vandetanib, Infigratinib, Midostaurin, Linifanib, Rociletinib, belumosudil, Lapatinib, Momelotinib, Quizartinib, Sorafenib, Axitinib, Dasatinib, Larotrectinib, Mitoxantrone, Neratinib, Osimertinib, Upadacitinib, Alisertib, Alvocidib, Canertinib, Cediranib, Dactolisib, Dovitinib, Entospletinib, Quercetin, Ruboxistaurin, Semaxanib