Alectinib
drugOn this page
Also known as AF-802AF802AlecensaCH-5424802CH5424802RO-5424802RO5424802CH 5424802ALECTINIB HYDROCHLORIDERG-7853ALECTINIBCH-5424802CH5424802CT-CH542RG7853ALECTINIB (CH5424802)SID174006440Alectinib
Summary
Alectinib (CHEMBL1738797) is an approved small-molecule EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor (ATC L01ED03) targeting MET and ALK; indicated across 27 conditions including neoplasm and non-small cell lung carcinoma; with CIViC clinical evidence for 32 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: L01ED03
- Targets: 2 (MET, ALK)
- Indications: 27 conditions
- Clinical trials: 67
- Precision-oncology evidence (CIViC): 32 variant–indication associations
- Chemistry: 482.6 Da · C30H34N4O2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1738797 |
| Name | Alectinib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 49806720 |
| ChEBI | CHEBI:90936 |
| ATC | L01ED03 |
| Molecular formula | C30H34N4O2 |
| Molecular weight | 482.6 |
| InChIKey | KDGFLJKFZUIJMX-UHFFFAOYSA-N |
SMILES: CCC1=CC2=C(C=C1N3CCC(CC3)N4CCOCC4)C(C5=C(C2=O)C6=C(N5)C=C(C=C6)C#N)(C)C
IUPAC name: 9-ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[b]carbazole-3-carbonitrile
ChEBI definition: An organic heterotetracyclic compound that is 6,6-dimethyl-5,6-dihydro-11H-benzo[b]carbazol-11-one carrying additional cyano, 4-(morpholin-4-yl)piperidin-1-yl and ethyl substituents at positions 3, 8 and 9 respectively. Used (as the hydrochloride salt) for the treatment of patients with anaplastic lymphoma kinase-positive, metastatic non-small cell lung cancer.
Pharmacological roles (ChEBI): EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, antineoplastic agent.
Also known as: AF-802, AF802, Alecensa, Alectinib, CH-5424802, CH5424802, RO-5424802, RO5424802, ALECTINIB, CH 5424802, ALECTINIB HYDROCHLORIDE, ALECENSA
Parent form; salt/anhydrous children: CHEMBL3707320
Patent coverage: 2,824 distinct patent families (6,731 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 6,207 (92%) 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 |
|---|---|---|---|---|---|
| MET | MET proto-oncogene, receptor tyrosine kinase | Inhibition | 5.3 | 2.4% | P08581 |
| ALK | ALK receptor tyrosine kinase | Inhibition | 8.72 | 0.8% | Q9UM73 |
Broader ChEMBL bioactivity targets: 33 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Epidermal growth factor receptor, Proto-oncogene tyrosine-protein kinase receptor Ret, D(1A) dopamine receptor, Estrogen receptor, Progesterone receptor, Sodium-dependent noradrenaline transporter, Sodium-dependent serotonin transporter, D(3) dopamine receptor, Phosphorylase b kinase gamma catalytic chain, liver/testis isoform.
Bioactivity
ChEMBL activities: 97 potent at pChembl ≥ 5 of 101 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| ALK | 9.23 | IC50 | 0.59 | nM | CHEMBL_ACT_22775265 |
| ALK | 9.02 | IC50 | 0.96 | nM | CHEMBL_ACT_22775391 |
| ALK | 8.82 | IC50 | 1.5 | nM | CHEMBL_ACT_22775387 |
| ALK | 8.81 | IC50 | 1.56 | nM | CHEMBL_ACT_24867175 |
| ALK | 8.72 | IC50 | 1.9 | nM | CHEMBL_ACT_19036772 |
| ALK | 8.72 | IC50 | 1.9 | nM | CHEMBL_ACT_19145426 |
| ALK | 8.72 | IC50 | 1.9 | nM | CHEMBL_ACT_24867174 |
| ALK | 8.72 | IC50 | 1.9 | nM | CHEMBL_ACT_7997506 |
| EML4 | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_16426638 |
| EML4 | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_16426656 |
| EML4 | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_16427358 |
| ALK | 8.68 | IC50 | 2.07 | nM | CHEMBL_ACT_19145475 |
| ALK | 8.55 | IC50 | 2.8 | nM | CHEMBL_ACT_29154955 |
| ALK | 8.54 | IC50 | 2.9 | nM | CHEMBL_ACT_29065666 |
| EML4 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_16427309 |
| ALK | 8.41 | IC50 | 3.9 | nM | CHEMBL_ACT_22775383 |
| EML4 | 8.35 | IC50 | 4.5 | nM | CHEMBL_ACT_19145445 |
| RET | 8.32 | IC50 | 4.8 | nM | CHEMBL_ACT_16655171 |
| RET | 8.32 | IC50 | 4.8 | nM | CHEMBL_ACT_24867179 |
| RET | 8.32 | IC50 | 4.8 | nM | CHEMBL_ACT_25935697 |
| RET | 8.32 | IC50 | 4.8 | nM | CHEMBL_ACT_25935698 |
| RET | 8.32 | IC50 | 4.8 | nM | CHEMBL_ACT_25935699 |
| RET | 8.32 | IC50 | 4.8 | nM | CHEMBL_ACT_25935700 |
| RET | 8.32 | IC50 | 4.8 | nM | CHEMBL_ACT_25935701 |
| RET | 8.32 | IC50 | 4.8 | nM | CHEMBL_ACT_25935702 |
| RET | 8.32 | IC50 | 4.8 | nM | CHEMBL_ACT_29065580 |
| ALK | 8.28 | IC50 | 5.3 | nM | CHEMBL_ACT_17704364 |
| RET | 8.24 | IC50 | 5.7 | nM | CHEMBL_ACT_24867185 |
| RET | 8.08 | IC50 | 8.3 | nM | CHEMBL_ACT_24867184 |
| EML4 | 8.05 | IC50 | 9 | nM | CHEMBL_ACT_16427340 |
Target pathways
Aggregated over 2 target gene(s): MET, ALK.
Top Reactome pathways
57 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 2 | ALK, MET |
| Disease | 2 | ALK, MET |
| Diseases of signal transduction by growth factor receptors and second messengers | 2 | ALK, MET |
| Signaling by Receptor Tyrosine Kinases | 2 | ALK, MET |
| PIP3 activates AKT signaling | 1 | MET |
| Developmental Biology | 1 | MET |
| Negative regulation of the PI3K/AKT network | 1 | MET |
| Signaling by ALK | 1 | ALK |
| Generic Transcription Pathway | 1 | MET |
| PI3K/AKT Signaling in Cancer | 1 | MET |
| Constitutive Signaling by Aberrant PI3K in Cancer | 1 | MET |
| Semaphorin interactions | 1 | MET |
| Sema4D in semaphorin signaling | 1 | MET |
| Sema4D mediated inhibition of cell attachment and migration | 1 | MET |
| Axon guidance | 1 | MET |
| Infectious disease | 1 | MET |
| RAF/MAP kinase cascade | 1 | MET |
| MAPK family signaling cascades | 1 | MET |
| MAPK1/MAPK3 signaling | 1 | MET |
| Signaling by MET | 1 | MET |
| MET Receptor Activation | 1 | MET |
| Negative regulation of MET activity | 1 | MET |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 1 | MET |
| RNA Polymerase II Transcription | 1 | MET |
| Gene expression (Transcription) | 1 | MET |
| MET activates RAS signaling | 1 | MET |
| MET activates PI3K/AKT signaling | 1 | MET |
| MET activates PTPN11 | 1 | MET |
| MET activates PTK2 signaling | 1 | MET |
| InlB-mediated entry of Listeria monocytogenes into host cell | 1 | MET |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| cell surface receptor protein tyrosine kinase signaling pathway | 2 |
| protein phosphorylation | 2 |
| signal transduction | 2 |
| endothelial cell morphogenesis | 1 |
| liver development | 1 |
| cell surface receptor signaling pathway | 1 |
| negative regulation of autophagy | 1 |
| neuron differentiation | 1 |
| pancreas development | 1 |
| positive regulation of transcription by RNA polymerase II | 1 |
| hepatocyte growth factor receptor signaling pathway | 1 |
| branching morphogenesis of an epithelial tube | 1 |
| positive chemotaxis | 1 |
| excitatory postsynaptic potential | 1 |
| semaphorin-plexin signaling pathway | 1 |
Indications & clinical
Indications
27 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 |
| thyroid gland papillary carcinoma | 2 | MONDO:0005075 | EFO:0000641 |
| sarcoma | 2 | MONDO:0005089 | EFO:0000691 |
| melanoma | 2 | MONDO:0005105 | EFO:0000756 |
| anaplastic large cell lymphoma | 2 | MONDO:0020325 | EFO:0003032 |
| salivary gland cancer | 2 | MONDO:0004669 | EFO:0003826 |
| brain neoplasm | 2 | MONDO:0021211 | EFO:0003833 |
| pancreatic neoplasm | 2 | MONDO:0021040 | EFO:0003860 |
| ovarian neoplasm | 2 | MONDO:0021068 | EFO:0003893 |
| colorectal neoplasm | 2 | MONDO:0005335 | EFO:0004142 |
| upper aerodigestive tract neoplasm | 2 | MONDO:0005398 | EFO:0004284 |
| cholangiocarcinoma | 2 | MONDO:0019087 | EFO:0005221 |
| bronchial neoplasm | 2 | MONDO:0002807 | EFO:1000849 |
| lung neoplasm | 2 | MONDO:0021117 | MONDO:0021117 |
| lymphoid neoplasm | 2 | MONDO:0005157 | EFO:0001642 |
| neuroendocrine neoplasm | 2 | MONDO:0019496 | EFO:1001901 |
| respiratory system disorder | 2 | MONDO:0005087 | EFO:0000684 |
| thyroid tumor | 2 | MONDO:0015074 | EFO:0003841 |
| respiratory tract neoplasm | 2 | MONDO:0020641 | EFO:0003853 |
| digestive system neoplasm | 2 | MONDO:0021223 | EFO:0008549 |
| intestinal cancer | 2 | MONDO:0005814 | MONDO:0021118 |
| liver disorder | 1 | MONDO:0005154 | EFO:0001421 |
| glioblastoma | 1 | MONDO:0018177 | EFO:0000519 |
| central nervous system cancer | 1 | MONDO:0002714 | EFO:0000326 |
| hepatocellular carcinoma | 1 | MONDO:0007256 | EFO:0000182 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 67.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 24 |
| Not specified | 12 |
| PHASE1/PHASE2 | 11 |
| PHASE3 | 8 |
| PHASE1 | 7 |
| PHASE2/PHASE3 | 3 |
| PHASE4 | 1 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05525338 | PHASE4 | RECRUITING | Comparison of Standard Dose Alectinib to Alectinib in Adjusted Dose Based on Alectinib Bloodlevels |
| NCT02838420 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Evaluate and Compare the Efficacy and Safety of Alectinib Versus Crizotinib and to Evaluate the Pharmacokinetics of Alectinib in Asian Participants With Treatment-Naive Anaplastic Lymphoma Kinase (ALK)-Positive Advanced Non-Small Cell Lung Cancer (NSCLC) |
| NCT03178552 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Evaluate the Efficacy and Safety of Multiple Targeted Therapies as Treatments for Participants With Non-Small Cell Lung Cancer (NSCLC) |
| NCT03194893 | PHASE3 | ACTIVE_NOT_RECRUITING | A Rollover Study of Alectinib in Patients With Anaplastic Lymphoma Kinase (ALK)-Positive or Rearranged During Transfection (RET)-Positive Cancer |
| NCT03768063 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study in Patients Previously Enrolled in a Genentech and/or F. Hoffmann-La Roche Ltd Sponsored Atezolizumab Study |
| NCT05170204 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study Evaluating the Efficacy and Safety of Multiple Therapies in Cohorts of Participants With Locally Advanced, Unresectable, Stage III Non-Small Cell Lung Cancer (NSCLC) |
| NCT05722886 | PHASE2/PHASE3 | RECRUITING | DETERMINE (Determining Extended Therapeutic Indications for Existing Drugs in Rare Molecularly Defined Indications Using a National Evaluation Platform Trial) - Master Screening Protocol |
| NCT05770037 | PHASE2/PHASE3 | RECRUITING | DETERMINE Trial Treatment Arm 01: Alectinib in Adult, Paediatric and Teenage/Young Adult Patients With ALK Positive Cancers |
| NCT06765109 | PHASE3 | RECRUITING | Neladalkib (NVL-655) for TKI-naive Patients With Advanced ALK-Positive NSCLC |
| NCT02075840 | PHASE3 | COMPLETED | A Study Comparing Alectinib With Crizotinib in Treatment-Naive Anaplastic Lymphoma Kinase-Positive Advanced Non-Small Cell Lung Cancer Participants |
| NCT02604342 | PHASE3 | COMPLETED | Alectinib Versus Pemetrexed or Docetaxel in Anaplastic Lymphoma Kinase (ALK)-Positive Advanced Non-Small Cell Lung Cancer (NSCLC) Participants Previously Treated With Platinum-Based Chemotherapy and Crizotinib |
| NCT03596866 | PHASE3 | COMPLETED | A Study of Brigatinib Compared to Alectinib in Adults With Non-Small-Cell Lung Cancer |
| NCT02925234 | PHASE2 | RECRUITING | The Drug Rediscovery Protocol (DRUP Trial) |
| NCT03202940 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | A Phase IB/II Study of Alectinib Combined With Cobimetinib in Advanced ALK-Rearranged (ALK+) NSCLC |
| NCT03944772 | PHASE2 | ACTIVE_NOT_RECRUITING | Phase 2 Platform Study in Patients With Advanced Non-Small Lung Cancer Who Progressed on First-Line Osimertinib Therapy (ORCHARD) |
| NCT04116541 | PHASE2 | RECRUITING | A Study Evaluating the Activity of Anti-cancer Treatments Targeting Tumor Molecular Alterations/Characteristics in Advanced / Metastatic Tumors. |
| NCT04302025 | PHASE2 | RECRUITING | A Study of Multiple Therapies in Biomarker-selected Participants With Resectable Stages IB-III Non-small Cell Lung Cancer (NSCLC) |
| NCT04322890 | PHASE2 | RECRUITING | Treatment Strategies and Survival Outcome for Non-small Cell Lung Cancer With Oncogenic Mutation |
| NCT04341181 | PHASE2 | RECRUITING | ProTarget - A Danish Nationwide Clinical Trial on Targeted Cancer Treatment Based on Genomic Profiling |
| NCT04423185 | PHASE2 | RECRUITING | PLATFORM Study of Precision Medicine for Rare Tumors |
| NCT04589845 | PHASE2 | ACTIVE_NOT_RECRUITING | Tumor-agnostic Precision Immuno-oncology and Somatic Targeting Rational for You (TAPISTRY) Platform Study |
| NCT04774718 | PHASE1/PHASE2 | RECRUITING | A Study Evaluating the Safety, Pharmacokinetics, and Efficacy of Alectinib in Pediatric Participants With ALK Fusion-Positive Solid or CNS Tumors |
| NCT05015010 | PHASE2 | ACTIVE_NOT_RECRUITING | Alectinib in Neo-adjuvant Treatment of Stage III NSCLC |
| NCT05159245 | PHASE2 | RECRUITING | The Finnish National Study to Facilitate Patient Access to Targeted Anti-cancer Drugs |
| NCT05713006 | PHASE1/PHASE2 | RECRUITING | Alectinib Pharmacokinetic in Patients With NSCLC |
| NCT05725200 | PHASE2 | RECRUITING | Study to Investigate Outcome of Individualized Treatment in Patients With Metastatic Colorectal Cancer |
| NCT05987644 | PHASE1/PHASE2 | RECRUITING | Delayed or Upfront Brain RAdiotherapy in Treatment naïve Lung Cancer Patients With Asymptomatic or Minimally Symptomatic Brain Metastases and ALK rEarrangements |
| NCT06624059 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | A Study to See How Well and How Safely Different Treatments Work in a Group of Participants With Non-Small Cell Lung Cancer (NSCLC) |
| NCT06692491 | PHASE2 | NOT_YET_RECRUITING | Study of Precision Treatment for Rare Tumours in China Guided by PDO and NGS |
| NCT07560410 | PHASE1/PHASE2 | NOT_YET_RECRUITING | Treatment of Truncated ALK-positive Bone Cancer Using Crizotinib (Xalkori) or Alectinib (Alecensa) |
| NCT01801111 | PHASE1/PHASE2 | COMPLETED | A Study of Alectinib (RO5424802) in Participants With Non-Small Cell Lung Cancer Who Have Anaplastic Lymphoma Kinase (ALK) Mutation and Failed Crizotinib Treatment |
| NCT01871805 | PHASE1/PHASE2 | COMPLETED | A Study of Alectinib (CH5424802/RO5424802) in Participants With Anaplastic Lymphoma Kinase (ALK)-Rearranged Non-Small Cell Lung Cancer (NSCLC) |
| NCT02091141 | PHASE2 | COMPLETED | My Pathway: A Study Evaluating Herceptin/Perjeta, Tarceva, Zelboraf/Cotellic, Erivedge, Alecensa, and Tecentriq Treatment Targeted Against Certain Molecular Alterations in Participants With Advanced Solid Tumors |
| NCT02314481 | PHASE2 | COMPLETED | Deciphering Antitumour Response and Resistance With INtratumour Heterogeneity |
| NCT02521051 | PHASE1/PHASE2 | TERMINATED | Phase I/II Trial of Alectinib and Bevacizumab in Patients With Advanced, Anaplastic Lymphoma Kinase (ALK)-Positive, Non-Small Cell Lung Cancer |
| NCT03131206 | PHASE1/PHASE2 | TERMINATED | A Study of Alectinib in RET-rearranged Non-small Cell Lung Cancer or RET-mutated Thyroid Cancer |
| NCT03155009 | PHASE2 | COMPLETED | A Study of the Efficacy and Safety of Alectinib in Participants With Anaplastic Lymphoma Kinase (ALK)-Rearranged Non-Small Cell Lung Cancer |
| NCT03158389 | PHASE1/PHASE2 | COMPLETED | NCT Neuro Master Match - N²M² (NOA-20) |
| NCT03445000 | PHASE2 | TERMINATED | ALEctinib for the Treatment of Pretreated RET-rearranged Advanced Non-small Cell Lung Cancer |
| NCT03498521 | PHASE2 | COMPLETED | A Phase II Randomized Study Comparing the Efficacy and Safety of Targeted Therapy or Cancer Immunotherapy Versus Platinum-Based Chemotherapy in Patients With Cancer of Unknown Primary Site |
Clinical evidence (CIViC)
Variant × indication × effect (32 predictive associations from 41 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| ALK Fusion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Alectinib | CIViC A | EID12012 +8 |
| ALK Fusion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Crizotinib + Alectinib | CIViC B | EID4858 |
| ALK Fusion | Gastrointestinal Carcinoma | Sensitivity/Response | Alectinib + Crizotinib + Entrectinib | CIViC C | EID10324 |
| EML4::ALK Fusion | Malignant Pleural Mesothelioma | Sensitivity/Response | Alectinib | CIViC C | EID9228 |
| FUS::TFCP2 Fusion AND ALK Exon 2-18 Deletion | Spindle Cell Rhabdomyosarcoma | Sensitivity/Response | Alectinib | CIViC C | EID12406 |
| KANK4::ALK Fusion | Pancreatic Acinar Cell Adenocarcinoma | Sensitivity/Response | Alectinib | CIViC C | EID10327 |
| RET Fusion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Alectinib | CIViC C | EID4850 |
| ALK I1171 | Lung Non-small Cell Carcinoma | Resistance | Alectinib | CIViC C | EID1283 +1 |
| ALK I1171N AND HIP1::ALK Fusion | Lung Non-small Cell Carcinoma | Resistance | Alectinib + Crizotinib | CIViC C | EID1483 |
| EML4::ALK Fusion AND ALK I1171N AND ALK L1196M | Malignant Pleural Mesothelioma | Resistance | Alectinib | CIViC C | EID11115 |
| EML4::ALK Fusion AND ALK I1171S | Lung Non-small Cell Carcinoma | Resistance | Alectinib + Crizotinib | CIViC C | EID1484 |
| ALK Alternative Transcript (ATI) | Melanoma | Sensitivity/Response | Ceritinib + Crizotinib + Alectinib + ALK Inhibitor ASP3026 + Entrectinib | CIViC D | EID7484 |
| ALK F1174L | Neuroblastoma | Sensitivity/Response | Alectinib | CIViC D | EID37 |
| EML4::ALK Fusion AND ALK L1196M | Lung Non-small Cell Carcinoma | Sensitivity/Response | Alectinib | CIViC D | EID141 |
| EML4::ALK Fusion AND ALK L1196M | Cancer | Sensitivity/Response | Brigatinib + Lorlatinib + Alectinib + Ceritinib | CIViC D | EID7597 |
| ALK F1174L AND NPM1::ALK Fusion | Cancer | Resistance | Alectinib | CIViC D | EID12665 |
| ALK G1269A AND NPM1::ALK Fusion | Cancer | Resistance | Alectinib | CIViC D | EID12664 |
| ALK G1269A AND v::ALK Fusion | Cancer | Resistance | Alectinib | CIViC D | EID1354 |
| 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 F1174L | Cancer | Resistance | Alectinib | CIViC D | EID12666 |
| EML4::ALK Fusion AND ALK G1202R | Cancer | Resistance | Alectinib | CIViC D | EID1350 |
| 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 |
| EML4::ALK Fusion AND ALK G1269A | Cancer | Resistance | Alectinib | CIViC D | EID12669 |
| EML4::ALK Fusion AND ALK I1171S | Cancer | Resistance | Alectinib | CIViC D | EID12670 |
| EML4::ALK Fusion AND ALK R1192P | Cancer | Resistance | Alectinib | CIViC D | EID12667 |
| EML4::ALK Fusion AND ALK T1151M | Cancer | Resistance | Alectinib | CIViC D | EID12668 |
| EML4::ALK Fusion AND ALK T1151dup | Lung Non-small Cell Carcinoma | Resistance | Alectinib | CIViC D | EID1347 |
| EML4::ALK Fusion AND ALK V1180L | Lung Non-small Cell Carcinoma | Resistance | Alectinib | CIViC D | EID1286 |
+2 more predictive associations (showing top 30 by level).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 6 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.
102 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| AFATINIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, MET |
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, MET |
| GEFITINIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, MET |
| PAZOPANIB | ChEMBL + PubChem | Phase 4 (approved) | ALK, MET |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | ALK, MET |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | ALK, MET |
| CERITINIB | ChEMBL | Phase 4 (approved) | ALK, MET |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | ALK, MET |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | ALK, MET |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | ALK, MET |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | ALK, MET |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | ALK, MET |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | ALK, MET |
| PALBOCICLIB | ChEMBL | Phase 4 (approved) | ALK, MET |
| SUNITINIB | ChEMBL | Phase 4 (approved) | ALK, MET |
| VANDETANIB | ChEMBL | Phase 4 (approved) | ALK, MET |
| CANERTINIB | ChEMBL | Phase 3 | ALK, MET |
| CEDIRANIB | ChEMBL | Phase 3 | ALK, MET |
| DACTOLISIB | ChEMBL | Phase 3 | ALK, MET |
| LESTAURTINIB | ChEMBL | Phase 3 | ALK, MET |
| LINIFANIB | ChEMBL | Phase 3 | ALK, MET |
| QUERCETIN | ChEMBL | Phase 3 | ALK, MET |
| BEMCENTINIB | ChEMBL | Phase 2 | ALK, MET |
| BI-2536 | ChEMBL | Phase 2 | ALK, MET |
| BMS-754807 | ChEMBL | Phase 2 | ALK, MET |
| CENISERTIB | ChEMBL | Phase 2 | ALK, MET |
| ENVONALKIB | ChEMBL | Phase 2 | ALK, MET |
| FORETINIB | ChEMBL | Phase 2 | ALK, MET |
| ILORASERTIB | ChEMBL | Phase 2 | ALK, MET |
| OSI-632 | ChEMBL | Phase 2 | ALK, MET |
| PELITINIB | ChEMBL | Phase 2 | ALK, MET |
| R-406 | ChEMBL | Phase 2 | ALK, MET |
| SU-014813 | ChEMBL | Phase 2 | ALK, MET |
| TOZASERTIB | ChEMBL | Phase 2 | ALK, MET |
| Idelalisib | PubChem | Approved | ALK, MET |
| Selumetinib | PubChem | Approved | ALK, MET |
| AFATINIB DIMALEATE | ChEMBL | Phase 4 (approved) | MET |
| AXITINIB | ChEMBL | Phase 4 (approved) | MET |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | MET |
| CABOZANTINIB S-MALATE | ChEMBL | Phase 4 (approved) | MET |
| CAPMATINIB | ChEMBL | Phase 4 (approved) | MET |
| DABRAFENIB | ChEMBL | Phase 4 (approved) | MET |
| ENSARTINIB | ChEMBL | Phase 4 (approved) | MET |
| GILTERITINIB | ChEMBL | Phase 4 (approved) | ALK |
| LORLATINIB | ChEMBL | Phase 4 (approved) | ALK |
| NERATINIB | ChEMBL | Phase 4 (approved) | MET |
| OSIMERTINIB | ChEMBL | Phase 4 (approved) | ALK |
| REPOTRECTINIB | ChEMBL | Phase 4 (approved) | ALK |
| RUXOLITINIB | ChEMBL | Phase 4 (approved) | ALK |
| SORAFENIB | ChEMBL | Phase 4 (approved) | MET |
| TEPOTINIB | ChEMBL | Phase 4 (approved) | MET |
| TIVOZANIB | ChEMBL | Phase 4 (approved) | MET |
| UPADACITINIB | ChEMBL | Phase 4 (approved) | ALK |
| ALVOCIDIB | ChEMBL | Phase 3 | ALK |
| DOVITINIB | ChEMBL | Phase 3 | ALK |
| ENZASTAURIN | ChEMBL | Phase 3 | MET |
| EPIGALOCATECHIN GALLATE | ChEMBL | Phase 3 | MET |
| LINSITINIB | ChEMBL | Phase 3 | MET |
| POZIOTINIB | ChEMBL | Phase 3 | MET |
| RIGOSERTIB | ChEMBL | Phase 3 | MET |
Related Atlas pages
- Genes: MET, ALK
- Diseases: neoplasm, non-small cell lung carcinoma, digestive system carcinoma, malignant pleural mesothelioma, spindle cell rhabdomyosarcoma, pancreatic acinar cell carcinoma, melanoma, neuroblastoma, cancer, lung adenocarcinoma
- Drugs: Afatinib, Crizotinib, Gefitinib, Pazopanib, Bosutinib, Brigatinib, Ceritinib, Entrectinib, Erlotinib, Fedratinib, Infigratinib, Midostaurin, Nintedanib, Palbociclib, Sunitinib, Vandetanib, Canertinib, Cediranib, Dactolisib, Lestaurtinib, Linifanib, Quercetin, Idelalisib, Selumetinib, Axitinib, Cabozantinib, Capmatinib, Dabrafenib, Ensartinib, Gilteritinib, Lorlatinib, Neratinib, Osimertinib, Repotrectinib, Ruxolitinib, Sorafenib, Tepotinib, Tivozanib, Upadacitinib, Alvocidib, Dovitinib, Enzastaurin, Epigalocatechin Gallate, Linsitinib, Poziotinib, Rigosertib