Drug · CHEMBL554
LAPATINIB
7 sourcespipelines-2026-09-18-0.3.1
Cite this record
ConductScience Library. LAPATINIB. Drugs and targets, record CHEMBL554. Release pipelines-2026-09-18-0.3.1, 18 Sept 2026. https://conductscience.org/library/drugs/CHEMBL554
On this page
Drug
Names and IDs as ChEMBL gives them, through Open Targets.
- Other names
FMM, GSK 572016, GSK-572016, GSK572016, GW-2016, GW-572016, GW-572016X, GW2016, GW572016, GW572016F, LAPATANIB, LAPATINIB (FREE BASE), LAPATINIB (GW-572016), LAPATINIB DITOSYLATE, LAPATINIB DITOSYLATE MONOHYDRATE, LAPATINIB FREE BASETYKERBLAPATINIBGW 572016N-(3-CHLORO-4-{[(3-FLUOROPHENYL)METHYL]OXY}PHENYL)-6-[5-({[2-(METHYLSULFONYL)ETHYL]AMINO}METHYL)-2-FURANYL]-4-QUINAZOLINAMINE, TYKERB, TYVERB
- ChEMBL
- Open Targets' highest stage
- Approval, for 3 of its 68 diseases, from ATC, ClinicalTrials.gov, EMA Human Drugs and TTD
- Open Targets
Targets2
The targets ChEMBL's mechanism records give for the drug, through Open Targets. A mechanism record says what the drug acts on, not how strongly.
| Target | Protein | Mechanism | Action | Gene in Genes |
|---|---|---|---|---|
| EGFR | Epidermal growth factor receptor | Epidermal growth factor receptor erbB1 inhibitor | INHIBITOR | https://conductscience.org/library/genes/1956 |
| ERBB2 | Receptor tyrosine-protein kinase erbB-2 | Receptor protein-tyrosine kinase erbB-2 inhibitor | INHIBITOR | https://conductscience.org/library/genes/2064 |
Source ChEMBL
Diseases68
The diseases Open Targets' clinical reports study the drug for, the most trial reports first. The stage is Open Targets', the highest any of its sources reports for the pair, and each row names the sources that report it.
| Disease | Open Targets' stage | Stage reported by | Reports | Of them trials | Its drugs |
|---|---|---|---|---|---|
| breast cancer | Approval | ClinicalTrials.gov and TTD | 152 | 151 | https://conductscience.org/library/drugs?q=MONDO_0007254 |
| colorectal cancer | Phase 2 | ClinicalTrials.gov | 6 | 6 | https://conductscience.org/library/drugs?q=MONDO_0005575 |
| gastric cancer | Phase 3 | ClinicalTrials.gov | 6 | 6 | https://conductscience.org/library/drugs?q=MONDO_0001056 |
| gastroesophageal junction adenocarcinoma | Phase 3 | ClinicalTrials.gov | 6 | 6 | https://conductscience.org/library/drugs?q=MONDO_0003219 |
| head and neck squamous cell carcinoma | Phase 3 | ClinicalTrials.gov | 5 | 5 | https://conductscience.org/library/drugs?q=MONDO_0010150 |
| non-small cell lung carcinoma | Phase 2 | ClinicalTrials.gov | 5 | 5 | https://conductscience.org/library/drugs?q=MONDO_0005233 |
| ovarian cancer | Phase 2 | ClinicalTrials.gov | 5 | 5 | https://conductscience.org/library/drugs?q=MONDO_0008170 |
| prostate cancer | Phase 2 | ClinicalTrials.gov | 5 | 5 | https://conductscience.org/library/drugs?q=MONDO_0008315 |
| inflammatory breast carcinoma | Phase 2 | ClinicalTrials.gov and TTD | 5 | 4 | https://conductscience.org/library/drugs?q=MONDO_0006804 |
| esophageal adenocarcinoma | Phase 3 | ClinicalTrials.gov | 4 | 4 | https://conductscience.org/library/drugs?q=MONDO_0005028 |
1 to 10 of 68Source Open Targets
See all 68 diseasesTrials253
Trials whose record names the drug by a name ChEMBL states, posted results first, then the largest. Open Targets read each trial's text to find its drugs. 1 more that Open Targets linked to it is not shown, since the release's checks do not confirm it.
| Trial | Title | Phase | Participants | Results first posted | Named as | Linked by | Source |
|---|---|---|---|---|---|---|---|
| NCT00490139 | ALTTO (Adjuvant Lapatinib And/Or Trastuzumab Treatment Optimisation) Study; BIG 2-06/N063D | Phase 3 | 8,381 | 2014-08-18 | lapatinib | Its name | ClinicalTrials.gov |
| NCT00374322 | Tykerb Evaluation After Chemotherapy (TEACH): Lapatinib Versus Placebo In Women With Early-Stage Breast Cancer | Phase 3 | 3,166 | 2014-08-18 | lapatinib | Its name | ClinicalTrials.gov |
| NCT00073528 | Study Comparing Lapatinib (GW572016) And Letrozole Versus Letrozole In Subjects With Advanced Or Metastatic Breast Cancer | Phase 3 | 1,286 | 2012-05-17 | lapatinib | Its name | ClinicalTrials.gov |
| NCT00829166 | A Study of Trastuzumab Emtansine Versus Capecitabine + Lapatinib in Participants With HER2-positive Locally Advanced or Metastatic Breast Cancer | Phase 3 | 991 | 2013-04-23 | lapatinib | Its name | ClinicalTrials.gov |
| NCT00424255 | Study Of Adjuvant Lapatinib In High-Risk Head And Neck Cancer Subjects After Surgery | Phase 3 | 688 | 2014-02-11 | lapatinib | Its name | ClinicalTrials.gov |
| NCT00667251 | Chemotherapy and Lapatinib or Trastuzumab in Treating Women With HER2/Neu-Positive Metastatic Breast Cancer | Phase 3 | 652 | 2014-06-18 | lapatinib | Its name | ClinicalTrials.gov |
| NCT01306045 | Molecular Profiling and Targeted Therapy for Advanced Non-Small Cell Lung Cancer, Small Cell Lung Cancer, and Thymic Malignancies | Phase 2 | 647 | 2023-04-11 | lapatinib | Its name | ClinicalTrials.gov |
| NCT01808573 | A Study of Neratinib Plus Capecitabine Versus Lapatinib Plus Capecitabine in Patients With HER2+ Metastatic Breast Cancer Who Have Received Two or More Prior HER2 Directed Regimens in the Metastatic Setting | Phase 3 | 621 | 2019-12-11 | lapatinib | Its name | ClinicalTrials.gov |
| NCT00075270 | Paclitaxel With / Without GW572016 (Lapatinib) As First Line Therapy For Women With Advanced Or Metastatic Breast Cancer | Phase 3 | 580 | 2014-03-31 | lapatinib | Its name | ClinicalTrials.gov |
| NCT00680901 | LOGiC - Lapatinib Optimization Study in ErbB2 (HER2) Positive Gastric Cancer: A Phase III Global, Blinded Study Designed to Evaluate Clinical Endpoints and Safety of Chemotherapy Plus Lapatinib | Phase 3 | 545 | 2013-10-29 | lapatinib | Its name | ClinicalTrials.gov |
1 to 10 of 253
See all 253 trialsComparisons in its trials77
Comparisons Trial comparisons calculated in the trials whose record names the drug, most participants first. A comparison in one of its trials does not always compare the drug, so read the two groups.
| Comparison | Group 1, with the outcome | Group 2, with the outcome | Participants | Trial | Source |
|---|---|---|---|---|---|
| Lapatinib 1500 mg vs Placebo: Number of Participants With CNS Recurrence | 15 of 1,571 | 21 of 1,576 | 3,147 | NCT00374322 | Trial comparisons |
| Lapatinib 1500 mg vs Placebo: Number of Participants With Any Recurrence of the Initial Disease, Contralateral Breast Cancer, or Death (Disease-free Survival [DFS]) | 184 of 1,571 | 231 of 1,576 | 3,147 | NCT00374322 | Trial comparisons |
| Lapatinib 1500 mg vs Placebo: serious adverse events | 99 of 1,573 | 78 of 1,574 | 3,147 | NCT00374322 | Trial comparisons |
| Placebo + Letrozole 2.5 mg vs Lapatinib 1500 mg + Letrozole 2.5 mg: Number of Participants With PFS in the Intent-To-Treat (ITT) Population as Assessed by the Investigator | 476 of 644 | 413 of 642 | 1,286 | NCT00073528 | Trial comparisons |
| Placebo + Letrozole 2.5 mg vs Lapatinib 1500 mg + Letrozole 2.5 mg: Number of Participants With Evidence of Brain Metastases From the ITT Population | 4 of 644 | 6 of 642 | 1,286 | NCT00073528 | Trial comparisons |
| Placebo + Letrozole 2.5 mg vs Lapatinib 1500 mg + Letrozole 2.5 mg: deaths from any cause | 23 of 624 | 18 of 654 | 1,278 | NCT00073528 | Trial comparisons |
| Placebo + Letrozole 2.5 mg vs Lapatinib 1500 mg + Letrozole 2.5 mg: serious adverse events | 103 of 624 | 150 of 654 | 1,278 | NCT00073528 | Trial comparisons |
| Lapatinib 1500 mg vs Placebo: Number of Participants With a Second Primary Tumor | 9 of 346 | 5 of 342 | 688 | NCT00424255 | Trial comparisons |
| Lapatinib 1500 mg vs Placebo: serious adverse events | 169 of 349 | 133 of 336 | 685 | NCT00424255 | Trial comparisons |
| Neratinib Plus Capecitabine vs Lapatinib Plus Capecitabine: deaths from any cause | 219 of 307 | 243 of 314 | 621 | NCT01808573 | Trial comparisons |
1 to 10 of 77
See all 77 comparisons in its trialsPapers from its trials156
The papers the trials whose record names the drug list on ClinicalTrials.gov as their results (RESULT) or as drawn from them (DERIVED), results first, newest first.
Tests in its trials0
The tests ConductCognition runs that the trials whose record names the drug name in their registered outcomes, as ScienceGraph matched them. ConductCognition's list names the tests it runs, not every test a trial used.
None in this release.
Data dates
The date of each source this release read.
Sources 7
- ClinicalTrials.gov's posted results, through CTTI's AACTFreely available. Acknowledgement requested
- ChEMBL, through Open TargetsCC BY-SA 3.0
- ConductCognition's list of its testsOur own data
- ClinicalTrials.govNo license stated
- NLM's MeSHNLM's terms
- Open TargetsCC0 1.0
- PubMedNLM's terms
Each source's terms
- ClinicalTrials.gov's posted results, through CTTI's AACTClinicalTrials.gov data via Aggregate Analysis of ClinicalTrials.gov (AACT), CTTI. CTTI makes its materials freely available and requests acknowledgement. https://aact.ctti-clinicaltrials.org/documentation/299
- ChEMBL, through Open TargetsCC BY-SA 3.0, for the parts from ChEMBL. Read on 8 Nov 2026 at https://platform-docs.opentargets.org/licence
- ConductCognition's list of its testsOur own data: ConductCognition's list of its tests, https://conductcognition.com
- ClinicalTrials.govnone stated
- NLM's MeSHNLM's
- Open TargetsCC0 1.0. Open Targets asks that users cite its latest paper: Buniello et al. 2025, Open Targets Platform: facilitating therapeutic hypotheses building in drug discovery, Nucleic Acids Research 53(D1):D1467, PMID 39657122. Read on 8 Nov 2026 at https://platform-docs.opentargets.org/licence
- PubMedNLM's terms
ClinicalTrials.gov's data carry an international copyright outside the United States: https://clinicaltrials.gov/about-site/terms-conditions.
For software
Read this drug from software.
The record and each of its lists are JSON, twenty rows a page. No key.
GET https://conductscience.org/api/drugs/v1/CHEMBL554
GET https://conductscience.org/api/drugs/v1/CHEMBL554/diseases?page=2