Drug · Small Molecule

Lapatinib

CI-DRUG-00000330Explore in graph →NCIt C26653 CHEMBL554 CIViC Approved

Regulatory

Approvals (7)

Each record names the authority, jurisdiction, indication text and status. A drug approved in one jurisdiction for one indication is not 'approved' in general.

openfdaRegulatory5 approval records · authority, jurisdiction and indication text as published.

Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
US FDA	—	Efficacy supplement 2018-12-06 (see label)	approved	Dec 6, 2018	openfda
US FDA	—	Efficacy supplement 2013-10-18 (see label)	approved	Oct 18, 2013

Health Canada records are DIN-level: one row per marketed product (brand, strength, form). The Drug Product Database does not publish indications, so no cancer is stated for these rows, and a cancelled or dormant DIN is the status of that one product — not a withdrawal of the molecule.

Data updated 12 hours agoSource updated unknown

Derived

Development pipeline

Most advanced stage across all cancers, then per top-level cancer reached through trial conditions or approval indications. Approval in any ingested jurisdiction outranks trial phase; counts are interventional studies.

Scope	Stage	Max phase	Active	Recruiting	Phase 3	Trials	Approvals	Jurisdictions	First approval	First trial
All cancers	Approved	Phase 4	4	1	33	217	7	CA, EU, US	Mar 13, 2007	2002-09
Malignant Breast Neoplasm	Approved	Phase 3	1	0	13	82	2	EU, US	Mar 13, 2007	2004-03
Malignant Bladder Neoplasm	Phase3	Phase 3	0	0	1	5	0	—	—	2006-02
Malignant Central Nervous System Neoplasm	Phase2	Phase 2	0	0	0	4

Curated evidence

Clinical evidence (86)

CIViC items in which this therapy appears, grouped by cancer context, then molecular profile. 50 items per page.

civicCuratedShowing 1–50 of 86 evidence items · levels, directions and significance as curated at the source; each row links to its CIViC record.

Therapy	Cancer	Type	Level	Direction · significance	Rating (1–5)	Status	Evidence	Source
ERBB2 D277H1
Lapatinib	Bladder Urothelial Carcinoma

Clinical trials

Trials with this intervention (222)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 101–150 of 222 studies · status and phase as posted by the registrant; each row links to the study record.

NCT	Title	Status	Phase	Enrollment (n)	Sponsor	Countries	Last update	Source
NCT00528281	A Phase II Trial of Lapatinib (TYKERB) + Pemetrexed (ALIMTA) in Advanced Non Small Cell Lung Cancer With an Initial Dose Finding Phase	completed	Phase 1	18	GlaxoSmithKlineINDUSTRY	4	Nov 17, 2017	clinicaltrials
NCT00650910	Study To Examine The Effects Of Lapatinib On The Pharmacokinetics Of Digoxin In Subjects w/ ErbB2 Positive Breast Cancer	completed

Molecule

Record

Kind: Small Molecule
Mechanism: Receptor protein-tyrosine kinase erbB-2 inhibitor; Epidermal growth factor receptor erbB1 inhibitor
Targets: 2 genes
UNII: G873GX646R
Aliases: FMM, GSK 572016, GSK-572016, GSK572016, GW 2016, GW-2016, GW2016, GW 572016, GW-572016, GW572016, GW572016F, GW-572016X, LAPATANIB, Lapatinib, Lapatinib Ditosylate, LAPATINIB DITOSYLATE, LAPATINIB DITOSYLATE MONOHYDRATE, LAPATINIB (FREE BASE), LAPATINIB FREE BASETYKERBLAPATINIBGW 572016N-(3-CHLORO-4-{[(3-FLUOROPHENYL)METHYL]OXY}PHENYL)-6-[5-({[2-(METHYLSULFONYL)ETHYL]AMINO}METHYL)-2-FURANYL]-4-QUINAZOLINAMINE, LAPATINIB (GW-572016), TYKERB, Tyverb, TYVERB

Data updated 15 hours agoSource updated unknown

Identifiers

Codes (4)

Upstream identifiers kept as first-class codes; each links to its registry where a stable public URL exists.

System	Code	Label
ATC (WHO)	L01EH01	LAPATINIB
DIN (Health Canada)	02326442

ERBB2 Amplification11
Lapatinib	Childhood Ependymoma	Predictive	B	Supports Sensitivity Response	1	accepted	EID9778 From a phase one clinical trial, pediatric patients with refractory CNS malignancies were administered 300-1150 mg/m2 twice daily of ERBB2 and EGFR inhibitor lapatinib. The maximum-tolerated dose was … (full text at CIViC) PMID 20713864 · Fouladi et al., 2010 · Open in CIViC	civic
〃	Gastric Adenocarcinoma	Predictive	B	Supports Sensitivity Response	3	accepted	EID1023 TyTAN, a Phase III study in Asian patients, looked at addition of tyrosine kinase inhibitor lapatinib to chemptherapy in advanced HER2 positive gastric cancer. Primary endpoint was Overall Survival (… (full text at CIViC) PMID 24868024 · Satoh et al., 2014 · Open in CIViC	civic
Afatinib + Lapatinib + TrastuzumabSubstitutes	HER2-Positive Breast CarcinomaALIAS	Predictive	B	Supports Sensitivity Response	2	accepted	EID887 In this phase 2 trial, treatment-naive, ERBB2-positive (by IHC) breast cancer patients with stage IIIA, B, C or inflammatory disease were randomized 1:1:1 to afatinib (n = 10), lapatinib (n = 8), or t… (full text at CIViC) PMID 25537159 · Rimawi et al., 2015 · Open in CIViC	civic
Capecitabine + LapatinibCombination	HER2-Positive Breast CarcinomaALIAS	Predictive	B	Supports Sensitivity Response	4	accepted	EID1132 This Phase III trial took patients with locally advanced or metastatic HER2 (ERBB2) positive breast cancer that had progressed on prior trastuzumab treatment. Patients were given capecitabine (n=161)… (full text at CIViC) PMID 17192538 · Geyer et al., 2006 · Open in CIViC	civic
Lapatinib + TrastuzumabCombination	HER2-Positive Breast CarcinomaALIAS	Predictive	B	Supports Sensitivity Response	4	accepted	EID1007 In light of results showing increased PFS using mAB plus TKI in heavily pretreated patients, the efficacy of trastuzumab plus lapatinib in a neoadjuvant setting with untreated stage II or IIIA HER2 po… (full text at CIViC) PMID 22493419 · Guarneri et al., 2012 · Open in CIViC	civic
〃	HER2-Positive Breast CarcinomaALIAS	Predictive	B	Supports Sensitivity Response	4	accepted	EID1009 This Phase III study (EGF104900) was motivated by preclinical and other data demonstrating synergistic activity between lapatinib and trastuzumab against HER2 positive breast cancer (BC) cells. In th… (full text at CIViC) PMID 20124187 · Blackwell et al., 2010 · Open in CIViC	civic
〃	HER2-Positive Breast CarcinomaALIAS	Predictive	B	Supports Sensitivity Response	4	accepted	EID1439 In a randomized open label phase 3 study (NCT00553358), women with HER2 positive primary breast cancer treated with lapatinib plus trasuzumab had higher rates of pathological complete responses than s… (full text at CIViC) PMID 22257673 · Baselga et al., 2012 · Open in CIViC	civic
Lapatinib + TrastuzumabCombination	HER2-Positive Breast CarcinomaALIAS	Predictive	B	Does Not Support Sensitivity Response	4	accepted	EID1008 This Phase III trial compared the activity of lapatinib vs. trastuzumab vs. sequential trastuzumab followed by lapatinib vs. lapatinib plus trastuzumab in an adjuvant treatment setting. 8381 women we… (full text at CIViC) PMID 26255196 · Zardavas et al., 2015 · Open in CIViC	civic
Capecitabine + LapatinibCombination	Malignant Breast Neoplasm	Predictive	A	Supports Sensitivity Response	4	submitted	EID11247 In a phase III, randomized, open-label trial, 408 women with HER2-positive, locally advanced or metastatic breast cancer that, after treatment with regimens that included an anthracycline, a taxane, a… (full text at CIViC) PMID 17192538 · Geyer et al., 2006 · Open in CIViC	civic
Lapatinib + LetrozoleCombination	Malignant Breast Neoplasm	Predictive	A	Supports Sensitivity Response	4	submitted	EID11248 In a phase III, randomized, double-blind, controlled trial, 219 post-menopausal women with HER2-positive, histologically confirmed stage IIIB/IIIC or IV estrogen receptor-positive and/or progesterone … (full text at CIViC) PMID 19786658 · Johnston et al., 2009 · Open in CIViC	civic
Lapatinib + TrastuzumabCombination	Malignant Breast Neoplasm	Predictive	D	Supports Sensitivity Response	3	accepted	EID1006 In-vitro studies using ERBB2 over-expressing breast cancer cell lines BT474 and SKBR3 (with ERBB2 amplification) showed apoptosis under either labatinib or trastuzumab treatment. A marked synergistic… (full text at CIViC) PMID 16091755 · Xia et al., 2005 · Open in CIViC	civic

PTEN Loss2
Lapatinib + TrastuzumabSubstitutes	Gastric Adenocarcinoma	Predictive	B	Supports Resistance	2	accepted	EID864 In 48 patients with advanced gastric cancer, retrospectively analyzed for PTEN expression using IHC, PTEN loss was associated with a shorter duration of response (median 4.2 vs. 6.1 months, p = 0.04) … (full text at CIViC) PMID 25300346 · Zhang et al., 2015 · Open in CIViC	civic
Dactolisib + Lapatinib + TrastuzumabCombination	HER2-Positive Breast CarcinomaALIAS	Predictive	D	Supports Sensitivity Response	2	submitted	EID8280 In a preclinical study, efficacy of NVP-BEZ235 (dactolisib), lapatinib, and trastuzumab combination therapy was evaluated in vitro against HER2 amplified breast cancer cell line BT474 with shRNA-induc… (full text at CIViC) PMID 19010894 · Eichhorn et al., 2008 · Open in CIViC	civic

SEPTIN14 Fusion2
Erlotinib + LapatinibSequential	GlioblastomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	3	submitted	EID11002 Analysing whole transcriptome data from 185 GBM samples from TCGA, EGFR fusion events were found in 7.6% (14) of the cohort. In 6 of 14 cases, in-frame EGFR::SEPT14 (e24:e10) fusions were detected (3.… (full text at CIViC) PMID 23917401 · Frattini et al., 2013 · Open in CIViC	civic
〃	GlioblastomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	2	submitted	EID11155 The primary aim of the study was the characterisation of fusion events in 185 GBM samples. As part of this study, a GBM xenograft with EGFR::SEPT14 fusion, derived from a heavily pre-treated patient, … (full text at CIViC) PMID 23917401 · Frattini et al., 2013 · Open in CIViC	civic

PIK3CA Amplification2
Dactolisib + Lapatinib + TrastuzumabCombination	HER2-Positive Breast CarcinomaALIAS	Predictive	D	Supports Sensitivity Response	2	submitted	EID8273 In a preclinical study, efficacy of NVP-BEZ235 (dactolisib), lapatinib, and trastuzumab combination therapy was evaluated in vitro against HER2 amplified breast cancer cell line BT474 with retrovirall… (full text at CIViC) PMID 19010894 · Eichhorn et al., 2008 · Open in CIViC	civic
Dactolisib + LapatinibSubstitutes	HER2-Positive Breast CarcinomaALIAS	Predictive	D	Supports Sensitivity Response	2	accepted	EID8271 This preclinical study tested the sensitivity of HER2-positive breast cancer cell line BT-474 (heterozygous for PIK3CA K111N) retrovirally transduced with wildtype PIK3CA to NVP-BEZ235 (dactolisib; a … (full text at CIViC) PMID 19010894 · Eichhorn et al., 2008 · Open in CIViC	civic

PIK3CA E545K4
Lapatinib	HER2-Positive Breast CarcinomaALIAS	Predictive	D	Supports Resistance	3	accepted	EID6207 This preclinical study tested, in vitro, the resistance to lapatinib (an anti-HER2 drug) of HER2-positive breast cancer cell lines (BT474 and SKBR3) retrovirally transduced with E545K. The study found… (full text at CIViC) PMID 19010894 · Eichhorn et al., 2008 · Open in CIViC	civic
Dactolisib + LapatinibCombination	HER2-Positive Breast CarcinomaALIAS	Predictive	D	Does Not Support Resistance	2	submitted	EID6212 This preclinical study tested the sensitivity of HER2-positive breast cancer cell line BT-474 (heterozygous for PIK3CA K111N) retrovirally transduced with PIK3CA E545K to NVP-BEZ235 (dactolisib; a dua… (full text at CIViC) PMID 19010894 · Eichhorn et al., 2008 · Open in CIViC	civic
Lapatinib + TrastuzumabCombination	HER2-Positive Breast CarcinomaALIAS	Predictive	D	Supports Resistance	3	accepted	EID6211 In a preclinical study, efficacy of lapatinib and trastuzumab was evaluated in vitro against HER2 amplified breast cancer cell lines BT474 (heterozygous for PIK3CA K111N) or SKBR3, retrovirally transd… (full text at CIViC) PMID 19010894 · Eichhorn et al., 2008 · Open in CIViC	civic
Dactolisib + Lapatinib + TrastuzumabCombination	HER2-Positive Breast CarcinomaALIAS	Predictive	D	Supports Sensitivity Response	2	submitted	EID8181 In a preclinical study, efficacy of trastuzumab, lapatinib, and NVP-BEZ235 (dactolisib) combination therapy was evaluated in vitro against HER2 amplified breast cancer cell line BT474 with retrovirall… (full text at CIViC) PMID 19010894 · Eichhorn et al., 2008 · Open in CIViC	civic

PIK3CA H1047R4
Capivasertib + LapatinibCombination	HER2-Positive Breast CarcinomaALIAS	Predictive	D	Supports Sensitivity Response	3	accepted	EID1506 The HER2 breast cancer cell line KPL4 with PIK3CA H1047R shows sub-optimal responses to trastuzumab and lapatinib, and was used to establish mouse xenografts. Treatment of mice with monotherapy of AZD… (full text at CIViC) PMID 22294718 · Davies et al., 2012 · Open in CIViC	civic
Lapatinib	HER2-Positive Breast CarcinomaALIAS	Predictive	D	Supports Resistance	3	accepted	EID6202 This preclinical study tested, in vitro, the resistance to lapatinib (an anti-HER2 drug) of HER2-positive breast cancer cell lines (BT474 and SKBR3) retrovirally transduced with H1047R. The study foun… (full text at CIViC) PMID 19010894 · Eichhorn et al., 2008 · Open in CIViC	civic
Dactolisib + LapatinibCombination	HER2-Positive Breast CarcinomaALIAS	Predictive	D	Does Not Support Resistance	3	submitted	EID6205 This preclinical study tested the sensitivity to lapatinib and NVP-BEZ235 (dactolisib; a dual PI3K/mTOR inhibitor) of a HER2-positive breast cancer cell line (BT474) retrovirally transduced with PIK3C… (full text at CIViC) PMID 19010894 · Eichhorn et al., 2008 · Open in CIViC	civic
Lapatinib + TrastuzumabCombination	HER2-Positive Breast CarcinomaALIAS	Predictive	D	Supports Resistance	4	accepted	EID6204 In a preclinical study, efficacy of lapatinib and trastuzumab was evaluated in vitro against HER2 amplified breast cancer cell line BT474 (heterozygous for PIK3CA K111N) retrovirally transduced with P… (full text at CIViC) PMID 19010894 · Eichhorn et al., 2008 · Open in CIViC	civic