Clinical Trials

Lapatinib Ditosylate has been evaluated across numerous clinical trials spanning early-phase to Phase 3 designs, primarily targeting HER2-overexpressing and metastatic breast cancer alongside head and neck, platinum-resistant ovarian, thyroid, and glioblastoma malignancies. Sponsored by academic centers, cooperative networks like the EORTC, and industry partners including Novartis and GlaxoSmithKline, these studies encompass completed, active not recruiting, terminated, and withdrawn statuses. Together, these protocols demonstrate extensive clinical investigation across diverse oncology indications.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01947023 ACTIVE_NOT_RECRUITING
Metastatic Thyroid Gland Carcinoma; Unresectable Thyroid Gland Carcinoma
National Cancer Institute (NCI)
 2013-09-27 PHASE1
NCT00455039 Withdrawn
Breast Cancer
University of New Mexico
 2023-07-31 Phase 1|Phase 2
NCT02101905 COMPLETED
Anaplastic Astrocytoma; Anaplastic Ependymoma; Anaplastic Oligodendroglioma; Gliosarcoma; Mixed Glioma; Recurrent Adult Brain Neoplasm; Recurrent Glioblastoma
National Cancer Institute (NCI)
 2016-11-07 PHASE1
NCT01873833 TERMINATED
HER2-positive Breast Cancer; Recurrent Breast Cancer; Stage IV Breast Cancer
University of Southern California
 2013-07-29 PHASE2
NCT04608409 Active not recruiting
Ovarian Cancer
Frederick R. Ueland M.D.|National Cancer Institute (NCI)|University of Kentucky
 2021-03-17 Phase 1
NCT01622868 COMPLETED
HER2-Positive Breast Carcinoma; Invasive Breast Carcinoma; Metastatic Malignant Neoplasm in the Brain; Recurrent Breast Carcinoma; Stage IV Breast Cancer AJCC v6 and v7
National Cancer Institute (NCI)
 2012-12-06 PHASE2
NCT01783756 COMPLETED
Central Nervous System Metastases; HER2-positive Breast Cancer; Male Breast Cancer; Recurrent Breast Cancer; Stage IV Breast Cancer
Jonsson Comprehensive Cancer Center
 2013-06-26 PHASE1; PHASE2
NCT01104571 UNKNOWN
Breast Cancer
Institute of Cancer Research, United Kingdom
 2010-04 PHASE3
NCT03075995 Unknown status
Breast Cancer
Sun Yat-sen University
 2017-04-12 Not Applicable
NCT01557764 WITHDRAWN
Breast Neoplasms
Washington University School of Medicine
 2012-09 PHASE2
NCT01434303 COMPLETED
HER2/Neu Positive; Invasive Breast Carcinoma; Recurrent Breast Carcinoma; Stage IV Breast Cancer AJCC v6 and v7
National Cancer Institute (NCI)
 2012-01-10 PHASE1
NCT01044433 COMPLETED
Head and Neck Cancer; Metastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma; Recurrent Metastatic Squamous Neck Cancer With Occult Primary; Recurrent Salivary Gland Cancer; Recurrent Squamous Cell Carcinoma of the Hypopharynx; Recurrent Squamous Cell Carcinoma of the Larynx; Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity; Recurrent Squamous Cell Carcinoma of the Oropharynx; Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity; Recurrent Verrucous Carcinoma of the Larynx; Recurrent Verrucous Carcinoma of the Oral Cavity; Salivary Gland Squamous Cell Carcinoma; Stage IV Salivary Gland Cancer; Stage IV Squamous Cell Carcinoma of the Hypopharynx; Stage IV Squamous Cell Carcinoma of the Larynx; Stage IV Squamous Cell Carcinoma of the Lip and Oral Cavity; Stage IV Squamous Cell Carcinoma of the Oropharynx; Stage IV Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity; Stage IV Verrucous Carcinoma of the Larynx; Stage IV Verrucous Carcinoma of the Oral Cavity
Abramson Cancer Center at Penn Medicine
 2009-10 PHASE2
NCT00949455 UNKNOWN
Bladder Cancer
Queen Mary University of London
 2009-03 PHASE2; PHASE3
NCT00662636 COMPLETED
Unspecified Adult Solid Tumor, Protocol Specific
Mayo Clinic
 2008-08 PHASE1
NCT02338245 Completed
Metastatic Breast Cancer
ASLAN Pharmaceuticals
 2014-12-29 Phase 2
NCT02294786 Terminated
Cancer
Novartis Pharmaceuticals|Novartis
 2014-12-17 Phase 2
NCT01868503 TERMINATED
Male Breast Cancer; Recurrent Breast Cancer; Stage IIIA Breast Cancer; Stage IIIB Breast Cancer; Stage IIIC Breast Cancer
Stanford University
 2013-07 PHASE2
NCT02158507 Active not recruiting
Metastatic Triple Negative Breast Cancer
University of Alabama at Birmingham|Breast Cancer Research Foundation of Alabama|GlaxoSmithKline|AbbVie
 2014-09 Not Applicable
NCT00555152 COMPLETED
Ductal Breast Carcinoma In Situ; HER2/Neu Positive
National Cancer Institute (NCI)
 2009-08-19
NCT01245205 COMPLETED
HER2-positive Breast Cancer; Male Breast Cancer; Recurrent Breast Cancer; Stage IIIB Breast Cancer; Stage IIIC Breast Cancer; Stage IV Breast Cancer; Unspecified Adult Solid Tumor, Protocol Specific
National Cancer Institute (NCI)
 2010-11 PHASE1
NCT00390455 COMPLETED
Estrogen Receptor Positive; HER2 Positive Breast Carcinoma; HER2/Neu Negative; Progesterone Receptor Positive; Recurrent Breast Carcinoma; Stage IIIB Breast Cancer AJCC v7; Stage IIIC Breast Cancer AJCC v7; Stage IV Breast Cancer AJCC v6 and v7
National Cancer Institute (NCI)
 2006-09-15 PHASE3
NCT00770809 COMPLETED
Male Breast Carcinoma; Stage IIA Breast Cancer AJCC v6 and v7; Stage IIB Breast Cancer AJCC v6 and v7; Stage IIIA Breast Cancer AJCC v7; Stage IIIB Breast Cancer AJCC v7; Stage IIIC Breast Cancer AJCC v7
National Cancer Institute (NCI)
 2009-02-24 PHASE3
NCT00684983 COMPLETED
HER2 Positive Breast Carcinoma; Recurrent Breast Carcinoma; Stage IIIB Breast Cancer AJCC v7; Stage IIIC Breast Cancer AJCC v7; Stage IV Breast Cancer AJCC v6 and v7
National Cancer Institute (NCI)
 2008-07-30 PHASE2
NCT01281163 TERMINATED
Estrogen Receptor Negative; Estrogen Receptor Positive; HER2/Neu Positive; Progesterone Receptor Negative; Progesterone Receptor Positive; Recurrent Breast Carcinoma; Stage IV Breast Cancer
National Cancer Institute (NCI)
 2011-01 PHASE1
NCT01688609 COMPLETED
HER2-positive Breast Cancer; Stage II Breast Cancer; Stage IIIA Breast Cancer
National Cancer Institute (NCI)
 2012-07 PHASE2
NCT00769470 COMPLETED
Breast Cancer
Translational Oncology Research International
 2009-04 PHASE2
NCT01123473 TERMINATED
Adenocarcinoma of the Gastroesophageal Junction; Gastric Cancer
European Organisation for Research and Treatment of Cancer - EORTC
 2010-12 PHASE2
NCT01382706 TERMINATED
Recurrent Bladder Cancer; Stage III Bladder Cancer; Stage IV Bladder Cancer; Transitional Cell Carcinoma of the Bladder
University of Southern California
 2011-06-13 PHASE2
NCT00544804 COMPLETED
Breast Cancer; Metastatic Cancer
University of California, San Francisco
 2007-08 PHASE1
NCT00103194 COMPLETED
Recurrent Prostate Cancer; Stage I Prostate Cancer; Stage IIA Prostate Cancer; Stage IIB Prostate Cancer; Stage III Prostate Cancer
National Cancer Institute (NCI)
 2005-09 PHASE2
NCT00688194 UNKNOWN
Breast Cancer
Gruppo Italiano Mammella (GIM)
 2008-05 PHASE3
NCT01705340 TERMINATED
Adenocarcinoma of the Gastroesophageal Junction; HER2-positive Breast Cancer; Male Breast Cancer; Recurrent Breast Cancer; Recurrent Esophageal Cancer; Recurrent Gastric Cancer; Stage IIIC Breast Cancer; Stage IIIC Esophageal Cancer; Stage IIIC Gastric Cancer; Stage IV Breast Cancer; Stage IV Esophageal Cancer; Stage IV Gastric Cancer
National Cancer Institute (NCI)
 2012-09 PHASE1
NCT00667251 COMPLETED
Breast Cancer
Novartis Pharmaceuticals
 2008-10-07 PHASE3
NCT00246753 COMPLETED
Prostate Cancer
UNC Lineberger Comprehensive Cancer Center
 2005-10 PHASE2
NCT00623064 COMPLETED
Bladder Cancer; Transitional Cell Cancer of the Renal Pelvis and Ureter
European Organisation for Research and Treatment of Cancer - EORTC
 2007-11 PHASE1
NCT00967031 COMPLETED
Breast Cancer; Metastatic Cancer
UNICANCER
 2009-04 PHASE2
NCT00804310 TERMINATED
Unspecified Adult Solid Tumor, Protocol Specific
University of California, Davis
 2009-08 PHASE1
NCT00316875 COMPLETED
Breast Cancer
Northwestern University
 2006-05 PHASE1
NCT00118157 COMPLETED
Estrogen Receptor Positive; Male Breast Carcinoma; Progesterone Receptor Positive; Recurrent Breast Carcinoma; Stage IIIB Breast Cancer; Stage IIIC Breast Cancer; Stage IV Breast Cancer
National Cancer Institute (NCI)
 2005-05 PHASE2
NCT00482391 COMPLETED
Breast Cancer
Memorial Sloan Kettering Cancer Center
 2007-03 PHASE2
NCT00096447 COMPLETED
Recurrent Endometrial Carcinoma
National Cancer Institute (NCI)
 2004-11 PHASE2
NCT00113373 COMPLETED
Primary Peritoneal Cavity Cancer; Recurrent Ovarian Epithelial Cancer
National Cancer Institute (NCI)
 2005-05 PHASE2
NCT00820872 COMPLETED
Breast Cancer
Alliance for Clinical Trials in Oncology
 2009-02 PHASE2
NCT00962312 COMPLETED
Pancreatic Cancer
Cancer Trials Ireland
 2009-01 PHASE2
NCT00095940 COMPLETED
Recurrent Childhood Anaplastic Astrocytoma; Recurrent Childhood Brain Stem Glioma; Recurrent Childhood Ependymoma; Recurrent Childhood Giant Cell Glioblastoma; Recurrent Childhood Glioblastoma; Recurrent Childhood Gliosarcoma; Recurrent Childhood Medulloblastoma; Recurrent Childhood Oligodendroglioma
National Cancer Institute (NCI)
 2004-10 PHASE1; PHASE2
NCT00379509 COMPLETED
Breast Cancer
UNC Lineberger Comprehensive Cancer Center
 2006-04 PHASE1
NCT00499681 TERMINATED
Breast Cancer
Vanderbilt-Ingram Cancer Center
 2007-07 PHASE2
NCT00424164 COMPLETED
Breast Cancer
European Organisation for Research and Treatment of Cancer - EORTC
 2006-11 PHASE1
NCT00107536 COMPLETED
Adult Primary Hepatocellular Carcinoma; Advanced Adult Primary Liver Cancer; Localized Unresectable Adult Primary Liver Cancer; Recurrent Adult Primary Liver Cancer; Recurrent Extrahepatic Bile Duct Cancer; Recurrent Gallbladder Cancer; Unresectable Extrahepatic Bile Duct Cancer; Unresectable Gallbladder Cancer
National Cancer Institute (NCI)
 2005-10 PHASE2
NCT00389922 COMPLETED
Unspecified Adult Solid Tumor, Protocol Specific
University of California, Davis
 2005-12 PHASE1
NCT00436566 COMPLETED
Breast Cancer; Cardiac Toxicity
Mayo Clinic
 2007-03-16 PHASE2
NCT00095563 COMPLETED
High-grade Salivary Gland Carcinoma; High-grade Salivary Gland Mucoepidermoid Carcinoma; Low-grade Salivary Gland Carcinoma; Low-grade Salivary Gland Mucoepidermoid Carcinoma; Recurrent Adenoid Cystic Carcinoma of the Oral Cavity; Recurrent Salivary Gland Cancer; Salivary Gland Acinic Cell Tumor; Salivary Gland Adenocarcinoma; Salivary Gland Adenoid Cystic Carcinoma; Salivary Gland Malignant Mixed Cell Type Tumor
National Cancer Institute (NCI)
 2004-09 PHASE2
NCT00101036 COMPLETED
Adult Primary Hepatocellular Carcinoma; Advanced Adult Primary Liver Cancer; Localized Unresectable Adult Primary Liver Cancer; Recurrent Adult Primary Liver Cancer; Recurrent Extrahepatic Bile Duct Cancer; Recurrent Gallbladder Cancer; Unresectable Extrahepatic Bile Duct Cancer; Unresectable Gallbladder Cancer
National Cancer Institute (NCI)
 2004-11 PHASE2
NCT00498953 COMPLETED
Head and Neck Cancer
European Organisation for Research and Treatment of Cancer - EORTC
 2007-05 PHASE1; PHASE2
NCT00753207 COMPLETED
Breast Cancer
Cancer Trials Ireland
 2007-10 PHASE1
NCT00107003 COMPLETED
Glioma; Brain Tumor; Glioblastoma Multiforme; GBM; Gliosarcoma; GS
National Cancer Institute (NCI)
 2005-03-30 PHASE2
NCT00099060 COMPLETED
Brain and Central Nervous System Tumors
National Cancer Institute (NCI)
 2004-12 PHASE1; PHASE2
NCT00095667 COMPLETED
Recurrent Prostate Cancer; Stage IV Prostate Cancer
National Cancer Institute (NCI)
 2004-11 PHASE2
NCT00352443 COMPLETED
Lymphoma; Unspecified Adult Solid Tumor, Protocol Specific
SWOG Cancer Research Network
 2006-09 PHASE1
NCT00103324 COMPLETED
Diffuse Adenocarcinoma of the Stomach; Intestinal Adenocarcinoma of the Stomach; Mixed Adenocarcinoma of the Stomach; Recurrent Gastric Cancer; Stage III Gastric Cancer; Stage IV Gastric Cancer
National Cancer Institute (NCI)
 2004-12 PHASE2
NCT00098631 COMPLETED
Metastatic Squamous Neck Cancer With Occult Primary; Recurrent Metastatic Squamous Neck Cancer With Occult Primary; Recurrent Squamous Cell Carcinoma of the Hypopharynx; Recurrent Squamous Cell Carcinoma of the Larynx; Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity; Recurrent Squamous Cell Carcinoma of the Nasopharynx; Recurrent Squamous Cell Carcinoma of the Oropharynx; Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity; Salivary Gland Squamous Cell Carcinoma; Stage IV Squamous Cell Carcinoma of the Hypopharynx; Stage IV Squamous Cell Carcinoma of the Larynx; Stage IV Squamous Cell Carcinoma of the Lip and Oral Cavity; Stage IV Squamous Cell Carcinoma of the Nasopharynx; Stage IV Squamous Cell Carcinoma of the Oropharynx; Stage IV Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity; Untreated Metastatic Squamous Neck Cancer With Occult Primary
National Cancer Institute (NCI)
 2004-10 PHASE2
NCT00331630 COMPLETED
Breast Cancer
Northwestern University
 2006-05-04 EARLY_PHASE1
NCT00114283 COMPLETED
Recurrent Salivary Gland Cancer; Recurrent Squamous Cell Carcinoma of the Hypopharynx; Recurrent Squamous Cell Carcinoma of the Larynx; Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity; Recurrent Squamous Cell Carcinoma of the Nasopharynx; Recurrent Squamous Cell Carcinoma of the Oropharynx; Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity; Recurrent Verrucous Carcinoma of the Larynx; Recurrent Verrucous Carcinoma of the Oral Cavity; Salivary Gland Squamous Cell Carcinoma; Stage IV Squamous Cell Carcinoma of the Hypopharynx; Stage IV Squamous Cell Carcinoma of the Nasopharynx; Stage IVA Salivary Gland Cancer; Stage IVA Squamous Cell Carcinoma of the Larynx; Stage IVA Squamous Cell Carcinoma of the Lip and Oral Cavity; Stage IVA Squamous Cell Carcinoma of the Oropharynx; Stage IVA Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity; Stage IVA Verrucous Carcinoma of the Larynx; Stage IVA Verrucous Carcinoma of the Oral Cavity; Stage IVB Salivary Gland Cancer; Stage IVB Squamous Cell Carcinoma of the Larynx; Stage IVB Squamous Cell Carcinoma of the Lip and Oral Cavity; Stage IVB Squamous Cell Carcinoma of the Oropharynx; Stage IVB Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity; Stage IVB Verrucous Carcinoma of the Larynx; Stage IVB Verrucous Carcinoma of the Oral Cavity; Stage IVC Salivary Gland Cancer; Stage IVC Squamous Cell Carcinoma of the Larynx; Stage IVC Squamous Cell Carcinoma of the Lip and Oral Cavity; Stage IVC Squamous Cell Carcinoma of the Oropharynx; Stage IVC Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity; Stage IVC Verrucous Carcinoma of the Larynx; Stage IVC Verrucous Carcinoma of the Oral Cavity; Tongue Cancer
National Cancer Institute (NCI)
 2005-03 PHASE2
NCT00098605 COMPLETED
Central Nervous System Metastases; HER2-positive Breast Cancer; Male Breast Cancer; Recurrent Breast Cancer; Stage IV Breast Cancer; Tumors Metastatic to Brain
National Cancer Institute (NCI)
 2004-10 PHASE2
NCT00085020 COMPLETED
Breast Cancer
Jonsson Comprehensive Cancer Center
 2004-03 PHASE1

(data from https://clinicaltrials.gov, updated on 2026-05-14)

Check the Lapatinib Ditosylate product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Lapatinib Ditosylate reversibly binds to the intracellular ATP-binding domains of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), blocking receptor autophosphorylation and suppressing downstream signaling pathways. This dual tyrosine kinase inhibition disrupts cellular proliferation and survival, providing therapeutic activity against target-driven solid tumors investigated in clinical trials, including breast cancer, head and neck cancer, and ovarian cancer.

Appendix RUO and cGMP Quality Standards

Quality Dimension RUO (Research Use Only) cGMP (Current Good Manufacturing Practice)
Clinical Applicability Prohibited in human clinical trials or medical diagnostics. Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status Non-regulated grade; exempt from drug manufacturing laws. Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment Unclassified analytical or research laboratories. Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control Basic purity and activity testing. Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation Basic equipment calibration; no process validation required. Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance Vendor self-declared without required formal QMS. Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact High risk of IND rejection if used as a critical raw material. Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).

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Note: Technical data last updated: Sep 1, 2026.