Tykerb

(lapatinib ditosylate)

ApprovedSmall molecule

Lapatinib ditosylate is used to treat certain types of breast cancer, particularly in patients whose tumors have specific genetic markers. It works by blocking proteins that help cancer cells grow and divide.[2] Tykerb is currently approved and in use across 11 indications[4].[1]

Tykerb is one of 187 small molecule programs targeting Gallbladder Cancer. It is currently in Approved.

Indications

Total Trials

Active Trials

186

Competitors

FDA Application

NDA/BLA/ANDA regulatory filings

Patents

Pipeline

Status by Indication[4][1]

Indication

Gallbladder CancerApproved

Central Nervous System NeoplasmApproved

Urinary Bladder CancerApproved

GliosarcomaApproved

Breast NeoplasmActive, not recruiting

Breast CarcinomaActive, not recruiting

Inflammatory Breast CarcinomaApproved

Adult Hepatocellular CarcinomaApproved

Breast Carcinoma in SituActive, not recruiting

Male Breast CarcinomaCompleted

Gallbladder CancerApproved

Approved

Central Nervous System NeoplasmApproved

Approved

Urinary Bladder CancerApproved

Approved

GliosarcomaApproved

Approved

Breast NeoplasmApproved

Active, not recruiting

Breast CarcinomaApproved

Active, not recruiting

Inflammatory Breast CarcinomaApproved

Approved

Adult Hepatocellular CarcinomaApproved

Approved

Breast Carcinoma in SituPreclinical

Active, not recruiting

Male Breast CarcinomaApproved

Completed

Showing 10 of 11 indications

Competition

Competitive Landscape

71 competitors in Breast Neoplasm

#DrugCompanyPhaseTrials

Tykerb

Novartis

Approved

61 2

Nolvadex

AstraZeneca

Approved

1 3

Bayer Aspirin

Afinitor

Arava

Aromasin

Talzenna

Venclexta

Estrace

Piqray

Ranked by pipeline maturity and clinical activity. Current drug highlighted in teal.

Clinical

Trials by Indication[1]

Breast Cancer29 trials

Lapatinib Ditosylate and Capecitabine in Treating Patients With Stage IV Breast Cancer and Brain Metastases

Completed·UUNICANCER·Phase 2·NCT00967031·45 enrolled

Docetaxel, Carboplatin, and Trastuzumab and/or Lapatinib in Treating Women With Stage I, Stage II, or Stage III Breast Cancer That Can Be Removed by Surgery

Completed·TTranslational Oncology Research International·Phase 2·NCT00769470·18 enrolled

Lapatinib and Doxorubicin Hydrochloride Liposome in Treating Patients With Metastatic Breast Cancer

Completed·NNorthwestern University·Phase 1·NCT00316875·23 enrolled

Show 26 more trials

Lapatinib Resistance in Patients With Breast Cancer

Withdrawn·—··NCT00898573

Lapatinib and Tamoxifen in Treating Patients With Advanced or Metastatic Breast Cancer

Completed·EEuropean Organisation for Research and Treatment of Cancer - EORTC·Phase 1·NCT00424164·20 enrolled

Fulvestrant With or Without Lapatinib and/or Aromatase Inhibitor Therapy in Treating Postmenopausal Women With Metastatic Breast Cancer That Progressed After Previous Aromatase Inhibitor Therapy

Unknown status·GGruppo Italiano Mammella (GIM)·Phase 3·NCT00688194·396 enrolled

Lapatinib and Radiation Therapy in Treating Patients With Locally Recurrent or Chemotherapy-Refractory Locally Advanced or Metastatic Breast Cancer

Completed·UUNC Lineberger Comprehensive Cancer Center·Phase 1·NCT00379509·20 enrolled

Lapatinib in Treating Patients With Advanced or Metastatic Breast Cancer That Overexpresses HER2

Completed·UUniversity of California, San Francisco·Phase 1·NCT00544804·41 enrolled

Lapatinib in Treating Brain Metastases in Patients With Stage IV Breast Cancer and Brain Metastases

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT00098605·37 enrolled

Abraxane and Lapatinib in Treating Patients With Stage I, Stage II, or Stage III Breast Cancer

Completed·NNorthwestern University·Phase 1·NCT00331630·30 enrolled

Capecitabine, Cyclophosphamide, Lapatinib Ditosylate, and Trastuzumab in Treating Patients With HER2-Positive Metastatic Breast Cancer

Terminated·UUniversity of Southern California·Phase 2·NCT01873833·10 enrolled

Lapatinib and Tamoxifen in Treating Patients With Locally Advanced or Metastatic Breast Cancer That Did Not Respond to Previous Tamoxifen

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT00118157·19 enrolled

Trastuzumab or Lapatinib Ditosylate in Treating Women With Early Breast Cancer

Unknown status·IInstitute of Cancer Research, United Kingdom·Phase 3·NCT01104571·257 enrolled

Lapatinib With Trastuzumab in Treating Patients With HER2-Negative/HER2 Mutant Metastatic Breast Cancer

Withdrawn·WWashington University School of Medicine·Phase 2·NCT01557764

Docetaxel, Carboplatin, Trastuzumab, and Lapatinib in Treating Patients With Early Stage Breast Cancer

Completed·AAlliance for Clinical Trials in Oncology·Phase 2·NCT00820872·30 enrolled

Doxorubicin and Cyclophosphamide Followed By Trastuzumab, Paclitaxel, and Lapatinib in Treating Patients With Early-Stage HER2-Positive Breast Cancer That Has Been Removed By Surgery

Completed·MMayo Clinic·Phase 2·NCT00436566·122 enrolled

Chemotherapy and Lapatinib or Trastuzumab in Treating Women With HER2/Neu-Positive Metastatic Breast Cancer

Completed· Novartis logo

Novartis·Phase 3·NCT00667251·652 enrolled

Phase 1b/2 Trial Using Lapatinib, Everolimus and Capecitabine for Treatment of HER-2 Positive Breast Cancer With CNS Metastasis

Completed·JJonsson Comprehensive Cancer Center·Phase 1/2·NCT01783756·9 enrolled

Whole-Brain Radiation Therapy or Stereotactic Radiosurgery With or Without Lapatinib Ditosylate in Treating Patients With Brain Metastasis From HER2-Positive Breast Cancer

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT01622868·143 enrolled

Lapatinib Ditosylate, Trastuzumab, Paclitaxel, and Surgery in Treating Patients With Breast Cancer

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT01688609·18 enrolled

GW572016 and Trastuzumab in Treating Patients With Metastatic Breast Cancer That Overexpresses HER2/Neu

Completed·JJonsson Comprehensive Cancer Center·Phase 1·NCT00085020·13 enrolled

Lapatinib and Epirubicin in Treating Patients With Metastatic Breast Cancer. ICORG 06-30

Completed·CCancer Trials Ireland·Phase 1·NCT00753207·10 enrolled

Lapatinib Ditosylate and Radiation Therapy in Treating Patients With Locally Advanced or Locally Recurrent Breast Cancer

Terminated·SStanford University·Phase 2·NCT01868503·7 enrolled

Lapatinib Ditosylate and Akt Inhibitor MK2206 in Treating Women With Metastatic Breast Cancer

Terminated·NNational Cancer Institute (NCI)·Phase 1·NCT01281163·4 enrolled

Entinostat, Lapatinib Ditosylate and Trastuzumab in Treating Patients With Locally Recurrent or Distant Relapsed Metastatic Breast Cancer Previously Treated With Trastuzumab Only

Completed·NNational Cancer Institute (NCI)·Phase 1·NCT01434303·37 enrolled

Fulvestrant With or Without Lapatinib in Treating Postmenopausal Women With Stage III or Stage IV Breast Cancer That is Hormone Receptor-Positive

Completed·NNational Cancer Institute (NCI)·Phase 3·NCT00390455·295 enrolled

Doxorubicin and Cyclophosphamide Followed by Paclitaxel, Trastuzumab, and Lapatinib in Treating Patients With HER2/Neu-Overexpressed Breast Cancer

Completed·MMemorial Sloan Kettering Cancer Center·Phase 2·NCT00482391·95 enrolled

Akt Inhibitor MK2206 in Combination With Lapatinib Ditosylate in Patients With Advanced or Metastatic Solid Tumors or Breast Cancer

Completed·NNational Cancer Institute (NCI)·Phase 1·NCT01245205·28 enrolled

Capecitabine and Lapatinib Ditosylate With or Without Cixutumumab in Treating Patients With Previously Treated HER2-Positive Stage IIIB-IV Breast Cancer

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT00684983·64 enrolled

Patients With Advanced Solid Tumors3 trials

Dasatinib and Lapatinib Ditolsylate in Treating Patients With Advanced Solid Tumors That Cannot Be Removed By Surgery

Completed·MMayo Clinic·Phase 1·NCT00662636·27 enrolled

Lapatinib and Vinorelbine in Treating Patients With Advanced Solid Tumors

Completed·UUniversity of California, Davis·Phase 1·NCT00389922·22 enrolled

Lapatinib and Ixabepilone in Treating Patients With Advanced Solid Tumors

Terminated·UUniversity of California, Davis·Phase 1·NCT00804310·5 enrolled

Prostate Cancer2 trials

Lapatinib Ditosylate in Treating Patients With a Rising PSA Indicating Recurrent Prostate Cancer

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT00103194·49 enrolled

Lapatinib in Treating Patients With Prostate Cancer That Did Not Respond to Hormone Therapy

Completed·UUNC Lineberger Comprehensive Cancer Center·Phase 2·NCT00246753·29 enrolled

Locally Advanced Cancer1 trial

Combination Chemotherapy and Radiation Therapy With or Without Lapatinib in Treating Patients With Locally Advanced Cancer of the Larynx or Hypopharynx

Completed·EEuropean Organisation for Research and Treatment of Cancer - EORTC·Phase 1/2·NCT00498953·7 enrolled

Glioblastoma Multiforme1 trial

Lapatinib in Treating Patients With Recurrent Glioblastoma Multiforme

Completed·NNational Cancer Institute (NCI)·Phase 1/2·NCT00099060·24 enrolled

25 more indications

Locally Advanced1 trial

S0413 Lapatinib in Treating Patients With Locally Advanced or Metastatic Stomach Cancer

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT00103324·40 enrolled

Biliary Tract Cancer1 trial

Lapatinib Ditosylate in Treating Patients With Unresectable Liver or Biliary Tract Cancer

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT00107536·26 enrolled

Breast1 trial

Chemotherapeutic Agents in Brain/Breast

Completed·—··NCT00795678·10 enrolled

Transitional Cell Carcinoma1 trial

Docetaxel and Lapatinib in Metastatic Transitional Cell Carcinoma in Bladder

Terminated·UUniversity of Southern California·Phase 2·NCT01382706·15 enrolled

Apatinib1 trial

PhII Neo-Adjuvant Letrozole & Lapatinib in Pts w/HER2+ & Hormone Receptor+ Operable Breast CA SPORE

Terminated·VVanderbilt-Ingram Cancer Center·Phase 2·NCT00499681·6 enrolled

Esophageal Cancer1 trial

Akt Inhibitor MK2206, Lapatinib Ditosylate, and Trastuzumab in Treating Patients With Locally Advanced or Metastatic HER2-Positive Breast , Gastric, or Gastroesophageal Cancer That Cannot Be Removed By Surgery

Terminated·NNational Cancer Institute (NCI)·Phase 1·NCT01705340·60 enrolled

Squamous Cell Cancer of the Head and Neck1 trial

Capecitabine and Lapatinib Ditosylate in Treating Patients With Squamous Cell Cancer of the Head and Neck

Completed·—·Phase 2·NCT01044433·44 enrolled

Metastatic Prostate Cancer1 trial

Lapatinib in Treating Patients With Recurrent or Metastatic Prostate Cancer

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT00095667·41 enrolled

Central Nervous System Tumor1 trial

Lapatinib in Treating Young Patients With Recurrent or Refractory Central Nervous System Tumors

Completed·NNational Cancer Institute (NCI)·Phase 1/2·NCT00095940·52 enrolled

Lymphoma1 trial

S0528 Lapatinib and Everolimus in Treating Patients With Advanced Solid Tumors or Non-Hodgkin's Lymphoma

Completed·SSWOG Cancer Research Network·Phase 1·NCT00352443·66 enrolled

Thyroid Cancer1 trial

Dabrafenib and Lapatinib in Treating Patients With Refractory Thyroid Cancer That Cannot Be Removed by Surgery

Active, not recruiting·NNational Cancer Institute (NCI)·Phase 1·NCT01947023·21 enrolled

Metastatic1 trial

A Double Blind Randomised Study of Lapatinib and Placebo in Metastatic TCC of the Urothelium

Unknown status·QQueen Mary University of London·Phase 2/3·NCT00949455·204 enrolled

Metastatic Head and Neck Cancer1 trial

Lapatinib in Treating Patients With Recurrent and/or Metastatic Head and Neck Cancer

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT00098631·88 enrolled

Malignant Brain Tumors1 trial

GW572016 to Treat Recurrent Malignant Brain Tumors

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT00107003·9 enrolled

Recurrent Head and Neck Cancer1 trial

Lapatinib Ditosylate in Treating Patients With Metastatic or Recurrent Head and Neck Cancer

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT00114283·30 enrolled

Breast Carcinoma in Situ1 trial

Lapatinib Ditosylate in Treating Patients With Ductal Breast Carcinoma In Situ

Completed·NNational Cancer Institute (NCI)·N/A·NCT00555152·22 enrolled

Pancreatic Cancer1 trial

Lapatinib Ditosylate and Capecitabine in Treating Patients With Metastatic Pancreatic Cancer

Completed·CCancer Trials Ireland·Phase 2·NCT00962312·9 enrolled

Gastroesophageal Junction Cancer1 trial

Epirubicin Hydrochloride, Cisplatin, and Fluorouracil or Capecitabine With or Without Lapatinib Ditosylate as First-Line Therapy in Treating Patients With Stomach Cancer or Gastroesophageal Junction Cancer

Terminated·EEuropean Organisation for Research and Treatment of Cancer - EORTC·Phase 2·NCT01123473·29 enrolled

Salivary Gland Cancer1 trial

Lapatinib in Treating Patients With Recurrent and/or Metastatic Adenoid Cystic Cancer or Other Salivary Gland Cancers

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT00095563·40 enrolled

Glioma1 trial

Lapatinib Ditosylate Before Surgery in Treating Patients With Recurrent High-Grade Glioma

Completed·NNational Cancer Institute (NCI)·Phase 1·NCT02101905·29 enrolled

Peritoneal Cancer1 trial

Lapatinib in Treating Patients With Persistent or Recurrent Ovarian Epithelial or Peritoneal Cancer

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT00113373·28 enrolled

Endometrial Cancer1 trial

Lapatinib in Treating Patients With Recurrent or Persistent Endometrial Cancer

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT00096447·31 enrolled

Liver Cancer1 trial

Lapatinib in Treating Patients With Locally Advanced or Metastatic Biliary Tract or Liver Cancer That Cannot Be Removed By Surgery

Completed·NNational Cancer Institute (NCI)·Phase 2·NCT00101036·57 enrolled

Metastatic Urothelial Cancer1 trial

Lapatinib, Cisplatin, Gemcitabine as First-Line Therapy in Treating Patients With Locally Advanced or Metastatic Urothelial Cancer

Completed·EEuropean Organisation for Research and Treatment of Cancer - EORTC·Phase 1·NCT00623064·18 enrolled

Male Breast Carcinoma1 trial

Randomized Phase III Trial of Paclitaxel +Trastuzumab + Lapatinib Versus Paclitaxel + Trastuzumab as Neoadjuvant Treatment of HER2-Positive Primary Breast Cancer

Completed·NNational Cancer Institute (NCI)·Phase 3·NCT00770809·305 enrolled

Regulatory

FDA Approval Timeline[5]

Mar 13, 2007

TYKERB

NDA NDA022059

Sources

References

[1]
ClinicalTrials.gov — 61 trial records for lapatinib ditosylate. U.S. National Library of Medicine, National Institutes of Health.
[2]
MedlinePlus Drug Information — Tykerb drug information. U.S. National Library of Medicine, National Institutes of Health.
[3]
ChEMBL — lapatinib ditosylate compound record. European Bioinformatics Institute (EMBL-EBI).
[4]
Open Targets Platform — Drug–disease associations for lapatinib ditosylate. EMBL-EBI & Wellcome Sanger Institute.
[5]
OpenFDA — FDA approval records (NDA NDA022059). U.S. Food & Drug Administration.
[6]
FDA Orange Book — Patent and exclusivity data for Tykerb. U.S. Food & Drug Administration.
[7]
SEC EDGAR — Novartis company filings. U.S. Securities and Exchange Commission.

Details

Drug Info

Quick Facts

Mechanism of Action: Epidermal Growth Factor Receptor Erbb1 Inhibitor; Receptor Protein-Tyrosine Kinase Erbb-2 Inhibitor[3]
Modality: Small molecule[3]
Highest Phase: Approved[1]
Company: Novartis

Patent Landscape[6]

Patent Cliff

Sep 18, 2029

Earliest patent expiration — generic entry possible after this date

Patent #Expires

8821927Sep 18, 2029

Tykerb

Status by Indication[4][1]

Competitive Landscape

Trials by Indication[1]

Breast Cancer29 trials

Patients With Advanced Solid Tumors3 trials

Prostate Cancer2 trials

Locally Advanced Cancer1 trial

Glioblastoma Multiforme1 trial

Locally Advanced1 trial

Biliary Tract Cancer1 trial

Breast1 trial

Transitional Cell Carcinoma1 trial

Apatinib1 trial

Esophageal Cancer1 trial

Squamous Cell Cancer of the Head and Neck1 trial

Metastatic Prostate Cancer1 trial

Central Nervous System Tumor1 trial

Lymphoma1 trial

Thyroid Cancer1 trial

Metastatic1 trial

Metastatic Head and Neck Cancer1 trial

Malignant Brain Tumors1 trial

Recurrent Head and Neck Cancer1 trial

Breast Carcinoma in Situ1 trial

Pancreatic Cancer1 trial

Gastroesophageal Junction Cancer1 trial

Salivary Gland Cancer1 trial

Glioma1 trial

Peritoneal Cancer1 trial

Endometrial Cancer1 trial

Liver Cancer1 trial

Metastatic Urothelial Cancer1 trial

Male Breast Carcinoma1 trial

FDA Approval Timeline[5]

References

Drug Info

Quick Facts

Patent Landscape[6]

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