TYKERB (lapatinib ditosylate)
Tykerb is a kinase inhibitor indicated for two specific combinations in treating advanced or metastatic breast cancer that overexpresses the HER2 protein. First, it is used with capecitabine for patients who have received prior therapy including an anthracycline, a taxane, and trastuzumab; clinical use requires that the disease has progressed specifically on trastuzumab. Second, it is indicated in combination with letrozole for the treatment of postmenopausal women with hormone receptor-positive (HR+), HER2-overexpressing metastatic breast cancer for whom hormonal therapy is indicated.
How TYKERB Works
Lapatinib is a 4-anilinoquinazoline kinase inhibitor that targets the intracellular tyrosine kinase domains of both the Epidermal Growth Factor Receptor (EGFR/ErbB1) and the Human Epidermal Receptor Type 2 (HER2/ErbB2). By inhibiting these pathways, it suppresses the growth of ErbB-driven tumor cells. Notably, lapatinib retains significant activity in breast cancer cell lines that have developed resistance to trastuzumab, suggesting a lack of cross-resistance between the two agents. It also addresses resistance in HR+ tumors that upregulate EGFR or HER2 to bypass standard endocrine therapies.
Development Insights
Details
- Status
- Prescription
- First Approved
- 2007-03-13
- Patent Cliff
- 2029
- Routes
- ORAL
- Dosage Forms
- TABLET
TYKERB Approval History
What TYKERB Treats
1 indicationsTYKERB is approved for 1 conditions since its original approval in 2007. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Breast Cancer
TYKERB Boxed Warning
HEPATOTOXICITY Hepatotoxicity has been observed in clinical trials and postmarketing experience. The hepatotoxicity may be severe and deaths have been reported. Causality of the deaths is uncertain [see Warnings and Precautions (5.2)] . WARNING: HEPATOTOXICITY See full prescribing information for complete boxed warning. Hepatotoxicity has been observed in clinical trials and postmarketing experience. The hepatotoxicity may be severe and deaths have been reported. Causality of the deaths is uncer...
WARNING: HEPATOTOXICITY Hepatotoxicity has been observed in clinical trials and postmarketing experience. The hepatotoxicity may be severe and deaths have been reported. Causality of the deaths is uncertain [see Warnings and Precautions (5.2)] . WARNING: HEPATOTOXICITY See full prescribing information for complete boxed warning. Hepatotoxicity has been observed in clinical trials and postmarketing experience. The hepatotoxicity may be severe and deaths have been reported. Causality of the deaths is uncertain. ( 5.2 )
TYKERB Target & Pathway
ProTarget
A receptor tyrosine kinase that promotes cell growth and division. Approximately 20% of breast cancers overexpress HER2, leading to aggressive tumor growth. Targeting HER2 blocks these growth signals and can trigger immune-mediated destruction of cancer cells.
Pathway Context
HER2 forms dimers with other HER family members to activate growth signaling
A receptor that triggers cell growth, proliferation, and survival when activated. Mutations or overexpression of EGFR drive many cancers, particularly lung cancer. Blocking EGFR stops the growth signals that fuel tumor progression.
TYKERB Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
Direct competitors
Same target(s) AND same indication — head-to-head.
MoA expansion candidates
Same target(s), different indications — where else is this mechanism being explored?
Indication competitors
Same indication, different mechanism — what else might this patient receive?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
What's emerging in TYKERB's indications
See all emerging drugs →Phase 3 candidates targeting molecules with no FDA-approved drug, in indications TYKERB treats. First-in-class if their pivotal trials read out positive.
Drugs Similar to TYKERB
3 of 20FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Clinical Trial Registry
24 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT01947023 | NCI-2013-01748 NCI-2013-01748, 13-061 | Ph 1 | active not recruiting | Dabrafenib and Lapatinib in Treating Patients With Refractory Thyroid Cancer That Cannot Be Removed by Surgery |
| NCT01382706 results posted | 4B-10-4 NCI-2011-01108 | Ph 2 | terminated | Docetaxel and Lapatinib in Metastatic Transitional Cell Carcinoma in Bladder |
| NCT00770809 results posted | NCI-2009-01073 NCI-2009-01073, CDR0000616648 | Ph 3 | completed | Paclitaxel and Trastuzumab With or Without Lapatinib in Treating Patients With Stage II or Stage III Breast Cancer That Can Be Removed by Surgery |
| NCT00667251 results posted | 108919 CLAP016A2303, CAN-NCIC-MA31 | Ph 3 | completed | Chemotherapy and Lapatinib or Trastuzumab in Treating Women With HER2/Neu-Positive Metastatic Breast Cancer |
| NCT02101905 | NCI-2014-00634 NCI-2014-00634, ABTC-1302 | Ph 1 | completed | Lapatinib Ditosylate Before Surgery in Treating Patients With Recurrent High-Grade Glioma |
| NCT01622868 results posted | NCI-2012-01977 NCI-2012-01977, RTOG-1119 | Ph 2 | completed | Whole-Brain Radiation Therapy or Stereotactic Radiosurgery With or Without Lapatinib Ditosylate in Treating Patients With Brain Metastasis From HER2-Positive Breast Cancer |
| NCT01873833 results posted | 1B-12-10 NCI-2013-01086, P30CA014089 | Ph 2 | terminated | Capecitabine, Cyclophosphamide, Lapatinib Ditosylate, and Trastuzumab in Treating Patients With HER2-Positive Metastatic Breast Cancer |
| NCT00684983 results posted | NCI-2009-00665 NCI-2009-00665, PN0733_A15PAMDREVW01 | Ph 2 | completed | Capecitabine and Lapatinib Ditosylate With or Without Cixutumumab in Treating Patients With Previously Treated HER2-Positive Stage IIIB-IV Breast Cancer |
| NCT01044433 results posted | UPCC 15309 NCI-2009-01492 | Ph 2 | completed | Capecitabine and Lapatinib Ditosylate in Treating Patients With Squamous Cell Cancer of the Head and Neck |
| NCT01783756 | TRIO-US B09 NCI-2013-00082, 12-001358 | Ph 1, Ph 2 | completed | Phase 1b/2 Trial Using Lapatinib, Everolimus and Capecitabine for Treatment of HER-2 Positive Breast Cancer With CNS Metastasis |
| NCT00820872 results posted | NCCTG-N083E NCI-2009-00671, CDR0000631625 | Ph 2 | completed | Docetaxel, Carboplatin, Trastuzumab, and Lapatinib in Treating Patients With Early Stage Breast Cancer |
| NCT01434303 | NCI-2011-03222 NCI-2011-03222, NCI 8871 | Ph 1 | completed | Entinostat, Lapatinib Ditosylate and Trastuzumab in Treating Patients With Locally Recurrent or Distant Relapsed Metastatic Breast Cancer Previously Treated With Trastuzumab Only |
| NCT01688609 results posted | NCI-2012-01970 NCI-2012-01970, CDR0000734375 | Ph 2 | completed | Lapatinib Ditosylate, Trastuzumab, Paclitaxel, and Surgery in Treating Patients With Breast Cancer |
| NCT01868503 results posted | BRS0027 NCI-2013-01065, P30CA124435 | Ph 2 | terminated | Lapatinib Ditosylate and Radiation Therapy in Treating Patients With Locally Advanced or Locally Recurrent Breast Cancer |
| NCT00662636 | MC0616 NCI-2009-01197, MC0616 | Ph 1 | completed | Dasatinib and Lapatinib Ditolsylate in Treating Patients With Advanced Solid Tumors That Cannot Be Removed By Surgery |
| NCT01123473 | EORTC-40071 EU-21036, 2009-011580-36 | Ph 2 | terminated | 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 |
| NCT00769470 | CDR0000616008 P30CA016042, TRIO-TORI-B-07 | Ph 2 | completed | 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 |
| NCT01281163 | NCI-2011-02574 NCI-2011-02574, WSU# 2010-109 | Ph 1 | terminated | Lapatinib Ditosylate and Akt Inhibitor MK2206 in Treating Women With Metastatic Breast Cancer |
| NCT00962312 | 08-39 ICORG ICORG-08-39, EUDRACT-2008-006907-22 | Ph 2 | completed | Lapatinib Ditosylate and Capecitabine in Treating Patients With Metastatic Pancreatic Cancer |
| NCT01245205 | NCI-2011-02550 NCI-2011-02550, WCCC-CO-10904 | Ph 1 | completed | Akt Inhibitor MK2206 in Combination With Lapatinib Ditosylate in Patients With Advanced or Metastatic Solid Tumors or Breast Cancer |
| NCT01705340 | NCI-2012-01759 NCI-2012-01759, MSKCC IRB# 12-129 | Ph 1 | terminated | 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 |
| NCT01557764 | 201206025 | Ph 2 | withdrawn | Lapatinib With Trastuzumab in Treating Patients With HER2-Negative/HER2 Mutant Metastatic Breast Cancer |
| NCT00967031 | CDR0000642631 EU-20940, GEP 02-0801 | Ph 2 | completed | Lapatinib Ditosylate and Capecitabine in Treating Patients With Stage IV Breast Cancer and Brain Metastases |
| NCT00804310 UCDCC#207 | CDR0000626165 P30CA093373 | Ph 1 | terminated | Lapatinib and Ixabepilone in Treating Patients With Advanced Solid Tumors |
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
TYKERB FDA Label Details
Indications & Usage
FDA Label (PDF)TYKERB is indicated for the treatment of Breast Cancer.
WARNING: HEPATOTOXICITY Hepatotoxicity has been observed in clinical trials and postmarketing experience. The hepatotoxicity may be severe and deaths have been reported. Causality of the deaths is uncertain [see Warnings and Precautions (5.2)] . WARNING: HEPATOTOXICITY See full prescribing informati...
TYKERB Patents & Exclusivity
Patents (1 active)
Pro Intelligence Preview
Deep insights for TYKERB
Revenue Insights
- • Quarterly revenue tracking
- • Historical trend analysis
Patent Timeline
- • Cliff: 2029
- • 1 active patents
Trial Analysis
- • 24 total trials
- • Stage: Declining
Competitive Landscape
- • 20 similar drugs
- • Same target/indication analysis
Full approval history • All patents • Revenue trends • Competitor analysis
Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.
How We Calculate These Metrics
Trial Activity Stage
Measures the current development activity pattern based on trial phases, status, and trends. Important: This measures R&D activity, not commercial lifecycle.
Trial statuses: "Active" means recruiting or ongoing. "Completed" means reached planned endpoint. "Terminated" means stopped early—often due to safety, efficacy, or business reasons.
- Growth: High proportion of early-phase trials (Phase 1/2), active development
- Expansion: Significant Phase 3 activity, approaching or pursuing approvals
- Mature: Substantial Phase 4 post-marketing studies
- Stable: Mixed phase distribution, steady development
- Declining: Low active trial ratio, reduced R&D investment