Prescription medicine
Lapatinib ditosylate Brand names: Tykerb
Lapatinib ditosylate (Tykerb) is a prescription medicine with an FDA approval on record since 2007. FDA's NDC Directory lists it from 3 generic labelers.
- Generic listed
- Boxed warning
Check it at the source: the lapatinib ditosylate FDA label on DailyMed (effective November 30, 2023, Teva Pharmaceuticals, Inc.); the NDA 22059 record on Drugs@FDA; every lapatinib ditosylate label on DailyMed.
Highlights of the record
FDA label of November 30, 2023; NDC Directory, Drugs@FDA and Orange Book, October 8, 2026
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.
Used for
From the label: indications and usageLapatinib tablets are indicated in combination with: capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress human epidermal growth factor receptor 2 (HER2) and who have received prior therapy, including an anthracycline, a taxane, and trastuzumab.
Forms and strengths
- 250 mg
Film-coated tablet; tablet.
On the market
- Earliest approval on file
- March 13, 2007 Tykerb, Novartis; Drugs@FDA’s file, where older or withdrawn approvals can be missing
- Generic approvals
- 2 first September 29, 2020; 2 with a marketed status in Drugs@FDA
- Labelers listed (NDC)
- 4 of which 3 under generic applications, 1 under brand applications, repackagers included
- Last listed patent
- September 18, 2029 Tykerb tablets; not a generic launch date
Supply and safety
- Pharmacy cost (NADAC)
- Not in the survey
- Shortage (FDA)
- No current entry
- Recalls by its makers (FDA)
- No recall recorded
- FAERS reports
- 15,427 through July 30, 2026
What is lapatinib ditosylate used for?
From the label: indications and usageLapatinib tablets are indicated in combination with: capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress human epidermal growth factor receptor 2 (HER2) and who have received prior therapy, including an anthracycline, a taxane, and trastuzumab. Limitations of Use: Patients should have disease progression on trastuzumab prior to initiation of treatment with lapatinib tablets in combination with capecitabine. letrozole for the treatment of postmenopausal women with hormone receptor-positive metastatic breast cancer that overexpresses the HER2 receptor for whom hormonal therapy is indicated. […]
Conditions named in the indications of lapatinib ditosylate's FDA labels, with every medicine labeled for each:
FDA pharmacologic class: Kinase Inhibitor.
Source: FDA drug label (Lapatinib), Teva Pharmaceuticals, Inc., effective November 30, 2023 (SPL set b09abf73-1eef-4e12-b400-c030d546d223), via openFDA; the full label on DailyMed
Is there a generic for lapatinib ditosylate (Tykerb)?
The FDA approved the first generic lapatinib ditosylate on September 29, 2020. 2 generic applications are approved; 2 of them carry a current (not discontinued) marketing status in Drugs@FDA; that status is not evidence that the generic is on sale.
FDA's NDC Directory lists lapatinib ditosylate from 3 labelers under a generic (ANDA) application and from 1 brand labeler. A listing means the company has registered the product for sale; it does not show that every pharmacy stocks it.
The Orange Book lists 1 patent for Tykerb tablets: the compound patent runs to September 18, 2029. A patent or exclusivity date is not the date a generic goes on sale: court cases and settlements move it either way.
- 2007 earliest approval on file
- 2020 first generic approved
- 2029 last listed patent
Source: Drugs@FDA, FDA NDC Directory and the Orange Book (openFDA bulk files, October 8, 2026)
What does the lapatinib ditosylate label say about other medicines?
The lapatinib ditosylate label names 8 other medicines in its interaction, contraindication or warning sections. The sentences are the labels' own; a label lists what its studies and reports found, not every interaction.
| Medicine named | Section | What the label says |
|---|---|---|
| Capecitabine | warnings and precautions | … exposures that were ≥ 3.3 times the human clinical exposure based on AUC following 1,250 mg dose of lapatinib plus capecitabine. |
| Carbamazepine | drug interactions | Inhibit or Induce Cytochrome P450 3A4 Enzymes Lapatinib undergoes extensive metabolism by CYP3A4, and concomitant administration of strong inhibitors or inducers of CYP3A4 alter lapatinib concentrations significantly (see Ketoconazole and Carbamazepine sections, below). |
| Digoxin | drug interactions | Following coadministration of lapatinib and digoxin (P-gp substrate), systemic AUC of an oral digoxin dose increased approximately 2.8-fold. |
| Esomeprazole | drug interactions | However, esomeprazole, a proton pump inhibitor, administered at a dose of 40 mg once daily for 7 days, did not result in a clinically meaningful reduction in lapatinib steady-state exposure. |
| Ketoconazole | drug interactions | Inhibit or Induce Cytochrome P450 3A4 Enzymes Lapatinib undergoes extensive metabolism by CYP3A4, and concomitant administration of strong inhibitors or inducers of CYP3A4 alter lapatinib concentrations significantly (see Ketoconazole and Carbamazepine sections, below). |
| Loperamide | warnings and precautions | Prompt treatment of diarrhea with antidiarrheal agents (such as loperamide) after the first unformed stool is recommended. |
| Midazolam | drug interactions | Following coadministration of lapatinib and midazolam (CYP3A4 substrate), 24-hour systemic exposure (AUC) of orally administered midazolam increased 45%, while 24-hour AUC of intravenously administered midazolam increased 22%. |
| Paclitaxel | drug interactions | In cancer patients receiving lapatinib and paclitaxel (CYP2C8 and P-gp substrate), 24-hour systemic exposure (AUC) of paclitaxel was increased 23%. |
Source: FDA drug label (Lapatinib), Teva Pharmaceuticals, Inc., effective November 30, 2023 (SPL set b09abf73-1eef-4e12-b400-c030d546d223), via openFDA; the full label on DailyMed
What do FAERS reports show for lapatinib ditosylate?
The FDA Adverse Event Reporting System holds 15,427 reports that list lapatinib ditosylate among the medicines taken, through July 30, 2026, each a report of something that happened, not proof the medicine caused it; 2,475 are coded as a death and 4,010 as a hospital stay. Counts follow how widely a medicine is used and watched, and they are not a measure of how risky it is.
Reports received each year
The most reported reactions
Source: FDA Adverse Event Reporting System (FAERS) via openFDA, reports through July 30, 2026
What else is labeled for the same conditions as lapatinib ditosylate?
17 other medicines are given the same way (oral) and in the same FDA class as lapatinib ditosylate or labeled mainly for the same use (breast cancer), the same class first. Breast cancer lists all 44 medicines labeled for it, by any route. The first 8 are below. They are listed as records, not as substitutes: whether one can replace another is a prescriber's decision.
| Medicine | Shared indication | Generic labelers (oral) | Pharmacy cost | Shortage |
|---|---|---|---|---|
| Everolimus | Breast cancer | 14 labelers | $26.32 per tablet 10 mg tablet | A presentation being discontinued |
| Palbociclib | Breast cancer | none listed | n/a | A presentation being discontinued |
| Abemaciclib | Breast cancer | none listed | n/a | No current entry |
| Ribociclib | Breast cancer | none listed | $289.72 per unit 600 mg daily dose | No current entry |
| Tucatinib | Breast cancer | none listed | n/a | No current entry |
| Neratinib | Breast cancer | none listed | n/a | No current entry |
| Anastrozole | Breast cancer | 24 labelers | $0.142 per tablet 1 mg tablet | No current entry |
| Letrozole | Breast cancer | 19 labelers | $0.145 per tablet 2.5 mg tablet | No current entry |
Every medicine labeled for the same conditions as lapatinib ditosylate
Source: FDA drug labels (indications), NDC Directory, NADAC of October 7, 2026, FDA shortages (October 8, 2026)
What next?
- Alternatives to lapatinib ditosylate
- 17 medicines for the same use
- Other kinase inhibitors
- the pharmacologic class, with prices and generics
- Lapatinib ditosylate side effects
- the label's list beside FAERS reports
- Check an interaction
- what two or more labels say about each other