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Lapatinib side effects: what 15,427 FDA adverse event reports show

Lapatinib · 1,024 reaction terms · 51,086 drug–reaction co-reports · data 2026-09-14
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Drug class

Kinase inhibitor

FDA label, Indications wording

Who reports

15,427 reports · 68% serious · 2,475 with death outcome · 95% female

openFDA FAERS counts, all years, deduplication not applied

Used for

Lapatinib tablets are kinase inhibitor indicated in combination with: ( 1 ) 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.

FDA label, Indications and Usage

What it is

Lapatinib is a small molecule and a member of the 4-anilinoquinazoline class of kinase inhibitors. It is present as the ditosylate salt, with chemical name N -(3 chloro-4-[(3-fluorophenyl)methyl]oxy}phenyl)-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furanyl]-4-quinazolinamine bis(4-methylbenzenesulfonate).

FDA label, Description section

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.

FDA label
How to read this page. FAERS is a spontaneous-reporting system: counts are not incidence rates and a signal is not proof of causation. Each reaction below is run through an automated screen — is the term in the FDA label (known), in the indications (the disease being treated), an administrative/coding term, or none of these (unlabeled)? That screen is mechanical text matching, not a causality assessment. The 30 hand-written Bradford Hill assessments are on the causality assessment page. Not medical advice.

Causality screen of the 40 strongest signals

Labeled adverse reaction 4Labeled (related wording) 4Likely indication confounding 3Lab value / disease marker 1Not in label — unassessed 28
What the badges mean

Strongest disproportionality signals

Flagged terms (PRR ≥ 2, χ² ≥ 4, n ≥ 10), ranked by PRR; infinite PRRs (no comparator reports) excluded. The EBGM column is a second, shrinkage-based estimate (MGPS) with its 5th percentile EB05 and the BCPNN IC025; a pair flagged by PRR alone is marked PRR-only and should be read as fragile. The strata column recomputes the PRR on serious reports only and flags pairs whose reports are unusually skewed by sex or come mostly from consumers rather than clinicians. 984 further terms are in the interactive explorer. Reaction links open the term's cross-drug page.

Show:
ReactionReportsPRR 95% CI · ROR · χ²/pEBGM EB05 · IC025Label screenSerious-only & strataTrial cross-check
Skin chapped99435.1
347.0–545.5ROR 437.9 · χ² 32,045 / p <1e-300
309.1 EB05 261.3 · IC025 +6.6
3/3 methods agree
Not in label — unassessedserious n=44 · 83% consumernot reported in cached trials
Transaminases10273.6
138.6–540.0ROR 273.7 · χ² 2,035 / p <1e-300
159.0 EB05 92.3 · IC025 +3.2
3/3 methods agree
Labeled adverse reaction
exact term
serious n=10NCT00374322: 1/1,573 (0.1%) on Lapatinib (serious AE)
Her-2 positive breast cancer13136.1
77.0–240.8ROR 136.3 · χ² 1,463 / p <1e-300
105.0 EB05 65.3 · IC025 +3.5
3/3 methods agree
Not in label — unassessedserious n=12not reported in cached trials
Nasal mucosal disorder3894.5
68.0–131.3ROR 94.7 · χ² 3,197 / p <1e-300
84.7 EB05 64.4 · IC025 +4.8
3/3 methods agree
Not in label — unassessedserious n=37not reported in cached trials
Metastases to skin5983.1
63.9–108.0ROR 83.4 · χ² 4,428 / p <1e-300
76.4 EB05 61.4 · IC025 +5.1
3/3 methods agree
Not in label — unassessedserious n=59not reported in cached trials
Streptococcal sepsis5768.2
52.3–88.9ROR 68.4 · χ² 3,526 / p <1e-300
63.6 EB05 50.9 · IC025 +4.9
3/3 methods agree
Not in label — unassessedserious n=57NCT00490139: 1/2,056 (0.0%) on Lapatinib (serious AE)
Her2 positive breast cancer1661.6
37.3–101.7ROR 61.7 · χ² 855 / p 2e-188
55.3 EB05 36.1 · IC025 +3.6
3/3 methods agree
Likely indication confounding
term in indications; also in warnings
serious n=16not reported in cached trials
Hormone receptor positive breast cancer1159.2
32.4–108.3ROR 59.3 · χ² 548 / p 1e-121
52.0 EB05 31.0 · IC025 +3.0
3/3 methods agree
Likely indication confounding
term in indications; also in warnings
serious n=11not reported in cached trials
Paronychia17456.9
49.0–66.2ROR 57.6 · χ² 9,120 / p <1e-300
54.3 EB05 47.9 · IC025 +5.3
3/3 methods agree
Labeled adverse reaction
exact term
serious n=157NCT00490139: 1/2,076 (0.0%) on Lapatinib (serious AE)
Palmar-plantar erythrodysaesthesia syndrome92856.1
52.7–59.8ROR 59.7 · χ² 48,247 / p <1e-300
53.9 EB05 51.0 · IC025 +5.6
3/3 methods agree
Not in label — unassessedserious PRR 54.9NCT00490139: 1/2,061 (0.0%) on Lapatinib (serious AE)
Metastases to central nervous system48353.2
48.7–58.2ROR 54.9 · χ² 23,781 / p <1e-300
51.2 EB05 47.4 · IC025 +5.5
3/3 methods agree
Not in label — unassessedserious PRR 43.0NCT00490139: 1/2,056 (0.0%) on Lapatinib (serious AE)
Metastases to the mediastinum1550.9
30.4–85.2ROR 51.0 · χ² 660 / p 9e-146
46.4 EB05 29.8 · IC025 +3.4
3/3 methods agree
Not in label — unassessedserious n=15not reported in cached trials
Onychalgia3447.8
33.9–67.2ROR 47.9 · χ² 1,459 / p <1e-300
45.1 EB05 33.7 · IC025 +4.2
3/3 methods agree
Not in label — unassessedserious n=15 · 79% consumernot reported in cached trials
Breast cancer metastatic35947.0
42.4–52.2ROR 48.1 · χ² 15,594 / p <1e-300
45.4 EB05 41.6 · IC025 +5.2
3/3 methods agree
Likely indication confounding
term in indications; also in warnings
serious PRR 39.3not reported in cached trials
Lymphangiosis carcinomatosa3445.8
32.6–64.4ROR 45.9 · χ² 1,398 / p <1e-300
43.3 EB05 32.4 · IC025 +4.2
3/3 methods agree
Not in label — unassessedserious n=33 · 94% cliniciannot reported in cached trials
Pseudomonal sepsis5644.6
34.2–58.2ROR 44.8 · χ² 2,268 / p <1e-300
42.6 EB05 34.0 · IC025 +4.5
3/3 methods agree
Not in label — unassessedserious n=56not reported in cached trials
Nail bed bleeding1639.5
24.0–64.9ROR 39.5 · χ² 546 / p 4e-121
36.9 EB05 24.1 · IC025 +3.3
3/3 methods agree
Not in label — unassessedserious n=9not reported in cached trials
Superior vena cava syndrome1636.9
22.4–60.5ROR 36.9 · χ² 509 / p 6e-113
34.6 EB05 22.5 · IC025 +3.3
3/3 methods agree
Not in label — unassessedserious n=16not reported in cached trials
Breast neoplasm2635.2
23.8–51.9ROR 35.2 · χ² 808 / p 5e-178
33.5 EB05 24.0 · IC025 +3.7
3/3 methods agree
Not in label — unassessedserious n=26NCT00490139: 1/2,076 (0.0%) on Lapatinib (serious AE)
Radiation necrosis1434.2
20.2–58.2ROR 34.3 · χ² 409 / p 3e-91
32.1 EB05 20.3 · IC025 +3.1
3/3 methods agree
Not in label — unassessedserious n=14not reported in cached trials
Metastases to lymph nodes15131.3
26.7–36.8ROR 31.6 · χ² 4,300 / p <1e-300
30.5 EB05 26.6 · IC025 +4.5
3/3 methods agree
Not in label — unassessedserious n=152not reported in cached trials
Stent occlusion1128.3
15.6–51.4ROR 28.3 · χ² 258 / p 3e-58
26.5 EB05 15.6 · IC025 +2.7
3/3 methods agree
Not in label — unassessedserious n=11not reported in cached trials
Onycholysis3127.7
19.4–39.5ROR 27.7 · χ² 755 / p 2e-166
26.7 EB05 19.7 · IC025 +3.7
3/3 methods agree
Not in label — unassessedserious n=20not reported in cached trials
Joint ankylosis1126.6
14.6–48.2ROR 26.6 · χ² 241 / p 1e-54
24.9 EB05 14.6 · IC025 +2.6
3/3 methods agree
Not in label — unassessedserious n=11not reported in cached trials
Metastases to lung20224.2
21.1–27.8ROR 24.5 · χ² 4,392 / p <1e-300
23.7 EB05 21.1 · IC025 +4.3
3/3 methods agree
Not in label — unassessedserious PRR 20.0not reported in cached trials
Subclavian vein thrombosis1923.0
14.6–36.1ROR 23.0 · χ² 371 / p 5e-83
22.1 EB05 14.9 · IC025 +3.1
3/3 methods agree
Not in label — unassessedserious n=19NCT00490139: 1/2,076 (0.0%) on Lapatinib (serious AE)
Vascular device infection7422.6
18.0–28.5ROR 22.7 · χ² 1,484 / p <1e-300
22.2 EB05 18.2 · IC025 +3.9
3/3 methods agree
Not in label — unassessedserious n=74not reported in cached trials
Dermatitis acneiform9421.4
17.5–26.3ROR 21.6 · χ² 1,783 / p <1e-300
21.0 EB05 17.7 · IC025 +3.9
3/3 methods agree
Labeled adverse reaction
exact term
serious n=52NCT00490139: 2/2,056 (0.1%) on Lapatinib (serious AE)
Metastases to spine5221.4
16.3–28.1ROR 21.5 · χ² 976 / p 2e-214
20.9 EB05 16.6 · IC025 +3.7
3/3 methods agree
Not in label — unassessedserious n=51not reported in cached trials
Brain cancer metastatic1019.9
10.7–37.1ROR 19.9 · χ² 159 / p 1e-36
18.4 EB05 9.7 · IC025 +2.3
3/3 methods agree
Not in label — unassessedserious n=10not reported in cached trials
Metastases to liver24719.4
17.1–22.0ROR 19.7 · χ² 4,237 / p <1e-300
19.1 EB05 17.2 · IC025 +4.0
3/3 methods agree
Not in label — unassessedserious PRR 16.2not reported in cached trials
Biliary dilatation2018.7
12.0–29.0ROR 18.7 · χ² 312 / p 3e-70
18.0 EB05 12.1 · IC025 +2.9
3/3 methods agree
Not in label — unassessedserious n=20not reported in cached trials
Nail disorder11618.4
15.3–22.1ROR 18.5 · χ² 1,864 / p <1e-300
18.1 EB05 15.5 · IC025 +3.8
3/3 methods agree
Labeled adverse reaction
exact term
serious n=67NCT00490139: 1/2,061 (0.0%) on Lapatinib (serious AE)
Invasive ductal breast carcinoma3618.2
13.1–25.3ROR 18.2 · χ² 561 / p 3e-124
17.8 EB05 13.4 · IC025 +3.3
3/3 methods agree
Not in label — unassessedserious n=36not reported in cached trials
Ejection fraction abnormal1617.9
10.9–29.3ROR 17.9 · χ² 236 / p 2e-53
17.1 EB05 10.7 · IC025 +2.7
3/3 methods agree
Lab value / disease markerserious n=14NCT00490139: 1/2,076 (0.0%) on Lapatinib (serious AE)
Breast cancer recurrent4017.5
12.8–23.8ROR 17.5 · χ² 597 / p 4e-132
17.1 EB05 13.0 · IC025 +3.3
3/3 methods agree
Not in label — unassessedserious n=39not reported in cached trials

Trial evidence (ClinicalTrials.gov)

✓ Trial adverse-event data found on ClinicalTrials.gov

Largest completed trials with posted results that list Lapatinib as a study intervention. The right-hand column of the signal table shows whether each FAERS term was also recorded in these trials, with a real denominator (12 of 40 signal terms matched).

Caveats: trial populations, doses and follow-up differ from the reporting population; AE terms are sponsor-coded and matched here by wording; absence from a trial list means the term was not reported above the sponsor's frequency threshold, not that it cannot occur.

Most frequently reported reactions

By raw co-report count, regardless of disproportionality. Common terms here are often the illness itself or generic outcomes.

ReactionReportsPRR 95% CI · ROR · χ²/pEBGM EB05 · IC025Label screenSerious-only & strataTrial cross-check
Diarrhoea (diarrhea)4,1738.9
8.6–9.1ROR 11.8 · χ² 29,862 / p <1e-300
8.8 EB05 8.6 · IC025 +3.1
3/3 methods agree
Labeled — boxed warning
exact term
serious PRR 6.8NCT00490139: 44/2,056 (2.1%) on Lapatinib (serious AE)
Nausea1,6152.8
2.7–2.9ROR 3.0 · χ² 1,916 / p <1e-300
2.8 EB05 2.7 · IC025 +1.4
3/3 methods agree
Labeled adverse reaction
exact term
serious PRR 2.4NCT00490139: 7/2,056 (0.3%) on Lapatinib (serious AE)
Death1,4622.3
2.2–2.4ROR 2.4 · χ² 1,129 / p 7e-248
2.3 EB05 2.2 · IC025 +1.1
3/3 methods agree
Outcome field, not a reaction
boxed warning mentions mortality
serious PRR 1.9NCT00490139: 1/2,056 (0.0%) on Lapatinib (serious AE)
Fatigue (tiredness)1,3062.3
2.2–2.4ROR 2.4 · χ² 980 / p 2e-215
2.3 EB05 2.2 · IC025 +1.1
3/3 methods agree
Labeled adverse reaction
exact term
serious PRR 1.9NCT00490139: 1/2,056 (0.0%) on Lapatinib (serious AE)
Vomiting1,2093.5
3.3–3.7ROR 3.7 · χ² 2,214 / p <1e-300
3.5 EB05 3.3 · IC025 +1.7
3/3 methods agree
Labeled adverse reaction
exact term
serious PRR 3.0NCT00490139: 9/2,056 (0.4%) on Lapatinib (serious AE)
Rash1,0623.3
3.1–3.5ROR 3.5 · χ² 1,766 / p <1e-300
3.3 EB05 3.2 · IC025 +1.6
3/3 methods agree
Labeled adverse reaction
exact term
serious PRR 3.0NCT00490139: 1/2,061 (0.0%) on Lapatinib (serious AE)
Disease progression1,00511.7
11.0–12.4ROR 12.4 · χ² 9,771 / p <1e-300
11.6 EB05 11.0 · IC025 +3.4
3/3 methods agree
Reporting / coding artifactserious PRR 9.6not reported in cached trials
Palmar-plantar erythrodysaesthesia syndrome92856.1
52.7–59.8ROR 59.7 · χ² 48,247 / p <1e-300
53.9 EB05 51.0 · IC025 +5.6
3/3 methods agree
Not in label — unassessedserious PRR 54.9NCT00490139: 1/2,061 (0.0%) on Lapatinib (serious AE)
Asthenia (weakness)6072.2
2.0–2.4ROR 2.2 · χ² 401 / p 2e-89
2.2 EB05 2.0 · IC025 +1.0
3/3 methods agree
Labeled adverse reaction
exact term
serious PRR 2.1NCT00490139: 4/2,056 (0.2%) on Lapatinib (serious AE)
Malignant neoplasm progression5657.6
7.0–8.2ROR 7.8 · χ² 3,217 / p <1e-300
7.5 EB05 7.0 · IC025 +2.8
3/3 methods agree
Reporting / coding artifactserious PRR 6.4not reported in cached trials
Drug ineffective (drug did not work)5610.6
0.5–0.6ROR 0.6 · χ² 183 / p 6e-42
0.6 EB05 0.5 · IC025 -0.9
PRR-only: not supported by EBGM or IC
Reporting / coding artifactserious PRR 0.7not reported in cached trials
Dyspnoea (shortness of breath)5601.3
1.2–1.5ROR 1.4 · χ² 51 / p 5e-13
1.3 EB05 1.3 · IC025 +0.3Labeled adverse reaction
exact term
serious PRR 1.3NCT00490139: 2/2,056 (0.1%) on Lapatinib (serious AE)
Dehydration5245.4
4.9–5.8ROR 5.5 · χ² 1,857 / p <1e-300
5.3 EB05 4.9 · IC025 +2.3
3/3 methods agree
Not in label — unassessedserious PRR 4.5NCT00490139: 12/2,056 (0.6%) on Lapatinib (serious AE)
Decreased appetite (loss of appetite)5193.1
2.8–3.3ROR 3.1 · χ² 720 / p 7e-159
3.0 EB05 2.8 · IC025 +1.5
3/3 methods agree
Labeled adverse reaction
exact term
serious PRR 2.5NCT00490139: 3/2,056 (0.1%) on Lapatinib (serious AE)

Unlabeled candidate signals

These flagged terms were not found in the FDA label text and do not match an artifact pattern. They are the pairs that would merit a structured assessment (temporality, dose-response, biological plausibility, consistency across databases, trial or cohort evidence). The screen has not done that; string-matching misses label wording, and a strong PRR can still be stimulated reporting, co-medication, or the disease itself.

Want to assess one of these properly? The runbook describes the Bradford Hill / trial-evidence workflow used on the assessment page, and handoff_top1000_signals.csv lists the strongest unassessed pairs across all drugs.

Common questions

What are the most reported side effects of Lapatinib?

In FDA FAERS, the most frequently co-reported reaction terms for Lapatinib are diarrhoea, nausea, fatigue, vomiting, rash, palmar-plantar erythrodysaesthesia syndrome. These are report counts, not rates: FAERS has no denominator, reporting is voluntary and uneven, and a term can be reported because of the illness being treated rather than the drug.

Does Lapatinib have an FDA boxed warning?

Yes. The current FDA label carries a 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.

Do FAERS signals prove that Lapatinib causes these side effects?

No. A disproportionality signal (PRR, ROR) means a reaction is reported more often with this drug than with others in the database. That can reflect a real effect, but also the disease being treated, stimulated reporting after news or litigation, co-medications, or how reports are coded. Causality needs temporality, dose-response, biological plausibility, consistency across data sources and, ideally, trial or cohort evidence. This page screens each term against the FDA label and ClinicalTrials.gov results; it does not establish causation.

Sources & methods

Page generated 2026-10-08. Label and PubChem text are retrieved automatically and may lag the current label; always check the current prescribing information. OpenPV is a beta research tool of the Open Source Medicine Foundation.