Drug intelligence / Profile preview

lapatinib + taxane chemotherapy

Development stage
Unknown
Lead developer
GSK
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral (lapatinib), Intravenous (taxane: Paclitaxel Or Docetaxel)
01

Overview

**Lapatinib + taxane chemotherapy** is a combination regimen used primarily for the treatment of HER2-positive metastatic breast cancer. Lapatinib is a dual tyrosine kinase inhibitor targeting the intracellular domains of both HER2 (human epidermal growth factor receptor 2) and EGFR (epidermal growth factor receptor), inhibiting downstream signaling that promotes tumor cell proliferation and survival[3][6]. Taxanes—such as paclitaxel or docetaxel—are cytotoxic chemotherapies that disrupt microtubule function and induce cell cycle arrest and apoptosis in rapidly dividing cells[2][4]. In clinical studies, this combination has been shown to improve pathological complete response (pCR) rates relative to chemotherapy alone, particularly in HER2-positive breast cancer, but with increased incidence of adverse events such as diarrhea, dermatological toxicity, hepatic toxicity, and neutropenia[2][4][5]. Compared with trastuzumab plus taxane, lapatinib plus taxane is associated with inferior progression-free survival and higher toxicity[2][4]. Lapatinib is approved for use with capecitabine in advanced HER2+ breast cancer after prior treatment with anthracycline, taxane, and trastuzumab[6].

Brand names
Tykerb
Other names
lapatinib plus taxanelapatinib-taxane combinationlapatinib + paclitaxellapatinib + docetaxel
02

Targets

ABCG2 (Breast cancer resistance protein)EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)Microtubule

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