Drug intelligence / Profile preview

lapatinib + nab-paclitaxel + trastuzumab emtansine

Development stage
Unknown
Lead developer
Genentech
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Oral, Intravenous
01

Overview

This is a combination regimen of three agents used primarily in the treatment of HER2-positive breast cancer: - **Lapatinib** is an oral small molecule tyrosine kinase inhibitor targeting both human epidermal growth factor receptor 2 (HER2/ERBB2) and epidermal growth factor receptor (EGFR/ERBB1), inhibiting downstream signaling pathways involved in cell proliferation. - **Nab-paclitaxel** (nanoparticle albumin-bound paclitaxel; brand name Abraxane) is a microtubule inhibitor formulated as albumin-bound nanoparticles to improve solubility and delivery. It disrupts microtubule function during cell division. - **Trastuzumab emtansine** (T-DM1; brand name Kadcyla) is an antibody-drug conjugate consisting of the anti-HER2 monoclonal antibody trastuzumab linked to the cytotoxic agent DM1. It delivers targeted chemotherapy directly to HER2-overexpressing tumor cells. The combination has been studied in phase I and II clinical trials for patients with metastatic or early-stage HER2-positive breast cancer. The regimen aims for dual or triple blockade of HER2 signaling while delivering cytotoxic therapy[1][2][3][5]. Clinical studies have shown significant anti-tumor activity with manageable toxicity profiles.

Brand names
KadcylaAbraxane
Other names
lapatinib + Abraxane + T-DM1lapatinib + nab-paclitaxel + T-DM1lapatinib + Abraxane + trastuzumab emtansine
02

Targets

EGFR (Epidermal growth factor receptor)TUBB (Tubulin (alpha and beta subunits))

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