Drug intelligence / Profile preview

lapatinib + veliparib

Development stage
Unknown
Lead developer
AbbVie
Modality
Small Molecules
Administration
Oral
01

Overview

Lapatinib + veliparib is an investigational combination therapy consisting of two small molecule drugs. Lapatinib is a dual tyrosine kinase inhibitor targeting both the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2/ERBB2), while veliparib is a poly(ADP-ribose) polymerase (PARP) inhibitor. This combination has been studied primarily in patients with metastatic triple-negative breast cancer (TNBC), particularly those without germline BRCA1/2 mutations. The rationale for this combination stems from preclinical evidence that simultaneous inhibition of EGFR/HER2 and PARP induces synthetic lethality in TNBC cells with intact DNA repair mechanisms. Clinical studies have shown that the regimen has a manageable safety profile and promising antitumor activity, with most adverse events being mild to moderate[1][2]. The primary mechanism involves disruption of DNA repair pathways via PARP inhibition alongside blockade of proliferative signaling through EGFR/HER2 inhibition.

Brand names
TykerbTyverb
02

Targets

PARP2 (Poly (adp-ribose) polymerase 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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