Overview

Generic Name(s):
lapatinib
Trade Name(s):
Tykerb
NCI Definition [1]:
A synthetic, orally-active quinazoline with potential antineoplastic properties. Lapatinib reversibly blocks phosphorylation of the epidermal growth factor receptor (EGFR), ErbB2, and the Erk-1 and-2 and AKT kinases; it also inhibits cyclin D protein levels in human tumor cell lines and xenografts. EGFR and ErbB2 have been implicated in the growth of various tumor types.

Biomarker-Directed Therapies

Lapatinib has been investigated in 28 clinical trials, of which 16 are open and 12 are closed. Of the trials investigating lapatinib, 2 are early phase 1 (1 open), 6 are phase 1 (2 open), 2 are phase 1/phase 2 (1 open), 10 are phase 2 (5 open), 6 are phase 3 (5 open), and 2 are no phase specified (2 open).

ERBB2 Amplification, HER2 Overexpression, and HER2 Positive are the most frequent biomarker inclusion criteria for lapatinib clinical trials.

Breast carcinoma, glioblastoma, and non-small cell lung carcinoma are the most common diseases being investigated in lapatinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Lapatinib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Lapatinib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating lapatinib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
gsk572016, gw2016, gw-572016, Tykerb, lapatinib, n-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, gw 572016, lapatinib tosilate hydrate, lapatinib, lapatinib (substance), lapatinib [chemical/ingredient], n-(3-chloro-4-(((3-fluorobenzyl)oxy)phenyl)-6-(5-(((2-methylsulfonyl)ethyl)amino)methyl) -2-furyl)-4-quinazolinamine, gw 2016, fmm, gw572016, n-(3-chloro-4-((3-fluorophenyl)methoxy)phenyl)-6-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)-2-furanyl)-4-quinazolinamine, lapatinib (product)
Drug Categories [2]:
AKT inhibitors, ERK inhibitor, Serine/threonine kinase inhibitors, Tyrosine kinase inhibitors
Drug Target(s) [2]:
AKT1, AKT2, AKT3, EGFR, ERBB2, MAPK1, MAPK3
NCIT ID [1]:
C26653
SNOMED ID [1]:
C-1019A

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.