Drug intelligence / Profile preview

ARRY-334543 + gemcitabine

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

ARRY-334543 + gemcitabine is a **combination therapy** consisting of ARRY-334543, an oral, reversible, small molecule tyrosine kinase inhibitor targeting ErbB-2 (HER2/neu) and EGFR, and gemcitabine, a nucleoside analog chemotherapeutic agent[1][2][3][5]. ARRY-334543 selectively inhibits ErbB-2 and EGFR signaling pathways, frequently dysregulated in advanced cancers, and has also been shown to antagonize ABCG2-mediated multidrug resistance[2][3]. Gemcitabine is incorporated into DNA and inhibits DNA synthesis, resulting in cytotoxicity in proliferating tumor cells. The combination was investigated in phase 1/2 clinical trials for advanced solid tumors, most notably metastatic pancreatic cancer, with the aim to improve therapeutic efficacy by combining targeted pathway inhibition with cytotoxic chemotherapy[1][5]. The developer of the therapy is Array BioPharma (now a subsidiary of Pfizer)[2][4].

Brand names
ARRY-334543 + gemcitabine
Other names
ARRY-334543 and gemcitabineARRY334543 and gemcitabineARRY 334543 and gemcitabine
02

Targets

DNA polymerase familyABCB1 (P-glycoprotein)ABCC10 (Multidrug resistance-associated protein 7)ERBB2 (Erb-b2 receptor tyrosine kinase 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)ABCG2 (Breast cancer resistance protein)

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