CPX-847 for the Treatment of Breast Cancer

Online Inquiry

erb-b2 Receptor Tyrosine Kinase 2 (ERBB2; HER2)

This gene encodes a member of the epidermal growth factor (EGF) receptor family of receptor tyrosine kinases. This protein has no ligand binding domain of its own and therefore cannot bind growth factors. However, it does bind tightly to other ligand-bound EGF receptor family members to form a heterodimer, stabilizing ligand binding and enhancing kinase-mediated activation of downstream signalling pathways, such as those involving mitogen-activated protein kinase and phosphatidylinositol-3 kinase. Overexpression of this gene has been reported in numerous cancers, including breast and ovarian tumors. Alternative splicing results in several additional transcript variants, some encoding different isoforms and others that have not been fully characterized.

Fc Fragment of IgG Receptor IIIa (CD16)

This gene encodes a receptor for the Fc portion of immunoglobulin G, and it is involved in the removal of antigen-antibody complexes from the circulation, as well as other other antibody-dependent responses. This gene (FCGR3A) is highly similar to another nearby gene (FCGR3B) located on chromosome 1. The receptor encoded by this gene is expressed on natural killer (NK) cells as an integral membrane glycoprotein anchored through a transmembrane peptide, whereas FCGR3B is expressed on polymorphonuclear neutrophils (PMN) where the receptor is anchored through a phosphatidylinositol (PI) linkage.

Breast Cancer

Breast cancer is a type of cancer that specifically affects cells in the breast tissue. About 80% of breast cancers originate in the mammary ducts, while the remaining 20% originate in the lobules.

According to the World Health Organization, breast cancer is the most commonly diagnosed cancer in females worldwide, and the third most common cancer overall. In 2017, more than 1.96 million new cases of breast cancer were diagnosed worldwide. Based on incidence data from the Globocan 2008 database extrapolated to the projected world population in 2030, the World Economic Forum estimates that nearly 2.2 million new cases of breast cancer will be diagnosed worldwide in 2030.

According to the Global Burden of Disease (GBD) 2017 study, breast cancer claimed the lives of 601,000 women as well as 11,000 men worldwide in 2017, and incurred 17.7 million disability-adjusted life years (DALYs) in both sexes worldwide. Moreover, the breast cancer death toll continues to increase. However, in developed countries, breast cancer mortality rates have declined significantly in recent decades, largely due to the introduction of a multidisciplinary approach to management that involves diagnostic imaging, surgical resection, pathological analysis of resected lymph nodes and/or breast tissue and a treatment strategy based on the identification of the individual molecular subtype that may include surgery, radiation therapy, and/or systemic hormonal, biologic or chemotherapy.

Although the rate of successful treatments for localized disease is currently quite high, with five-year survival rates more than 98% in countries such as the U.S., the natural course of the disease is still fatal. In spite of a high treatment success rate, breast cancer remains the number one cause of cancer death in women, and the fifth most common cause of cancer death in both sexes combined.

Signal Transduction Modulators

The Status of CPX-847

The international patent applications under the PCT have been granted.

	Discovery/Optimization	Preclinical	Clinical
CPX-847