Plexxikon Inc. and Roche announced that they have entered into an agreement to develop and commercialise PLX4032, Plexxikon's investigational targeted cancer therapy that selectively inhibits B-RafV600E, a mutated form of the BRAF kinase gene.
The BRAFV600E gene has been associated with increased tumour aggressiveness and decreased survival in many types of cancers and is a common cancer-causing kinase gene. The BRAFV600E gene is found in approximately 70 per cent of malignant melanomas and a large number of colorectal and thyroid tumours. PLX4032 may offer a new treatment modality for the estimated 100,000 cancer patients in the US who carry the BRAFV600E gene. Plexxikon recently filed an Investigational New Drug (IND) application for PLX4032 and plans to initiate a phase 1 clinical trial by the end of this year.
Separately, Roche Molecular Diagnostics, a business unit of Roche Diagnostics, and Plexxikon announced they would collaborate on development of an in vitro assay to screen for the presence of the BRAFV600E mutation in biological samples taken from patient tumours. An assay that correlates the presence of this mutation with clinical outcome may aid clinical development of PLX4032.
"As one of the leading pharmaceutical companies in oncology, together with their commitment to personalized medicine, Roche makes an ideal partner for the development of this unique compound," said K Peter Hirth, PhD, CEO of Plexxikon Inc. "We believe PLX4032 could be a first-in-class oral cancer therapeutic which selectively targets an oncogenic protein found only in diseased tissue. Along with our phase 2 diabetes product and preclinical stage portfolio in multiple therapeutic areas, PLX4032's entry into development further validates Plexxikon's discovery platform for novel drug candidates."
"There is a growing body of evidence demonstrating that agents such as PLX4032, which selectively inhibit activated kinases, are increasingly useful in treating cancer and improving patient outcomes," said Peter Hug, Roche's Global Head of Pharma Partnering. "We are very excited to partner with Plexxikon for the development of PLX4032 and other B-RafV600E targeted compounds. This could be a further example of the potential of personalized medicine. With our combined expertise in diagnostic and therapeutic development as well as commercialisation, we are confident in our capability to develop this potential drug to make a difference to patients' lives."
PLX4032 is a selective inhibitor of the B-RafV600E kinase found in approximately 70 per cent of malignant melanomas, a large percentage of colorectal and thyroid cancers and many other tumour types. In preclinical studies in both melanoma and colorectal cancer models, PLX4032 reduces tumour size and slows the progression of the tumours even after the completion of treatment, without evidence of side effects. Highly selective against B-RafV600E compared to a panel of over 70 other kinases, PLX4032 is designed to work specifically on cancer cells, leaving healthy cells untouched in contrast to chemotherapeutic agents.