PHILADELPHIA — Preclinical findings recently published in Cancer Research, a journal of the American Association for Cancer Research, showed RG7204 (PLX4032) inhibited proliferation of tumor cell lines that expressed V600E-BRAF, a mutation found in several human cancers, including melanoma.
The compound also showed partial or complete tumor regression and improved survival in a dose-dependent manner in preclinical efficacy models in rodents, without associated toxicity.
BRAF mutations are found in about 8 percent of all solid tumors but in about 50 percent of melanomas.
“Patients with advanced melanoma currently do not have a lot of options. There are some therapies, but the response rates are very low. Based on this promising preclinical data, we believe this compound merits further study in patients with advanced melanoma,” said Dave Heimbrook, Ph.D., global head of discovery oncology at Roche and one of the study authors.
The Cancer Research paper is the first published report of RG7204, which shows tumor regressions in preclinical models. Roche and Plexxikon scientists and their academic collaborators have presented Phase I clinical data at medical meetings.
William Pao, M.D., Ph.D., associate professor of medicine, cancer biology and pathology at Vanderbilt University, said this preclinical research represents a significant step forward in establishing a basis for additional study in melanoma patients.
“This drug will have an impact,” said Pao. “The response rates with currently available therapies are only in the 10 percent to 20 percent range, so this represents a large step forward.”
Pao, a senior editor with Cancer Research, was not involved with the study and has no financial relationship with Roche.
Clinical studies are in progress with RG7204 (PLX4032). A Phase II trial has completed enrollment and a Phase III trial is currently enrolling patients. For this study, Roche is actively recruiting patients who have previously untreated metastatic melanoma with the V600E BRAF mutation. More information can be found at www.roche-trials.com.
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The mission of the American Association for Cancer Research is to prevent and cure cancer. Founded in 1907, the AACR is the world’s oldest and largest professional organization dedicated to advancing cancer research. The membership includes 31,000 basic, translational and clinical researchers; health care professionals; and cancer survivors and advocates in the United States and more than 90 other countries. The AACR marshals the full spectrum of expertise from the cancer community to accelerate progress in the prevention, diagnosis and treatment of cancer through high-quality scientific and educational programs. It funds innovative, meritorious research grants, research fellowship and career development awards. The AACR Annual Meeting attracts more than 17,000 participants who share the latest discoveries and developments in the field. Special conferences throughout the year present novel data across a wide variety of topics in cancer research, treatment and patient care. The AACR publishes six major peer-reviewed journals: Cancer Research; Clinical Cancer Research; Molecular Cancer Therapeutics; Molecular Cancer Research; Cancer Epidemiology, Biomarkers & Prevention; and Cancer Prevention Research. The AACR also publishes CR, a magazine for cancer survivors and their families, patient advocates, physicians and scientists. CR provides a forum for sharing essential, evidence-based information and perspectives on progress in cancer research, survivorship and advocacy.