Plexxikon Announces Data Presentations of Oncology Pipeline, Including Phase 3 Vemurafenib Data, at ASCO 2011 Annual Meeting
Phase 3 Vemurafenib Data to be Presented in Plenary Session and to be Included in ASCO's Official Press Program
Berkeley, CA - May 18, 2011 – Plexxikon Inc., a member of the Daiichi Sankyo Group, today announced that data related to vemurafenib and PLX3397, two promising oncology drugs in its pipeline, will be presented in ten separate presentations at the American Society of Clinical Oncology (ASCO) 2011 Annual Meeting taking place June 3 through June 7, 2011 in Chicago, Illinois.
Importantly, final data from the Phase 3 study (BRIM3) of vemurafenib in metastatic melanoma will be presented in the General Oncology Plenary Session on Sunday, June 5th:
Abstract #LBA4: “Phase III randomized, open-label, multicenter trial (BRIM3) comparing BRAF inhibitor vemurafenib with dacarbazine (DTIC) in patients with V600E BRAF mutated melanoma.”
Oral presentation to be made in the General Oncology Plenary Session on June 5, 2011 at 3:15 p.m. CDT by Paul B. Chapman, M.D., Memorial Sloan-Kettering Cancer Center (Hall B1).
Other Vemurafenib (PLX4032) Presentations
Abstract #8509: “BRIM-2: An open-label, multicenter phase II study of vemurafenib in previously treated patients with BRAFV600E mutation-positive metastatic melanoma."
Oral presentation to be made on June 4, 2011 at 4:00 p.m. CDT by Antoni Ribas, M.D., Associate Professor, Department of Medicine, Hematology/Oncology, UCLA Jonsson Comprehensive Cancer Center, during the Melanoma/Skin Cancers oral abstract session (Arie Crown Theater).
Abstract #10523: “Molecular testing for BRAFV600 mutations in the BRIM-2 trial of the BRAF inhibitor vemurafenib (V) in metastatic melanoma.”
Poster to be presented on June 4, 2011, 2:00 p.m. to 6:00 p.m. CDT by Kenneth J. Bloom, M.D., Chief Medical Officer, Medical Diagnostics, GE Healthcare, in the Tumor Biology poster discussion session (S103, Poster Board #15). Subsequent discussion session to be held in S100bc from 5:00 p.m. to 6:00 p.m. CDT.
Abstract #8548: “An open-label pilot study of vemurafenib in previously treated metastatic melanoma patients with brain metastases.”
Poster to be presented on June 5, 2011, 8:00 a.m. to 12:00 p.m. CDT by Reinhard Dummer, M.D., Professor of Dermatology, University of Zurich, in the Melanoma/Skin Cancers general poster session (Hall A, Poster Board #25C).
Abstract #8517: “Molecular mechanisms underlying disease relapse on treatment with selective BRAF inhibitor vemurafenib (RG7204, PLX4032).”
Poster to be presented on June 6, 2011, 8:00 a.m. to 12:00 p.m. CDT by Fei Su, Ph.D., Research Leader, Roche Pharmaceuticals, in the Melanoma/Skin ancers poster discussion session (S403, Poster Board #5). Subsequent discussion session to be held in S406 from 11:30 a.m. to 12:30 p.m. CDT.
Abstract #8518: “Induction of apoptosis by the BRAFV600E kinase inhibitor PLX4032 in BRAFV600E melanoma cells through regulation of endoplasmic reticulum stress-related genes.”
Poster to be presented on June 6, 2011, 8:00 a.m. – 12:00 p.m. CDT by Friedegund E. Meier, Professor of Dermatology, Eberhard Karls University, in the Melanoma/Skin Cancers poster discussion (S403, Poster Board #6). Subsequent discussion session to be held in S406 from 11:30 a.m. to 12:30 p.m.
Abstract #8519: “Pattern and outcome of disease progression in phase I study of vemurafenib in patients with metastatic melanoma (MM).”
Poster to be presented on June 6, 2011, 8:00 a.m. – 12:00 p.m. CDT by Kevin B. Kim, Associate Professor, Department of Melanoma Medical Oncology, The University of Texas MD Anderson Cancer Center, in the Melanoma/Skin Cancers poster discussion (S403, Poster Board #7). Subsequent discussion session to be held in S406 from 11:30 a.m. to 12:30 p.m.
Abstract #8520: “Presence of frequent underlying RAS mutations in cutaneous squamous cell carcinomas and keratoacanthomas (cuSCC/KA) that develop in patients during vemurafenib therapy.”
Poster to be presented on June 6, 2011, 8:00 a.m. – 12:00 p.m. CDT by Mario E. Lacouture, M.D., Memorial Sloan-Kettering Cancer Center, in the Melanoma/Skin Cancers poster discussion (S403, Poster Board #8). Subsequent discussion session to be held in S406 from 11:30 a.m. to 12:30 p.m.
Abstract #8502: “Molecular analyses from a phase I trial of vemurafenib to study mechanism of action (MOA) and resistance in repeated biopsies from BRAF mutation–positive metastatic melanoma patients.”
Oral presentation to be made on June 6, 2011 at 2:00 p.m. CDT by Grant A. McArthur, MBBS, Ph.D., FRACP, Associate Professor, Head, Melanoma & Skin Medical Oncology, Peter MacCallum Cancer Centre, in the Melanoma/Skin Cancers Clinical Science Symposium (Room E354B).
Abstract #3093: “Pharmacodynamic activity demonstrated in phase I for PLX3397, a selective inhibitor of FMS and Kit.”
Poster to be presented on June 6, 2011 from 8:00 a.m. to 12:00 p.m. CDT by Stephen P. Anthony, D.O., Molecular Hematologist & Oncologist, Evergreen Hematology & Oncology, in the Developmental Therapeutics / Experimental Therapeutics general poster session (Hall A, Poster Board #18B).
The abstracts will be available for review online on May 18th, 2011 at 6 pm ET, at www.asco.org. Abstracts are submitted in early 2011, while comprehensive clinical data to date will be delivered during the presentations at the Annual Meeting itself.
About Vemurafenib (PLX4032)—A Personalized Medicine for Cancer Treatment
Vemurafenib is an investigational, novel, oral small molecule for treating melanoma harboring the oncogenic BRAF mutation. Plexxikon utilized its structure-guided chemistry platform to discover vemurafenib, and initiated clinical development in 2006. Plexxikon and Roche signed a license and collaboration agreement in 2006 to co-develop vemurafenib. Under a 2005 agreement, a DNA-based companion diagnostic to identify patients whose tumors carry the BRAF mutation, the cobas 4800 BRAF V600 Mutation Test, is being co-developed by Roche and Plexxikon in parallel with the therapeutic development of vemurafenib. Roche has submitted applications with the health authorities in the U.S. and Europe for market approval for vemurafenib, and in the U.S. for the companion diagnostic. The test will also be registered in Europe.
PLX3397 is an orally available inhibitor that selectively co-inhibits three key targets—FMS, Kit and FIt3-ITD—allowing for down-modulation of a number of cell types, including macrophages, microglia, osteoclasts and mast cells, as well as selectively targeting the Flt3 mutation, a driver in AML. Growth factors for these cells are elevated in significant subsets of different human cancers, including glioblastoma, AML, breast, colorectal, lung and prostate cancer. These growth factors consequently activate the target cells, leading to a microenvironment that supports tumor growth and enables metastases to distant sites, particularly to bone. Additionally, PLX3397 has the ability to penetrate the blood-brain barrier, indicating potential efficacy in central nervous system primary or metastatic tumors, as well as a range of other diseases. Plexxikon is currently conducting a Phase 2 trial of PLX3397 in Hodgkin lymphoma.
Plexxikon, a member of the Daiichi Sankyo Group, is a leader in the structure-guided discovery and development of novel small molecule pharmaceuticals to treat human disease. The company’s lead compound, vemurafenib (PLX4032), is in late-stage clinical trials for the treatment of melanoma, and the subject of recent applications for marketing approval in the U.S. and Europe. PLX3397, the company’s next oncology candidate, has advanced to Phase 2 testing. The company is developing a portfolio of clinical and preclinical stage compounds to address significant unmet medical needs in oncology, as well as in several other therapeutic indications. Plexxikon’s proprietary Scaffold-Based Drug Discovery™ platform integrates multiple state-of-the-art technologies, including structural screening as a key component that provides a significant competitive advantage over other drug discovery approaches.
In April 2011, Daiichi Sankyo acquired Plexxikon. Plexxikon continues research and development operations as an independent unit of and member of the Daiichi Sankyo Group. Under Plexxikon’s U.S. co-promotion agreement with Genentech signed in 2010, Daiichi Sankyo, Inc. will co-promote vemurafenib, subject to market approval by FDA.