Research and Development Overview

Discovering Medicines by Design

Over the past two decades, Exelixis has gained substantial experience in the process of discovering, optimizing and developing candidate drugs to treat cancer. We have assembled an industry-leading small molecule chemical compound library consisting of over four million discrete drug leads. This resource maximizes our chances of identifying attractive starting points for drug optimization against a wide variety of targets. Optimized drug candidates are then extensively tested for anti-cancer activity, alone and in combination with other therapies, in laboratory tumor models, and only those that meet rigorous standards of activity and safety are advanced into the clinic.

Our approach to discovery research begins by mining the latest advances in our understanding of tumor biology — the processes by which tumors grow, disrupt the function of normal tissues, and become resistant to treatment. This allows us to assemble portfolios of targets that form the input to our small molecule drug discovery platform. By a careful process of optimization, we seek to identify drug leads that modulate the activity of these targets and thereby inhibit the growth of tumors.

Inspired by Science, Compelled by Data

Our rational approach to drug development begins by matching the features of our drug candidates with the specific characteristics of patients’ tumors to increase the chances of success. In some cases this involves the testing of specific drug combinations to target multiple mechanisms of tumor growth. To date, Exelixis’ research and development efforts have yielded three small molecule therapeutics with broad potential in the treatment of cancer. The first novel medicine to emerge from Exelixis’ pipeline, cabozantinib, is a small molecule inhibitor of tyrosine kinases MET, AXL, RET, VEGFR2 and others, which are involved in both normal cellular function and pathologic process, such as tumor growth, metastasis and angiogenesis. It is currently the subject of more than 50 clinical trials across nine different tumor types in clinical studies being conducted by Exelixis, its development partners and outside investigators.

Collaborative Studies Maximize Clinical Potential

Collaboration with leading oncologists and other pharmaceutical and biotechnology partners accelerates our ability to bring new medicines to market for patients living with cancer. This strategic approach is also how we maximize the potential of Exelixis’ FDA-approved and investigational therapeutics.

Our flagship molecule, cabozantinib, is currently being investigated in combination with immune checkpoint inhibitors nivolumab, ipilimumab and atezolizumab, all of which have shown efficacy in different cancer indications. The combination of these active compounds with different mechanisms of action provides a compelling opportunity for the next wave of clinical trials for cabozantinib moving forward.

Explore our Pipeline

Exelixis’ pipeline contains four approved or investigational agents.

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