About ArQule
Mission and Core Skills
Our mission as a biotechnology company is to research, develop, and commercialize broadly effective cancer drugs with reduced toxicities compared to conventional cancer chemotherapeutics. Our complementary strengths in molecular biology and chemistry technology are driving the discovery and development of a next generation of broad-spectrum, small molecule drugs to treat human cancers. We maintain a strong commitment to basic research, and the programs in our pipeline are the direct result of our internal discovery efforts.
Cancer is the result of a range of complex genetic mutations and abnormal physiological processes that take place within the body, beginning in cells. Our molecular biology expertise enables us to understand and to affect certain key mechanisms that are common across numerous cancers and thus to halt tumor formation and progression. Our chemistry capabilities make it possible for us to imbue our products with pre-selected, drug-like characteristics and a high degree of specificity for cancer cells. We believe that these qualities, when present from the earliest stages of product development, increase the likelihood of generating safe, effective and marketable drugs.
Clinical Programs
Activated Checkpoint Therapy® / ARQ 501
Our lead cancer therapy is based on our innovative and proprietary Activated Checkpoint Therapy® (ACT) platform. The ACT platform is designed to produce small molecule compounds that selectively kill cancer cells while leaving normal cells unharmed. Based on the knowledge that cancer cells fail to adequately respond to cell damage, ACT is intended to activate and restore the proofreading mechanism by which cells respond to this damage and consequently initiate apoptosis (cell suicide) in cancer cells specifically. Unlike conventional chemotherapy, ArQule’s ACT platform bypasses the need to create further damage to cells, by directly activating the cancer cell checkpoints. The intended result is a less toxic class of drugs that will be more effective across multiple cancer types than chemotherapy.
Patient recruitment has been completed in a Phase 2 program with our most advanced ACT drug candidate, ARQ 501. This program includes monotherapy trials in leiomyosarcoma and head and neck cancer, as well as a combination trial with gemcitabine in pancreatic cancer. Patient recruitment is underway in a Phase 1 trial with a second-generation ACT candidate, ARQ 171. ARQ 501 and ARQ 171 are being developed in partnership with Hoffmann-La Roche.
c-Met Cancer Survival Pathway / ARQ 197
We began Phase 1 trials with a second product, ARQ 197, in early 2006. ARQ 197 is an orally administered, proprietary small molecule designed to inhibit c-MET, a receptor tyrosine kinase with significant potential as a therapeutic target to treat cancer. In healthy cells, c-Met is present at normal levels to support natural function and growth. In cancerous cells, c-Met is over-expressed or mutated so that it is inappropriately and continuously activated. The inappropriate expression of c-Met in most cancers and its role in controlling multiple signaling pathways involved in tumor growth and metastasis render this enzyme a highly compelling therapeutic target. By disrupting c-Met signals in cancer cells, ARQ 197 is designed to lead to the death of those cells while sparing normal cells, the latter of which are not dependent on c-Met for survival. We retain all rights to ARQ 197 and all other compounds generated from our ARQ-650RP Cancer Survival Pathway Program.
Pipeline
We are bringing our biology and chemistry capabilities to bear upon a number of additional targets that are believed to contribute to the development of human cancer. Please see our Pipeline page under Research and Development for additional products in our portfolio.