Profile: ArQule Inc (ARQL.OQ)
18 Apr 2019
ArQule, Inc., incorporated on January 1, 1994, is a biopharmaceutical company. The Company is engaged in the research and development of therapeutics to treat cancers and rare diseases. These drugs focuses on the biological pathways implicated in a range of cancers and certain non-oncology indications. Its clinical-stage pipeline consists of approximately four drug candidates, all of which are in targeted patient populations. The Company's lead product candidate is tivantinib (ARQ 197), an orally administered, small molecule inhibitor of the c-Met receptor tyrosine kinase (MET) and its biological pathway. The Company's product candidates include ARQ 092, designed to inhibit the AKT serine/threonine kinase; ARQ 087, a multi-kinase inhibitor designed to inhibit the fibroblast growth factor receptor (FGFR) family, and ARQ 761, a Beta lapachone analog being evaluated in investigator-sponsored testing as a promoter of NQO1-mediated programmed cancer cell necrosis.
Tivantinib (ARQ 197)
The Company is engaged in developing its lead product candidate, tivantinib, with its partner, Daiichi Sankyo Co., Ltd. (Daiichi Sankyo), in the United States, Europe, South America and the rest of the world, excluding Japan and certain other Asian countries, where it has licensed commercial rights to Kyowa Hakko Kirin Co., Ltd. (Kyowa Hakko Kirin). Tivantinib is an inhibitor of MET. MET is a target for cancer therapy, based on its multiple roles in cancerous cell proliferation, tumor spread, new blood vessel formation and resistance to certain drug therapies. It has also earlier-stage combination therapy trials, and pre-clinical experiments with tivantinib and other anti-cancer agents. Its lead indication is liver cancer. It has conducted the MARQUEE Phase III trial, ATTENTION Phase III trial, KRAS Mutation-Positive Phase II trial and colorectal cancer trial.
ARQ 092 is designed to inhibit the AKT serine/threonine kinase inhibitor. It is an early clinical-stage product. It has also conducted or is conducting Phase Ia/Ib and Phase II clinical testing of ARQ 092. ARQ 092 is part of its pipeline of product candidates directed toward molecular targets and biological processes with demonstrated roles in the development of human cancers. It is collaborating with the National Human Genome Research Institute of the National Institutes of Health (NIH), a Phase I clinical trial investigating ARQ 092 as a potential treatment for Proteus syndrome.
ARQ 087 is a multi-kinase inhibitor designed to inhibit the FGFR family. Its an early clinical-stage product. It has completed Phase Ia dose escalation trials. ARQ 087, an orally bioavailable compound, is a dual kinase inhibitor that binds to the inactive form of FGFR1 and FGFR2, and potently inhibits the active forms of FGFR1 and FGFR2. ARQ 087 has demonstrated inhibition of tumor growth and downstream signaling in vivo in tumors whose growth is driven by these targets. The Company is conducting a Phase I/II trial with ARQ 087.
ARQ 751 is an inhibitor of AKT. It is in late pre-clinical development. The Company has conducted or are conducting Phase Ia/Ib or Phase II clinical testing of ARQ 751.
ARQ 761 is a Beta lapachone analog being evaluated in investigator-sponsored testing as a promoter of NQO1-mediated programmed cancer cell necrosis. The Company, in collaboration with the University of Texas Southwestern Medical Center, is engaged in the clinical development of ARQ 761. ARQ 761 is a pro-drug of ARQ 501, which has demonstrated in vitro activity against a range of solid tumors. Phase Ia testing with ARQ 761 identified anti-cancer activity as measured by tumor responses that occurred in a portion of the patient population with high levels of NQO1, the mechanistic target of the compound.
The Company competes with Amgen, Inc. Ariad Pharmaceuticals, Inc., Astellas Pharma, Inc., Array BioPharma Inc., Astex Therapeutics, Cell Therapeutics, Inc., Curis, Inc., Cytokinetics, Inc., Exelixis, Inc., Evotec AG, GlaxoSmithKline, Gilead, FORMA Therapeutics, Incyte Corporation, Infinity Pharmaceuticals, Inc., Novartis, Pfizer, Roche, AstraZeneca/Hutchison MediPharma, AVEO Pharmaceuticals, Inc., Bristol-Myers Squibb Company, Johnson & Johnson, Merck, Takeda, Abbott, Bayer, Celgene, Dainippon Sumitomo, Eisai Co., Eli Lilly, Polaris Group, Servier, 4SC AG, Debiopharm, Boeheringer Ingelheim, Clovis, BioClin, Five Prime, Concordia Healthcare, Agios, Exelexis, Oncotherapy, Spectrum, Delcath, Cellact Pharma Gmbh and Rexahn.
1 Wall St Fl 6
BURLINGTON MA 01803-4757