On September 9, 2020 Apros Therapeutics, Inc., a drug discovery and development company focused on tissue-targeted Toll-Like Receptor 7 (TLR7) agonists for the treatment of cancer and infectious diseases, reported that its Investigational New Drug (IND) application for a Phase 1 dose escalation trial of APR003, the company’s first-in-class orally-administered gastrointestinal- and liver-targeted TLR7 agonist development candidate, was cleared by the FDA (Press release, Apros Therapeutics, SEP 9, 2020, View Source [SID1234564866]). The Phase 1 trial aims to evaluate safety, tolerability, pharmacokinetics, pharmacodynamics, and initial anti-tumor activity of APR003 in patients with advanced unresectable CRC with malignant liver lesions. The trial will be conducted at multiple sites in the United States, and the company intends to report top-line results upon completion.
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"We are excited to enter the clinic with our lead drug APR003 that was designed utilizing our tissue-targeted chemistry to deliver a TLR7 agonist in abundance to liver and GI tissue with little-to-no systemic distribution," stated Dr. Aaron Weitzman, M.D., FACP, Acting Chief Medical Officer at Apros Therapeutics. "We are encouraged by APR003’s unique profile and significant single agent efficacy at well-tolerated doses observed in our preclinical studies, and we are pleased to advance this program into the clinic as we believe it will offer an important step forward in creating a new immunotherapeutic treatment option for advanced colorectal cancer patients, a disease with a large unmet medical need."
ABOUT APR003
APR003 is a first-in-class, orally-administered, TLR7 agonist designed specifically to localize to the GI and liver to promote local immune activation in the targeted tissues and drive tumor eradication. Given the immune-activating capacity of this class of drugs, the tissue-targeted approach taken with APR003 is predicted to exhibit an improved tolerability profile compared to other oral non-targeted approaches, which possess side effects associated with systemic immune activation and inflammation. TLR7 activation in the liver of patients with malignancies that are metastatic to the liver may lead to innate immune priming, release of cytokines and, ultimately, enhanced anti-tumor immune responses. Although APR003 may have applications in several GI and liver malignancies, Apros will focus the initial evaluation of APR003 in patients with unresectable CRC that is metastatic to the liver given the unique bio-distribution and mechanism of action of this first-in-human investigational agent. CRC is the 3rd most common cancer in the world, and 50% of patients with advanced disease will develop liver metastasis. While most patients with CRC are non-responsive to immunotherapies, largely due to the immune-quiescent nature of the disease, APR003 aims to turn these "cold" tumors into "hot" immune-permissive tumors.