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2,4,5-Trisubstituted imidazoles and their use as anti-microbial agents
WO-2006126177, nov 2006
WO-2010102393, sept 2010
Description of LOR-253, LT253: LOR-253 HCl is the hydrochloride salt of a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1) with potential antitumor activity. MTF-1 inhibitor LOR-253 inhibits MTF-1 activity and thereby induces the expression of MTF-1 dependent tumor suppressor factor Kruppel like factor 4 (KLF4). This subsequently leads to the downregulation of cyclin D1, blocking cell cycle progression and proliferation. This agent also causes decreased expression of genes involved in tumor hypoxia and angiogenesis.
ClinicalTrials.gov Identifier: NCT01281592
This is an open-label, phase 1 study to determine the maximum tolerated dose (MTD) or appropriate target dose if MTD not reached to identify the recommended phase 2 dose of LOR-253 HCl in patients with advanced or metastatic solid tumours.
March 5, 2013) – Lorus Therapeutics Inc. (“Lorus”), a biopharmaceutical company specializing in the discovery, research and development of pharmaceutical products and technologies for the management of cancer, today announced that Lorus’ patent for its lead small molecule anticancer drug LOR-253 has been allowed in China. The patent provides Lorus with exclusive rights to LOR-253 in China until 2026.
The Chinese patent provides composition of matter protection for LOR-253 and for use in the manufacture of therapies for the treatment of cancer. The patent covers a wide range of cancers, including leukemia, melanoma, as well as non-small cell lung, colon, prostate, and breast tumors. This patent extends the Company’s international patent portfolio which includes similar protection for LOR-253 in the United States, Canada, and Australia. Applications are pending in Europe and Japan.
“This increased patent protection for our anticancer therapies supports our business discussions with potential partners,” said Dr. Aiping Young, Lorus’ President and CEO. “This Chinese patent is an important addition to our global IP portfolio for LOR-253, and demonstrates our commitment to the development of innovative cancer therapies intended for significant markets.”
LOR-253 is currently in a clinical study at Memorial Sloan Kettering Cancer Center and MD Anderson Cancer Center evaluating tumor biomarkers in biopsy-suitable patients with advanced or metastatic solid tumors.
LOR-253 represents a new class of anticancer agent, which we believe may offer a competitive advantage over conventional drugs. This drug candidate has shown selective and potent antitumor activity in preclinical investigations with a variety of human cancers, including colon cancer and non-small cell lung cancer, and has demonstrated an excellent therapeutic window due to its low toxicity. LOR-253 is a first-in-class small molecule that has been optimized to induce the novel tumor suppressor Krüppel-like factor 4 (KLF4), leading to cancer cell cycle arrest and apoptosis as well as inhibition of metastasis.
Lorus is a biopharmaceutical company focused on the discovery, research and development of novel therapeutics in cancer. Lorus’ goal is to capitalize on its research, preclinical, clinical and regulatory expertise by developing new drug candidates that can be used, either alone, or in combination with other drugs, to successfully manage cancer. The Company also has expertise in antimicrobial drug discovery. Lorus Therapeutics Inc. is listed on the Toronto Stock Exchange under the symbol LOR.