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LEAD Therapeutics, a privately held drug discovery company, today announced the discovery of a novel, orally available, PARP inhibitor with potent anti-tumor activity both as single-agent treatment and in combination with chemotherapy drugs
SAN BRUNO, CA, USA & SHANGHAI, CHINA | November 16, 2009 | LEAD Therapeutics, a privately held drug discovery company, today announced the discovery of a novel, orally available, PARP inhibitor with potent anti-tumor activity both as single-agent treatment and in combination with chemotherapy drugs. The new compound, designated LT-673, is in preclinical development as a potential cancer therapeutic.
Dr. Jerry Shen, Vice President of Biology at LEAD Therapeutics, commented, "LT-673 is the most potent PARP inhibitor reported to date. This compound's potency and pharmacokinetics have resulted in a very active anticancer profile in mouse xenograft models of human cancer. We believe that this compound may hold considerable promise for a variety of therapeutic applications in oncology."
LEAD will present its findings of the new PARP inhibitor, LT-673, for the first time today as a poster at the 2009 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics. The conference is being held November 15-19 in Boston, MA.
PARP is an enzyme involved in repair of DNA damage, and is a validated target for anticancer therapeutics. LEAD selected LT-673 for development after synthesizing and testing several hundred proprietary compounds. Compounds were tested in a panel of in vitro assays that selected for very potent PARP inhibitors, and also optimized for desirable pharmacokinetics and lack of undesirable activities. LT-673 is highly active in mouse xenograft models of human cancer, using low once-daily oral dosing. LEAD has begun exploring possibilities for corporate partnering to accelerate the molecule's development.
In addition to authors from LEAD Therapeutics, the poster was co-authored by Xin Yu, who represents the research team at HD Biosciences Corp., Shanghai, China. The medicinal chemistry program that led to the discovery of LT-673 was conducted at ChemPartner, LEAD's strategic partner in Shanghai, China. Other LEAD collaborators acknowledged in the poster include Shanghai Sundia MediTech, Shanghai Institute of Materia Medica; Southern Research Institute (Birmingham, AL) and Dr. Myron Jacobson (University of Arizona, Tucson, AR).
A copy of the poster on LT-673 and further information on LEAD Therapeutics is available by writing to
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About LEAD Therapeutics
LEAD Therapeutics began operations in April 2007 as a drug discovery company. LEAD has offices in San Bruno, California, and in Shanghai, China. Drug discovery programs are conducted through an extensive network of collaborations with contract research organizations in China and North America, including a strategic relationship with ChemPartner in Shanghai. In addition to drug discovery activities, LEAD currently has two compounds in preclinical development: LT-673, a PARP inhibitor being developed for oncology indications; and LT-29, a glycopeptide antibiotic for gram-positive infections.
SOURCE: LEAD Therapeutics, Inc. |
