LEAD Therapeutics discovers orally available PARP inhibitor

Nov 17 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.