LEAD Therapeutics discovers orally available PARP inhibitor

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.


  1. Amr Amr U.A.E. says:

    Dear Sir, pursuant to the above mentioned subject I request you to help us to save a life of woman suffering from cancer and she is in-need of medicine called PAPR inhibitor as per the doctor report it is only existing in Belgium so please do your best to help us and we are able to pay all the fees and charges.

    thanks and best regards

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