BMN673 is an orally bioavailable inhibitor of the nuclear enzyme poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. PARP inhibitor BMN-673 selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. BMN-673 has been proven to be highly active in mouse models of human cancer and also appears to be more selectively cytotoxic with a longer half-life and better bioavailability as compared to other compounds in development. BMN 673 selectively kills cancer cells with BRCA-1 or BRCA-2 mutations. Oral dosing of BMN 673 results in complete regression of the BRCA-deficient tumors in xenograft tumor model studies. In addition, we found that tumor cells with PTEN mutation are highly sensitive to BMN 673 treatment in vitro. Xenograft tumor models that harbor PTEN deficiency responded to oral BMN 673 treatment with significant tumor growth delay. Currently, BMN 673 is in phase 1 clinical trials with solid tumors or hematological malignancies.
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|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Structure and preclinical characterization of BMN 673, a potent and orally active PARP inhibitor as an anticancer agent.
Yuqiao, et al. Mol Cancer Ther. 2011 Nov;10(11 Suppl).
Correlation of pharmacokinetics (PK), pharmacodynamics (PD) and in vivo antitumor activity of BMN 673 in preclinical models.
Ying, et al. Mol Cancer Ther. 2011 Nov;10(11 Suppl).
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