Finally: An Active Prostate Cancer Drug That Doesn’t Target Androgen

Most of the recent developments in prostate cancer treatment have addressed the timing and duration of androgen deprivation, who should receive radiation treatments, and the timing of the few available chemotherapy options. But this month’s big news is a welcome change: metastatic castration-resistant prostate cancers (mCRPCs) that harbor mutations in BRCA2 or one of a few other genes have a remarkable response to olaparib (Lynparza), a drug that inhibits the enzyme PARP1. Continue reading…

New Prospects for Small Cell Lung Cancer Patients (Part I)

Small cell lung carcinoma (SCLC) accounts for about 15% of lung cancers, but it is the deadliest form of lung malignancy. Only 6% of patients with SCLC survive beyond 5 years after diagnosis. In the last few years, new therapies—targeted therapies in particular—have been developed and approved by the U.S. Food and Drug Administration (FDA) for treating other, more common forms of lung cancer such as adenocarcinoma. However, not much progress has been made in addressing SCLC, which is usually treated with a combination of fairly toxic chemotherapeutics and radiotherapy. Many patients respond to these harsh treatments (ie, their tumors shrink), but only transiently. The disease recurs within a few months to 1 year and, at that point, is no longer treatable. Continue reading…

BMN 673, a Novel and Highly Potent PARP1/2 Inhibitor for the Treatment of Human Cancers with DNA Repair Deficiency

PARP1/2 inhibitors are a class of anticancer agents that target tumor-specific defects in DNA repair. Here, we describe BMN 673, a novel, highly potent PARP1/2 inhibitor with favorable metabolic stability, oral bioavailability, and pharmacokinetic properties. BMN 673 is currently in early-phase clinical development.

PARP Inhibitors May Offer New Option in Lung Cancer Treatment

A new class of drugs called PARP inhibitors could help patients with non-small cell lung cancer (NSCLC) who have become resistant to cisplatin (Platinol), a study suggests. Researchers found that Platinol-resistant NSCLC cells contain high levels of a protein called PARP1 in an unusually hyperactive form. PARP1 inhibitors killed these cancer cells and slowed the growth of Platinol-resistant NSCLC tumors implanted into mice. High levels of a protein called PAR predicted greater effectiveness of PARP inhibitors and may be a future biomarker for identifying patients who would benefit from the treatment.

Landes Bioscience Journals: Cell Cycle

The antineoplastic agent cis-diammineplatinum(II) dichloride (cisplatin, CDDP) is part of the poorly effective standard treatment of non-small cell lung carcinoma (NSCLC). Here, we report a novel strategy to improve the efficacy of CDDP.