PCM-075 Overview

PCM-075 is a highly-selective adenosine triphosphate (ATP) competitive inhibitor of the serine/threonine polo-like-kinase 1 (PLK 1) enzyme, which is over-expressed in several different hematologic malignancies, as well as solid tumors such as breast, prostate, ovarian, lung, gastric and colon cancers. PCM-075 is orally bioavailable and has been explored in an initial Phase 1, open-label, dose-escalation safety study in patients with advanced metastatic solid tumor cancers, and recently published in the journal Investigational New Drugs. Trovagene plans to initiate a Phase 1b/2 clinical trial of PCM-075 in acute myeloid leukemia (AML), since it has significant advantages over prior PLK1 inhibitors evaluated in this indication, including a higher selectivity, greater potency, oral bioavailability and shorter half-life.

plk1 Inhibitor - PCM-075 stages

What Makes PCM-075 Such an Attractive Drug Candidate?

PLK1, the most well understood family member, is over expressed in many cancers, including AML. Among the five members of the PLK family, PLK1 is recognized to be the fundamental component for cell division to take place correctly, which makes PCM-075 such an attractive drug candidate.

PCM-075 is selective only for PLK1, has a short half-life of approximately 24- hours, and is oral (not IV) making it a potentially safer and more efficacious PLK inhibitor than a prior investigative pan-PLK inhibitor.

See Clinical Evidence

Trovagene Announces Peer-Reviewed Publication of First-in-Human Phase 1 Trial Results with PCM-075, its Polo-like Kinase 1 (PLK1) Inhibitor.

Greater selectivity for PLK1, potency, oral bioavailability and short half-life underscore PCM-075’s potential as safe and effective treatment for solid tumor and hematological malignancies.

PCM-075 Clinical Development Plan

We believe PCM-075 has a clear clinical development path. On June 26th, 2017, we filed our Investigational New Drug (IND) Application and Phase 1b/2 protocol for the treatment of patients with acute myeloid leukemia (AML) with the FDA. We received notification of acceptance of our IND and protocol from the FDA on July 24th, 2017. We are proceeding with our plans to initiate our Phase 1b/2 clinical trial in AML to evaluate the safety, tolerability, dose and dosing schedule, and preliminary antitumor activity of PCM-075. We are also exploring the use of correlative biomarker analysis to select patients most likely to respond to treatment.