Novelos Therapeutics Successfully Completes First Cohort In Phase 1b Solid Tumor Trial With I-131-CLR1404 (HOT) Cancer-Targeted Molecular Radiotherapeutic

MADISON, Wis., May 15, 2012 /PRNewswire/ -- Novelos Therapeutics, Inc. (OTCQX: NVLT), a pharmaceutical company developing novel drugs for the treatment and diagnosis of cancer, today announced that it has successfully completed the first cohort in a U.S. multi-center Phase 1b dose-escalation trial of its cancer-targeted molecular radiotherapeutic compound I-131-CLR1404 (HOT) in cancer patients with advanced solid tumors.  The first two-patient cohort was successfully dosed with approximately 20 mCi of HOT, triggering enrollment into the second cohort at approximately 40 mCi.  Details of the trial design are available on www.clinicaltrials.gov ID: NCT01495663, or at www.novelos.com in the 'Clinical Trials' section.  Glenn Liu, M.D., University of Wisconsin Carbone Cancer Center, is the trial's principal investigator.  Detailed trial results are expected to be presented at a scientific venue at a later date.

"Patients with advanced solid tumors need safer and more effective therapies," said Dr. Liu.  "Based on animal data, results from a completed Phase 1a dosimetry trial, and now initial data from this Phase 1b trial, HOT appears to deliver radiation directly and selectively to cancerous tumors.  Data from the first cohort indicates HOT was well-tolerated, without any grade 3 or 4 toxicities, enabling enrollment of the first patient in the second cohort.  HOT uptake in cancerous tumors persisted for at least 21 days.  One patient with advanced prostate cancer remains on trial at two months following treatment with HOT, while another patient with advanced colorectal cancer has completed the trial."

"We are pleased with HOT's safety profile and selective cancerous tumor uptake and retention in this first cohort at a dose of approximately 20 mCi," said Kim Hawkins, Vice President of Clinical Development of Novelos.  "We now look forward to evaluating HOT at approximately 40 mCi in cancer patients with advanced solid tumors, as per the trial protocol.  We also look forward to adding two additional clinical investigators to the trial, Joanne Mortimer, M.D., at the City of Hope and Michael Pishvaian, M.D., Ph.D., at Georgetown University."

"We intend to combine the data from this trial with calculation of effective doses for HOT based on quantitative positron emission tomography (PET) tumor imaging data using I-124-CLR1404 (LIGHT), our small-molecule cancer-targeted PET imaging agent," said Harry Palmin, President and CEO of Novelos.  "Together, we believe these data will enable us to commence HOT Phase 2 proof-of-concept trials in the first quarter of 2013 in cancer patients that have significant unmet medical need."

About HOT
HOT (iodine-131 radiolabeled CLR1404) is a small-molecule, broad-spectrum, cancer-targeted molecular radiotherapeutic that we believe has first-in-class potential.  HOT is comprised of a small, non-pharmacological quantity of CLR1404 (COLD) acting as a cancer-targeted delivery and retention vehicle and incorporating a cytotoxic (cell-killing) dose of radiotherapy (in the form of iodine-131, a radioisotope that is already in common use to treat thyroid and other cancer types).  The ongoing Phase 1b dose-escalation trial is aimed at determining the Maximum Tolerated Dose of HOT.  We expect to initiate HOT Phase 2 efficacy trials as a monotherapy for solid tumors with significant unmet medical need as soon as a minimal efficacious dose is established, subject to additional funding.  We may determine such an effective dose upon calculating it from ongoing PET imaging trials in cancer patients with LIGHT (since PET imaging is quantitative, enabling determination of tumor radiation exposure at a given dose level) or seeing a tumor response in the Phase 1b trial.  Preclinical experiments in vitro (in cell culture) and in more than a dozen in vivo (in animals) models have demonstrated selective killing of cancer cells along with a benign safety profile.  In view of HOT's selective uptake and retention in a wide range of solid tumors and in cancer stem cells, its single-agent efficacy in animal models and its non-specific mechanism of cancer-killing (radiation), we are first developing HOT as a monotherapy for solid tumors with significant unmet medical need.

About Novelos Therapeutics, Inc.
We are a pharmaceutical company developing novel drugs for the treatment and diagnosis of cancer.  Our three cancer-targeted compounds are selectively taken up and retained in cancer cells, including cancer stem cells, versus normal cells.  Thus, our therapeutic compounds appear to directly kill cancer cells while minimizing harm to normal cells.  This offers the potential for a paradigm shift in cancer therapy by providing efficacy versus all three major drivers of mortality in cancer: primary tumors, metastases and stem cell-based relapse.  I-124-CLR1404 (LIGHT) is a small-molecule cancer-targeted PET imaging agent.  We believe LIGHT has first-in-class potential and Phase 1-2 clinical trials are ongoing.  I-131-CLR1404 (HOT) is a small-molecule, broad-spectrum, cancer-targeted molecular radiotherapeutic that delivers cytotoxic radiation directly and selectively to cancer cells and cancer stem cells.  We believe HOT also has first-in-class potential.  HOT Phase 1b dose-escalation trial is ongoing and we expect HOT to enter Phase 2 trials in the first quarter of 2013 as a monotherapy for solid tumors with significant unmet medical need, subject to additional funding.  CLR1404 (COLD), a pre-clinical cancer-targeted non-radioactive chemotherapy, works primarily through Akt inhibition.  Together, we believe our compounds are able to "find, treat and follow" cancer anywhere in the body in a novel, effective and highly selective way.  For additional information please visit www.novelos.com

This news release contains forward-looking statements.  You can identify these statements by our use of words such as "may," "expect," "believe," "anticipate," "intend," "could," "estimate," "continue," "plans," or their negatives or cognates.  Such statements are valid only as of today, and we disclaim any obligation to update this information.  These statements are only estimates and predictions and are subject to known and unknown risks and uncertainties that may cause actual future experience and results to differ materially from the statements made.  These statements are based on our current beliefs and expectations as to such future outcomes.  Drug discovery and development involve a high degree of risk.  Factors that might cause such a material difference include, among others, uncertainties related to the ability to attract and retain partners for our technologies, the identification of lead compounds, the successful preclinical development thereof, the completion of clinical trials, the FDA review process and other government regulation, our  pharmaceutical collaborators' ability to successfully develop and commercialize drug candidates, competition from other pharmaceutical companies, product pricing and third-party reimbursement.

SOURCE Novelos Therapeutics, Inc.