Firm will take lead camptothecin-based candidate into Phase IIb NSCLC studies.

Nanopharmaceuticals firm Cerulean Pharma closed a $24 million Series C fundraising round led by Lilly Ventures. All other existing investors also participated. The firm said it has also been approved to receive over $733,000 in Therapeutic Discovery Tax Credit Grants to support three of its therapeutic discovery programs.

The Series C funds will be used to take Cerulean’s lead candidate, CRLX101, into Phase II development for non-small cell lung cancer (NSCLC), and progress docetaxel nanopharmaceutical candidate CRLX288 into the clinic.

Cerulean is dedicated to the development of nanopharmaceuticals, initially for the treatment of cancer. The nanopharmaceuticals are constructed as drug-containing nanoparticles designed and optimized to enhance the efficacy and tolerability of therapeutic agents including small molecules, therapeutic peptides, or RNAi molecules.

The firm is exploiting two complementary technologies it claims allow for the formation of stable and consistent biocompatible nanoparticles that have high drug-loading capacity and are able to release active drug in a controlled fashion. The Polymeric Nanoparticle Technology (PNP) platform allows for nanoparticle customization through conjugation chemistry, particle composition, formulation, and fine-tuning of nanoparticle size. The Cyclodextrin Nanoparticle Technology (CDP) has been developed to generate self-assembled nanoparticles of a defined size range.

The firm says the CDP technology has been applied to several classes of molecules. CRLX101, the most advanced product derived from the CDP platform, is currently being evaluated in advanced cancer patients through Phase IIa clinical studies. The candidate comprises the antitumor agent camptothecin coupled to a cyclodextrin-based polymer that self-assembles into nanoparticles.

Cerulean claims that when its nanoparticles are administered in the bloodstream they maintain their integrity in the circulation, minimizing nonspecific systemic drug dissemination and clearance. The size and surface properties of the nanoparticles also favor extravasation through leaky vasculature and deep penetration and retention at the tumor site. Their physical properties not only facilitate endocytic intracellular uptake, but also help to avoid multidrug resistance because they are not substrates of multidrug transporters, the firm adds. Moreover, the polymer-drug conjugation chemistry provides for controlled and sustained drug release, maximizing drug exposure to target tumor cells.

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