EntreMed, Inc. (Nasdaq: ENMD) is a clinical-stage pharmaceutical company developing a new generation of multi-mechanism drugs for the treatment of cancer and inflammatory diseases. EntreMed’s drug candidates target disease cells and the blood vessels that nourish them. The Company’s goal is to develop and commercialize therapeutic products based on its scientific expertise in angiogenesis, cell cycle regulation, cell signaling, and inflammation – processes that are vital to the progression of cancer and other diseases.

EntreMed is a clinical-stage pharmaceutical company focused on developing ENMD-2076, an Aurora A and angiogenic kinase inhibitor for the treatment of cancer. ENMD-2076 has completed Phase 1 studies in patients with solid tumors and leukemia and is currently in a multi-center Phase 2 study in ovarian cancer as well as a Phase 1 study in multiple myeloma. The selection of ENMD-2076 as our active clinical program allows us to target our resources to accelerate clinical development in order to deliver value to our shareholders.

EntreMed’s other therapeutic candidates include MKC-1, an oral cell-cycle inhibitor with activity against the mTOR pathway that has completed multiple Phase 2 clinical trials for cancer, and ENMD-1198, a novel antimitotic agent that has completed a Phase 1 study in advanced cancers. The Company also has an approved Investigational New Drug Application (“IND”) for the use of Panzem® in rheumatoid arthritis (“RA”) treatment. All of our drug candidates are multi-mechanism in that they target disease cells and the blood vessels that nourish them, which we believe can be developed to be safe and convenient, and provide the potential for improved patient outcomes. EntreMed owns the intellectual property of all its other early-stage therapeutic candidates

Primary Drug Candidate

ENMD-2076 for Oncology. Our primary focus is the clinical development of our priority program, ENMD-2076. ENMD-2076 is a novel orally-active, Aurora A/angiogenic kinase inhibitor with potent activity against Aurora A and multiple tyrosine kinases linked to cancer and inflammatory diseases. ENMD-2076 is relatively selective for the Aurora A isoform in comparison to Aurora B. Aurora kinases are key regulators of the process of mitosis, or cell division, and are often over-expressed in human cancers.

Other Drug Candidates

MKC-1 for Oncology. MKC-1 is an orally-active, small molecule, cell cycle inhibitor with in vitro and in vivo efficacy against a broad range of human solid tumor cell lines, including multi-drug resistant cell lines. MKC-1 acts through multiple mechanisms of action, arresting cellular mitosis and inducing cell death (apoptosis) by binding to a number of different cellular proteins including tubulin and members of the importin β family. MKC-1 also inhibits activation of the oncogenic kinase Akt and the mTOR pathway through a mechanism that is a subject of intensive investigation by EntreMed scientists.

ENMD-1198 for Oncology. ENMD-1198 is a potent, orally-active, antimitotic agent that induces cell cycle arrest and apoptosis in tumor cells. ENMD-1198 has shown pronounced antitumor activity as well as substantial synergistic effects in combination with standard of care chemotherapeutic agents in numerous preclinical models.

Panzem® (2ME2) for Rheumatoid Arthritis. Panzem® is an orally active compound that has antiproliferative, antiangiogenic and anti-inflammatory properties. Panzem® attacks tumor cells through multiple mechanisms of action including the inhibition of angiogenesis. Panzem® inhibits production of the transcription factor hypoxia inducible factor-1 alpha (HIF-1α), which is a protein required for angiogenesis and cell survival. The inhibition of angiogenesis is an important approach to the treatment of both cancer and rheumatoid arthritis. Panzem® has potential as a single agent in rheumatoid arthritis based on its antiangiogenic, anti-inflammatory, and anti-osteoclastic (bone resorption) properties.

Science Overview

All of EntreMed’s product candidates are orally-administered compounds that have demonstrated potential in oncology and inflammatory diseases. The Company will continue to target its resources for the clinical development of its priority program, ENMD-2076, which is currently in multiple Phase 1 oncology studies and a multi-center Phase 2 study in ovarian cancer. Our other clinical product candidates (MKC-1 and ENMD-1198) continue to be in various stages of Phase 1 and 2 oncology studies but would require additional significant funding to further clinical investigation. In addition to our oncology drug candidates, we have a Phase 1 candidate, Panzem®, for the treatment of rheumatoid arthritis.

Multiple Mechanisms of Action
Diseases such as cancer employ multiple strategies to survive involving various cellular signaling pathways that promote their transformation and growth. Cancer cells can rapidly evade drugs that are highly specific for a target within one of these pathways through the development of resistance mechanisms. If more than one of these redundant signaling pathways can be interrupted at once, then the chance for resistance to develop is greatly reduced. EntreMed’s drug candidates act by attacking cancer cells through multiple pathways that promote the formation and replication of tumor cells, while also interrupting the formation of blood vessels that nourish and sustain tumor growth. EntreMed has pursued oncology indications that could provide proof-of-concept data to support the design of pivotal trials.

Versatility

While the Company’s clinical efforts continue to focus on oncology, EntreMed believes that other diseases where angiogenesis plays a role in pathology represent future opportunities.

Convenient Dosing

EntreMed is developing drug candidates that will be easy to use as compared to other modes of drug administration. The Company is focusing specifically on drugs that can be administered orally.

Intellectual Property Position

All EntreMed pipeline programs are backed by strong intellectual property rights. Each product candidate is covered by issued or pending composition, method and use patents. The Company owns or has licensed over 60 patent applications and issued patents in the United States for our product candidates. The Company has well over 100 pending patent applications and issued patents in the United States and other countries.