Santarus, Inc. (NASDAQ: SNTS) today announced that it has begun patient enrollment in a multicenter, multinational, randomized, double-blind, placebo-controlled, multiple ascending dose study with the investigational drug SAN-300, its novel antibody that inhibits very late antigen-1 (VLA-1; α1β1 integrin). The Phase IIa study is designed to evaluate the safety and tolerability of repeat subcutaneous (SC) doses of SAN-300 in patients with active rheumatoid arthritis (RA) with inadequate response to disease-modifying anti-rheumatic drugs (DMARDs). Approximately 90 patients will be enrolled in the study.

“SAN-300 is a novel humanized monoclonal antibody that inhibits VLA-1, a cell adhesion molecule which plays a key role at sites of chronic inflammation,” said Mark C. Totoritis, M.D., senior vice president of clinical research at Santarus. “We believe that SAN-300 has potential application as a drug candidate in multiple inflammatory and autoimmune diseases, including RA, inflammatory bowel disease, and psoriasis.”

Overview of the Phase IIa Clinical Study in Patients with Active RA

Primary Objective
  • To evaluate the safety and tolerability of repeat doses of SAN-300 SC in patients with active RA

Secondary Objectives
  • To evaluate the following with repeat doses of SC SAN-300 in patients with active RA:
    • Pharmacokinetics and pharmacodynamics
    • Preliminary efficacy
    • Immunogenicity

Study Design
  • A total of 90 patients in 5 cohorts to be enrolled in a multicenter, multinational, randomized, double-blind, placebo-controlled, multiple ascending dose study to evaluate the SC administration of SAN-300 in patients with active RA with inadequate response to DMARDs.
  • Planned doses of SAN-300 to be studied:
    • 0.5 mg/kg SC once weekly
    • 1.0 mg/kg SC once weekly
    • 2.0 mg/kg SC every other week
    • 2.0 mg/kg SC once weekly
    • 4.0 mg/kg SC every other week
  • All patients from each cohort will receive a total of 6 weeks of exposure to SAN-300 or placebo at their assigned dose and administration frequency.
  • There is a 4 week follow-up period for safety and efficacy assessments.

Additional information on the SAN-300 Phase IIa clinical study can be found at www.clinicaltrials.gov.

About Rheumatoid Arthritis

Rheumatoid arthritis (RA) is a chronic, inflammatory autoimmune disorder of unknown etiology that primarily affects the joints. Typical symptoms include pain, morning stiffness, and swelling of multiple joints in a symmetrical distribution. Current therapies are focused on controlling symptoms and preventing joint damage. Left untreated, RA can result in the gradual erosion of bone and cartilage leading to joint destruction and significant disability. RA can occur in patients of any age, but has a peak onset between 50 and 75 years of age. It is estimated that approximately 0.5% to 1% of the general U.S. population – or up to 1.5 million people – are affected by RA.

About Santarus

Santarus, Inc. is a specialty biopharmaceutical company focused on acquiring, developing and commercializing proprietary products that address the needs of patients treated by physician specialists. The company's current commercial efforts are focused on five products. UCERIS® (budesonide) extended release tablets for the induction of remission in patients with active, mild to moderate ulcerative colitis and ZEGERID® (omeprazole/sodium bicarbonate) for the treatment of certain upper gastrointestinal disorders are promoted to gastroenterologists. GLUMETZA® (metformin hydrochloride extended release tablets) and CYCLOSET® (bromocriptine mesylate) tablets, which are indicated as adjuncts to diet and exercise to improve glycemic control in adults with type 2 diabetes, and FENOGLIDE® (fenofibrate) tablets, which is indicated as an adjunct to diet to reduce high cholesterol, are promoted to endocrinologists and other physicians who treat patients with type 2 diabetes. Full prescribing and safety information for Santarus’ products is available at www.santarus.com or by contacting Santarus at 1-888-778-0887.

Santarus’ product development pipeline includes the investigational drug RUCONEST ® (recombinant human C1 esterase inhibitor). A Biologics License Application for RUCONEST for the treatment of acute angioedema attacks in patients with hereditary angioedema is under review by the U.S. Food and Drug Administration with a response expected in April 2014. Santarus is also developing rifamycin SV MMX ®, which is in Phase III clinical testing for treatment of travelers’ diarrhea. In addition, the company is conducting a Phase IIa clinical study with SAN-300, an investigational monoclonal antibody, in patients with active rheumatoid arthritis. More information about Santarus is available at www.santarus.com.

Santarus cautions you that statements included in this press release that are not a description of historical facts are forward-looking statements. The inclusion of forward-looking statements should not be regarded as a representation by Santarus that any of its plans or objectives will be achieved. Actual results may differ materially from those set forth in this release due to the risks and uncertainties inherent in Santarus’ business, including, without limitation: whether the Phase IIa study is completed in a timely or successful manner; unexpected adverse side effects or inadequate therapeutic efficacy of Santarus’ products and product candidates; the scope and validity of patent protection for Santarus’ products and product candidates; and other difficulties or delays relating to the development, testing, manufacturing and marketing of, and obtaining and maintaining regulatory approvals for, Santarus’ products and product candidates; and other risks detailed in Santarus’ prior press releases as well as in prior public periodic filings with the Securities and Exchange Commission, including its Quarterly Report on Form 10-Q for the quarter ended September 30, 2013.

You are cautioned not to place undue reliance on these forward-looking statements, which speak only as of the date hereof. All forward-looking statements are qualified in their entirety by this cautionary statement and Santarus undertakes no obligation to revise or update this news release to reflect events or circumstances after the date hereof. This caution is made under the safe harbor provisions of Section 21E of the Private Securities Litigation Reform Act of 1995.

Santarus ® , FENOGLIDE ® , UCERIS ® and ZEGERID ® are registered trademarks of Santarus, Inc. GLUMETZA ® is a trademark of Biovail Laboratories International S.r.l. licensed exclusively in the United States to Depomed, Inc. CYCLOSET ® is a trademark of VeroScience LLC. MMX ® is a trademark of Cosmo Technologies Limited. RUCONEST ® is a trademark of Pharming Group N.V.

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