Basilea Pharmaceutica Initiates First-in-Human Study with its Novel Anti-Cancer Drug BAL101553

BASEL, SWITZERLAND--(Marketwire - June 30, 2011) - Basilea Pharmaceutica AG / Basilea initiates first-in-human study with its novel anti-cancer drug BAL101553 . Processed and transmitted by Thomson Reuters ONE. The issuer is solely responsible for the content of this announcement.

Basel, Switzerland, June 30, 2011 - Basilea Pharmaceutica Ltd. (SWISS: BSLN) today announced the start of the first clinical study with its anti-cancer drug BAL101553. The open-label phase I study will determine the safety, tolerability and pharmacokinetic profile of BAL101553, a novel microtubule-targeting agent which has demonstrated anti-cancer activity in many drug-resistant tumor models.

Cancer remains a significant challenge in healthcare despite progress in the development of agents with anti-tumor activity. Specifically, there is an increasing medical need for novel agents with new mechanisms of action that overcome tumor resistance against current therapies.

BAL101553 - a novel anti-cancer drug with unique properties

BAL101553 is a highly water-soluble prodrug of the synthetic small molecule BAL27862 that allows intravenous and oral administration without solubilizing excipients associated with adverse effects. BAL27862 arrests tumor cell proliferation and induces tumor cell death through a characteristic destabilizing effect on microtubules that is distinct from other anti- cancer agents also directed against the microtubule network. Anti-tumor activity has been demonstrated across a broad panel of solid tumor models, including those resistant against conventional microtubule-targeting drugs such as taxanes or Vinca alkaloids.

The phase I open-label, dose-escalation study investigates safety, tolerability and pharmacokinetics of intravenous BAL101553 to establish dose and administration schedule for phase II studies. The study includes adult patients with advanced solid tumors who have failed standard therapy or for whom no effective standard therapy is available.

“There is a high need for novel anti-cancer therapies to treat patients whose cancers are resistant to current agents such as taxanes,” said Dr. Anthony Man, CEO of Basilea Pharmaceutica Ltd. “BAL101553 is a novel small-molecule drug active against a well-validated cancer cell target and showing broad anti- tumor activity in preclinical models. We are delighted to see this innovative anti- cancer drug move into clinical development to broaden our hospital-focused product portfolio.”

About Basilea

Basilea Pharmaceutica Ltd. is headquartered in Basel, Switzerland, and listed on the SIX Swiss Exchange (SWISS: BSLN). Its fully integrated research and development operations are focused on antibiotics, antifungals and oncology drugs, as well as on the development of dermatology drugs, targeting the medical challenge of resistance and non-response to current treatment options in the hospital and specialty care setting.

Basilea is currently marketing Toctino® (alitretinoin), the only approved treatment for severe chronic hand eczema unresponsive to potent topical corticosteroids, in Denmark, Finland, France, Germany, Norway, Switzerland and the United Kingdom and has appointed distributors for Toctino® in other selected European markets, Canada, Israel and Mexico. Furthermore, a phase III clinical program on alitretinoin for the treatment of severe chronic hand eczema is ongoing in the U.S. For its phase III compound isavuconazole, a potential best- in-class azole antifungal for the treatment of life-threatening invasive fungal infections, the company has entered into a license, co-development and co- promotion agreement with Astellas Pharma Inc. In addition, Basilea is developing ceftobiprole, a late-stage novel anti-MRSA broad-spectrum cephalosporin antibiotic, for the first-line treatment of potentially life-threatening resistant bacterial infections. Ceftobiprole has a broad coverage of both Gram- positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), and many clinically important Gram-negative bacteria such as Pseudomonas spp.

Disclaimer

This communication expressly or implicitly contains certain forward-looking statements concerning Basilea Pharmaceutica Ltd. and its business. Such statements involve certain known and unknown risks, uncertainties and other factors, which could cause the actual results, financial condition, performance or achievements of Basilea Pharmaceutica Ltd. to be materially different from any future results, performance or achievements expressed or implied by such forward-looking statements. Basilea Pharmaceutica Ltd. is providing this communication as of this date and does not undertake to update any forward- looking statements contained herein as a result of new information, future events or otherwise.

This press release can be downloaded from www.basilea.com.

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Basilea Pharmaceutica AG Grenzacherstrasse 487
P.O Box Basel Switzerland

Listed: Freiverkehr in Börse Stuttgart, Freiverkehr in Börse Berlin, Open Market (Freiverkehr) in Frankfurter Wertpapierbörse, Freiverkehr in Bayerische Börse München;

Press release (PDF): http://hugin.info/134390/R/1527031/462735.pdf

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